Synthesis and anticancer activity of 3-amino-N-phenyl-1H-indazole-1-carboxamide and 1-(1H)indazol-3-yl-3-phenylureido derivatives

Antimicrobial peptides from echinoderms as antibiofilm agents: a natural strategy to combat bacterial infections

AbstractIncreased attention has been focused on marine invertebrates as a source of bioactive molecules for biomedical applications. Many bioactive molecules are part of the innate immune system. Some more recently isolated compounds, mainly from the sea urchin and the sea cucumber, are antimicrobial peptides (AMPs) active against Gram-positive and Gram-negative bacteria, and fungi. In this review we described the most recent studies on AMPs isolated from echinoderms. AMPs are small peptides (< 10 kDa) with cationic charge and amphipathic structure. Recently, it was demonstrated that in the coelomocyte lysates of Paracentrotus lividus and Holothuria tubulosa, AMPs possess activity against s…

Synthesis and biological activity of new anti-inflammatory compounds containing the 1,4-benzodioxine and/or pyrrole system

A series of substituted derivatives containing the 1,4-benzodioxine or pyrrole nucleus are described. All the newly synthesized compounds were examined for their in vitro and in vivo anti-inflammatory activity. Several derivatives, including (S)-2, 14 and 17, showed more anti-inflammatory activity in vivo in these assays (rat paw oedema induced by carrageenan) than the known classical anti-inflammatory agent ibuprofen, whereas other compounds like 1 were equipotent to ibuprofen. Compound 17 was the most outstanding derivative because of its remarkable in vivo anti-inflammatory activity. In this paper, we examine and discuss the structure-activity relationships and anti-inflammatory activiti…

Antimicrobial and antistaphylococcal biofilm activity from the sea urchin Paracentrotus lividus

Aims:  Staphylococcal biofilm-associated infections are resistant to conventional antibiotics. Consequently, new agents are needed to treat them. With this aim, we focused on the effector cells (coelomocytes) of the sea urchin Paracentrotus lividus immune system. Methods and Results:  We tested the activity of the 5-kDa peptide fraction of the cytosol from coelomocytes (5-CC) against a group of Gram-positive, Gram-negative bacteria and fungi. We determined minimal inhibitory concentrations (MICs) ranging from 253·7 to 15·8 mg ml−1. We observed an inhibitory activity and antibiofilm properties of 5-CC against staphylococcal biofilms of reference strains Staphylococcus epidermidis DSM 3269 an…

Chemical composition and antimicrobial activity of some oleogum resin essential oils from Boswellia spp. (Burseraceae).

The chemical composition of Boswellia carteri (Somalia), B. papyrifera (Ethiopia), B. serrata (India) and B. rivae (Ethiopia) oleogum resin essential oils was investigated using GC-MS to identify chemotaxonomy marker components. Total ion current peak areas gave good approximations to relative concentrations based on GC-MS peak areas. B. carteri and B. serrata oleogum resin oils showed similar chemical profiles, with isoincensole and isoincensole acetate as the main diterpenic components. Both n-octanol and n-octyl acetate, along with the diterpenic components incensole and incensole acetate, were the characteristic compounds of B. papyrifera oleogum resin oil. Hydrocarbon and oxygenated mo…

Amoxicillin-loaded polyethylcyanoacrylate nanoparticles: influence of PEG coating on the particle size, drug release rate and phagocytic uptake.

Polyethyleneglycol (PEG)-coated polyethylcyanoacrylate (PECA) nanoparticles loaded with amoxicillin were prepared and the influence of the PEG coating on the particle size, zeta potential, drug release rate and phagocytic uptake by murine macrophages was studied. Experimental results show that this colloidal drug delivery system could be useful for intravenous or oral administration. The profile of amoxicillin release from PECA nanoparticles system was studied under various conditions similar to those of some corporeal fluids. In all these experiments, amoxicillin release in the free form was studied by HPLC analysis. Experimental results showed that at pH 7.4 drug release rises when molecu…

Echinoderm Antimicrobial Peptides

Abstract Antimicrobial peptides (AMPs) are widely expressed in organisms and have been linked to innate and acquired immunity in vertebrates. These compounds are constitutively expressed from different cellular types to interact directly with infectious agents and/or modulate immunoreactions. In invertebrates, including echinoderms, which lack a vertebrate-type adaptive immune system, AMPs represent the major humoral defense system against infection, showing a diverse spectrum of action mechanisms, most of them related to plasma membrane disturbance and lethal alteration of microbial integrity. Here, we summarize the knowledge of AMPs in echinoderms as Strongylocins identified in the sea ur…

Thiazole Analogues of the Marine Alkaloid Nortopsentin as Inhibitors of Bacterial Biofilm Formation

Anti-virulence strategy is currently considered a promising approach to overcome the global threat of the antibiotic resistance. Among different bacterial virulence factors, the biofilm formation is recognized as one of the most relevant. Considering the high and growing percentage of multi-drug resistant infections that are biofilm-mediated, new therapeutic agents capable of counteracting the formation of biofilms are urgently required. In this scenario, a new series of 18 thiazole derivatives was efficiently synthesized and evaluated for its ability to inhibit biofilm formation against the Gram-positive bacterial reference strains Staphylococcus aureus ATCC 25923 and S. aureus ATCC 6538 a…

Antibacterial activity of Pleurotus species

Basidiomycetes express promising antitumor, immune modulating, cardiovascular and hypercholesterolemia, antiviral, antibacterial and antiparasitic effects (Wasser & Weis, 1999; Reshetnikov et al., 2001; Wasser, 2002, Didukh et al., 2003). They are also well known for their safety and efficacy as functional foods and dietary supplements (Wasser & Akavia, 2008). The antibacterial and antiviral value of different genera of Basidiomycetes has been tested by different authors (Benedict & Brady, 1972; Donnelly et al., 1986; Gao et al., 2003;). In particular the antibacterial and antiparasitic therapeutic effects were investigated in the genera Flammulina P. Karst, Fomes (Fr.) Fr., Ganoderma P. Ka…

Borgo Vecchio Factory

ADI Design Index è la selezione annuale del miglior design italiano ed è parte integrante del sistema di selezione del Premio Compasso d’Oro ADI: ogni anno, grazie all’Osservatorio Permanente del Design ADI – un gruppo di lavoro costituito da oltre cento esperti, anche esterni all’associazione – prende in esame su tutto il territorio italiano il design dei nuovi prodotti messi in produzione. Dopo una strutturata selezione (commissioni territoriali, tematiche e comitato di selezione finale), i migliori prodotti di design vengono presentati, con un commento critico che evidenzia i motivi della scelta, su ADI Design Index. I volumi diventano la base su cui lavora la giuria internazionale del C…

Synthesis and in vitro antileukemic activity of new 4-triazenopyrazole derivatives

Several new 4-(3,3-dimethyltriazeno)-5-benzamidopyrazole derivatives were prepared by reacting 4-diazo-5-benzamidopyrazole derivatives with dimethylamine. The compounds were tested at 10 microM for their vitro antileukemic activity against K562 (Human chronic myelogenous leukemia) and Raji (human Burkitt limphoma ) cell lines. Dacarbazine and methotrexate were used for comparative purpose. The 3-methyl-4-(3,3-dimethyltriazeno)-5-(substituted benzamido)pyrazoles, bearing the pyrazole nucleus free at 1 position, resulted more active than the 1-(substituted phenyl)-3-methyl-4-(3,3-dimethyltriazeno)-5-benzamidopyrazoles. Dacarbazine at 10 microM showed no activity in the above tests. The observ…

Curcumin derivatives as inhibitors of Gram positive and Gram negative biofilm formation

Bacterial biofilms: a challenge in the discovery of new anti-infective agents.

The ability to form a biofilm, bacterial communities able to grow on surfaces and surrounded by an extracellular polymeric substance biofilm agents.Our research group focused on discovering of novel chemical agents of potential therapeutic utility in the treatment of staphylococcal biofilm-associatedinfections by screening novel compounds (synthetic or natural). In a recent study, the antistaphylococcalbiofilm activity of pyrrolomycins C,D, F1, F2a, F2b, F3 a family of halogenated pyrroles which are naturally produced byActinosporangium vitaminophylum and of the synthesized related compounds I, II, III were investigated and compared (Schillaci et al, 2010). We also focused on marine inverte…

Anti-adhesion agents against Gram-positive pathogens

The rise of antibiotic-resistance as well as the deficiency of investments by pharmaceutical companies in the development of new antibiotics, have stimulated the investigation of alternative strategies to conventional antibiotics for counteracting the pathogens. A fundamental step of Gram positive pathogenesis is the bacterial adhesion to the host tissue involving a direct and a specific interaction between bacterial surface molecules and host ligands. Targeting the adhesion is a good strategy to design novel anti-infective drugs agents useful to interfere with the pathogenic process and with a virulence mechanism as biofilm formation. This review is focused on anti-virulence compounds whic…

ChemInform Abstract: Synthesis and Antineoplastic Activity of New 4-Diazopyrazole Derivatives.

Several new 4-diazopyrazole derivatives were synthesized by reaction of 1-(R-substituted)phenyl-3-methyl-5-benzamidopyrazoles with a sevenfold excess of nitrous acid in acetic media. The compounds were tested at 20 microM concentration for their antineoplastic activity in vitro against Raji (human Burkitt lymphoma), K562 (human chronic myelogenous leukemia) and U937 (human histiocytic lymphoma) cell lines. They showed a percent of growth inhibition in the range 23.4-100%.

Biological responses of Rhynchophorus ferrugineus (Coleoptera: Curculionidae) to Steinernema carpocapsae (Nematoda: Steinernematidae).

Rhynchophorus ferrugineus (Olivier 1790) (Coleoptera: Curculionidae) is becoming a serious problem in Mediterranean areas where it is well-adapted, and now is present even in the United States (California). The infestations are primarily in urban areas where chemical control is not advisable and million of Euros are spent to control it. The effects of the entomopathogenic nematode Steinernema carpocapsae (Nematoda: Steinernematidae) on mortality, growth, as well as the immune activity of R. ferrugineus larvae, were investigated. R. ferrugineus mortality exhibited a positive trend with the dosage and duration of exposure to S. carpocapsae. The median lethal dose and median lethal time, impor…

Synthesis of New 2-{[(Phenoxy or Phenyl)acetyl]amino}benzoic Acid Derivatives as 3α-Hydroxysteroid Dehydrogenase Inhibitors and Potential Antiinflammatory Agents

A number of 2-([(phenoxy or phenyl)acetyl]amino)benzoic acid derivatives were prepared in about 50% yield from (phenoxy or phenyl)acetyl chloride and anthranilic acid derivatives. All the compounds were tested as in vitro inhibitors of 3 alpha-hydroxysteroid dehydrogenase, since enzyme inhibition predicts potential antiinflammatory activity in vivo. The most active compounds 3 l, m, s are about 3.5 times more active than acetylsalicylic acid (ASA). Activity is influenced by electronic as well as steric effects.

FRAGMENTS OF BETA-THYMOSIN FROM THE SEA-URCHIN PARACENTROTUS LIVIDUS AS NOVEL ANTIMICROBIAL PEPTIDES AGAINST STAPHYLOCOCCAL BIOFILMS

With the aim to face the threat of pathogen biofilms intrinsically resistant to conventional antibiotics, we focused on coelomocytes, the immune mediators in echinoderms, as source of novel antimicrobial peptides (AMPs). The proteic fraction <5kDa from coelomocytes cytosol of the sea-urchin Paracentrotus lividus (5-CC) was tested against a group of Gram positive and Gram negative pathogen reference strains. The 5-CC of P. lividus resulted active against all tested strains at concentrations ranging from 15.8 to 253.7 mg/mL. The ability to prevent staphylococcal biofilm formation was evaluated against the biofilm of clinical strain S.epidermidis 1457 using live/dead staining in combination wi…

Rivalutazione degli Idrolati dell’industria agrumaria siciliana.

Gli idrolati, o acque aromatiche, sono i prodotti dell'idrodistillazione di specie aromatiche. Possono essere ottenuti dall'intera pianta o parti di essa, allo stato fresco o in buona conservazione come fiori o, nel nostro caso, dai frutti del Genere Citrus. Le sue proprietà sono utilizzate nella produzione di alimenti, cosmetici e profumi, o in farmacia e aromaterapia. Essi sono comunemente considerati un sottoprodotto degli oli essenziali, ma in realtà, data la diversa composizione e la conseguente maggiore delicatezza, hanno un loro apprezzabile utilizzo, legato comunque al mantenimento delle proprietà delle piante da cui derivano. La produzione degli oli essenziali nell'industria agruma…

Paracentrin1, a synthetic antimicrobial peptide fragment of a beta-thymosin from the sea-urchin Paracentrotus lividus, interferes whith staphylococcal and Pseudomonas aeruginosa biofilm formation

Pyrrolomycins as novel agents against staphylococcal biofilms

Synthesis and Antiproliferative Activity of Novel 3-(Indazol-3-yl)-quinazolin-4(3H)-one and 3-(Indazol-3-yl)-benzotriazin-4(3H)-one Derivatives

Several new 3-(indazol-3-yl)-quinazolin-4(3H)-one and 3-(indazol-3-yl)-benzotriazin-4(3H)-one derivatives 5 and 6 were synthesized and tested for their in vitro antiproliferative activity against Raji, K562, and K562-R cell lines. The pharmacological screening showed that some 2, 6, or 7-substituted quinazolinones 5 posses a significant antiproliferative activity, with a percentage growth inhibition ranging from 44.8% to 100% at 50 microM, which was higher than that showed by the unsubstituted derivative 5a previously synthesized. For the most active compounds 5d, 5f, and 5g the IC50 were recorded.

ChemInform Abstract: Synthesis and Antifungal Activity of New N-Isoxazolyl-2-iodobenzamides.

N-Isoxazolyl-2-iodobenzamides 3 and 9, with a benodanil-like structure, were synthesized by refluxing in acetic acid the corresponding benzotriazinones 2 and 8 with potassium iodide for 1 h with the aim to ascertain if they were active as fungicides against Phytophthora citricola Saw., Botrytis cinerea Pers., Rhizoctonia sp. and Alternaria sp. Among the tested iodo derivatives, compounds 3b and 9a possess interesting activities against the aforesaid fungal strains in several cases similar to that of benodanil I taken as reference drug.

Sortase A Inhibitors: Recent Advances and Future Perspectives

Here, we describe the most promising small synthetic organic compounds that act as potent Sortase A inhibitors and cater the potential to be developed as antivirulence drugs. Sortase A is a polypeptide of 206 amino acids, which catalyzes two sequential reactions: (i) thioesterification and (ii) transpeptidation. Sortase A is involved in the process of bacterial adhesion by anchoring LPXTG-containing proteins to lipid II. Sortase A inhibitors do not affect bacterial growth, but they restrain the virulence of pathogenic bacterial strains, thereby preventing infections caused by Staphylococcus aureus or other Gram-positive bacteria. The efficacy of the most promising inhibitors needs to be com…

Staphylococcal Biofilms: Challenges in the discovery of Novel Anti-Infective Agents

In Vitro Antimicrobial Activity of Frankincense Oils from Boswellia sacra Grown in Different Locations of the Dhofar Region (Oman)

Frankincense essential oils from Boswellia sacra have been commonly used to treat microbial infections from as early as the 11th century. The main feature of the plant is its gum resin, from which it is possible to obtain essential oils. In the present study, we focused on the comparative study of the oils extracted from the resins of three different Boswellia sacra cultivars (Najdi, Sahli and Houjri). From each of frankincense resin three successive essential oil samples (Grade 1, Grade 2, Grade 3) were obtained. Houjri gum resin gave the lowest percentage (5%) of total essential oil content but showed the maximum number of volatile components in all three grades. Najdi Grade 2 essential o…

Anti biofilm activity of Paracentrotus lividus coelomocytes

Attività antibatterica di peptidi estratti da celomociti di echinodermi

Negli echinodermi la difesa dell’organismo dalle invasioni microbiche avviene tramite meccanismi cellulari e umorali dell’immunità innata. Una componente fondamentale dei fattori umorali è costituita dai peptidi antimicrobici (AMPs) molto conservati con un ampio spettro di attività antimicrobica contro batteri, virus e funghi. Solitamente gli AMPs sono costituiti da meno di 100 amminoacidi, sono cationici e formano strutture anfipatiche. In questo lavoro dimostriamo che i celomociti dell’Echinoideo Paracentrotus lividus e dell’Oloturoideo Holothuria tubulosa contengono sostanze con attività antimicrobica verso diversi ceppi batterici patogeni umani. In entrambe le specie, nel precipitato ac…

Chemical composition, cytotoxic effects, antimicrobial and antibiofilm activity of Artemisia arborescens (Vaill.) L. growing wild in the province of Agrigento, Sicily, Italy

Artemisia arborescens (Vaill.) L. is a perennial shrubby plant growing along the coastal strips of the Mediterranean region. It is used in traditional medicine. Its essential oil and solvent extracts exhibit a very interesting chemotherapeutic potential, which makes this plant useful in maintaining human health. The goal of this study was to determine the phytochemical composition of the petroleum ether and methanol extracts, as well as to evaluate anticancer activities and antimicrobial and biofilm formation reduction. Thirty-nine phytochemical compounds in negative ion mode, and 25 in positive ion mode were identified by HPLC-ESI-QTOF-MS. All four extracts reduced the viability of human M…

Chemical constituents and antiproliferative activity of Euphorbia bivonae

Euphorbia is a genus of plants belonging to the family Euphorbiaceae, consisting of about 2160 species. This family occurs mainly in the Indo-Malayan region and tropical America. Euphorbia also has many species in non-tropical areas such as the Mediterranean area, the Middle East, South Africa, and southern USA. Phytochemical studies of species from the genus Euphorbia report the presence of skin-irritating and tumor-promoting diterpenoids, several macrocyclic diterpenoids with antibacterial, anticancer, PGE2-inhibitory, antifeedant, anti-HIV, and analgesic activities. Some of the Euphorbiaceae species are used in folk medicine for the treatment of skin diseases, gonorrhea, migraines, intes…

Polyanion–tobramycin nanocomplexes into functional microparticles for the treatment of Pseudomonas aeruginosa infections in cystic fibrosis

Aim: Efficacy of antibiotics in cystic fibrosis (CF) is compromised by the poor penetration through mucus barrier. This work proposes a new ‘nano-into-micro’ approach, used to obtain a combinatorial effect: achieve a sustained delivery of tobramycin and overcome mucus barrier. Methods: Mannitol microparticles (MPs) were loaded with a tobramycin polymeric nanocomplex and characterized in presence of CF artificial mucus. Results &amp; discussion: MPs are able to alter the rheological properties of CF artificial mucus, enhancing drug penetration into it and allowing a prolonged drug release. MPs resulted to be effective in Pseudomonas aeruginosa infections if compared with free tobramycin. Co…

An asymmetric electrospun membrane for the controlled release of ciprofloxacin and FGF-2: Evaluation of antimicrobial and chemoattractant properties.

Here, an asymmetric double-layer membrane has been designed and fabricated by electrospinning as a tool for a potential wound healing application. A hydrophobic layer has been produced by using a polyurethane-polycaprolactone (PU-PCL) copolymer and loaded with the antibacterial ciprofloxacin whereas an ion responsive hydrophilic layer has been produced by using an octyl derivative of gellan gum (GG-C8) and polyvinyl alcohol (PVA) and loaded with the growth factor FGF-2. This study investigated how the properties of this asymmetric membrane loaded with actives, were influenced by the ionotropic crosslinking of the hydrophilic layer. In particular, the treatment in DPBS and the crosslinking i…

Synthesis and antiproliferative activity of triazenoindazoles and triazenopyrazoles: a comparative study.

Several triazenoindazoles and triazenopyrazoles were prepared transforming the appropriate aminoindazoles and aminopyrazoles in the corresponding diazonium salts which were reacted with dimethylamine, diethylamine and pyrrolidine. All the triazenes were tested for their antiproliferative activity against K562, HL60, L1210 and MCF7 cell lines. The biological data showed that the benzocondensation plays a positive role on the antiproliferative activity. The (1)H-NMR spectra showed that the rotational barrier around the N(2)-N(3) bond in the triazene group can be influenced both by the position of this group in the indazole nucleus and by the substitution pattern in the benzene moiety.

Novel antimicrobial and anti-biofilm agents from a marine invertebrate

In vitro anti-Gram-positive and anti-staphylococcal biofilm activity of newly halogenated pyrroles related to Pyrrolomycins

A High Sensitive Nested PCR for Toxoplasma gondii Detection in Animal and Food Samples

Toxoplasma gondii is a major food and waterborne transmitted parasite world-wide. The tissues and meat samples of many warm blooded animals can contain tissues cysts from chronic toxoplasmosis. Water and vegetable can be contaminated by the parasitic oocysts shed through the feces of infected cats, representing the definitive host of the parasite. A sensitive PCR for Toxoplasma gondii detection is described. The first step amplified the region between the 28S and 18S rDNA in the closely related T. gondii and Neospora caninum; RFLP analysis distinguished the DNA from the two morphologically identical parasites. Although N. caninum is not involved in human transmission, so far, it is importan…

ChemInform Abstract: Synthesis and Pharmacological Evaluation of 1-Methyl-5- [substituted-4(3H)-oxo-1,2,3-benzotriazin-3-yl]-1H-pyrazole-4-acetic Acid Derivatives.

Abstract Several new 1-methyl-5-[substituted-4-oxo-1,2,3-benzotriazin-3-yl]-1H-pyrazole-4-acetic acids and their ethyl ester derivatives were prepared. The compounds were tested for analgesic and antiinflammatory activities, acute toxicity, ulcerogenic effect, and as in vitro inhibitors of 3α-hydroxysteroid dehydrogenase (3α-HSD), since it is claimed that the inhibition of such an enzyme predicts in vivo antiinflammatory activity. Some compounds were more active than phenylbutazone in the phenylbenzoquinone and acetic acid peritonitis tests, and equiactive to the same drug in the carrageenin paw edema test. All the compounds inhibited the 3α-HSD, but no correlation was observed with the paw…

Solid lipid nanoparticles containing vancomycin: preparation, characterization and in vitro anti-Staphylococcus aureus biofilms activity

Coagulase-negative staphylococci and Staphylococcus aureus are the most common cause of nosocomial infections and can induce a wide spectrum of diseases associated with remarkable morbidity and mortality. Biofilms of staphylococci are intrinsically resistant to conventional antibiotics and, being commonly associated with implanted medical device, such as catheters and vascular grafts, have the potential to cause blood-stream infections. The paper describes the preparation and characterization of vancomycin-loaded Solid Lipid Nanoparticles (SLNs) and in vitro studies of the inhibition of Staphylococcus aureus ATCC 29213 biofilms in the presence of this nanoparticle system. Methods. The vanco…

Non-covalent interactions in organotin(IV) derivatives of 5,7-ditertbutyl- and 5,7-diphenyl-1,2,4-triazolo[1,5-a]pyrimidine as recognition motifs in crystalline self- assembly and their in vitro antistaphylococcal activity

Non-covalent interactions are known to play a key role in biological compounds due to their stabilization of the tertiary and quaternary structure of proteins [1]. Ligands similar to purine rings, such as triazolo pyrimidine ones, are very versatile in their interactions with metals and can act as model systems for natural bio-inorganic compounds [2]. A considerable series (twelve novel compounds are reported) of 5,7-ditertbutyl-1,2,4-triazolo[1,5-a]pyrimidine (dbtp) and 5,7-diphenyl- 1,2,4-triazolo[1,5-a]pyrimidine (dptp) were synthesized and investigated by FT-IR and 119Sn Mössbauer in the solid state and by 1H and 13C NMR spectroscopy, in solution [3]. The X-ray crystal and molecular str…

ChemInform Abstract: Synthesis of New 3-(3-Phenyl-isoxazol-5-yl) or 3-[(3-Phenyl-isoxazol-5-yl)amino] Substituted 4(3H)-Quinazolinone Derivatives with Antineoplastic Activity.

A novel series of 3-(3-phenyl-isoxazol-5-yl) or 3-[(3-phenyl-isoxazol-5-yl)amino] substituted 4(3H)-quinazolinone derivatives was synthesized. The compounds were tested for their antineoplastic activity in vitro against Raji (human Burkitt limphoma). K-562 (human chronic myelogeneous leukemia) and U937 (human histiocytic limphoma) cell lines. The most active quinazolinones showed IC50 values in the range 16-30 microM.

One-step synthesis, crystallographic studies and antimicrobial activity of new 4-diazopyrazole derivatives

Summary A number of new 4-diazopyrazole derivatives were prepared by the reaction of 1- R -3-methyl-5(R 1 -substituted)benzamidopyrazoles with a sevenfold excess of nitrous acid in acetic medium. The compounds were tested for activity against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus faecalis, Listeria monocytogenes, Candida albicans, Candida tropicalis and Paecilomyces varioti . The highest microbial susceptibility was shown by Gram-positive bacteria, with minimum inhibitory concentrations (MIC) in the range 0.5–12.5 μg/mL. For S aureus the R 1 substituents were screened utilizing the Topliss operational scheme. The 4-nitro g…

N-(INDAZOLYL)BENZAMIDO DERIVATIVES AS CDK1 INHIBITORS: DESIGN, SYNTHESIS, BIOLOGICAL ACTIVITY, AND MOLECULAR DOCKING STUDIES

A series of N-1H-indazole-1-carboxamides has been synthesized and their effects on both CDK1/cyclin B and the K-562 (human chronic myelogenus leukemia) cell line were evaluated. Using a computational model, we have observed that all the most active compounds 9e, f, i-n exhibited the same binding mode of purvanalol A in the ATP-binding cleft. Although they were able to moderately inhibit the leukemic cell line K-562 and to show inhibitory activity against the Cdc2-Cyclin B kinase in the low micromolar range, they turned out to be non-cytotoxic against HuDe (IZSL) primary cell cultures from human derm. These preliminary results are quite encouraging in view of the low toxicity demonstrated by…

ANTIPROLIFERATIVE ACTIVITY OF CITRUS JUICES AND HPLC EVALUATION OF THEIR FLAVONOID COMPOSITION

The antiproliferative activity of fresh fruit juices extracted from Citrus sinensis (cv. Washington Navel and cv. Sanguinello), C. deliciosa cv. Avana, C. clementina cv. Nules, C. aurantium subsp. myrtifolia , was evaluated against K562 (human chronic myelogenous leukemia), HL-60 (human leukemia) and MCF-7 (human breast adenocarcinoma) cell lines. All the juices tested showed antiproliferative activity. Moreover, the pattern of the main flavanone compounds in the juices has been determined by HPLC analysis.

Novel Sortase A Inhibitors to Counteract Gram-Positive Bacterial Biofilms

Sortase A (SrtA) is a membrane enzyme responsible for the covalent anchoring of surface proteins on the cell wall of Gram-positive bacteria. Nowadays it is considered an interesting target for the development of new anti-infective drugs which aim to interfere with important Gram-positive virulence mechanisms. Along the years, we studied the anti-staphylococcal and anti-biofilm activity of some natural and synthetic polyhalogenated pyrrolic compounds, called pyrrolomycins. Some of them were active on Gram-positive pathogens at a μg/mL range of concentration (1.5-0.045 μg/mL) and showed a biofilm inhibition in the range of 50-80%. [1-3] In light of these encouraging results, herein we present…

Novel chemical countermeasures against staphylococcal biofilms

Some natural and synthetic related pyrrolomycins, a family of halogenated pyrrole antibiotics, showed anti-biofilm properties in vitro at low concentration (0.045μg/mL) against preformed staphylococcal biofilms. Moreover, considering the human cell toxicity, the selectivity indexes (ratio of cytotoxicity to antibiofilm activity) of some of them were very interesting. The present study aims to investigate if the pyrrolomycins could also prevent staphylococcal biofilm formation. The evaluation of S.aureus ATCC 25923 biofilm formation inhibition was conducted by safranin staining method. At tested concentrations of 0.18, 0.09, 0.045 μg/mL (concentrations much lower than MIC value determined on…

Synthesis, characterization, crystal structures and in vitro antistaphylococcal activity of organotin(IV) derivatives with 5,7-disubstituted-1,2,4-triazolo[1,5-a]pyrimidine.

Abstract New organotin(IV) complexes of 5,7-ditertbutyl-1,2,4-triazolo[1,5-a]pyrimidine ( dbtp ) and 5,7-diphenyl-1,2,4-triazolo[1,5-a]pyrimidine ( dptp ) with 1:1 and/or 1:2 stoichiometry were synthesized and investigated by X-ray diffraction, FT-IR and 119 Sn Mossbauer in the solid state and by 1 H and 13 C NMR spectroscopy, in solution. Moreover, the crystal and molecular structures of Et 2 SnCl 2 (dbtp) 2 and Ph 2 SnCl 2 (EtOH) 2 (dptp) 2 are reported. The complexes contain hexacoordinated tin atoms: in Et 2 SnCl 2 (dbtp) 2 two 5,7-ditertbutyl-1,2,4-triazolo[1,5-a]pyrimidine molecules coordinate classically the tin atom through N(3) atom and the coordination around the tin atom shows a …

Selective decontamination of the digestive tract in adult-to-adult living related liver transplant patients: a single centre experience

Synthesis and biofilm formation reduction of pyrazole-4-carboxamide derivatives in some Staphylococcus aureus strains

The ability of several N-phenyl-1H-pyrazole-4-carboxamide derivatives and other pyrazoles opportunely modified at the positions 3, 4 and 5, to reduce the formation of the biofilm in some Staphylococcus aureus strains (ATCC 29213, ATCC 25923 and ATCC 6538) were investigated. All the tested compounds were able, although to a different extent, to reduce the biofilm formation of the three bacterial strains considered. Among these, the 1-(2,5-dichlorophenyl)-5-methyl-N-phenyl-1H-pyrazole-4-carboxamide 14 resulted as the best inhibitor of biofilm formation showing an IC50 ranging from 2.3 to 32 μM, against all the three strains of S. aureus. Compound 14 also shows a good protective effect in vivo…

Pharmaceutical potential of synthetic and natural pyrrolomycins

The emergence of antibiotic resistance is currently considered one of the most important global health problem. The continuous onset of multidrug-resistant Gram-positive and Gram-negative bacterial strains limits the clinical efficacy of most of the marketed antibiotics. Therefore, there is an urgent need for new antibiotics. Pyrrolomycins are a class of biologically active compounds that exhibit a broad spectrum of biological activities, including antibacterial, antifungal, anthelmintic, antiproliferative, insecticidal, and acaricidal activities. In this review we focus on the antibacterial activity and antibiofilm activity of pyrrolomycins against Gram-positive and Gram-negative pathogens…

Phytochemical-rich extracts of Helianthemum lippii possess antimicrobial, anticancer, and anti-biofilm activities

Helianthemum lippii is a perennial shrubby plant growing in the sandy environments of Italy, Mediterranean countries of North Africa and Middle East. H. lippii is used in traditional medicine but there are very few reports referring to the phytochemical characterization, the ethnopharmacology, and the biological activity of H. lippii. The goal of this study was todetermine the phytochemical composition of different H. lippii extracts, cold (CME) and hot (HME) methanol, cold (CPEE) and hot (HPEE) petroleum ether, as well as to evaluate their anticancer and antimicrobial activities and biofilm formation reduction. Fifty-fours phytocompounds have been determined by HPLC-UV-ESI-QTOF-MS analysis…

Synthesis and antifungal activity of new N-isoxazolyl-2-iodobenzamides

N-Isoxazolyl-2-iodobenzamides 3 and 9, with a benodanil-like structure, were synthesized by refluxing in acetic acid the corresponding benzotriazinones 2 and 8 with potassium iodide for 1 h with the aim to ascertain if they were active as fungicides against Phytophthora citricola Saw., Botrytis cinerea Pers., Rhizoctonia sp. and Alternaria sp. Among the tested iodo derivatives, compounds 3b and 9a possess interesting activities against the aforesaid fungal strains in several cases similar to that of benodanil I taken as reference drug.

Phytochemical and anti-staphylococcal biofilm assessment of Dracaena draco L. Spp. draco resin

Background: Dracaena draco L. ssp. draco is known as the “dragon's blood tree” and it is endemic from the Canary Islands and Morocco. Objective: Carry out phytochemical investigation of acetonic extracts of red resin obtained from the trunk of D. draco, to obtain to the isolation of the most abundant resin constituents, belonging to the class of flavonoids: flavans, along with homoisoflavans and homoisoflavanones. Materials and Methods: The structures of the isolated compounds were established by Nuclear Magnetic Resonance (NMR) and mass spectrometry data and comparison with literature data. The acetonic extract was evaluated for its anti-staphylococcal properties against two reference stra…

Photothermal nanofibrillar membrane based on hyaluronic acid and graphene oxide to treat Staphylococcus aureus and Pseudomonas aeruginosa infected wounds.

Here we reported the fabrication of an electrospun membrane based on a hyaluronic acid derivative (HA-EDA) to be used as a bandage for the potential treatment of chronic wounds. The membrane, loaded with graphene oxide (GO) and ciprofloxacin, showed photothermal properties and light-triggered drug release when irradiated with a near-infrared (NIR) laser beam. Free amino groups of HA-EDA derivative allowed autocrosslinking of the elec- trospun membrane; thus, a substantial enhancement in the hydrolytic resistance of the patch was obtained. In vitro antibacterial activity studies performed on Staphylococcus aureus and Pseudomonas aeruginosa revealed that such electrospun membranes, due to the…

Targeting the Sortase A Transpeptidase to Tackle Gram-positive Pathogens

The virulence factors include the cell-wall associated proteins called MSCRAMMs (microbial surface components recognizing adhesive matrix molecules) that can promote the adhesion to host proteins, for example, the fibronectin that is very common in host tissues. The cellwall associated proteins are necessary for host colonization, invasion, immune evasion and biofilm formation [4]. The biofilms, multistratified bacterial communities that grow on a biological or artificial surface, are responsible for chronic infectious diseases and for device or biomaterial associated infections, and are more resistant to host immune defence system and to conventional antibiotics [5].

Food Processing and Foodborne Illness

Food processing means manipulation of raw materials from plants or animals into food. Since agriculture and animal husbandry were established postharvest procedures were necessary to preserve for a longer time the increasing food supplies coming from the fields and domesticated animals. Food is one of the best culture medium for a lot of microorganisms and preventing food spoilage caused by enzymes and microorganisms is crucial. Deterioration of food is caused mainly by three natural processes: 1. Oxidation – vegetables after harvesting or meat after animal slaughtering get in contact with the oxygen in the air that makes them rancid and unpleasant. 2. Enzyme action – all food contains natu…

2-cinnamamido, 2-(3-phenylpropiolamido) and 2-(3-phenylpropanamido)benzamides: synthesis, antiproliferative activity and mechanism of action

Several new 2-cinnamamido, 2-(3-phenylpropiolamido) and 2-(3-phenylpropanamido)benzamides were synthesized by stirring in pyridine the opportune acid chlorides with the appropriate anthranilamide derivatives. Some of the synthesized compounds were evaluated for their in vitro antiproliferative activity against a panel of 5 human cell lines (K562 human chronic myelogenous leukemia cells, MCF-7 breast cancer cells, HTC-116 and HT26 colon cancer cells and NCI H460 non-small cell lung cancer cells).

Synthesis and anti-staphylococcal activity of new 4-diazopyrazole derivatives.

Abstract Several new 4-diazopyrazole derivatives 6a – g and 9a – c were obtained by the reaction of 1-(R-substituted-phenyl)-3-(1,3-dimethyl-1 H -pyrazol-5-yl)ureas 5a – g and N -(1,3-dimethyl-1 H -pyrazol-5-yl)-2-(R-substituted-phenyl)acetamides 8a – c respectively with a sevenfold excess of nitrous acid in acetic acid solution. The compounds were assayed for their activity against the Staphylococcus aureus reference strains ATCC 25923, ATCC 29213 and ATCC 6538, as well as six veterinary strains. The best anti-staphylococcal profile was showed by [(R-substituted-phenyl)acetyl](4-diazonio-1,3-dimethyl-1 H -pyrazol-5-yl)azanides 9a , c . Compound 9c was also able at 3.1 μg mL −1 to inhibit o…

Novel marine invertebrate-derived antimicrobial peptides against staphylococcal biofilm

Comparison among the responses of the greater wax moth, Galleria mellonella and red palm weevil Rhynchophorus ferrugineus to the entomopathogenic nematodes, Steinernema carpocapsae

The entomopathogenic nematode-bacterium complex of Steinernema-Xenorhabdus has high potential as lethal biological control agent against many insect pest species. The Red Palm Weevil (RPW) Rhynchophorus ferrugineus (Coleoptera: Curculionidae) is an important worldwide palm trees pest. This insect is a quarantined pest, accidentally introduced in Sicily in 2005. The pest is killed by Steirnenema carpocapsae, but nematodes are unable to reproduce in the RPW larvae. This research try to understand the reasons of the inability of S. carpocapsae to complete its life cycle in the host comparing what happens in one of the most suitable host, the greater wax moth, Galleria mellonella (Lepidoptera: …

ATTIVITA' ANTIBIOFILM DI OLI ESSENZIALI OTTENUTI DA RESINE NATURALI DEL GENERE BOSWELLIA (BURSERACEAE)

Fragments of β-thymosin from the sea urchinParacentrotus lividusas potential antimicrobial peptides against staphylococcal biofilms

The immune mediators in echinoderms can be a potential source of novel antimicrobial peptides (AMPs) applied toward controlling pathogenic staphylococcal biofilms that are intrinsically resistant to conventional antibiotics. The peptide fraction <5 kDa from the cytosol of coelomocytes of the sea urchin Paracentrotus lividus (5-CC) was tested against a group of Gram-positive and Gram-negative pathogen reference strains. The 5-CC of P. lividus was active against all planktonic-tested strains but also showed antibiofilm properties against staphylococcal strains. Additionally, we demonstrated the presence of three small peptides in the 5-CC belonging to segment 9-41 of a P. lividusβ-thymosin. T…

COMPOSIZIONE CHIMICA E ATTIVITA' BIOLOGICA DI OLI ESSENZIALI OTTENUTI DA RESINE NATURALI DEL GENERE BOSWELLIA(BURSERACEAE)

Sant'Anna Jamming

ADI Design Index è la selezione annuale del miglior design italiano ed è parte integrante del sistema di selezione del Premio Compasso d’Oro ADI: ogni anno, grazie all’Osservatorio Permanente del Design ADI – un gruppo di lavoro costituito da oltre cento esperti, anche esterni all’associazione – prende in esame su tutto il territorio italiano il design dei nuovi prodotti messi in produzione. Dopo una strutturata selezione (commissioni territoriali, tematiche e comitato di selezione finale), i migliori prodotti di design vengono presentati, con un commento critico che evidenzia i motivi della scelta, su ADI Design Index. I volumi diventano la base su cui lavora la giuria internazionale del C…

Synthesis and antiproliferative activity of 3-amino-N-phenyl-1H-indazole-1-carboxamides

Abstract A series of new 3-amino-N-phenyl-1H-indazole-1-carboxamides 10 have been prepared from commercially available phenyl isocyanate precursors 8 and 3-aminoindazole 9. Some of the synthesized compounds were evaluated for their in vitro antineoplastic activity against 60 human cell lines derived from seven clinically isolated cancer types (lung, colon, melanoma, renal, ovarian, brain, and leukemia) according to the NCI standard protocol. The test results indicated that 3-amino-1H-indazole-1-carboxamides 10 were endowed with an interesting antiproliferative activity. The most active compounds of this series, 10d,e, were able to inhibit cell growth of many neoplastic cell lines at concent…

Pursuing softer urban mobility behaviors through game-based apps

Cities are currently engaged through their urban policies in pushing people towards less environmentally impacting mobility modalities: therefore, cycling and walking are strongly promoted, especially by means of new and wider limited traffic and no-cars zones. In this paper, the effectiveness of the new smartphones and apps-based technologies in modifying the mobility behaviors of citizens towards more sustainable choices has been investigated. Specifically, the potential of a smartphone app, directly involving citizens by means of a game rewarding the most sustainable trips, has been tested on a university commuters' group. These latter, starting from their current mobility situation, wer…

It is Time for Action in the Struggle against Antibiotic-Resistance, Let’s Start Reducing or Replacing Antibiotics in Agriculture

Million people around the world are infected each year and thousands of them die from pathogens that are resistant to the treatment by any of known antibiotics [1]. The excessive use and abuse of antibiotics in clinical setting and in agriculture, added to the great ability of microorganisms to evolve, are the causes of the wide spread of isolates resistant to all major classes of current antibiotics. It is time for action in order to tackle antimicrobial-resistance (AMR), which can be considered a major threat to global health care and security. While we are waiting for new antimicrobial molecules and strategies, shorter-term approaches are needed to address the menace of AMR and preserve …

Popolazioni microbiche del corpo umano. Microbioti e Uomo: un rapporto intenso tra microrganismi ed esseri umani

ChemInform Abstract: Synthesis of New 2-(((Phenoxy or Phenyl)acetyl)amino)benzoic Acid Derivatives as 3α-Hydroxysteroid Dehydrogenase Inhibitors and Potential Antiinflammatory Agents.

A number of 2-([(phenoxy or phenyl)acetyl]amino)benzoic acid derivatives were prepared in about 50% yield from (phenoxy or phenyl)acetyl chloride and anthranilic acid derivatives. All the compounds were tested as in vitro inhibitors of 3 alpha-hydroxysteroid dehydrogenase, since enzyme inhibition predicts potential antiinflammatory activity in vivo. The most active compounds 3 l, m, s are about 3.5 times more active than acetylsalicylic acid (ASA). Activity is influenced by electronic as well as steric effects.

The gut bacterial community of the red palm weevil Rhynchophorus ferrugineus (Olivier, Coleoptera, Curculionidae) larvae

The red palm weevil (RPW), Rhynchophorus ferrugineus (Olivier, Coleoptera, Curculionidae) is the major pest of palm trees in the Mediterranean area. Damages are caused mainly by the endophytophagous larvae that consume the palm tender soft tissues making galleries and producing a wet “frass” with a characteristic fermented odour. The culturable bacterial community associated to the frass produced by RPW larvae inside Phoenix canariensis trees is mainly composed of facultative anaerobe gamma-proteobacteria that have their closest phylogenetic relatives in the gut microbiome of other endophytophagous and xilophagous coleopteran as bark beetles and other plant biomass-degrading insects (leaf-c…

ChemInform Abstract: Synthesis and Antiproliferative Activity of Novel 3-(Indazol-3-yl)-quinazolin-4(3H)-one and 3-(Indazol-3-yl)-benzotriazin-4(3H)-one Derivatives.

Several new 3-(indazol-3-yl)-quinazolin-4(3H)-one and 3-(indazol-3-yl)-benzotriazin-4(3H)-one derivatives 5 and 6 were synthesized and tested for their in vitro antiproliferative activity against Raji, K562, and K562-R cell lines. The pharmacological screening showed that some 2, 6, or 7-substituted quinazolinones 5 posses a significant antiproliferative activity, with a percentage growth inhibition ranging from 44.8% to 100% at 50 microM, which was higher than that showed by the unsubstituted derivative 5a previously synthesized. For the most active compounds 5d, 5f, and 5g the IC50 were recorded.

Oregano essential oils activity against Listeria monocitogenes biofilms

Synthesis, characterization and in vitro antimicrobial activity of triorganotin(IV)fusidate complexes

Synthesis and antioproliferative activity of new derivatives containing the policyclic sistem 5,7:7,13-dimethanopyrazolo[3,4-b]pyrazolo[3'.4':2,3]azepino[4,5-f]azocine

By reacting methylaminopyrazoles with hexane-2,5-dione in 1,4-dioxane in the presence of p-toluensulfonic acid, new derivatives containing the policyclic sistem 5,7:7,13-dimethanopyrazolo[3,4-b]pyrazolo[3'.4':2,3]azepino[4,5-f]azocine were obtained. The new synthesized compounds were tested preliminarly at 10 microM against five human cancer cell lines showing a range of inhibition of 20-62% against the most susceptible cell lines K562 and HCT116.

New digital instruments for the community building in housing cooperatives

The research starts from a study carried out for Confcooperative Habitat, which focused on the systematic analysis of the materials produced for the launch of a new season of the cooperative movement. The goal is to improve the active action on communities for a tangible social impact able to propose a model that knows how to enhance the common urban spaces within the interventions. Finding the new needs and the new processes that characterize living, outlined also in their condominium and urban dimension of ‘common good’, therefore of ‘common housing’. The procedural model proposed and modulated in an evolved platform, seeks to multiply the common practices of living in the city and live i…

Discovery of a new class of sortase a transpeptidase inhibitors to tackle gram-positive pathogens: 2-(2-phenylhydrazinylidene)alkanoic acids and related derivatives

A FRET-based random screening assay was used to generate hit compounds as sortase A inhibitors that allowed us to identify ethyl 3-oxo-2-(2-phenylhydrazinylidene)butanoate as an example of a new class of sortase A inhibitors. Other analogues were generated by changing the ethoxycarbonyl function for a carboxy, cyano or amide group, or introducing substituents in the phenyl ring of the ester and acid derivatives. The most active derivative found was 3-oxo-2-(2-(3,4dichlorophenyl)hydrazinylidene)butanoic acid (2b), showing an IC50 value of 50 µM. For a preliminary assessment of their antivirulence properties the new derivatives were tested for their antibiofilm activity. The most active compo…

Paracentrin 1, a synthetic antimicrobial peptide fragment of a beta-thymosin from the sea-urchin Paracentrotus lividus, interferes with staphylococcal and Pseudomonas aeruginosa biofilm formation

ANTI-STAPHYLOCOCCAL BIOFILM ACTIVITY OF NOVEL SORTASE A (SRTA) INHIBITORS

Pathogenic staphylococci have an extraordinary ability to form biofilms. This characteristic is likely the most important virulence factor of staphylococci in the development of the chronic form of infectious diseases and in biomaterial associated infections (BAI). Staphylococcal biofilms are particularly dangerous because they are more resistant to host immune defence system and have a significantly increased tolerance to conventional antibiotics. There is undoubtedly an urgent need for novel treatments, strategies and anti-staphylococcal biofilm agents. The Sortase A (SrtA) transpeptidase is responsible for covalent anchoring to the cell wall of various surface proteins (FnbpA, FnbpB, Clf…

New Bioactive Peptides from the Mediterranean Seagrass Posidonia oceanica (L.) Delile and Their Impact on Antimicrobial Activity and Apoptosis of Human Cancer Cells

The demand for new molecules to counter bacterial resistance to antibiotics and tumor cell resistance is increasingly pressing. The Mediterranean seagrass Posidonia oceanica is considered a promising source of new bioactive molecules. Polypeptide-enriched fractions of rhizomes and green leaves of the seagrass were tested against Gram-positive (e.g., Staphylococcus aureus, Enterococcus faecalis) and Gram-negative bacteria (e.g., Pseudomonas aeruginosa, Escherichia coli), as well as towards the yeast Candida albicans. The aforementioned extracts showed indicative MIC values, ranging from 1.61 &mu;g/mL to 7.5 &mu;g/mL, against the selected pathogens. Peptide fractions were further analyzed thr…

New Topsentin analogs as inhibitors of biofilm formation

ChemInform Abstract: Synthesis and anti-Staphylococcal Activity of New Halogenated Pyrroles Related to Pyrrolomycins F.

The chemical synthesis of new halogenated pyrroles related to pyrrolomycins F is described and the anti-staphylococcal activity compared. The replacement of 4′-bromo atom of parent compounds with two chloro atoms at 3′ and 5′ position increase the antibacterial activity against a reference strain of S. aureus.

Pharmaceutical Approaches to Target Antibiotic Resistance Mechanisms

There is urgent need for new therapeutic strategies to fight the global threat of antibiotic resistance. The focus of this Perspective is on chemical agents that target the most common mechanisms of antibiotic resistance such as enzymatic inactivation of antibiotics, changes in cell permeability, and induction/activation of efflux pumps. Here we assess the current landscape and challenges in the treatment of antibiotic resistance mechanisms at both bacterial cell and community levels. We also discuss the potential clinical application of chemical inhibitors of antibiotic resistance mechanisms as add-on treatments for serious drug-resistant infections. Enzymatic inhibitors, such as the deriv…

SYNTHESIS, CHARACTERIZATION AND IN VITRO CYTOTOXICITY STUDIES OF A MACROMOLECULAR CONJUGATE OF PACLITAXEL BEARING OXYTOCIN AS TARGETING MOIETY.

The present study describes the experimental synthetic procedure and the characterization of a new polyaspartamide macromolecular prodrug of paclitaxel, bearing oxytocin residues as targeting moieties. In vitro stability studies of bioconjugate, performed in media mimicking biological fluids (buffer solutions at pH 7.4 and 5.5) and in human plasma, evidenced the high stability of the targeting portion (oxytocin)-polymer linkage and the ability of this conjugate to release linked paclitaxel in a prolonged way in plasma. Moreover, preliminary in vitro antiproliferative studies, carried out on MCF-7 cells, that are oxytocin receptor positive cells, showed that the polymeric conjugate has the s…

Complessi di di- e triorganostagno(IV) con [1,2,4]triazolo-[1,5-a]pirimidina e suoi derivati 5- e 7-sostituiti

Branched High Molecular Weight Glycopolypeptide With Broad-Spectrum Antimicrobial Activity for the Treatment of Biofilm Related Infections.

There are few therapeutic options to simultaneously tackle Staphylococcus aureus and Pseudomonas aeruginosa, two of the most relevant nosocomial and antibiotic-resistant pathogens responsible for implant, catheters and wound severe infections. The design and synthesis of polymers with inherent antimicrobial activity have gained increasing attention as a safe strategy to treat multi-drug-resistant microbes. Here, we tested the activity of a new polymeric derivative with glycopolypeptide architecture (PAA-VC) bearing l-arginine, vancomycin, and colistin as side chains acting against multiple targets, which give rise to a broad spectrum antimicrobial activity favorably combining specific and n…

Synthesis and antimicrobial activity of new bromine-rich pyrrole derivatives related to monodeoxypyoluteorin

The synthesis and antimicrobial activity of new pyrrole derivatives structurally related to monodeoxypyoluteorin are described. The insertion of a keto or methylene spacer between the phenol group and the pyrroloyl moiety of brominated 2-(2'-hydroxybenzoyl)pyrroles leads to a decrease of the antibacterial activity.

Enzymatic Synthesis and Antimicrobial Activity of Oligomer Analogues of Medicinal Biopolymers from Comfrey and Other Species of the Boraginaceae Family

This study reports the first enzymatic synthesis leading to several oligomer analogues of poly[3-(3,4-dihydroxyphenyl)glyceric acid]. This biopolymer, extracted from plants of the Boraginaceae family has shown a wide spectrum of pharmacological properties, including antimicrobial activity. Enzymatic ring opening polymerization of 2-methoxycarbonyl-3-(3,4-dibenzyloxyphenyl)oxirane (MDBPO) using lipase from Candida rugosa leads to formation of poly[2-methoxycarbonyl-3-(3,4-dibenzyloxyphenyl)oxirane] (PMDBPO), with a degree of polymerization up to 5. Catalytic debenzylation of PMDBPO using H2 on Pd/C yields poly[2-methoxycarbonyl-3-(3,4-dihydroxyphenyl)oxirane] (PMDHPO) without loss in molecul…

Right to the future

Dalla fine della seconda guerra mondiale, le città hanno affrontato un rapido e incontrollabile sviluppo e pur coprendo, oggi, appena il 2% della superficie del pianeta, sono l’habitat per più del 50% degli abitanti della Terra, consumano oltre l’80% delle risorse disponibili ed emettono più del 70% delle sostanze inquinanti. È nel 1976 che l’assemblea generale delle Nazioni Unite indice la prima conferenza per gli insediamenti umani (human settlements) a Vancouver, riconoscendo l’impatto devastante che le condizioni degli insediamenti abitativi hanno sullo sviluppo sociale ed economico, sull’uomo e sull’ecologia urbana. Questa conferenza, oggi conosciuta come Habitat I, avvia un processo d…

In vitro anti-biofilm activity of Boswellia spp. oleogum resin essential oils

Aims:  To evaluate the anti-biofilm activity of the commercially available essential oils from two Boswellia species. Methods and Results:  The susceptibility of staphylococcal and Candida albicans biofilms was determined by methyltiazotetrazolium (MTT) staining. At concentrations ranging from 217·3 μg ml−1 (25% v/v) to 6·8 μg ml−1 (0·75% v/v), the essential oil of Boswellia papyrifera showed considerable activity against both Staphylococcus epidermidis DSM 3269 and Staphylococcus aureus ATCC 29213 biofilms. The anti-microbial efficacy of this oil against S. epidermidis RP62A biofilms was also tested using live/dead staining in combination with fluorescence microscopy, and we observed that …

Nano into Micro Formulations of Tobramycin for the Treatment of Pseudomonas aeruginosa Infections in Cystic Fibrosis.

Here, nano into micro formulations (NiMs) of tobramycin for the treatment of Pseudomonas aeruginosa airway infections in cystic fibrosis (CF) are described. NiMs were produced by spray drying a solution containing polymers or sugars and a nanometric polyanion–tobramcyin complex (PTC), able to achieve a prolonged antibiotic release. NiMs properties were compared to TOBIPodhaler(Novartis), the only one commercially available dry powder inhalatory formulation based on porous microparticles. Produced NiMs showed adequate characteristics for pulmonary administration, as spherical shape, micrometric size, and high cytocompatibility toward human bronchial epithelial cells. Contrarily to TOBIPodhal…

The immune mediators in echinoderms as souce of novel AMPs against microbial biofilms

A Novel Peptide with Antifungal Activity from Red Swamp Crayfish Procambarus clarkii

The defense system of freshwater crayfish Procambarus clarkii as a diversified source of bioactive molecules with antimicrobial properties was studied. Antimicrobial activity of two polypeptide-enriched extracts obtained from hemocytes and hemolymph of P. clarkii were assessed against Gram positive (Staphylococcus aureus, Enterococcus faecalis) and Gram negative (Pseudomonas aeruginosa, Escherichia coli) bacteria and toward the yeast Candida albicans. The two peptide fractions showed interesting MIC values (ranging from 11 to 700 μg/mL) against all tested pathogens. Polypeptide-enriched extracts were further investigated using a high-resolution mass spectrometry and database search and 14 n…

PRELIMINARY COMPARISON FOR GENES INVOLVED IN BIOFILMS IN COAGULASE-NEGATIVE STAPHYLOCOCCI (CONS) AND S. AUREUS STRAINS ISOLATED FROM MILK SAMPLES OF SICILIAN FARMS

New Anti-Adhesion Agents In The Development of Antivirulence Drugs

Gram-positive bacteria are a significant cause of nosocomial and community-acquired infections associated with diseases of high morbidity and mortality. Moreover, antibiotic resistance of important Gram-positive pathogens, such as Staphylococcus aureus, Streptococcus pneumoniae and Enterococcus faecalis is one of the major worldwide health problems. Over the last decade, many studies have focused on agents that target the virulence of important pathogens without killing or inhibiting their growth therefore imposing limited selective pressure to promote the development and spread of resistance mechanisms [1]enterococci and streptococci, sortase A plays a critical role in Gram-positive bacter…

NEW ANTIMICROBIAL AND ANTI-BIOFILM AGENTS FROM THE SEA URCHIN PARACENTROTUS LIVIDUS

Bacterial metal nanoparticles to develop new weapons against bacterial biofilms and infections

The widespread use of antibiotics has resulted in the outbreak and spread of antibiotic-resistant pathogens. Bacterial antibiotic resistance may develop at cellular and community levels. In the latter case, it is based on tolerance which implicates the shift from a free-living form of life (i.e., planktonic) to a sessile multi-stratified community (i.e., biofilm). Metal nanoparticles (MNPs) have been shown to be promising candidates as antimicrobial agents. MNPs are able to interact with and penetrate bacterial biofilms, thus, resulting effective antibiofilm compounds. Another interesting aspect is the possibility of using plants, fungi, yeasts, and bacteria to obtain biogenic MNPs (BMNP). …

1,2,4-Oxadiazole topsentin analogs as staphylococcal biofilm inhibitors targeting the bacterial transpeptidase sortase A

The inhibition or prevention of biofilm formation represents an emerging strategy in the war against antibiotic resistance, interfering with key players in bacterial virulence. This approach includes the inhibition of the catalytic activity of transpeptidase sortase A (Srt A), a membrane enzyme responsible for covalently attaching a wide variety of adhesive matrix molecules to the peptidoglycan cell wall in Gram-positive strains. A new series of seventeen 1,2,4-oxadiazole derivatives was efficiently synthesized and screened as potential new anti-virulence agents. The ability of inhibiting biofilm formation was evaluated against both Gram-positive and Gram-negative pathogens. Remarkably, all…

Developing Antibiofilm Fibrillar Scaffold with Intrinsic Capacity to Produce Silver Nanoparticles

The development of biomedical systems with antimicrobial and antibiofilm properties is a difficult medical task for preventing bacterial adhesion and growth on implanted devices. In this work, a fibrillar scaffold was produced by electrospinning a polymeric organic dispersion of polylactic acid (PLA) and poly(&alpha;,&beta;-(N-(3,4-dihydroxyphenethyl)-L-aspartamide-co-&alpha;,&beta;-N-(2-hydroxyethyl)-L-aspartamide) (PDAEA). The pendant catechol groups of PDAEA were used to reduce silver ions in situ and produce silver nanoparticles onto the surface of the electrospun fibers through a simple and reproducible procedure. The morphological and physicochemical characterization of the obtained s…

Solid lipid nanoparticles containing tamoxifen characterization and in vitro antitumoral activity.

Solid lipid nanoparticles (SLNs) containing tamoxifen, a nons- teroidal antiestrogen used in breast cancer therapy, were prepared by microemulsion and precipitation techniques. Tamoxifen loaded SLNs seem to have dimensional properties useful for parenteral administration, and in vitro plasmatic drug release studies demon- strated that these systems are able to give a prolonged release of the drug in the intact form. Preliminary study of antiproliferative ac- tivity in vitro, carried out on MCF-7 cell line (human breast cancer cells), demonstrated that SLNs, containing tamoxifen showed an antitumoral activity comparable to free drug. The results of char- acterization studies and of in vitro …

Synthesis and antileukemic activity of new 3-(1-phenyl-3-methylpyrazol-5-yl)-2-styrylquinazolin-4(3H)-ones.

Abstract 3-(1-Phenyl-3-methylpyrazol-5-yl)-2-styrylquinazolin-4(3H)-ones 14a–q and 15a–q were synthesized by refluxing in acetic acid the corresponding 2-methylquinazolinones 12 and 13 with the opportune benzoic aldehyde for 12 h. The synthesized styrylquinazolinones 14a–q and 15a–q were tested in vitro for their antileukemic activity against L1210 (murine leukemia), K562 (human chronic myelogenous leukemia) and HL60 (human leukemia) cell lines showing in some cases good activity.

Right to the Future

During the last decade, the city of Palermo has been undergoing relevant transformations from various perspectives. This has been the consequences of a multitude of circumstances, European financial crisis, migrants/refugees crisis, a new administration of the city and an increased awareness and responsibility among the citizens. Various national and international recognitions (Italian Cultural Capital 2018, the European Biennial of Contemporary Art, Manifesta 12, Youth Capital 2017) have confirmed that they are on the right path. This positive moment has been launched and, progressively, rid- den by many young professionals that decided to challenge the present situation by investing their…

Echinoderm Antimicrobial Peptides: The Ancient Arms of the Deuterostome Innate Immune System

Antimicrobial peptides (AMPs) are widely expressed in organisms and have been linked to innate and acquired immunity in vertebrates. These compounds are constitutively expressed from different cellular types to interact directly with infectious agents and/or modulate immunoreactions. In invertebrates, including echinoderms, which lack a vertebrate-type adaptive immune system, AMPs represent the major humoral defense system against infection, showing a diverse spectrum of action mechanisms, most of them related to plasma membrane disturbance and lethal alteration of microbial integrity. Here, we summarize the knowledge of AMPs in echinoderms as Strongylocins identified in the sea urchins, St…

Paracentrin 1, a synthetic antimicrobial peptide from the sea-urchin Paracentrotus lividus, interferes with staphylococcal and Pseudomonas aeruginosa biofilm formation

The rise of antibiotic-resistance as well as the reduction of investments by pharmaceutical companies in the development of new antibiotics have stimulated the investigation for alternative strategies to conventional antibiotics. Many antimicrobial peptides show a high specificity for prokaryotes and a low toxicity for eukaryotic cells and, due to their mode of action the development of resistance is considered unlikely. We recently characterized an antimicrobial peptide that was called Paracentrin 1 from the 5-kDa peptide fraction from the coelomocyte cytosol of the Paracentrotus lividus. In this study, the chemically synthesized Paracentrin 1, was tested for its antimicrobial and antibiof…

ANTIMICROBIAL PEPTIDES FROM COELOMOCYTES CYTOSOL OF PARACENTROTUS LIVIDUS WITH PHARMACEUTICAL POTENTIAL AS ANTI-STAPHYLOCOCCI BIOFILM AGENTS

Aims: To evaluate the anti-biofilm activity of the commercially available essential oils from two Boswellia species. Methods and Results: The susceptibility of staphylococcal and Candida albicans biofilms was determined by methyltiazotetrazolium (MTT) staining. At concentrations ranging from 217Æ3 lg ml)1 (25% v ⁄ v) to 6Æ8 lg ml)1 (0Æ75% v ⁄ v), the essential oil of Boswellia papyrifera showed considerable activity against both Staphylococcus epidermidis DSM 3269 and Staphylococcus aureus ATCC 29213 biofilms. The anti-microbial efficacy of this oil against S. epidermidis RP62A biofilms was also tested using live ⁄ dead staining in combination with fluorescence microscopy, and we observed t…

Synthesis and biological evaluation of new 2-{[(2E)-3-phenylprop-2-enoyl]amino}benzamides

Biological Responses of &lt;I&gt;Rhynchophorus ferrugineus&lt;/I&gt; (Coleoptera: Curculionidae) to &lt;I&gt;Steinernema carpocapsae&lt;/I&gt; (Nematoda: Steinernematidae)

Rhynchophorus ferrugineus (Olivier 1790) (Coleoptera: Curculionidae) is becoming a serious problem in Mediterranean areas where it is well-adapted, and now is present even in the United States (California). The infestations are primarily in urban areas where chemical control is not advisable and million of Euros are spent to control it. The effects of the entomopathogenic nematode Steinernema carpocapsae (Nematoda: Steinernematidae) on mortality, growth, as well as the immune activity of R. ferrugineus larvae, were investigated. R. ferrugineus mortality exhibited a positive trend with the dosage and duration of exposure to S. carpocapsae. The median lethal dose and median lethal time, impor…

ANTIMICROBIAL ACTIVITY FROM POLYPEPTIDE-RICH EXTRACTS OF THE SEAGRASS POSIDONIA OCEANICA

The present study was carried out to assess the antibacterial, antifungal and antibiofilm properties of polypeptide-rich extracts isolated from green leaves and rhizomes of Mediterranean seagrass Posidonia oceanica (L. Delile) (Posidoniaceae). The seagrass was collected, washed with freshwater, grinded with liquid nitrogen in order to obtain fine powders that were exposed to extraction by acetic acid and antiproteases. The crude extracts isolated from leaves and rhizomes of P. oceanica were subjected to microbiological assays to evaluate the antibacterial, antifungal and antibiofilm activity of polypeptide fraction against two reference bacterial strains Staphylococcus aureus ATCC 25923 and…

Biofilm Related to Animal Health, Zoonosis and Food Transmitted Diseases: Alternative Targets for Antimicrobial Strategy?

The biofilm is a complex community of microbial cells that are associated with a surface and enclosed in a self-produced biopolymer matrix. Such structured community is a response of bacteria to a signal system named quorum sensing (QS) constituted by inter-cell communication through the production of small molecules called autoinducers (AIs) that trigger a cascade of events in gene expression. When the concentration of the AIs molecules reach a certain threshold, the bacterial population acts as a single organism, collectively expressing virulence or biofilm forming genes. Gram-positive bacteria use modified oligopeptides as QS effectors molecules.

Biofilm capability of staphylococcus strains isolated from food and the anti-biofilm activity of a chemically synthesized pyrrolomycin

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Thiazoles, Their Benzofused Systems, and Thiazolidinone Derivatives: Versatile and Promising Tools to Combat Antibiotic Resistance.

Thiazoles, their benzofused systems, and thiazolidinone derivatives are widely recognized as nuclei of great value for obtaining molecules with various biological activities, including analgesic, anti-inflammatory, anti-HIV, antidiabetic, antitumor, and antimicrobial. In particular, in the past decade, many compounds bearing these heterocycles have been studied for their promising antibacterial properties due to their action on different microbial targets. Here we assess the recent development of this class of compounds to address mechanisms underlying antibiotic resistance at both bacterial-cell and community levels (biofilms). We also explore the SAR and the prospective clinical applicati…

Preliminary results on antimicrobial activity of Rhynchophorous ferrugineus hemolymph

Rhynchophorus ferrugineus (Coleoptera: Curculionidae), known as the Red Palm Weevil (RPW) and accidentally introduced in the Mediterranean areas, is considered a quarantine pest for tree palms especially in the urban environment. In order to understand the relationship among potential pathogens and RPW several studies were carried out on RPW immune system. Here we report the results of a preliminary study undertaken to investigate the effect of naturally occurring antimicrobial activities present both in the cell free hemolymph and in hemocytes lysate supernatant of RPW. The hemolymph was extracted from the older larvae sampled from infested palm trees. The protein fractions were extracted …

Synthesis and Antileukemic Activity of New 3-(5-Methylisoxazol-3-yl) and 3-(Pyrimidin-2-yl)-2-styrylquinazolin-4(3H)-ones.

3-(3-Methylisoxazol-5-yl) and 3-(pyrimidin-2-yl)-2-styrylquinazolin-4(3H)-ones 8a–l and 9a,c–e,h–l were synthesized by refluxing in acetic acid the corresponding 2-methylquinazolinones 6 and 8 with the opportune benzoic aldehyde for 12 h. The synthesized styrylquinazolinones 8a–l and 9a,c–e,h–l were tested in vitro for their antileukemic activity against L-1210 (murine leukemia), K-562 (human chronic myelogenous leukemia) and HL-60 (human leukemia) cell lines showing in some cases good activity.

GENETICS AND BIOFILM ANALYSIS ON STRAINS OF E.COLI ISOLATED FROM ANIMALS WITH DIARRHOEIC PROBLEMS

AMPs and biotechnology application for new generation of medical devices

Solid Lipid Nanoparticles Containing Vancomycin

Staphylococci coagulase-negative and Staphylococcus aureus are the most common cause of nosocomial infections and can induce a wide spectrum of diseases associated with remarkable morbidity and mortality. Biofilms of staphylococci are intrinsically resistant to conventional antibiotics and, being commonly associated with implanted medical device, such as catheters and vascular grafts, have the potential to cause blood-stream infections. In recent years increasing attention has been addressed to Solid Lipid Nanoparticles (SLNs), thanks to their biodegradability and ability to entrap a variety of biologically active compounds, in the area of modified drug delivery technology in the attempt to…

Synthesis, characterization, and in vitro antimicrobial activity of organotin(IV) complexes with triazolo-pyrimidine ligands containing exocyclic oxygen atoms

Abstract Tri-organotin(IV) complexes of the triazolo-pyrimidine derivatives 4,5-dihydro-5-oxo-[1,2,4]triazolo-[1,5 a ]pyrimidine (5HtpO), 4,7-dihydro-5-methyl-7-oxo-[1,2,4]triazolo-[1,5 a ]pyrimidine (HmtpO), and 4,5,6,7-tetrahydro-5,7-dioxo-[1,2,4]triazolo-[1,5 a ]pyrimidine (H 2 tpO 2 ), and the diorganotin derivative n -Bu 2 Sn(tpO 2 ), were synthesized and characterized by means of infrared and 119 Sn Mossbauer spectroscopy. In all the complexes obtained the triazolopyrimidines act as multidentate ligands producing polymeric structures. A trigonal bipyramidal arrangement of the ligands around the tin atom is proposed for triorganotin(IV) derivatives, with organic groups on the equatoria…

Gamification or Game Design? A case study in the field of sustainable commuting

In the last few years, the debate among designers and sustainability experts has brought attention to many different behavioural change approaches and techniques and particularly on “gamification” processes able to better motivate and engage students or even nudge people (consumers) to more environmentally and socially responsible habits (Mousumi, 2021).But since 2011, most of the contradictions about “gamifying” boring or unpleasant experiences have been loudly shared by game designers and thinkers worldwide (Bogost, 2014). It seems that the goal of changing people’s unsustainable behaviours can be achieved by designing brand new sustainable experiences instead of gamifying the unsustainab…

ChemInform Abstract: One-Step Synthesis, Crystallographic Studies and Antimicrobial Activity of New 4-Diazopyrazole Derivatives.

Summary A number of new 4-diazopyrazole derivatives were prepared by the reaction of 1- R -3-methyl-5(R 1 -substituted)benzamidopyrazoles with a sevenfold excess of nitrous acid in acetic medium. The compounds were tested for activity against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus faecalis, Listeria monocytogenes, Candida albicans, Candida tropicalis and Paecilomyces varioti . The highest microbial susceptibility was shown by Gram-positive bacteria, with minimum inhibitory concentrations (MIC) in the range 0.5–12.5 μg/mL. For S aureus the R 1 substituents were screened utilizing the Topliss operational scheme. The 4-nitro g…

Discovery of a New Class of Sortase A Transpeptidase Inhibitors to Tackle Gram-positive Pathogens: 2-Phenylhydrazonoalkanoic Acid Derivatives

There is an urgent need of anti-virulence agents effective in the prevention or eradication of biofilms that are intrinsically resistant to conventional antibiotics. If we consider that the first step of staphylococcal pathogenesis and of biofilm formation is the bacterial adhesion, promoted by the surface exposed proteins at the cell wall, we believe that new anti-virulence agents could be developed by using as a target the Sortase A (SrtA), the enzyme responsible of linking surface exposed proteins to peptidoglycan. Therefore, SrtA inhibitors could act as anti-adhesion agents useful to prevent Gram positive virulence mechanisms as well as a virulence mechanism based on biofilm formation. …

The potential of antimicrobial peptides isolated from freshwater crayfish species in new drug development: A review

Abstract The much-publicised increased resistance of pathogenic bacteria to conventional antibiotics has focused research effort on the characterization of new antimicrobial drugs. In this context, antimicrobial peptides (AMPs) extracted from animals are considered a promising alternative to conventional antibiotics. In recent years, freshwater crayfish species have emerged as an important source of bioactive compounds. In fact, these invertebrates rely on an innate immune system based on cellular responses and on the production of important effectors in the haemolymph, such as AMPs, which are produced and stored in granules in haemocytes and released after stimulation. These effectors are …

Identification of New Antimicrobial Peptides from Mediterranean Medical Plant Charybdis pancration (Steinh.) Speta

The present work was designed to identify and characterize novel antimicrobial peptides (AMPs) from Charybdis pancration (Steinh.) Speta, previously named Urginea maritima, is a Mediterranean plant, well-known for its biological properties in traditional medicine. Polypeptide-enriched extracts from different parts of the plant (roots, leaves and bulb), never studied before, were tested against two relevant pathogens, Staphylococcus aureus and Pseudomonas aeruginosa. With the aim of identifying novel natural AMPs, peptide fraction displaying antimicrobial activity (the bulb) that showed minimum inhibitory concentration (MICs) equal to 30 &micro

Multiple Theories of Change for innovation governance

The Theory of Change approach aims to clarify the underlying logic of an intervention by first identifying the problem addressed and the desired outcome, and then backwards mapping the actions taken and the expected results and outcomes. In so doing, it aims to simplify the expression of intermediate goals and indicators and provide a common reference for the participants and stakeholders of the intervention itself. As such, it is similar to corporate ‘mission statements’ in that it aims to provide a single, unifying description of the what, why and how of an intervention. By framing the approach in terms of the ‘change’ required as a means of addressing a problem, Theory of Change is essen…

Pyrrolomycins as potential anti-staphylococcal biofilms agents

With the goal of discovering new anti-infective agents active against microbial biofilms, this investigation focused on some natural pyrrolomycins, a family of halogenated pyrrole antibiotics. In this study the anti-staphylococcal biofilm activity of pyrrolomycins C, D, F1, F2a, F2b, F3 and of the synthesized related compounds I, II, III were investigated. The susceptibility of six staphylococcal biofilms was determined by methyltiazotetrazolium staining. Most of the compounds were active at concentrations of 1.5 microg ml(-1) with significant inhibition percentages. A few of the compounds were active at the lowest screening concentration of 0.045 microg ml(-1). The population log reduction…

Molecular characterization of biofilm-forming S.aureus field isolates and their treatment

A synthetic derivative of antimicrobial peptide holothuroidin 2 from mediterranean sea cucumber (Holothuria tubulosa) in the control of Listeria monocytogenes

Due to the limited number of available antibiotics, antimicrobial peptides (AMPs) are considered antimicrobial candidates to fight difficult-to-treat infections such as those associated with biofilms. Marine environments are precious sources of AMPs, as shown by the recent discovery of antibiofilm properties of Holothuroidin 2 (H2), an AMP produced by the Mediterranean sea cucumber Holothuria tubulosa. In this study, we considered the properties of a new H2 derivative, named H2d, and we tested it against seven strains of the dangerous foodborne pathogen Listeria monocytogenes. This peptide was more active than H2 in inhibiting the growth of planktonic L. monocytogenes and was able to interf…

MUV: A Game to Encourage Sustainable Mobility Habits

This working paper investigates the question of changing people mobility towards more sustainable habits involving them in an engaging gameplay. The work is performed within MUV H2020 research and innovation action. The game design, definition and features have been co-created through the involvement of different citizens and stakeholders in six European neighbourhoods. The paper discusses the game design as resulting from co-creation and co-design experiences with each neighbourhood communities involved in initial phases. The paper argues that the local co-design activities have influenced the game definition, together with the community engagement approach. The MUV gameplay approach resul…

Synthetic small molecules as anti-biofilm agents in the struggle against antibiotic resistance

Abstract Biofilm formation significantly contributes to microbial survival in hostile environments and it is currently considered a key virulence factor for pathogens responsible for serious chronic infections. In the last decade many efforts have been made to identify new agents able to modulate bacterial biofilm life cycle, and many compounds have shown interesting activities in inhibiting biofilm formation or in dispersing pre-formed biofilms. However, only a few of these compounds were tested using in vivo models for their clinical significance. Contrary to conventional antibiotics, most of the anti-biofilm compounds act as anti-virulence agents as they do not affect bacterial growth. I…

Salmo salar fish waste oil: Fatty acids composition and antibacterial activity

Background and aims Fish by-products are generally used to produce fishmeal or fertilizers, with fish oil as a by-product. Despite their importance, fish wastes are still poorly explored and characterized and more studies are needed to reveal their potentiality. The goal of the present study was to qualitatively characterize and investigate the antimicrobial effects of the fish oil extracted from Salmo salar waste samples and to evaluate the potential use of these compounds for treating pathogen infections. Methods Salmo salar waste samples were divided in two groups: heads and soft tissues. Fatty acids composition, and in particular the content in saturated (SAFAs), mono-unsaturated (MUFA…

Synthesis and Anti-Staphylococcal Activity of New Halogenated Pyrroles Related to Pyrrolomycins F

The chemical synthesis of new halogenated pyrroles related to pyrrolomycins F is described and the anti-staphylococcal activity compared. The replacement of 4′-bromo atom of parent compounds with two chloro atoms at 3′ and 5′ position increase the antibacterial activity against a reference strain of S. aureus.

2,6-Disubstituted imidazo[2,1-b][1,3,4]thiadiazole derivatives as potent staphylococcal biofilm inhibitors.

Abstract A class of 36 new 2-(6-phenylimidazo[2,-1-b][1,3,4]thiadiazol-2-yl)-1H-indoles was efficiently synthesized and evaluated for their anti-biofilm properties against the Gram-positive bacterial reference strains Staphylococcus aureus ATCC 25923, S. aureus ATCC 6538 and Staphylococcus epidermidis ATCC 12228, and the Gram-negative strains Pseudomonas aeruginosa ATCC 15442 and Escherichia coli ATCC 25922. Many of these new compounds, were able to inhibit biofilm formation of the tested staphylococcal strains showing BIC50 lower than 10 μg/ml. In particular, derivatives 9c and 9h showed remarkable anti-biofilm activity against S. aureus ATCC 25923 with BIC50 values of 0.5 and 0.8 μg/ml, r…

ANTIMICROBIAL AND ANTIBIOFILM ACTIVITY OF A PEPTIDE IDENTIFIED IN THE SEAGRASS POSIDONIA OCEANICA

Synthesis and antifungal activity of new N-(1-phenyl-4-carbetoxypyrazol-5-yl)-, N-(indazol-3-yl)- and N-(indazol-5-yl)-2-iodobenzamides

N-(1-Phenyl-4-carbetoxypyrazol-5-yl)-, N-(indazol-3-yl)- and N-(indazol-5-yl)-2-iodobenzamides 6, with a Benodanil-like structure, were synthesized by refluxing in acetic acid the corresponding benzotriazinones 5 with potassium iodide for 1 h in order to study the role on the antifungal activity of the N-substitution with an aromatic heterocyclic system on benzamide moiety. Among the tested iododerivatives, compounds 6d,f,g,h possess interesting activities toward some phytopathogenic fungal strains.

Biogenic iron-silver nanoparticles inhibit bacterial biofilm formation due to Ag+ release as determined by a novel phycoerythrin-based assay

Silver nanoparticles (Ag-NPs) can be considered as a cost-effective alternative to antibiotics. In the presence of Fe(III)-citrate and Ag+, Klebsiella oxytoca DSM 29614 produces biogenic Ag-NPs embedded in its peculiar exopolysaccharide (EPS). K. oxytoca DSM 29614 was cultivated in a defined growth medium–containing citrate (as sole carbon source) and supplemented with Ag+ and either low or high Fe(III) concentration. As inferred from elemental analysis, transmission and scanning electron microscopy, Fourier transform infrared spectrometry and dynamic light scattering, Ag-EPS NPs were produced in both conditions and contained also Fe. The production yield of high-Fe/Ag-EPS NPs was 12 times …

Composizione e attività biologica di “idrolati” di agrumi

Gli idrolati, o acque aromatiche, sono prodotti naturali ricavati dalla distillazione di piante o parti di piante fresche che conservano intatte le loro proprietà e possono essere utilizzati a diverso scopo1. Essi sono comunemente considerati un sottoprodotto degli oli essenziali, ma in realtà, data la diversa composizione e la conseguente maggiore delicatezza, hanno un loro apprezzabile utilizzo, legato comunque al mantenimento delle proprietà delle piante da cui derivano. Nell’industria agrumaria gli idrolati sono il risultato della produzione degli oli essenziali attraverso spremitura a freddo delle bucce degli agrumi e sono considerati un rifiuto da smaltire. Lo studio della composizion…

Antibacterial Activity of Desert Truffles from Saudi Arabia Against Staphylococcus aureus and Pseudomonas aeruginosa

Abstract Medicinal mushrooms represent an unlimited source of polysaccharides with nutritional, antitumoral, antibacterial, and immune-stimulating properties. Traditional studies of epigeous higher Basidiomycetes have recently been joined by studies of hypogeous fungi and, in particular, of so-called desert truffles. With the aim to obtain novel agents against bacteria of clinical importance, we focused on the edible desert truffle mushrooms Tirmania pinoyi, Terfezia claveryi, and Picoa juniperi as sources of new antimicrobial agents. In particular, we investigated the in vitro antibacterial activity of acid-soluble protein extracts (aqueous extracts) of these 3 species against the Gram-pos…

Chemical composition and antimicrobial activity of some oleogum resin essential oils from Boswellia spp. (Burseraceae)

The chemical composition of Boswellia carteri (Somalia), B. papyrifera (Ethiopia), B. serrata (India) and B. rivae (Ethiopia) oleogum resin essential oils was investigated using GC-MS to identify chemotaxonomy marker components. Total ion current peak areas gave good approximations to relative concentrations based on GCMS peak areas. B. carteri and B. serrata oleogum resin oils showed similar chemical profiles, with isoincensole and isoincensole acetate as the main diterpenic components. Both n-octanol and n-octyl acetate, along with the diterpenic components incensole and incensole acetate, were the characteristic compounds of B. papyrifera oleogum resin oil. Hydrocarbon and oxygenated mon…

In Vitro Antiproliferative properties and flavanone profiles of six grapefruit (Citrus paradisi Macf.) cultivars

A Gamified Mobility Experience

We believe in the use of urban games to define new enjoyable experiences, change citizens’ unsustainable habits and educate them to new environment-and social-friendly ones. This paper presents MUV, an innovative action that has the power to engage citizens and foster sustainable mobility behaviors. MUV complements engaging HMIs with a participatory method within an iterative innovation process called the virtuous cycle (understand, involve, co-create, implement, experiment). The innovation process has led to a new game dynamic: Mobility as a Sport. It results in a rewarding personal mobility experience; the same rewarding sensations the athletes feel when they improve their results.

Fabrication of silver nanoparticles by a diethylene triamine-hyaluronic acid derivative and use as antibacterial coating

In this work a synthetic protocol for the functionalization of hyaluronic acid with diethylenetriamine (DETA) was standardized. HA-DETA derivatives were characterized by NMR and proton carbon correlation analysis HSQC and HMBC to confirm chemical structure. A selected derivative was used to set up a green fabrication procedure for HA-DETA capped silver nanoparticles with the aim to achieve a polymeric based coating with potential application in the treatment of medical devices associated infections. Data from UV-visible spectroscopy, electron scanning and transmission microscope (STEM), photoelectric spectroscopy (XPS) and rheological characterization were combined to characterize the HA-DE…

A multifunctional peptidomimetic macromolecule to fight polymicrobial infections

Echinoderm Antimicrobial Peptides to Contrast Human Pathogens

Increased attention has been focused in marine invertebrates as a source of bioactive molecules for biomedical applications. Many bioactive molecules are part of the innate immune system. Some more recently isolated compounds, mainly from sea urchin and sea cucumber are antimicrobial peptides (AMP) active against Gram positive, Gram negative and fungi. In this review we described the most recent studies on AMP isolated from echinoderms. The AMP are little peptides <10 kDa with cationic charge and amphipathic structure. Recently, it was demonstrated that in the coelomocyte lysates of Paracentrotus. lividus and Holothuria tubulosa AMP are present with activity against staphylococcal and Pseud…

Gender differences in the immune system activities of sea urchin Paracentrotus lividus

In the immune system of vertebrates, gender-specific differences in individual immune competence are well known. In general, females possess more powerful immune response than males. In invertebrates, the situation is much less clear. For this purpose we have chosen to study the immune response of the two sexes of the echinoderm Paracentrotus lividus in pre- and post-spawning phases. The coelomic fluid from the echinoderms contains several coelomocyte types and molecules involved in innate immune defenses. In this article we report that the degree of immune responses in the P. lividus differs according to sex in both pre- and post-spawning phases. We found in all tests that females were mor…

Novel Sortase A (SrtA) inhibitors interfere with the formation of staphylococcal biofilms

Staphylococcus aureus, due to its wide arsenal of virulence factors, is a very versatile pathogen responsible for a wide variety of infectious diseases. The virulence factors include the cell-wall associated proteins that have a direct role in the first stage of pathogenesis. The Sortase A (SrtA) transpeptidase is responsible for covalent anchoring to the cell wall of various surface proteins and it is considered a good target to design new antivirulence agents. In this study, we report the identification of an inhibitor of SrtA afforded from the random screening of a small molecular library of around 150 synthetic compounds, through a high throughput assay by using the standard Dabcyl-QALP…

Sortase A: An ideal target for anti-virulence drug development

Sortase A is a membrane enzyme responsible for the anchoring of surface-exposed proteins to the cell wall envelope of Gram-positive bacteria. As a well-studied member of the sortase subfamily catalysing the cell wall anchoring of important virulence factors to the surface of staphylococci, enterococci and streptococci, sortase A plays a critical role in Gram-positive bacterial pathogenesis. It is thus considered a promising target for the development of new anti-infective drugs that aim to interfere with important Gram-positive virulence mechanisms, such as adhesion to host tissues, evasion of host defences, and bio fi lm formation. The additional properties of sortase A as an enzyme that i…

Antimicrobial Activity of the Desert Truffles "Tirmania pinoyi" and "Terfezia claveryi" Against Human Pathogens

The development of novel antimicrobials in the struggle against pathogens and antibiotic resistance is one of the most important global challenges of our time. Medicinal mushrooms represent an unlimited source of polysaccharides with nutritional, antitumoral, antibacterial and immune stimulating properties1. In recent years the traditional studies on epigeous higher Basidiomycetes have been joined by those on hypogeous fungi and in particular on the so-named “desert truffles”. Ali2 demonstrated that organic extraction of truffles of genus Tirmania and Terfezia possess antimicrobial activity with broad-spectrum effects against Gram positive, Gram negative, aerobic and anaerobic bacteria …

Antibiofilm activity of a novel pyrrolomycin against staphylococcal biofilms of veterinary interest

Staphylococcal Biofilms:Challenges in the Discovery of Novel Antiinfective Agents

Staphylococci can induce a wide spectrum of infectious diseases that are associated with remarkable morbidity and mortality [1]. In fact, community and hospital-acquired methicillin resistant Staphylococcus aureus (MRSA) is a major health problem that has created a pressing need for novel therapeutic options [2]. Importantly, pathogenic staphylococci have not only an amazing ability to acquire resistance to antibiotics, but also to form biofilms, bacterial communities that grow on surfaces and are surrounded by a self-produced polymer matrix. This latter characteristic is likely the most important virulence factor of staphylococci in the development of the chronic form of infectious disease…

The Re-Discovering of Old Molecules to face the Antibiotic Crisis

Drug-resistant bacteria are responsible for 5,000 deaths a year in the UK, 25,000 deaths a year in Europe and it is estimated that at least two million people in the United States are infected each year and 23,000 of those die from pathogens that are not susceptible to the treatment by any of current antibiotics [13]. Antibiotic resistance of common pathogenic microorganisms is a topic of great concern and it has finally attracted the attention of mass-media and of some global leaders. For example, President Obama, answering the question “Is antibiotic resistance a threat to global security?” has replied ”Effective antibiotics are vital to our national security... They are, quite simply, es…

The Future of Antibiotic: From the Magic Bullet to the Smart Bullet

Antimicrobial and Antibiofilm Activity of a Recombinant Fragment of β-Thymosin of Sea Urchin Paracentrotus lividus

With the aim to obtain new antimicrobials against important pathogens such as Staphylococcus aureus and Pseudomonas aeruginosa, we focused on antimicrobial peptides (AMPs) from Echinoderms. An example of such peptides is Paracentrin 1 (SP1), a chemically synthesised peptide fragment of a sea urchin thymosin. In the present paper, we report on the biological activity of a Paracentrin 1 derivative obtained by recombination. The recombinant paracentrin RP1, in comparison to the synthetic SP1, is 22 amino acids longer and it was considerably more active against the planktonic forms of S. aureus ATCC 25923 and P. aeruginosa ATCC 15442 at concentrations of 50 &micro

Immune mediators of sea-cucumber Holothuria tubulosa (Echinodermata) as source of novel antimicrobial and anti-staphylococcal biofilm agents

The present study aims to investigate coelomocytes, immune mediators cells in the echinoderm Holothuria tubulosa, as an unusual source of antimicrobial and antibiofilm agents. The activity of the 5kDa peptide fraction of the cytosol from H. tubulosa coelomocytes (5-HCC) was tested against a reference group of Gram-negative and Gram-positive human pathogens. Minimal inhibitory concentrations (MICs) ranging from 125 to 500 mg/ml were determined against tested strains. The observed biological activity of 5-HCC could be due to two novel peptides, identified by capillary RP-HPLC/nESI-MS/MS, which present the common chemical-physical characteristics of antimicrobial peptides. Such peptides were c…

Antibacterial activity of Mediterranean Oyster mushrooms, species of genus Pleurotus (higher Basidiomycetes).

Extracts of the Mediterranean culinary-medicinal Oyster mushrooms Pleurotus eryngii var. eryngii, P. eryngii var. ferulae, P. eryngii var. elaeoselini, and P. nebrodensis were tested for their in vitro growth inhibitory activity against a group of bacterial reference strains of medical relevance: Staphylococcus aureus ATCC 25923, S. epidermidis RP62A, Pseudomonas aeruginosa ATCC 15442, and Escherichia coli ATCC10536. All of the Pleurotus species analyzed inhibited the tested microorganisms in varying degrees. The data included in this paper for P. nebrodensis and P. eryngii var. elaeoselinii are new reports.

Antimicrobial and antiproliferative activity of Athamanta sicula L. (Apiaceae).

Background: Athamanta sicula L., a member of Apiaceae, is an annual perennial herb and it is known in Sicilian popular medicine with the name of “spaccapietre” (rock splitters), because fresh roots infusions are indicated as diuretic and used in the treatment of diseases of the urinary tract, and to dissolve kidney stones. Materials and Methods: Acetone extracts of leaves, flowers, and stems of A. sicula L. were investigated in vitro for antibacterial and cytotoxic activities. Antimicrobial activity was carried out against bacterial and fungal strains and antiproliferative activity against a group of human cancer cell lines (K-562, NCI-H460, and MCF-7). Results: All acetone extracts, apiol …

Control of Growth and Persistence of Listeria monocytogenes and β-Lactam-Resistant Escherichia coli by Thymol in Food Processing Settings

The main objective of this study was to evaluate the efficacy of thymol in controlling environmental contamination in food processing facilities. The effect of thymol was tested as an agent to prevent planktonic and bacterial biofilm growth of twenty-five Listeria monocytogenes isolates from a variety of foods and five Escherichia coli isolates from a farm. The E. coli isolates were positive for extended spectrum &beta

3,4,5,3',5'-Pentabromo-2-(2'idrossibenzoil) pirrolo I: un potenziale lead-compound nella ricerca di nuovi agenti antibatterici e antibiofilm

Pyrrolomycins as antimicrobial agents. Microwave-assisted organic synthesis and insights into their antimicrobial mechanism of action

Abstract New compounds able to counteract staphylococcal biofilm formation are needed. In this study we investigate the mechanism of action of pyrrolomycins, whose potential as antimicrobial agents has been demonstrated. We performed a new efficient and easy method to use microwave organic synthesis suitable for obtaining pyrrolomycins in good yields and in suitable amount for their in vitro in-depth investigation. We evaluate the inhibitory activity towards Sortase A (SrtA), a transpeptidase responsible for covalent anchoring in Gram-positive peptidoglycan of many surface proteins involved in adhesion and in biofilm formation. All compounds show a good inhibitory activity toward SrtA, havi…

ChemInform Abstract: Synthesis, Crystallographic Studies and Biological Evaluation of Some 2-Substituted 3-Indazolyl-4(3H)-quinazolinones and 3-Indazolyl-4(3H)- benzotriazinones.

Essential oil components of orange peels and antimicrobial activity

In this study, the orange peel of 12 cultivars of Citrus sinensis from central-eastern Sicily was employed to obtain essential oils and extracts. The ones were extracted through steam distillation, the others through extraction in hexane. Chemical constituents were evaluated in terms of qualitative and quantitative analyses by gas chromatography/mass spectrometry. Fifty-four components were identified in the steam essential oils and 44 in the extracts. In all the cultivars, the main component is d-limonene (73.9–97%); discrete percentages of linalool, geraniol and nerol were also found. Cluster analysis based on essential oils composition showed a certain degree of affinity between cultivar…

Antimicrobial and anti-staphylococcal biofilm peptides from the sea-urchin Paracentrotus lividus

Correction to: Echinodermata: The Complex Immune System in Echinoderms

A Win-Win Scheme for Improving the Environmental Sustainability of University Commuters’ Mobility and Getting Environmental Credits

European Union Member States are called upon to meet internationally proposed environmental goals. This study is based, in particular, on the recommendation of the European Union (EU), which encourages Member States to pursue effective policies to reduce greenhouse gas (GHGs) emissions, including through appropriate changes in the behavioral habits of citizens. In this respect, among the main sectors involved, transport and mobility should certainly be mentioned. National institutions should be adequately involved in order to achieve the objectives set; in this regard, universities must certainly be considered for their educational value. These latter, for instance, could commit to improvin…

Synthesis, spectroscopic characterization and in vitro antimicrobial activity of diorganotin(IV) dichloride adducts with [1,2,4]triazolo-[1,5-a]pyrimidine and 5,7-dimethyl-[1,2,4]triazolo-[1,5-a]pyrimidine

Abstract The heterocyclic ligands [1,2,4]triazolo-[1,5-a]pyrimidine (tp) and 5,7-dimethyl-[1,2,4]triazolo-[1,5-a]pyrimidine (dmtp), react with diorganotin dichlorides giving the addition compounds Me2SnCl2(tp)2, Et2SnCl2(tp)2, Me2SnCl2(dmtp)2, Et2SnCl2(dmtp)2, Bu2SnCl2(dmtp), Ph2SnCl2(dmtp). The organotin:ligand stoichiometry goes from 1:2 to 1:1 by increasing the steric hindrance of the organic groups bound to tin. The compounds have been characterized by means of infrared, 119Sn Mossbauer and 1H AND 13C NMR spectroscopy. The ligands presumably coordinate to tin classically through the nitrogen atom at the position 3. The 1:1 complexes adopt trigonal bipyramidal structures, with the organi…

3,4,5,3’,5’-pentabromo-2-(2’-hydroxybenzoyl) pyrrole: a potential lead compound as anti Gram-positive and anti biofilm agent

The activity against Gram-positive bacteria of 3,4,5,3 ,5 -pentabromo-2-(2 -hydroxybenzoyl)pyrrole I, a synthetic anti-bacterial compound related to pyrrolomycins, was tested in vitro using seven reference bacterial strains and Staphylococcus epidermidis and Staphylococcus aureus preformed biofilms. Compound I was active against all strains tested, with minimum inhibitory concentration (MIC) values ranging from 0.002 to 0.097 mg/l and minimum bactericidal concentrations (MBCs) from 0.37 to 12.5 mg/l. Compound I was also active at low concentrations against preformed S. epidermidis and S. aureus biofilms.

Echinodermata: The complex immune system in echinoderms

View references (418) The Echinodermata are an ancient phylum of benthic marine invertebrates with a dispersal-stage planktonic larva. These animals have innate immune systems characterized initially by clearance of foreign particles, including microbes, from the body cavity of both larvae and adults, and allograft tissue rejection in adults. Immune responsiveness is mediated by a variety of adult coelomocytes and larval mesenchyme cells. Echinoderm diseases from a range of pathogens can lead to mass die-offs and impact aquaculture, but some individuals can recover. Genome sequences of several echinoderms have identified genes with immune function, including expanded families of Toll-like r…

EFFECTOR CELLS FROM PARACENTROTUS LIVIDUS AS SOURCE OF NEW ANTI-STAPHYLOCOCCI BIOFILM AGENTS

Art for Change

Una serie di documentari brevi (26 minuti ad episodio) che racconta quattro progetti di design per il sociale tra Italia e Spagna. Quando l’arte entra nelle aree marginali delle nostre città produce concrete trasformazioni: la street art del progetto di Borgo Vecchio Factory a Palermo, l’Accademia del Cinema dei Ragazzi di Enziteto a Bari, il Museo dell’Altro e dell’Altrove nelle ex fabbriche Fiorucci di Roma, la comunità di Puerta del Angel a Madrid.

IN VITRO ANTI-STAPHYLOCOCCAL BIOFILM ACTIVITY OF SOME NATURAL PYRROLOMYCINS AND SYNTHETIC DERIVATIVES

Synthesis and pharmacological evaluation of 1-methyl-5- [substituted-4(3H)-oxo-1,2,3-benzotriazin-3-yl]-1H-pyrazole-4-acetic acid derivatives

Several new 1-methyl-5-[substituted-4-oxo-1,2,3-benzotriazin-3-yl] -1H-pyrazole-4-acetic acids and their ethyl ester derivatives were prepared. The compounds were tested for analgesic and antiinflammatory activities, acute toxicity, ulcerogenic effect, and as in vitro inhibitors of 3 alpha-hydroxysteroid dehydrogenase (3 alpha-HSD), since it is claimed that the inhibition of such an enzyme predicts in vivo antiinflammatory activity. Some compounds were more active than phenylbutazone in the phenylbenzoquinone and acetic acid peritonitis tests, and equiactive to the same drug in the carrageenin paw edema test. All the compounds inhibited the 3 alpha-HSD, but no correlation was observed with …

A POLYCARBOXYLIC/AMINO FUNCTIONALIZED HYALURONIC ACID DERIVATIVE FOR THE PRODUCTION OF pH SENSIBLE HYDROGELS IN THE PREVENTION OF BACTERIAL ADHESION ON BIOMEDICAL SURFACES

A graft copolymer derivative of hyaluronic acid bearing pendant amino and short polymethacrylate portions (HA-EDA-BMP-MANa) has been employed for the production of a pH sensible vancomycin releasing hydrogel and studied in vitro to test its potential anti adhesive property against Staphylococcus aureus colonization. The copolymer obtained through atom transfer radical polymerization bears chargeable (carboxyl and amino groups) portions and it could be formulated as a hydrogel at a concentration of 10% w/v. The HA-EDA-BMP-MANa hydrogels, produced at three different pH values (5, 6 and 7, respectively), were formulated with or without the addition of vancomycin (2% w/v). The vancomycin releas…

4-Diazopyrazole Derivatives as Potential New Antibiofilm Agents

&lt;i&gt;Background:&lt;/i&gt; The recognition that chronic infections and infections associated with medical devices are biofilm related has been the impulse for investigating the antibiofilm properties of some diazopyrazoles biologically active as antimicrobials. &lt;i&gt;Methods:&lt;/i&gt; The susceptibility of staphylococcal biofilms was determined at concentrations ranging from 25 to 1.5 µg/ml using crystal violet and methylthiazotetrazolium (MTT) staining. In the case of &lt;i&gt;Candida albicans,&lt;/i&gt; we first assessed the anti-germ tube formation effect of 4-NO&lt;sub&gt;2&lt;/sub&gt; (compound 1c) and then we evaluated its antibiofilm activity at concentrations ranging from 10…

Synthesis, crystallographic studies and biological evaluation of some 2-substituted 3-indazolyl-4(3H)-quinazolinones and 3-indazolyl-4(3H)-benzotriazinones

Antimicrobial and antiproliferative activity of Peucedanum nebrodense (Guss.) Strohl.

Abstract Acetone extract of Peucedanum nebrodense (Guss.) Strohl., a rare endemic species from the Madonie mountains (Sicily), was tested in vitro for its antimicrobial activity against bacterial reference strains and antiproliferative activity against K562 (human chronic myelogenous leukemia), HL-60 (human leukemia) and L1210 (murine leukemia) cell lines. The acetone extract showed antiproliferative IC 50 values in the range of 14–0.27 μg/ml.

Oxidative halogenation of substituted pyrroles with Cu(II). PartIV.Bromination of 2-(2′-hydroxybenzoyl)pyrrole. A new synthesis of bioactive analogs of monodeoxypyoluteorin

The selective bromination with copper(II) bromide of the pyrrole ring in 2-(2'-hydroxybenzoyl)pyrrole (II) in the heterogeneous phase is des- cribed giving in almost quantitative yield the 4,5-dibromo derivative (VI). The subsequent introduction of halogen into the phenol moiety was observed when the reaction was perfomed in the homogeneous phase with an excess of halogenating agent. The pentabromo derivative (IX), a com- pound very active against Staphylococcus aureus (mic=17 nmoles per dm -3 ), was obtained by exhaustive bromination of the title compound. Poor yields of chloro derivatives of (II) were obtained by reaction of the parent compound with copper(II) chloride

A peptide from human β thymosin as a platform for the development of new anti-biofilm agents for Staphylococcus spp. and Pseudomonas aeruginosa

Conventional antibiotics might fail in the treatment of biofilm-associated infections causing infection recurrence and chronicity. The search for antimicrobial peptides has been performed with the aim to discover novel anti-infective agents active on pathogens in both planktonic and biofilm associated forms. The fragment 9-19 of human thymosin β4 was studied through 1 μs MD simulation. Two main conformations of the peptide were detected, both constituted by a central hydrophobic core and by the presence of peripheral charged residues suggesting a possible mechanism of interaction with two models of biological membranes, related to eukaryotic or bacterial membrane respectively. In addition, …

A new class of phenylhydrazinylidene derivatives as inhibitors of Staphylococcus aureus biofilm formation

In the struggle against the emergence of the antibiotic resistance, new molecules targeting biofilm formation could be useful as adjuvant of conventional antibiotics. This study focused on a new class of 2-phenylhydrazinylidene derivatives as antivirulence agents. The compound 12e showed interesting activities against biofilm formation of all tested Staphylococcus aureus strains with IC50 ranging from 1.7 to 43 µM; compounds 12f and 13a resulted strong inhibitors of S. aureus ATCC 6538 and ATCC 29213 biofilm formation with IC50 of 0.9 and 0.8 µM, respectively. A preliminary study on the mechanism of action was carried on evaluating the inhibition of sortase A transpeptidase. Compound 12e re…

Origanum vulgare subsp. hirtum Essential Oil Prevented Biofilm formation and showed antibacterial activity against planktonic and sessile bacterial cells

Essential oils from six different populations of Origanum vulgare subsp. hirtum were compared for their antibiofilm properties. The six essential oils (A to F) were characterized by a combination of gas chromatography with flame ionization detector and gas chromatography with mass spectrometer detector analyses. All oils showed weak activity against the planktonic form of a group of Staphylococcus aureus strains and against a Pseudomonas aeruginosa ATCC 15442 reference strain. The ability to inhibit biofilm formation was investigated at sub-MIC levels of 200, 100, and 50 m g/ml by staining sessile cells with safranin. Sample E showed the highest average effectiveness against all tested stra…

Synthesis, Characterization and in vitro antimicrobial activity of dialkyltin(IV)bis(fusidate) complexes.

The complexation of one steroid antibiotic of the fusidane family, sodium fusidate [sodium 2-16-acetyloxy-3,11-dihydroxy-4,8,10,14-tetramethyl-2,3,4,5,6,7,9,11,12, 13,15,16-dodeca hydro-1H-cyclopenta[a]phenanthren-7-ylidene)-6-methyl-hept-5-enoate = (Nafus)], by dialkyltin(IV) has been studied by conventional technique as FT-IR, Mössbauer and NMR spectroscopies. Analytical data supported the general formula Alk2Sn(IV)fus2 (Alk = Me, Bu). Infrared spectral data of the complexes imply the presence of both uni- and bidentate, ester-type and bridging carboxylate group, respectively. On the basis of FT-IR and 119Sn Mössbauer spectroscopy, in both Me2Sn(IV)fus2 and Bu2Sn(IV)fus2, trigonal bipyram…

Antimicrobial activity of the red palm weevil Rhynchophorus ferrugineus

The red palm weevil, Rhynchophorus ferrugineus (Olivier) (Coleoptera Dryophthoridae), is an important pest of palms. Knowl- edge of both its natural enemies and its defensive mechanisms against predators and microorganisms is important to develop methods for an integrated pest control. Antimicrobial activity of the cuticular surface of adults and larvae, as well as of eggs, of this invasive species was investigated. This activity was tested against the Gram-positive bacteria Bacillus subtilis (Ehrenberg) Cohn and Bacillus thuringiensis Berliner, the Gram-negative bacterium Escherichia coli Escherich, and the entomopathogenic fungi Beauveria bassiana (Balsamo) Vuillemin and Metarhizium aniso…

New Thiazole Nortopsentin Analogues Inhibit Bacterial Biofilm Formation.

New thiazole nortopsentin analogues were conveniently synthesized and evaluated for their activity as inhibitors of biofilm formation of relevant Gram-positive and Gram-negative pathogens. All compounds were able to interfere with the first step of biofilm formation in a dose-dependent manner, showing a selectivity against the staphylococcal strains. The most active derivatives elicited IC50 values against Staphylococcus aureus ATCC 25923, ranging from 0.40&ndash

MUV – MOBILITY URBAN VALUES

Un gioco digitale per smartphone che promuove la mobilità individuale sostenibile, in cui i cittadini si sfidano in tornei: chi ha abitudini di mobilità più rispettose dell’ambiente vince. I dati raccolti dall’app attraverso processi aperti e partecipati sostengono i processi decisionali e stimolano nuove soluzioni di mobilità. Frutto di un progetto Horizon2020, è il risultato di sette anni di ricerca con più di venti partner internazionali (pubbliche amministrazioni, università, centri di ricerca) ed è stato testato in 21 città del mondo. I cittadini che hanno partecipato alle diverse dinamiche di gioco, oltre ad aver registrato oltre 180.000 chilometri percorsi in modo sostenibile, hanno …

NEW 4-DIAZOPYRAZOLE DERIVATIVES AS POTENTIAL ANTIBIOFILM AGENTS

Many infections such as otitis media, sinusitis, cholesteatoma, tonsillitis and adenoiditis are caused by biofilm forming mucosal pathogens (P. aeruginosa, S. aureus, S. peneomoniae, H. influenzae and M. catarrhalis). Moreover, the role of biofilms in the chronic otolaryngologic infections has been recognized for otitis media, tonsillitis and rhinosinusitis. Finally, bacterial biofilms of S. aureus, S. epidermis and E. faecalis are the leading cause of medical device-related infections. Pathogens growing as biofilms are intrinsically resistant to conventional antibiotics and therefore the discovery of new compounds able to act against biofilm aggregated micro organisms is an urgent task. Pr…

CCDC 836072: Experimental Crystal Structure Determination

Related Article: Maria Assunta Girasolo, Loredana Canfora, Piera Sabatino, Domenico Schillaci, Elisabetta Foresti, Simona Rubino, Giuseppe Ruisi, Giancarlo Stocco|2012|J.Inorg.Biochem.|106|156|doi:10.1016/j.jinorgbio.2011.09.010

CCDC 836073: Experimental Crystal Structure Determination

Related Article: Maria Assunta Girasolo, Loredana Canfora, Piera Sabatino, Domenico Schillaci, Elisabetta Foresti, Simona Rubino, Giuseppe Ruisi, Giancarlo Stocco|2012|J.Inorg.Biochem.|106|156|doi:10.1016/j.jinorgbio.2011.09.010

Menzione d'Onore Borgo Vecchio Factory

Il Premio Compasso d’Oro ADI è il massimo riconoscimento italiano al progetto, al prodotto, alla ricerca di disegno industriale. È stato istituito a Milano nel 1954 dai grandi magazzini la Rinascente per incentivare l’“estetica del prodotto” e il nascente design italiano. Il marchio del premio, che fa riferimento al compasso di Adalbert Göringer e alla proporzione aurea, è stato disegnato dal grafico Albe Steiner, mentre il compasso d’oro tridimensionale è a firma degli architetti Alberto Rosselli e Marco Zanuso. Nel 1958 il premio è stato ceduto da la Rinascente all’ADI Associazione per il Disegno Industriale, che ogni due anni ne cura l’organizzazione attraverso le selezioni di una giuria…

Right to the future: ideas kit for the future of Palermo

La città di Palermo, soggetta ai sempre più costanti fenomeni di brain drain e di immigrazione, si trova necessariamente a decidere cosa vuole fare da grande. Gli input che arrivano dall’esterno, e non solo, spingono la città prevalentemente verso una sola possibilità: il turismo. Eppure la visione del turismo come unica via possibile si è rivelata la condanna a morte al diritto di vivere e praticare la città dove si e nati, cresciuti ma soprattutto si è scelto di abitare. In contrapposizione a questa visione, città come Barcellona, Bogotà o Medellin si sono messe in gioco sfidando la formazione/conformazione storica a favore della praticità e benessere della quotidianità urbana. Dimostrand…