Search results for "Biomolecular"
showing 7 items of 507 documents
Phytochemical investigation of the needles of Abies nebrodensis (Lojac.) Mattei
2019
Abies nebrodensis (Lojac.) Mattei (Pinaceae) is a species living in a very small population only in a confined area of Sicily. In this study, the dichloromethane extract of the leaves was analyzed. Apart from three already known metabolites namely dehydroabietic acid; maltol; and rheosmin, previously detected in other species of Abies, a lanostane derivative was isolated. Its chemical structure was elucidated by means of extensive spectroscopic methods.
Synthesis and biological evaluation of novel peptidomimetics as rhodesain inhibitors
2016
Novel rhodesain inhibitors were developed by combining an enantiomerically pure 3-bromoisoxazoline warhead with a 1,4-benzodiazepine scaffold as specific recognition moiety. All compounds were proven to inhibit rhodesain with Ki values in the low-micromolar range. Their activity towards rhodesain was found to be coupled to an in vitro antitrypanosomal activity, with IC50 values ranging from the mid-micromolar to a low-micromolar value for the most active rhodesain inhibitor (R,S,S)-3. All compounds showed a good selectivity against the target enzyme since all of them were proven to be poor inhibitors of human cathepsin L. Novel rhodesain inhibitors were developed by combining an enantiomeri…
Chemical composition of the essential oil of Centaurea grinensis Reuter and Centaurea apiculata Ledeb: Growing wild in Croatia and Bulgaria, respecti…
2016
AbstractIn the present study, the chemical composition of the essential oils from aerial parts of Centaurea grinensis Reuter (K) collected at Žuta Lova, near Senj (Croatia), and aerial parts (L1) and flowers (L2) of C. apiculata Ledeb. collected near Rebro village, near Breznik town, Znepole Region (Bulgaria), both belonging to subgenus Lopholoma (Cass.) Dobrocz, was evaluated by GC and GC-MS. The main components of K were 4-vinyl guaiacol (21.5%), hexadecanoic acid (16.2%), acetophenone (12.5%). Caryophyllene oxide (15.8%) together with sphathulenol (14.5%) and humulene epoxide II (9.4%) were recognized as the main constituent of both the aerial part (L1) and flowers (L2) of C. apiculata. …
Synthesis and Structure-Affinity Relationships of Spirocyclic Benzopyrans with Exocyclic Amino Moiety
2019
σ1 and/or σ2 receptors play a crucial role in pathological conditions such as pain, neurodegenerative disorders, and cancer. A set of spirocyclic cyclohexanes with diverse O-heterocycles and amino moieties (general structure III) was prepared and pharmacologically evaluated. In structure-activity relationships studies, the σ1 receptor affinity and σ1:σ2 selectivity were correlated with the stereochemistry, the kind and substitution pattern of the O-heterocycle, and the substituents at the exocyclic amino moiety. cis-configured 2-benzopyran cis-11b bearing a methoxy group and a tertiary cyclohexylmethylamino moiety showed the highest σ1 affinity ( Ki = 1.9 nM) of this series of compounds. In…
Thiazole Analogues of the Marine Alkaloid Nortopsentin as Inhibitors of Bacterial Biofilm Formation
2020
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…
Chemical Composition of the Essential Oil of Bupleurum Fontanesii (Apiaceae) Growing Wild in Sicily and its Activity on Microorganisms Affecting Hist…
2016
Hydrodistillation of the flowers (BpFl) of and fruits (BpFr) of Bupleurum fontanesii Guss. ex Caruel gave two oils that were analyzed by GC and GC-MS. The main components were α-elemol (16.7%), caryophyllene oxide (16.4%) and heptacosane (15.9%) in BpFl, and spathulenol (16.8%), caryophylladienol I (13.2%) and α-elemol (12.8%) in BpFr. A good antimicrobial activity against several microorganisms, including Bacillus subtilis, Staphylococcus aureus, Fusarium oxysporum and Aspergillus niger, all infesting historical art craft, was also determined.
Chemical composition and biological activity of the essential oil of Ballota hispanica (L.) Benth. growing wild in Sicily
2015
Ballota L. comprises several relevant species largely used for their excellent therapeutic properties. Ballota hispanica (L.) Benth. is widely used in herbal medicine, and it is sold in herbalist shops for its sedative and antispasmodic properties. Considering its traditional medicinal use and the lack of scientific studies on the volatile components of this species as well as on its biological activities, in this study the chemical composition of the essential oil from aerial parts of B. hispanica, collected in Sicily, was evaluated by gas chromatography and gas chromatographyâmass spectrometry. α-Elemol was the most abundant component of the oil (10.9%), followed by α-ylangene (8.5%),…