Search results for " bioactivity"
showing 10 items of 10 documents
Partial thioamide scan on the lipopeptaibiotic trichogin GA IV. Effects on folding and bioactivity
2012
Backbone modification is a common chemical tool to control the conformation of linear peptides and to explore potentially useful effects on their biochemical and biophysical properties. The thioamide, ψ[CS-NH], group is a nearly isosteric structural mimic of the amide (peptide) functionality. In this paper, we describe the solution synthesis, chemical characterization, preferred conformation, and membrane and biological activities of three, carefully selected, peptide analogues of the lipopeptaibiotic [Leu11-OMe] trichogin GA IV. In each analogue, a single thioamide replacement was incorporated. Sequence positions near the N-terminus, at the center, and near the C-terminus were investigated…
Antinociceptive Effects of Turkish Endemic Eryngium kotschyi Boiss. Roots by Bioactivity Guided Fractionation
2010
Eryngium species (Apiaceae) are well known plants in ethnobotanical culture throughout world and also in Turkey. They are used as antitussive, diuretic as well as for analgesic and antiinflammatory purposes in traditional medicine. This study aimed to evaluate the antinociceptive activity of endemic Eryngium kotschyi Boiss. root extracts by bioguided fractionation. The antinociceptive activity of the extracts/fractions/compound was studied in mice using acetic acid induced writhing test and and hot plate test. The methanolic extract was sequentially partitioned with hexane, dichloromethane and water saturated n-butanol. Among the fractions, the n-BuOH fraction showed the most significant re…
Phenolic Composition of Hydrophilic Extract of Manna from Sicilian Fraxinus angustifolia Vahl and its Reducing, Antioxidant and Anti-Inflammatory Act…
2019
Manna, a very singular vegetable product derived from the spontaneous solidification of the sap of some Fraxinus species, has long been known for its mild laxative and emollient properties. In this work, a hydro-alcoholic extract of manna (HME) from Sicilian Fraxinus angustifolia Vahl was investigated using HPLC-DAD to find phenol components and using chemical and biological in vitro assays to determine its reducing, antioxidant and anti-inflammatory capacity. We identified elenolic acid, tyrosol, hydroxytyrosol, catechin, fraxetin, verbascoside, gallic acid, procyanidin-B1, and luteolin 3,7 glucoside, in order of abundance. Measurements of total antioxidant activity by Folin-Ciocalteu reac…
In vitro bioactivity study of composite scaffold prepared via thermally induced phase separation
Among porous materials suitable for Bone Tissue Engineering (BTE) scaffolds, bioactive ceramics (hydroxyapatite, HA) and bioactive glasses (BG) have been used for their excellent biocompatibility, bioactivity and efficient osteointegration (1). However, their major limitations are brittleness, low mechanical stability and low dissolution rate (2). Recent evidences suggest that composite scaffold based on biodegradable polymers (e.g. Poly-lacticacid (PLLA)) simultaneously loaded with HA and BG hold promising potential as efficient osteoconductive implants (3, 4). In this work we investigated the possibility to produce composite PLLA-HA-BG scaffolds via Thermally Induced Phase Separation (TIP…
An Updated Review on the Synthesis and Antibacterial Activity of Molecular Hybrids and Conjugates Bearing Imidazole Moiety
2020
The rapid growth of serious infections caused by antibiotic resistant bacteria, especially the nosocomial ESKAPE pathogens, has been acknowledged by Governments and scientists and is one of the world’s major health problems. Various strategies have been and are currently investigated and developed to reduce and/or delay the bacterial resistance. One of these strategies regards the design and development of antimicrobial hybrids and conjugates. This unprecedented critical review, in which our continuing interest in the synthesis and evaluation of the bioactivity of imidazole derivatives is testified, aims to summarise and comment on the results obtained from the end of the 1900s until Februa…
A green and efficient method for the synthesis of homodimeric (β-dicarbonyl) arylmethanes and dihydropyridine from dimedone in water
2018
A direct method has been developed for the synthesis of the dihydropyridine ring system by means of Michael reaction. The reaction of dimedone with 1 .0 equiv. of amines in water provides intermediate product, which allowed dihydropyridine derivatives by intramolecular cyclization in various yields. Of particular interest is the use of the water as solvent of reaction and in absence of catalyst. Also these operating conditions protect the environment and economic points of view.Keywords: aqueous synthesis; bioactivity; dihydropyridine; dimedone; green method; selective conditions
Edible Insects an Alternative Nutritional Source of Bioactive Compounds: A Review
2023
Edible insects have the potential to become one of the major future foods. In fact, they can be considered cheap, highly nutritious, and healthy food sources. International agencies, such as the Food and Agriculture Organization (FAO), have focused their attention on the consumption of edible insects, in particular, regarding their nutritional value and possible biological, toxicological, and allergenic risks, wishing the development of analytical methods to verify the authenticity, quality, and safety of insect-based products. Edible insects are rich in proteins, fats, fiber, vitamins, and minerals but also seem to contain large amounts of polyphenols able to have a key role in specific bi…
Current Bioactive Azole-Containing Natural Products
2010
The ethnobotany, phytochemistry and biological properties of genus Ferulago – A review
2020
Abstract Ethnopharmacological relevance The genus Ferulago, belonging to the Apiaceae family, is found mainly in the Mediterranean area, Southwest and Middle Asia, the Caucasus and North Africa. Since ancient times, species of this genus have been largely employed in traditional medicine for their biological properties such as antimicrobial, anti-inflammatory, antispasmodic, insecticidal, and anti-malaria, cholinesterase inhibition effects, etc. Aims The scope of this paper is to present a comprehensive respect review of this interesting genus including traditional uses, chemical composition of volatile and non-volatile metabolites, and in vitro and in vivo biological properties either util…
Deposition and characterization of Hydroxyapatite-Chitosan coatings on 304 SS for biomedical devices
2019
During the last years biomaterials have been largely investigated in order to perform and improve biomedical devices. As regards orthopedic field, the most common equipment used (such as implants, bone grafts or screws) are constituted by metallic materials (steel and titanium alloys), characterized by low/medium resistance to corrosion and low osteointegration ability. Furthermore, these factors could produce local inflammations of the tissues surrounding the implants, increasing kinetics of corrosion phenomena. Scientific community has focused the attention on biocoatings interposed between metal and aggressive environment in order to inhibit corrosion. Furthermore, these coatings are abl…