Search results for "AGENTS"
showing 10 items of 7330 documents
Structural basis for the potential antitumour activity of DNA-interacting benzo[kl]xanthene lignans
2010
The biological properties and possible pharmacological applications of benzo[kl]xanthene lignans, rare among natural products and synthetic compounds, are almost unexplored. In the present contribution, the possible interaction of six synthetic benzo[kl]xanthene lignans and the natural metabolite rufescidride with DNA has been investigated through a combined STD-NMR and molecular docking approach, paralleled by in vitro biological assays on their antiproliferative activity towards two different cancer cell lines: SW 480 and HepG2. Our data suggest that the benzo[kl]xanthene lignans are suitable lead compounds for the design of DNA selective ligands with potential antitumour properties.
Preparation of ferulic acid derivatives and evaluation of their xanthine oxidase inhibition activity.
2007
Several ferulic acid ethyl esters (3a-h) were synthesized under the Knoevengel reaction condition and they were further reduced to afford the respective allylic alcohol derivatives (4a-g). Some of them were evaluated for the xanthine oxidase (XO) inhibitory activity. Among them, 3h exhibited a significant inhibitory activity with an IC50 value of 1.35 x 10(-5) M, while the IC50 value of allopurinol used as the positive control was 1.49 x 10(-5) M. The study suggested that the higher acidity of the phenolic OH group in the ferulic acid derivatives might result in improved XO inhibitory activity.
Mangiferin nanoemulsions in treatment of inflammatory disorders and skin regeneration
2018
Abstract In this paper mangiferin nanoemulsions were developed using hyaluronic acid of different molecular weight, in absence or presence of Transcutol-P. An extensive study was carried out on the physico-chemical properties of nanoemulsions. Nanosizer and transmission electron microscopy showed oil droplets average size 296 nm with monodisperses distribution (PI ≤ 0.30). The zeta potential was highly negative (−30 mV). FTIR analysis confirms the existence of physical interactions among compounds. Rheological measurements allowed to conclude that all formulations present a pseudoplastic behavior (s ∼ 0.4) in presence of the biopolymer. Moreover, mangiferin release depends on the molecular …
Cytotoxicity and modes of action of three naturally occurring xanthones (8-hydroxycudraxanthone G, morusignin I and cudraxanthone I) against sensitiv…
2014
Abstract Background Resistance of cancer to chemotherapy remains a challenging issue for scientists as well as physicians. Naturally occurring xanthones possess a variety of biological activities such as anti-inflammatory, anti-bacterial, and anti-cancer effects. The present study was aimed at investigating the cytotoxicity and the modes of action of three naturally occurring xanthones namely, morusignin I (1), 8-hydroxycudraxanthone G (2) and cudraxanthone I (3) against a panel of nine cancer cell lines, including various sensitive and drug-resistant phenotypes. Methods The cytotoxicity of the compounds was determined using a resazurin reduction assay, whereas the caspase-Glo assay was use…
Cytotoxicity and modes of action of four Cameroonian dietary spices ethno-medically used to treat cancers: Echinops giganteus, Xylopia aethiopica, Im…
2013
Abstract Ethnopharmacological relevance. Echinops giganteus , Imperata cylindrica , Piper capense and Xylopia aethiopica are four medicinal spices used in Cameroon to treat cancers. Aim of the study The above plants previously displayed cytotoxicty against leukemia CCRF-CEM and CEM/ADR5000 cell lines as well as human pancreatic MiaPaCa-2 cells. The present study aims at emphasizing the study of the cytotoxicity and the modes of action of the above plants on a panel of ten cancer cell lines including various sensitive and drug-resistant phenotypes. The study has been extended to the isolation of the bioactive constituents from Echinops giganteus . Materials and methods The cytotoxicity of th…
Cytotoxicity of compounds from Xylopia aethiopica towards multi-factorial drug-resistant cancer cells.
2015
Abstract Introduction Multidrug resistance (MDR) in cancer represent a major hurdle in chemotherapy. Previously, the methanol extract of the medicinal spice Xylopia aethiopica displayed considerable cytotoxicity against multidrug resistant (MDR) cancer cell lines. Methods The present study was designed to assess the cytotoxicity of compounds, 16 α -hydroxy- ent -kauran-19-oic acid ( 2 ), 3,4′,5-trihydroxy-6″,6″-dimethylpyrano[2,3-g]flavone ( 3 ), isotetrandrine ( 5 ) and trans -tiliroside ( 6 ) derived from the methanol crude extract of Xylopia aethiopica against 9 drug-sensitive and -resistant cancer cell lines. The resazurin reduction assay was used to evaluate the cytotoxicity of these c…
Cytotoxicity of the crude extract and constituents of the bark of Fagara tessmannii towards multi-factorial drug resistant cancer cells.
2019
Abstract Ethnopharmacological relevance Fagara tessmannii Engl. is an African medicinal plant used in Cameroonian traditional medicine to treat various types of cancers. Aim of the study This work was designed to determine the cytotoxicity of the crude extract (FTB), fractions (FTBa-d) and compounds isolated from the bark of Fagara tessmannii, namely lupeol (1), fagaramide (2), zanthoxyline (3), hesperidin (4), nitidine chloride (5), fagaridine chloride (6), and β-sitosterol-3-O-β-D-glucopyranoside (7). The study was extended to the mode of induction of apoptosis by FTB, compounds 5 and 6. Materials and methods The resazurin reduction assay was used to evaluate the cytotoxicity of samples. …
Comparative efficacy of Zataria multiflora Boiss., Origanum compactum and Eugenia caryophyllus essential oils against E. coli O157:H7, feline caliciv…
2013
Abstract Ready-to-eat salads using baby-leaf and multi-leaf mixes are one of the most promising developments in the fresh-cut food industry. There is great interest in developing novel decontamination treatments, which are both safe for consumers and more efficient against foodborne pathogens. In this study, emulsions of essential oils (EOs) from Origanum compactum (oregano), Eugenia caryophyllus (clove), and Zataria multiflora Boiss (zataria) were applied by spray (0.8 ml) after the sanitizing washing step. The aim was to investigate their ability to control the growth of potentially cross-contaminating pathogens and endogenous microbiota in commercial baby leaves, processed in a fresh-cut…
GABAA-receptor Subtypes: Clinical Efficacy and Selectivity of Benzodiazepine Site Ligands
1997
The main inhibitory neurotransmitter receptor of the brain, the gamma-aminobutyric acid type A receptor (GABA[A]), mediates the actions of several classes of clinically important drugs, such as benzodiazepines, barbiturates and general anaesthetics. This review summarizes the current knowledge on how classical benzodiazepines and novel nonbenzodiazepine compounds act on the benzodiazepine site of GABA(A) receptors and on their clinical pharmacology related to anxiolytic, sedative, hypnotic and cognitive effects or side-effects. Partial agonism, receptor subtype selectivity and novel binding sites are discussed as possible strategies to develop new drugs with fewer adverse effects than are s…
Antimicrobial Activity of Resveratrol Analogues
2014
Stilbenes, especially resveratrol and its derivatives, have become famous for their positive effects on a wide range of medical disorders, as indicated by a huge number of published studies. A less investigated area of research is their antimicrobial properties. A series of 13 trans-resveratrol analogues was synthesized via Wittig or Heck reactions, and their antimicrobial activity assessed on two different grapevine pathogens responsible for severe diseases in the vineyard. The entire series, together with resveratrol, was first evaluated on the zoospore mobility and sporulation level of Plasmopara viticola (the oomycete responsible for downy mildew). Stilbenes displayed a spectrum of acti…