quercetin has been researched along with catechin-gallate* in 2 studies
2 other study(ies) available for quercetin and catechin-gallate
| Article | Year |
|---|---|
Integrated ligand and structure based studies of flavonoids as fatty acid biosynthesis inhibitors of Plasmodium falciparum.
A common feature pharmacophore with two hydrogen-bond acceptor and one aromatic hydrophobic feature has been generated using seven active flavonoids. Docking studies of these compounds well corroborates with the pharmacophore model. Therefore models could be useful for identification of potential novel FAS-II inhibitors. Topics: Antimalarials; Binding Sites; Catechin; Computer Simulation; Fatty Acid Synthase, Type II; Flavonoids; Ligands; Plasmodium falciparum | 2010 |
Inhibition of Plasmodium falciparum fatty acid biosynthesis: evaluation of FabG, FabZ, and FabI as drug targets for flavonoids.
After the discovery of a potent natural flavonoid glucoside as a potent inhibitor of FabI, a large flavonoid library was screened against three important enzymes (i.e., FabG, FabZ, and FabI) involved in the fatty acid biosynthesis of P. falciparum. Although flavones with a simple hydroxylation pattern (compounds 4-9) showed moderate inhibitory activity toward the enzymes tested (IC50 10-100 microM), the more complex flavonoids (12-16) exhibited strong activity toward all three enzymes (IC50 0.5-8 microM). Isoflavonoids 26-28 showed moderate (IC50 7-30 microM) but selective activity against FabZ. The most active compounds were C-3 gallic acid esters of catechins (32, 33, 37, 38), which are strong inhibitors of all three enzymes (IC50 0.2-1.1 microM). Kinetic analysis using luteolin (12) and (-)-catechin gallate (37) as model compounds revealed that FabG was inhibited in a noncompetitive manner. FabZ was inhibited competitively, whereas both compounds behaved as tight-binding noncompetitive inhibitors of FabI. In addition, these polyphenols showed in vitro activity against chloroquine-sensitive (NF54) and -resistant (K1) P. falciparum strains in the low to submicromolar range. Topics: 3-Oxoacyl-(Acyl-Carrier-Protein) Reductase; Alcohol Oxidoreductases; Animals; Antimalarials; Catechin; Cells, Cultured; Chloroquine; Drug Resistance; Enoyl-(Acyl-Carrier-Protein) Reductase (NADH); Fatty Acids; Flavones; Flavonoids; Humans; Hydro-Lyases; Kinetics; Luteolin; Phenols; Plasmodium falciparum; Polyphenols; Structure-Activity Relationship | 2006 |