1. Antimicrobial and anti-lipase activity of quercetin and its C2-C16 3-O-acyl-esters.
- Author
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Gatto MT, Falcocchio S, Grippa E, Mazzanti G, Battinelli L, Nicolosi G, Lambusta D, and Saso L
- Subjects
- Anti-Bacterial Agents, Anti-HIV Agents chemistry, Anti-HIV Agents pharmacology, Anti-Infective Agents chemistry, Bacteria drug effects, Candida drug effects, Candida enzymology, Drug Evaluation, Preclinical methods, Enzyme Inhibitors chemistry, Esters chemistry, Esters pharmacology, HIV-1 drug effects, Humans, Inhibitory Concentration 50, Quercetin chemistry, Anti-Infective Agents pharmacology, Enzyme Inhibitors pharmacology, Lipase antagonists & inhibitors, Quercetin pharmacology
- Abstract
Neither quercetin (Q), nor 3-O-acylquercetines, up to 100 microg/mL, had any significant activity on selected gram-positive strains (Staphylococcus aureus, Bacillus subtilis, Listeria ivanovi, Listeria monocytogenes, Listeria serligeri), gram-negative strains (Escherichia coli, Shigella flexneri, Shigella sonnei, Salmonella enteritidis, Salmonella tiphymurium) and yeasts (Candida albicans and Candida glabrata). In addition, we confirmed the known anti-HIV activity of Q (80% inhibition at 40 microM), which might depend on the free hydroxyl in the C-3 position, as suggested by the lack of activity of the 3-O-acylquercetines. Finally, we described an interesting inhibitory activity on Candida rugosa lipase by Q (IC(16)=10(-4) M) and its esters (3-O-acylquercetines) which, in vivo, could play an important role against lipase producing microorganisms. In particular, 3-O-acyl-quercetines, being more active (IC(16)=10(-4)-10(-6) M) and more lipophilic, could be more effective than Q when applied to the skin or mucosae, and deserve to be studied further.
- Published
- 2002
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