title: Antimicrobial and anti-lipase activity of quercetin and its C2-C16 3-O-acyl-esters.
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.
authors.affiliation: Department of Pharmacology of Natural Substances and General Physiology, University of Rome "La Sapienza", P.le Aldo Moro 5, 00185, Rome, Italy.
authors.forename: Maria Teresa
authors.initials: MT
authors.lastname: Gatto
authors.forename: Serena
authors.initials: S
authors.lastname: Falcocchio
authors.forename: Eleonora
authors.initials: E
authors.lastname: Grippa
authors.forename: Gabriela
authors.initials: G
authors.lastname: Mazzanti
authors.forename: Lucia
authors.initials: L
authors.lastname: Battinelli
authors.forename: Giovanni
authors.initials: G
authors.lastname: Nicolosi
authors.forename: Daniela
authors.initials: D
authors.lastname: Lambusta
authors.forename: Luciano
authors.initials: L
authors.lastname: Saso
mesh_terms: D000900:Anti-Bacterial Agents; D019380:Anti-HIV Agents / Q000737:chemistry / Q000494:pharmacology; D000890:Anti-Infective Agents / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D002175:Candida / Q000187:drug effects / Q000201:enzymology; D004353:Drug Evaluation, Preclinical / Q000379:methods; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D004952:Esters / Q000737:chemistry / Q000494:pharmacology; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D008049:Lipase / Q000037:antagonists & inhibitors*; D011794:Quercetin / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D019380:Anti-HIV Agents; D000890:Anti-Infective Agents; D004791:Enzyme Inhibitors; D004952:Esters; D011794:Quercetin; D008049:Lipase