Antimicrobial and anti-lipase activity of quercetin and its C2-C16 3-O-acyl-esters.
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.
Gatto
Maria Teresa
MT
Department of Pharmacology of Natural Substances and General Physiology, University of Rome "La Sapienza", P.le Aldo Moro 5, 00185, Rome, Italy.
Falcocchio
Serena
S
Grippa
Eleonora
E
Mazzanti
Gabriela
G
Battinelli
Lucia
L
Nicolosi
Giovanni
G
Lambusta
Daniela
D
Saso
Luciano
L
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*
D000900:Anti-Bacterial Agents; D019380:Anti-HIV Agents; D000890:Anti-Infective Agents; D004791:Enzyme Inhibitors; D004952:Esters; D011794:Quercetin; D008049:Lipase