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Antimicrobial and Anti-Lipase Activity of Quercetin and Its C2-C16 3-O-Acyl-Esters (Articolo in rivista)

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Antimicrobial and Anti-Lipase Activity of Quercetin and Its C2-C16 3-O-Acyl-Esters (Articolo in rivista) (literal)

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Maria Teresa Gatto,a Serena Falcocchio,a Eleonora Grippa,a Gabriela Mazzanti,a Lucia Battinelli,a Giovanni Nicolosi,b Daniela Lambusta b and Luciano Saso a,* (2002)
Antimicrobial and Anti-Lipase Activity of Quercetin and Its C2-C16 3-O-Acyl-Esters
in Bioorganic & medicinal chemistry (Online); Pergamon-Elsevier Science Ltd., Oxford (Regno Unito)
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Maria Teresa Gatto,a Serena Falcocchio,a Eleonora Grippa,a Gabriela Mazzanti,a Lucia Battinelli,a Giovanni Nicolosi,b Daniela Lambusta b and Luciano Saso a,* (literal)

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a Department of Pharmacology of Natural Substances and General Physiology, University of Rome ''La Sapienza'', P.le Aldo Moro 5, 00185 Rome, Italy b Istituto CNR per lo Studio delle Sostanze Naturali di Interesse Alimentare e Chimico-Farmaceutico, Via del Santuario 110, 95028 Valverde (CT), Italy (literal)

Titolo

Antimicrobial and Anti-Lipase Activity of Quercetin and Its C2-C16 3-O-Acyl-Esters (literal)

Abstract

Neither quercetin (Q), nor 3-O-acylquercetines, up to 100 mg/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 mM), 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 (IC16=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 (IC16=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. (literal)

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