Tyrosinase Inhibitor Activity of Coumarin-Resveratrol Hybrids 英文参考文献.docVIP

Molecules 2009, 14, 2514-2520; doi:10.3390/moleculeOPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Tyrosinase Inhibitor Activity of Coumarin-Resveratrol Hybrids Antonella Fais 1,*, Marcella Corda 1, Benedetta Era 1, M. Benedetta Fadda 1, Maria Joao Matos 2,3, Elias Quezada 2,3, Lourdes Santana 2, Carmen Picciau 3, Gianni Podda 3 and Giovanna Delogu 3,* 1 Dipartimento Scienze Applicate ai Biosistemi, Università degli Studi di Cagliari, Cittadella Universitaria di Monserrato, S.S. 554 Km 0.700 bivio per Sestu, 09042 Monserrato, CA, Italy; E-mails: corda@unica.it (M.C.), era@unica.it (B.E.), faddam@unica.it (M-B.F.) 2 Departamento de Química Orgánica, Facultade de Farmacia, Universidade de Santiago de Compostela, 15782 Santiago de Compostela, Spain; E-mail: lourdes.santana@usc.es (L.S.) 3 Dipartimento Farmaco Chimico Tecnologico, Università degli Studi di Cagliari, Via Ospedale 72, 09124 Cagliari, CA, Italy; E-mails: carmenpicciau@alice.it (C.P.), gpodda@unica.it (G.P.), mariacmatos@ (M-J.M), elias.quezada@usc.es (E.Q.) * Authors to whom correspondence should be addressed; E-mails: delogug@unica.it (G.D.), fais@unica.it (A.F.); Tel.: +390706758566 (G.D.), +390706754506 (A.F.); Fax: +390706758553 (G.D.), +390706754523 (A.F.) Received: 11 May 2009; in revised form: 9 July 2009 / Accepted: 10 July 2009 / Published: 13 July 2009 Abstract: In the present work we report on the contribution of the coumarin moiety to tyrosinase inhibition. Coumarin-resveratrol hybrids 1-8 have been resynthesized to investigate the structure-activity relationships and the IC50 values of these compounds were measured. The results showed that these compounds exhibited tyrosinase inhibitory activity. Compound 3-(3’,4’,5’-trihydroxyphenyl)-6,8-dihydroxycoumarin (8) is the most potent compound (0.27 mM), more so than umbelliferone (0.42 mM), used as reference compound. The kinetic studies revealed that compound