香豆素-白藜芦醇杂合物的酪氨酸酶抑制活性。
Tyrosinase inhibitor activity of coumarin-resveratrol hybrids.
作者信息
Fais Antonella, Corda Marcella, Era Benedetta, Fadda M Benedetta, Matos Maria Joao, Quezada Elias, Santana Lourdes, Picciau Carmen, Podda Gianni, Delogu Giovanna
机构信息
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.
出版信息
Molecules. 2009 Jul 13;14(7):2514-20. doi: 10.3390/molecules14072514.
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 IC(50) 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 potentcompound (0.27 mM), more so than umbelliferone (0.42 mM), used as reference compound. The kinetic studies revealed that compound 8 caused non-competitive tyrosinase inhibition.
在本研究中，我们报告了香豆素部分对酪氨酸酶抑制作用的贡献。已重新合成香豆素-白藜芦醇杂合物1-8，以研究构效关系并测定这些化合物的半数抑制浓度（IC50）值。结果表明，这些化合物具有酪氨酸酶抑制活性。化合物3-(3',4',5'-三羟基苯基)-6,8-二羟基香豆素（8）是最有效的化合物（0.27 mM），比用作参考化合物的伞形酮（0.42 mM）更有效。动力学研究表明，化合物8引起非竞争性酪氨酸酶抑制。
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