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作 者:涂增清[1] 杜志云[1] 张焜[1] 潘文龙 汤志恺[1] 莫容清[1]
机构地区:[1]广东工业大学轻工化工学院,广东广州510006 [2]中国广州分析测试研究中心,广东广州510070
出 处:《日用化学工业》2011年第1期27-31,共5页China Surfactant Detergent & Cosmetics
基 金:国家自然科学基金资助项目(21042003);广东省科技计划资助项目(2007A020300007-10)
摘 要:酪氨酸酶抑制剂广泛应用于皮肤美白化妆品中。通过芳香醛分别与丙酮和环戊酮在酸性条件下催化缩合,合成了两个系列共10个姜黄素多酚类似物(A1~5和B1~5),并研究了其对酪氨酸酶的抑制活性。结果表明,含邻二酚羟基的姜黄素多酚类似物(A4和B4)对酪氨酸酶具有很强的抑制作用,半抑制浓度(IC50)分别为1.19,1.24μmol/L,比曲酸(IC50为28.59μmol/L)的活性强20多倍。抑制动力学研究表明,该类姜黄素多酚类似物对酪氨酸酶的抑制属于非竞争性抑制类型。Tyrosinase inhibitors are widely used in skin whitening cosmetics. Two series covering ten compounds of cureumin polyphenolic analogs (A1-5 and B1-5 ) were synthesized by acidic catalytic condensation of an appropriate aromatic aldehyde with acetone and cyclopentanone respectively. Their tyrosinase inhibition activity was evaluated, and the results indicated that compound A4 and B4 that containing two hydroxy groups of ortho orientation similar to catechol exhibit very strong inhibitory effects on tyrosinase with IC50 values of 1.19,1.24 μmol/L respectively,which are more than twenty times higher than that of Kojic Acid ( IC50 = 28.59μmol/L). Inhibition kinetic study showed that the tyrosinase inhibition of this kind of curcumin polyphenolie analogs belong to non - competitive type.
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