酪氨酸酶抑制剂的研究进展

酪氨酸酶(EC 1.14.18.1,PPO),是一种含铜糖蛋白,广泛存在于自然界中.它是生物体合成黑色素的关键酶,而且与果蔬褐化、昆虫表皮鞣化、人的色素障碍性疾病及恶性黑色素肿瘤的发生与治疗有重要关系.目前,酪氨酸酶抑制剂已被用于果蔬保鲜、化妆品中的增白剂、生物农药的杀虫剂添加物.对酪氨酸酶抑制剂的研究已引起国内外的广泛重视,现已研究出许多具有新型结构的酪氨酸酶抑制剂.为了得到高效的酪氨酸酶抑制剂,对各种类型的化合物构效关系及抑制机理的研究是非常必要的.

Development of Tyrosinase Inhibitors

Tyrosinase(EC 1.14.18.1,PPO) is a copper-containing multifunctional oxidase that is widely distributed in nature.Tyrosinase is the key enzyme in melanin biosyntheisis.The browning of vegetable and fruit,various dermatological disorders and the curing of melanoma is correlation with tyrosinase.Hence,more and more attentions have been pay to the study of the structure,catalyzing mechanism and inhibitors of tyrosinase.At present,tyrosinase inhibitors have been used to keep fruit and vegetable fresh,to be skin-whitening additives in cosmetic,and to be pesticides.As so far,there are more novel tyrosinase inhibitors,which provide a plenty of structural information for design new potent tyrosinase inhibitors.It is necessary to investigate the structure-activity relationship and inhibitory mechanism of various tyrosinase inhibitors for obtaining the effective inhibitor.In this review,we compared the inhibitory kinetic constants and inhibitory potency of several groups of tyrosinase inhibitors such as phenol compounds,stilbenes,chalcones,flavonoids,benzaldehydes,benzoic acids,containing-sulfur compounds,and so on.We also summarized the structure-activity relationship and inhibitory mechanism of several groups of tyrosinase inhibitor analogs by the enzymological kinetics.According to these clues of structure information,we put forward the some ideas for designing the potent inhibitors of tyrosinase.