Takahashi T, Miyazawa M
Department of Applied Chemistry, Faculty of Science and Engineering, Kinki University, Osaka, Japan.
Pharmazie. 2010 Dec;65(12):913-8.
The aim of this study was to show how tyrosinase inhibitory activity is correlated with the structure of cinnamic acid derivatives. We synthesized cinnamic acid derivatives, and investigated their tyrosinase inhibitory and DPPH radical scavenging activities. The results show that reduction of C=C double bonds and the substituent group of cinnamic acid derivatives have an effect on antioxidant activity and tyrosinase inhibitory activity. Among these compounds, compounds 2, 6 and 6a showed a potent tyrosinase inhibitory activity with IC50 (50% inhibitory concentration) values of 115.6 microM, 114.9 microM and 195.7 microM, respectively. The results obtained provide a useful clue for the design and development of new tyrosinase inhibitors.
本研究的目的是展示酪氨酸酶抑制活性如何与肉桂酸衍生物的结构相关。我们合成了肉桂酸衍生物,并研究了它们的酪氨酸酶抑制活性和DPPH自由基清除活性。结果表明,肉桂酸衍生物的C=C双键还原和取代基对其抗氧化活性和酪氨酸酶抑制活性有影响。在这些化合物中,化合物2、6和6a表现出较强的酪氨酸酶抑制活性,IC50(50%抑制浓度)值分别为115.6 microM、114.9 microM和195.7 microM。所得结果为新型酪氨酸酶抑制剂的设计和开发提供了有用的线索。