Li Zhi-Cong, Chen Liang-Hua, Yu Xiao-Jie, Hu Yong-Hua, Song Kang-Kang, Zhou Xing-Wang, Chen Qing-Xi
Key Laboratory of the Ministry of Education for Coastal and Wetland Ecosystems, School of Life Sciences, Xiamen University, Xiamen 361005, China.
J Agric Food Chem. 2010 Dec 8;58(23):12537-40. doi: 10.1021/jf1033625. Epub 2010 Nov 9.
2-Chlorobenzaldehyde thiosemicarbazone (2-Cl-BT) and 4-chlorobenzaldehyde thiosemicarbazone (4-Cl-BT) were synthesized, and their inhibitory kinetics on the activity of mushroom tyrosinase were investigated. Results showed that these compounds exhibited significant inhibitory potency on both monophenolase activity and diphenolase activity of tyrosinase. For the monophenolase activity, both compounds could decrease the steady-state activity of the enzyme sharply, without any influence on the lag period. The IC50 values of them were estimated to be 15.4 μM and 6.7 μM, respectively. For the diphenolase activity, both compounds belonged to reversible inhibitors, but their mechanisms were different: 2-Cl-BT was a noncompetitive type inhibitor, while 4-Cl-BT was a mixed-type inhibitor. Their inhibition constants were determined and compared.
合成了2-氯苯甲醛缩氨基硫脲（2-Cl-BT）和4-氯苯甲醛缩氨基硫脲（4-Cl-BT），并研究了它们对蘑菇酪氨酸酶活性的抑制动力学。结果表明，这些化合物对酪氨酸酶的单酚酶活性和二酚酶活性均表现出显著的抑制效力。对于单酚酶活性，两种化合物均可急剧降低酶的稳态活性，而对延迟期无任何影响。它们的IC50值分别估计为15.4 μM和6.7 μM。对于二酚酶活性，两种化合物均属于可逆抑制剂，但其作用机制不同：2-Cl-BT为非竞争性抑制剂，而4-Cl-BT为混合型抑制剂。测定并比较了它们的抑制常数。
