摘要
目的探讨黑色素瘤药物异甘草素对酪氨酸酶的抑制作用机理。方法采用酶抑制动力学方法,研究异甘草素对酪氨酸酶单酚酶和二酚酶的抑制作用和抑制动力学,研究甘草素对黑色素瘤细胞A375生长的抑制作用。结果异甘草素对单酚酶和二酚酶都有良好的抑制作用,IC50分别为(11.22±0.92)μM和(48.53±4.75)μM,且异甘草素是一种可逆的竞争型酪氨酸酶二酚酶抑制剂,抑制常数Ki为(12.14±0.54)μM。异甘草素能显著抑制黑色素瘤细胞A375的生长,酪氨酸酶活性和黑色素含量不断降低。结论异甘草素是良好的酪氨酸酶抑制剂,能抑制黑色素瘤细胞的生长。
Objective To study the inhibitory mechanism of soliquiritigenin on tyrosinase.Methods The inhibition effect and inhibitory kinetics of tyrosinase induced by oliquiritigenin were investigated.The effect of isoliquiritigenin on A375 melanoma cell were preliminarily indicated.Results The inhibitory effect of isoliquiritigenin on monophenolase and diphenolase of tyrosinase was good, IC50 was （11.22 ±0.92） μM and （48.53 ±4.75） μM, isoliquiritigenin was a competitive inhibitor, the value of inhibition constant （ Ki ） was （ 12.14 ±0.54 ） μM.Isoliquiritigenin could inhibit the prolifevation of A375 cell significantly, and the tyrosinase activity and melanin synthesis decreased.Conclusion Isoliquiritigenin as a tyrosinase inhibitor, plays an important role in the regulation of melanin, which provides the theoretical basis for the clinical anti skin cancer.
出处
《中国生化药物杂志》
CAS
2015年第3期45-47,共3页
Chinese Journal of Biochemical Pharmaceutics
基金
河北省科技厅科研项目(112761175)
唐山市科技局指令性计划(12140209A-30)
关键词
异甘草素
酪氨酸酶
黑色素瘤
抑制
isoliquiritigenin
tyrosinase
melanoma
inhibitory mechanism
