桂枝茯苓胶囊提取物的体外抗肿瘤活性及机制

Inhibitory Effects and Mechanism of Extracts from Guizhi Fuling on the Proliferation in Human Cervical Carcinoma Cells

目的比较桂枝茯苓胶囊不同溶剂提取物的体外抗肿瘤活性,并探讨其可能的机制。方法采用四甲基偶氮唑蓝法观察桂枝茯苓胶囊不同溶剂提取物对HeLa和C33A 2种人宫颈癌细胞株增殖的影响,以酶联免疫吸附法测定蛋白酪氨酸激酶(protein tyrosine kinases,PTKs)活性,用二苯代苦味肼基(1,1-diphenyl-2-picrylhydrazyl,DPPH)清除率方法测定体外抗氧化活性。结果桂枝茯苓胶囊的多种溶剂提取物具有良好的人宫颈癌细胞生长抑制活性。对HeLa细胞的抑制强度最大者为正丁醇部分-30%乙醇洗脱物(提取物9),IC50为(7.09±1.25)μg.mL-1,对C33A细胞的抑制强度最大者为乙酸乙酯部分-丙酮洗脱物(提取物5),IC50为(5.14±0.70)μg.mL-1。结论桂枝茯苓胶囊提取物在体外显示不同的抗肿瘤活性,抑制蛋白酪氨酸激酶活性以及抗氧化作用可能是其提取物抗肿瘤作用的机制之一。

OBJECTIVE To investigate the inhibitory effects of different solvent extracts from Guizhi Fuling on the proliferation in human cervical carcinoma cells and its possible mechanisms. METHODS MTT assay was used to detect the proliferation in the HeLa and C33A human cervical carcinoma cells, and the enzyme-linked immunosorbent assay was used detect for the protein tyrosine kinases （PTKs） activity in vitro, and 1,1-diphenyl-2-picrylhydrazyl （DPPH） scavenging ratio displayed antioxidant activity of different extracts from Guizhi Fuling. RESULTS Most of different solvent extracts from Guizhi Fuling, including extracts of ethyl acetate, ethyl acetate-water, ethyl acetate-acetone, butyl alcohol-30% ethanol and butyl alcohol-50% ethanol, displayed good inhibitory activity on the proliferation in human cervical carcinoma cells. The inhibit potency to the largest for HeLa cells was butyl alcohol-30% ethanol eluate, its IC50 was （7.09 ± 1.25 ） μg·mL-1, and inhibit potency to the largest for C33A cells was ethyl acetate-acetone eluate, its ICs0 was （5. 14 ＋0. 70） μg·mL-1. CONCLUSION These results suggested that different solvent extracts from Guizhi Fuling, have different anticancer activity in vitro. Its mechanism may be associated with inhibition of PTKs and antioxidation activity.