羟基丹参酮ⅡA的合成及体外抗肿瘤作用

Synthesis and in vitro Anti-Tumor Effects of Hydroxytanshinone ⅡA

对丹参酮ⅡA进行结构修饰,合成了羟基丹参酮ⅡA。采用MTT法考察了羟基丹参酮ⅡA对人宫颈癌细胞株Hela细胞,人肝癌细胞株HepG-2细胞、人胃癌细胞株SGC-7901细胞的增殖抑制作用。结果表明:羟基丹参酮ⅡA对三种肿瘤细胞增殖都有很好的抑制作用,抑制作用呈剂量依赖性。羟基丹参酮ⅡA对SGC-7901细胞抑制作用最强,其IC_(50)为4.18μM;对HeLa细胞的抑制作用次之,其IC_(50)为6.08μM;对HepG-2细胞抑制作用较弱,其IC_(50)为10.20μM。而丹参酮ⅡA对SGC-7901细胞、HeLa细胞和HepG-2细胞的IC_(50)分别是17.15μM、27.28μM和46.34μM。羟基丹参酮ⅡA抑制肿瘤细胞增殖作用明显强于丹参酮ⅡA(P<0.05)。

Hydroxytanshinone IIA was synthesized with tanshinone IIA as lead compound. MTr assay was adopted to evaluate its inhibition effect against Hela, HepG-2 and SGC-7901 cells. Results indicated that hydroxytanshinone IIA inhibited cell proliferation in a dose-dependent manner. The half inhibitory concentrations （IC50） of hydroxytanshinone IIA against SGC-7901, HeLa and HepG-2 cells were 4.18 μM,6.08 μM and 10.20 μM, respectively. But the IC50 of tanshinone IIA against SGC-7901, HeLa and HepG-2 cells were 17.15 μM,27.28 μM and 46.34μM, respectively. The inhibition effect of hydroxytanshinone ILk to SGC-7901 cells was powerful. Compared with tanshinone IIA,hydroxytanshi- none IIA signhqcanfly increased inhibition effect （ P 〈 0.05 ）.