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作 者:张虹[1] 向俊锋[1] 谭莉[1] 戴玮[1] 刘岩[1] 张淼[1] 唐亚林[1]
机构地区:[1]中国科学院化学研究所分子动态与稳态结构国家重点实验室分子科学国家实验室,北京100190
出 处:《解放军药学学报》2010年第6期489-491,550,共4页Pharmaceutical Journal of Chinese People's Liberation Army
摘 要:目的探讨黑丑提取物的抗肿瘤活性,并对其作用机理进行研究。方法应用MTT法考察黑丑提取物在体外对人肝癌细胞BEL-7402、结肠癌细胞HCT-8、肺癌细胞A-549的细胞毒效应。为明确其体内抗肿瘤疗效,建立了Lew is肺癌的小鼠模型,通过对比各组小鼠的相对肿瘤增殖率、肿瘤生长曲线、抑瘤率、瘤重等指标考察黑丑提取物的抑瘤效果。通过G-四链体的稳定性实验,初步探讨了黑丑的抗肿瘤作用机制。结果黑丑提取物在体外对上述3种肿瘤细胞均具有抑制作用,对人肺癌细胞A-549的IC50值为30.19μg/ml。在体内的抗肿瘤药效实验中亦表现出明显的抗肿瘤活性,且其可有效稳定G-四链体结构。结论黑丑提取物在体内外均具有明显的抑瘤作用,并可通过稳定G-四链体结构进而抑制肿瘤细胞的端粒酶活性,最终导致肿瘤细胞凋亡。Objective To investigate the anti-tumor activities of Pharbitis nil(L.) Choisy extract,and to study its mechanism.Methods The MTT method was used to evaluate the inhibitory effects of the Pharbitis nil(L.) Choisy extract on proliferation of cancer cell lines.In order to determine its anti-tumor effect in vivo,the Lewis lung cancer mice model was established.By comparing the relative tumor proliferation rate,growth curves,inhibition rate of different groups,the anti-tumor effect was evaluated.Moreover,the anti-tumor mechanism of Pharbitis nil(L.) Choisy was studied by using G-quadruplex stability experiments.Results In the vitro anti-liver cancer experiment,the Pharbitis nil(L.) Choisy extract showed obvious anti-tumor effect on various tumor cells,with a IC50 value of 30.19 μg/ml to A-549 human lung cancer cell.In the vivo experiment,it exhibited significant anti-tumor effect.Besides,from the result of G-quadruplex stability experiments,it was observed that the quadruplex structure showed increasing Tm values with increasing amounts of Pharbitis nil(L.) Choisy extract.Conclusion In the vitro and vivo anti-liver cancer experiments,the Pharbitis nil(L.) Choisy extract has shown significant anti-tumor effects.And it could inhibit telomerase activity by stabilizing G-quadruplex and hence play an anti-caner role.
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