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目的从博落回的2个主要活性成分血根碱(San)和白屈菜红碱(Che)入手研究博落回的抗肿瘤作用分子机制。方法采用MTT法测定San与Che对3种肿瘤细胞(肺癌细胞A-549、结肠癌细胞HCT-8、肝癌细胞Bel-7402)的IC50值,从而确定这两种成分是否为博落回的抗肿瘤活性成分;采用UV-vis、FL、CD法研究San和Che与人体端粒DNA(HT4)的相互作用。结果 San与Che对肿瘤细胞有不同能力的杀伤作用,说明该2种成分是博落回的抗肿瘤活性成分;San和Che能够与HT4相互作用,可以得出San与HT4的结合常数为5×108,并能诱导单链HT4完全形成反平行结构,而Che与HT4的结合常数为930,并能诱导单链HT4部分形成反平行结构。结论博落回含有的2种活性成分San和Che具有诱导人体端粒DNA形成G-四链体结构的能力,从而抑制端粒酶活性,达到抑制肿瘤细胞增殖的目的 ,这可能是博落回抗肿瘤的分子机制之一。
OBJECTIVE To study the molecular mechanism of anti-tumor effects of the two major active ingredients of Dioscorea bulbata (San) and chelerythrine (Che). Methods The IC50 values of San and Che on three kinds of tumor cells (A-549 lung cancer cells, HCT-8 colon cancer cells and Bel-7402 liver cancer cells) were determined by MTT method to determine whether the two components The active components of tumor were studied. The interaction of San and Che with human telomere DNA (HT4) was studied by UV-vis, FL and CD methods. Results The killing ability of San and Che on tumor cells was different, which indicated that the two components were the antitumor active ingredients of Dioscorea nipponica. San and Che could interact with HT4, and the binding constant between San and HT4 was 5 × 108, and can induce single-stranded HT4 complete anti-parallel structure, and the binding constant of Che and HT4 is 930, and can induce single-stranded HT4 part to form anti-parallel structure. Conclusions The two active ingredients San and Che contained in this study can induce the formation of G-quadruplex structure of human telomere DNA and inhibit the activity of telomerase to inhibit the proliferation of tumor cells. Anti-tumor molecular mechanism.