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[摘要]
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。
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[Abstract]
Objective To study the antitumor molecular mechanism started on sanguinarine (San) and chelerythrine (Che) from Macleaya cordata. Methods Determining the ICSO values of San and Che against A-549, HCT 8, and Bet-7402 cell lines by using MTT to clarify whether these two alkaloids are the active components in M. cordata; studying the interaction between human telomeric DNA and two alkaloids respectively by using UV-Vis, FL, and CD Methods. Results San and Che are the active antitumor components of M. cordata; San could induce HT4 to form antiparallel G-quadruplex completely with Ka of SX 108 and Che could induce HT4 to form antiparallel G-quadruplex partially with Ka of 930. Conclusion One of the antitumor molecular mechanisms of M. cordata is that the two active components could induce human telomeric DNA to form G-quadruplex.
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