蓝萼甲、丙素细胞毒活性及其与Bcl-2蛋白关系的研究  

Studies on Cytotoxicity of Glaucocalyxin A, C and Its Relation with Bcl-2 Protein

作　　者：嵇源源[1] 高立文[1] 张健[1] 王剑文[1] 

机构地区：[1]苏州大学药学院,江苏苏州215123

出　　处：《抗感染药学》2013年第4期271-274,302,共5页Anti-infection Pharmacy

基　　金：江苏省普通高校研究生科研创新计划项目(编号:20130501)

摘　　要：目的:研究蓝萼甲素(GLA)和蓝萼丙素(GLC)对15株不同类型的肿瘤细胞的细胞毒性差异以及与Bcl-2蛋白的关系。方法:采用MTT法检测细胞存活率;用Western Blotting检测细胞凋亡关键蛋白Bcl-2的表达;应用分子对接Autodock程序,将GLA和GLC与Bcl-2蛋白进行分子对接,比较其结合的差异性。结果:用MTT法结果表明GLA对所选用的15株肿瘤细胞均有显著的抑制作用,而相同浓度的GLC对15株肿瘤细胞的生存率没有影响;用分子对接法结果显示GLA与Bcl-2蛋白的结合自由能和ki值均低于GLC。结论:GLA更易与Bcl-2蛋白结合从而抑制Bcl-2蛋白的功能,促进细胞凋亡。Objective： To investigate the cytotoxicity of glaucocalyxin A（GLA） and glaucocalyxin C（GLC） on 15 tumor cell lines and the relation with Bcl-2 protein. Methods： The cell viability was determined by MTT assay. Western blotting was used to detect the protein level of Bcl-2 and autodock technigue was applied to evaluate the binding energy. Results： GLA displayed a potent cytotoxic activity against all 15 tumor cell lines, but GLC had no cytotoxicity at the selective concentrations. The autodock result showed that the binding energy and ki between Bcl-2 and GLA were lower than those Bcl-2 and GLC. Conclusion： GLA is a potent anti-tumor compound to induce apoptosis by binding Bcl-2 protein.

关 键 词：蓝萼甲素 蓝萼丙素 细胞毒 BCL-2 分子对接 

分 类 号：R969[医药卫生—药理学]