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广西师范大学学报(自然科学版) ›› 2015, Vol. 33 ›› Issue (3): 91-97.doi: 10.16088/j.issn.1001-6600.2015.03.014
梅寒冰1,2, 王威1,2, 姚雪1,2, 程联彪1,2, 黄瑾1,2
MEI Han-bing1,2, WANG Wei1,2, YAO Xue1,2, CHENG Lian-biao1,2, HUANG Jin1,2
摘要: 本文利用荧光偏振法(FP)构建分子伴侣Hsp90的筛选平台,筛选得到黄酮类化合物木犀草苷,并用热稳定实验验证了它与蛋白的结合作用;评价了木犀草苷对14株癌细胞的体外增殖抑制作用,发现木犀草苷对非小细胞肺癌有良好的选择性抑制活性;利用细胞克隆形成、western blot以及流式细胞检测技术进一步深入研究其可能的作用机制,发现木犀草苷能剂量依赖性地抑制非小细胞肺癌的增殖;下调Hsp90的客户蛋白Raf-1、HER2的表达;将H460细胞阻滞在G2/M期;诱导细胞凋亡,并且引起Bax的表达上调。实验结果表明,黄酮类化合物木犀草苷可以通过抑制Hsp90的活性进而降解肿瘤细胞内的客户蛋白,诱导H460细胞G2/M期阻滞,上调Bax表达诱导细胞凋亡来发挥抗肿瘤活性。
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