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EFFECT OF HOWIINOL(GHM-10) ON THE STRUCTURE OF DNA MOLECULES AND ACTIVITY OF DNA TOPOISOMERASE II IN L1210 CELLS
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- Author:
- No author available
- Journal Title:
- ACTA PHARMACEUTICA SINICA
- Issue:
- 1
- DOI:
- 10.3321/j.issn:0513-4870.1999.01.002
- Key Word:
- 抗肿瘤药;海南哥纳香醇甲(GHM-10);DNA损伤;DNA拓扑异构酶II
Abstract： 目的: 研究海南哥纳香醇甲(GHM-10)抑癌细胞DNA合成的作用机制. 方法: 用单细胞凝胶电泳法检测GHM-10对L1210细胞DNA分子的损伤,碱洗脱法测定GHM-10对L1210细胞DNA单链长度的影响,用GHM-10对超螺旋pUC18 DNA的解旋能力测定它对DNA拓扑异构酶II活性的影响. 结果: L1210细胞用GHM-10 (4～10) μg·ml-1处理4.5 h后,DNA分子受损,表现为电泳后在荧光显微镜下可见彗星状拖尾.GHM-10 (4～25) μg·ml-1处理L1210细胞5 h,可引起DNA单链断裂. L1210细胞或从L1210细胞分离的蛋白质在用GHM-10处理后,DNA拓扑异构酶II的活性均被抑制.结论: GHM-10可引起L1210细胞DNA分子损伤;无论在细胞内还是细胞外,GHM-10可抑制拓扑异构酶II的活性.
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