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Topotecan(TPT)是类似天然抗癌药物喜树碱的半合成新药.为了阐明TPT对拓扑异构酶的毒性作用,将癌细胞系SUD4及DOHH2培养在不同浓度TPT的培养基中,分别在培养8h、18h后取样进行测试.结果表明:TPT不仅作用于拓扑酶Ⅰ,也作用于拓扑酶Ⅱ,尽管对酶Ⅱ的影响非常小.应用新的流体细胞测量仪(FACS-Vantage)及免疫分析法对细胞培养时间、TPT的浓度与拓扑酶中毒程度的动力学关系进行了研究.上述研究显示TPT能影响拓扑异构酶Ⅱ(新观点),同时强调在抗癌化学治疗中应结合使用酶Ⅰ及酶Ⅱ抑制剂.
Topotecan (TPT) is a semi-synthetic drug that resembles the natural anticancer drug camptothecin. In order to elucidate the toxic effect of TPT on topoisomerase, SUD4 and DOHH2 were cultured in different concentrations of TPT and cultured for 8h and 18h respectively. The results showed that TPT not only acted as topoisomerase I but also as topoisomerase II, although the effect on enzyme II was very small. The kinetics of cell culture time, the concentration of TPT and the degree of topoisomerase poisoning were investigated using a new FACS-Vantage and immunoassay. The above study shows that TPT can affect topoisomerase Ⅱ (new point of view), while emphasizing the combination of enzyme Ⅰ and enzyme Ⅱ inhibitors in anti-cancer chemotherapy.