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喜树碱(CPT)是存在于中国喜树的天然生物碱,拓扑替康(topotecan,TPT)则是半合成的CPT水溶性衍生物,它们都是DNA拓朴异构酶的强烈抑制剂。CPT具有广泛的抗肿瘤活性。CPT和TPT含有α-羟基-δ-内酯环,可发生与pH相关的可逆性水解,形
CPT is a natural alkaloid present in Chinese camptotheca acuminata and Topotecan (TPT) is a semisynthetic CPT water-soluble derivative, both of which are strong inhibitors of DNA topoisomerase. CPT has a wide range of anti-tumor activity. CPT and TPT contain alpha-hydroxy-delta-lactone rings that undergo reversible hydrolysis associated with pH,