Camptothecin (CPT) is a pentacyclic alkaloid isolated from wood and bark of Camptotheca acuminata. Initially it was found to be highly active in a number of mouse in vivo cancer assays. Subsequently, CPT was found to uniquely inhibit an enzyme, topoisomerase I, which is involved in DNA replication. A number of CPT analogs are in advanced clinical trial, and two, Topotecan and CPT-11, have been approved for marketing by the FDA. taxol, a taxane alkaloid, was isolated from Taxus brevifolia. Taxol is a highly cytotoxic compound active in several mouse antitumor assays. It was subsequently found to uniquely inhibit tubulin, a protein involved in mitosis. After clinical evaluation, it has become the drug of choice for treatment of ovarian cancer.

译文

喜树碱(CPT)是一种从喜树喜树的木材和树皮中分离出来的五环生物碱。最初发现它在许多小鼠体内癌症试验中具有很高的活性。随后,发现CPT独特地抑制了参与DNA复制的酶拓扑异构酶I。许多CPT类似物正在进行高级临床试验,而FDA已经批准了Topotecan和CPT-11这两种类似物。紫杉醇是一种紫杉烷生物碱,是从短叶红豆杉中分离得到的。紫杉酚是在几种小鼠抗肿瘤试验中有活性的高度细胞毒性化合物。随后发现它可以独特地抑制微管蛋白(一种参与有丝分裂的蛋白质)。经过临床评估,它已成为治疗卵巢癌的首选药物。

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