喜树碱是一种强效抗癌的天然化合物,其杀伤肿瘤能力突出,并且机理特殊,引起了科学界的兴趣,但是由于其溶解性差,不良反应强的原因限制了其临床应用。所以人们希望通过分子改造和剂型变化来增强喜树碱的成药性。本文针对喜树碱的作用机理、分子修饰及剂型变化进行了综述。 Camptothecin is a potent anti-cancer natural compound with prominent tumor-killing ability and unique mechanism, which has aroused the interest of the scientific community. However, its clinical application is limited due to its poor solubility and strong adverse reactions. Therefore, people hope that through the molecular modification and formulation changes to enhance the camptothecin drug-induced. In this paper, the mechanism of action of camptothecin, molecular modification and formulation changes are reviewed.