7-乙基-10-羟基喜树碱衍生物药理学性质研究进展

摘要

7-Ethyl-10-hydroxycamptothecin (SN-38) is a prominent anticancer agent, but it is insoluble in water and the most pharmaceutically acceptable solvents, the lactone ring of SN-38 shows reversible pH-dependent hydrolysis and forms to the open lactone in alkaline condition. All of these factors limit its application in clinic, and a variety of chemical modification studies have been reported to improve the efficient use of SN-38 by improving its solubility in water and pharmaceutical solvents, stabilizing the lactone form, and altering the pharmacological properties. This paper reviews the pharmacological properties of commercial SN-38 derivatives in clinical trials or preclinical studies and their research progress.%7-乙基-10-羟基喜树碱（SN-38）是一种很有应用前景的抗肿瘤药物，但其水溶性极差，在任何一种生物相容性试剂中都无法溶解，且内酯环（E环）在碱性条件下不稳定，这些因素都限制了其在临床上的应用。通过衍生化，可以在一定程度上改善其不足，提高溶解性和稳定性，改进药理学性质，对更好发挥SN-38的抗肿瘤作用具有重要意义。本文综述了已应用于临床、处于临床试验及临床前研究阶段的SN-38不同结构的衍生物及其药理学性质的研究进展。