摘要
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。
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.
出处
《国际药学研究杂志》
CAS
CSCD
北大核心
2015年第3期310-315,共6页
Journal of International Pharmaceutical Research
基金
上海市科学技术委员会纳米专项资助项目(12nm0501000)
