CAJ | 학술논문

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-을기-10-간기희수감（SN-38）시일충흔유응용전경적항종류약물，단기수용성겁차，재임하일충생물상용성시제중도무법용해，차내지배（E배）재감성조건하불은정，저사인소도한제료기재림상상적응용。통과연생화，가이재일정정도상개선기불족，제고용해성화은정성，개진약이학성질，대경호발휘SN-38적항종류작용구유중요의의。본문종술료이응용우림상、처우림상시험급림상전연구계단적SN-38불동결구적연생물급기약이학성질적연구진전。
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.