摘要
抗癌药物多西紫杉醇在临床使用中会引起许多毒副作用,开发低毒和具有靶向性的新型紫杉烷类药物制剂是一个非常重要的研究课题。本研究探索多西紫杉醇与人血清白蛋白化学交联药物的合成,试验将多西紫杉醇的2’羟基位与人血清白蛋白的34位半胱氨酸上的巯基处通过10-十一烯酸进行精确的共价交联。合成的中间产物及最终产物使用了质谱进行了鉴定和表征。测定结果证实了抗癌药物多西紫杉醇可通过10-十一烯酸与人血清白蛋白进行化学交联并能生成1:1的交联产物。本研究的结果对于进一步开发新型的紫杉烷类白蛋白化学共价交联药物制剂提供了一种新策略。
The formulation of docetaxel in clinical use has many severe side effects. Consequently, development of new kind of formulation of docetaxel with high efficiency and low side effects is a very important issue. In this study, we explored the exact covalent linkage of docetaxel and albumin by one small organic linker. 10-Undecenoic acid was applied to exactly link the 2＇ hydroxyl of docetaxel with the cysteine-34 of albumin to obtain 1：1 docetaxel-albumin conjugate. The obtained intermediate and final conjugate was characterized by MS spectrometry. The produced 1：1 docetaxel-albumin conjugate can be considered as the prodrugs of docetaxel. The present study provided a conjugation strategy for further development of new kind of docetaxel-albumin prodrugs.
作者
彪林海
王元林
刘志国
BiaO Linhai;Wang Yuanlin;Liu Zhiguo(Key Laboratory of Forest Plant Ecology, Ministry of Education, Northeast Forestry University, Harbin 150040, People＇s Republic of China)
出处
《生命科学仪器》
2017年第5期41-44,55,共5页
Life Science Instruments
基金
哈尔滨市创新人才项目(NO.2015RQQXJ053)
中央高校基本科研业务费专项资金基金(NO.2572017EY01)
黑龙江省科学基金(NO.LC2015008)
