生物素标记多杀菌素衍生物合成及其抗肿瘤活性研究  

Synthesis of biotin-labeled spinosyn and its anti-tumor activity

作　　者：许娜 彭婷[2] 罗志勇[2] 邹自征[2] 马大友 刘苏友 刘丽君[2] XU Na;PENG Ting;LUO Zhi-yong;ZOU Zi-zheng;MA Da-you;LIU Su-you;LIU Li-jun(Xiangya School of Pharmaceutical Sciences,Central South University,Changsha 410013;School of Life Sciences,Central South University,Changsha 410013)

机构地区：[1]中南大学湘雅药学院,长沙410013 [2]中南大学生命科学学院,长沙410013

出　　处：《中南药学》2021年第9期1828-1832,共5页Central South Pharmacy

摘　　要：目标合成生物素标记的多杀菌素探针分子。方法以多杀菌素A为原料,经去甲基反应、亲核取代反应、酯化等反应,合成生物素标记的多杀菌素衍生物,并经过1H-NMR、13C-NMR、HRMS进行结构表征。以人乳腺癌细胞MCF-7为模型研究该类化合物的体外抗肿瘤活性。结果生物素标记多杀菌素衍生物2、5、6表现出较好的抗肿瘤细胞增殖活性,其中化合物6的活性最好。结论化合物6可作为生物素标记探针进行多杀菌素衍生物的抗肿瘤作用机制研究。Objective To synthesize biotin-labeled spinosyn probes.Methods Biotin-spinosyn probes were synthesized from spinosyn A via demethylation,nucleophilic substitution and esterification.All the synthesized compounds were characterized and comfirmed by 1H-NMR,13C-NMR and HRMS.The in vitro anti-tumor activity against MCF-7 was evaluated.Results Biotin-labeled spinosyn probes 2,5 and 6 showed good anti-tumor activity,among which 6 was the best.Conclusion Compound 6 may be used as a probe to investigate the anti-tumor mechanism of spinosyns.

关 键 词：多杀菌素 合成 探针 生物素标记 抗肿瘤活性 

分 类 号：R916[医药卫生—药学] R914.5