吲哚查尔酮衍生物FC58的抗白血病多药耐药活性研究  

Cytotoxicity study on FC58,an indole-chalcone,against multi-drug resistant leukemia cells

作　　者：戴佳炜 施赛健 宋瑷蔚 王志斌 庄春林 夏春年[1] DAI Jiawei;SHI Saijian;SONG Aiwei;WANG Zhibin;ZHUANG Chunlin;XIA Chunnian(School of Pharmacy,Zhejiang University of Technology,Hangzhou 310014,China;School of Pharmacy,Naval Medical University,Shanghai 200433,China;Montverde Academy Shanghai,Shanghai 201201,China)

机构地区：[1]浙江工业大学药学院,浙江杭州310014 [2]海军军医大学药学院,上海200433 [3]上海蒙特沃德学院

出　　处：《药学实践杂志》2021年第4期305-308,共4页Journal of Pharmaceutical Practice

基　　金：上海市卫健委优秀青年人才培养计划(2017YQ052)。

摘　　要：目的合成吲哚查尔酮衍生物FC58,考察其对白血病细胞的抑制活性。方法以3,4,5-三甲氧基苯乙酮和吲哚-3-甲醛为原料,经羟醛缩合得到目标化合物。采用CellTiter-Blue法测试体外抗肿瘤活性,并通过细胞周期实验分析其作用特点。结果FC58对多种白血病细胞均有较强活性,活性抗耐药指数远高于传统微管蛋白抑制剂紫杉醇、长春碱和多柔比星,并使细胞周期停滞在G2/M期。结论FC58是一个极具潜力的抗耐药白血病的先导化合物。Objective To synthesize and investigate cytotoxicity of an indole-chalcone derivative FC58.Methods The target compound was synthesized through the Aldol condensation with 1-(3,4,5-trimethoxyphenyl)ethan-1-one and 1H-indole-3-carbaldehyde.The Cell Titer-Blue method was used to determine in vitro cytotoxicity.The cell cycle experiment was performed to analyze the action characteristics of FC58.Results FC58 exhibited high cytotoxicity against various leukemia cells and resulted in G2/M phase arrest.It showed stronger drug resistant index than traditional tubulin inhibitors such as paclitaxel,vinblastine and doxorubicin.Conclusion FC58 represents a promising lead compound for multi-drug resistant leukemia.

关 键 词：吲哚查尔酮 白血病 多药耐药 抗肿瘤活性 微管蛋白 

分 类 号：R914[医药卫生—药物化学]