| 吲哚查尔酮衍生物FC58的抗白血病多药耐药活性研究 |
| 投稿时间：2020-12-16 修订日期：2021-02-26 点此下载全文 |
| 引用本文：戴佳炜,施赛健,宋瑷蔚,王志斌,庄春林,夏春年.吲哚查尔酮衍生物FC58的抗白血病多药耐药活性研究[J].药学实践杂志,2021,39(4):305~308 |
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| 基金项目:上海市卫健委优秀青年人才培养计划 (2017YQ052) |
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| 中文摘要: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。 |
| 中文关键词:吲哚查尔酮 白血病 多药耐药 抗肿瘤活性 微管蛋白 |
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| Cytotoxicity study on FC58, an indole-chalcone, against multi-drug resistant leukemia cells |
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| Abstract: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. |
| keywords:indole-chalcone anti-leukemia multi-drug resistance cytotoxicity tubulin |
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