文章摘要
周芳,杨扬,郭举.新型槲皮素衍生物的合成及其抗肿瘤活性研究[J].安徽医药,2019,23(8):1505-1508.
新型槲皮素衍生物的合成及其抗肿瘤活性研究
Synthesis and antitumor activity of novel quercetin derivatives
投稿时间:2017-10-20  
DOI:
中文关键词: 槲皮素  化学技术,合成  药物筛选试验,抗肿瘤  核磁共振,生物分子  衍生物
英文关键词: Quercetin  Chemistry techniques,synthetic  Drug screening assays,antitumor  Nuclear magnetic resonance,biomolecular  Derivatives
基金项目:
作者单位
周芳 武汉大学中南医院药学部,湖北 武汉 430071 
杨扬 武汉工程大学绿色化工过程教育部重点实验室,湖北 武汉 430205 
郭举 武汉工程大学绿色化工过程教育部重点实验室,湖北 武汉 430205 
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中文摘要:
      目的 设计并合成以槲皮素为母核,研究3′-位羟基引入芳香丙烯基槲皮素衍生物的体外抗肿瘤活性。方法 以槲皮素为原料,用不同取代的芳香丙烯酸与其3′-位羟基缩合成酯,得目标槲皮素衍生物,并通过核磁共振波谱仪(1H-NMR)进行结构表征,同时用噻唑蓝比色法(MTT法)测试目标化合物对不同肿瘤细胞的抗肿瘤活性。结果 通过抗肿瘤活性测试显示,所合成的目标化合物对人结肠癌细胞和乳腺癌细胞表现出了较好的抗肿瘤活性,均达到了微摩尔级,其中化合物5C1和5C6对乳腺癌肿瘤细胞的细胞毒达到了10微摩尔级,半抑制浓度(IC50)分别为10.59 μmol/L和10.31 μmol/L。结论 该系列槲皮素衍生物的合成为后续槲皮素衍生物的合成研究和获得具有潜在抗肿瘤活性的先导化合物奠定了基础。
英文摘要:
      Objective To design and synthesize quercetin derivatives by introducing 3′-aryl acrylic groups and investigate their antitumor activities in vitro.Methods With quercetin as raw material,condensation of 3′-hydroxyl groups with different substituted aromatic acrylic acid was conducted to get target quercetin derivatives,and their structures were characterized by 1H-NMR,of which antitumor activity against different tumor cells was tested by MTT assay.Results The antitumor activity test showed that some compounds exhibited good antitumor activity against human colon cancer cells and breast cancer cells,which all reached the micromolar level.Especially,the cytotoxicity of compound 5C1 and 5C6 against breast cancer cells reached 10 micro-molar level,and their IC50 values were 10.59 and 10.31 μmol/L,respectivly.Conclusion The synthesis of these novel quercetin derivatives laid the foundation for further study on the synthesis of quercetin derivatives and obtaining lead compounds with potential antitumor activity.
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