| 高阳,王文慧,宋懿婧,等.海洋天然产物brefeldin A的衍生物制备及细胞毒活性评价(英文)[J].中国海洋药物,2024,43(4):28-34. |
| 海洋天然产物brefeldin A的衍生物制备及细胞毒活性评价(英文) |
| Preparation and cytotoxicity evaluation of marinenatural product brefeldin A derivatives |
| 投稿时间：2023-04-10 修订日期：2023-05-19 |
| DOI：10.13400/j.cnki.cjmd.2024.04.007 |
| 中文关键词: 结构修饰 brefeldin A衍生物 细胞毒活性 海洋天然产物 |
| English Keywords:structural modification brefeldin A derivatives cytotoxic activity marine natural product |
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| 中文摘要: |
| 目的 对海洋天然产物brefeldin A (1) 的双键以及羟基进行修饰，半合成9个衍生物2~10并考察其对人非小细胞肺癌细胞系A549细胞的抑制活性。方法 利用MTT法,用人非小细胞肺癌细胞系A549对衍生物进行细胞毒活性测定。结论 通过对化合物1的结构引入硫原子、乙酰化修饰分别得到衍生物2~7和8~10，所有衍生物均可在1 μmol/L以下抑制A549细胞生长，其中衍生物5和9活性较为显著，IC50值分别为40 nM和98 nM，可作为潜在的抗癌先导化合物。
关键词：结构修饰; brefeldin A衍生物；细胞毒活性；海洋天然产物 |
| English Summary: |
| Objective To modify the double bonds and hydroxyl groups of marine natural product brefeldin A (1), derivatives 2~10 were prepared and their inhibitory activities against lung adenocarcinoma epithelial A549 were evaluated. Methods The cytotoxic activities of all derivatives (2~10) against lung adenocarcinoma epithelial A549 were evaluated using MTT assay. Conclusion Derivatives 2~7 and 8~10 were designed and synthesized via introducing sulfur atoms and acetylation into the structure of 1, respectively. All derivatives can inhibit the growth of A549 cells below 1 μmol/L, among which derivatives 5 and 9 exhibited significant activities, with IC50 values of 40 nM and 98 nM respectively, which can be used as potential anticancer lead compounds.
Keywords: structural modification; brefeldin A derivatives; cytotoxic activity; marine natural product |
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