| 许颖,陈露,程相成,等.海洋天然产物geodin系列衍生物的细胞毒活性评价及构效关系初步研究(英文）[J].中国海洋药物,2023,42(5):54-58. |
| 海洋天然产物geodin系列衍生物的细胞毒活性评价及构效关系初步研究(英文） |
| Cytotoxic evaluation and preliminary structure-activity relationships of the marine natural product geodin and its derivatives |
| 投稿时间：2022-07-26 修订日期：2022-09-17 |
| DOI：10.13400/j.cnki.cjmd.2023.05.005 |
| 中文关键词: 海洋天然产物 geodin 衍生物 细胞毒活性 构效关系 |
| English Keywords:marine natural products geodin derivatives cytotoxic activity structure-activity relationship |
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| 中文摘要: |
| 摘 要：目的 目前癌症仍然是威胁人类健康的恶性疾病之一，临床使用的传统药物通常受到耐药性和副作用的限制，因此寻找新型高效的抗癌药物迫在眉睫。对具有grisan 骨架的海洋天然产物geodin (1) 及其衍生物（2?26）进行了细胞毒活性评价，并探究了其初步构效关系。方法 采用MTT法，用人非小细胞肺癌细胞系A549和人肝癌细胞系HepG2、Bel-7402对geodin (1) 及其衍生物（2?26）进行了细胞毒活性评价。结果 对Geodin 的4-OH修饰后得到的衍生物中，化合物2?4, 6, 7, 9?18和20?25表现出强到中等程度的细胞毒活性，IC50值在0.81 ~ 4.78 μM之间。特别是化合物16，对A549和HepG2细胞表现出强效的细胞毒活性，其IC50值分别为0.86和0.81 μM。结论 化合物16是一种潜在的抗癌先导化合物。 |
| English Summary: |
| Abstract: Objective Cancer is still one of the malignant diseases threatening human health. Traditional drugs used in clinic are usually limited by drug resistance and side effects, so it is urgent to discover new and efficient anticancer drugs. The cytotoxic activities of geodin (1), with the grisan skeleton isolated from marine fungus Aspergillus sp., and its derivatives (2?26) were evaluated against three cancer cell lines. The preliminary structure-activity relationships were also discussed. Methods The cytotoxic activities of geodin (1) and its derivatives against lung adenocarcinoma epithelial A549, hepatocellular carcinoma HepG2 and Bel-7402 cell lines were evaluated using MTT assay. Results Most of the 4-OH modified derivatives (2?4, 6, 7, 9?18 and 20?25) of geodin (1) showed strong to moderate cytotoxic activities，with IC50 values of ranging from 0.81 μM to 4.78 μM. Especially, compound 16 exhibited strong cytotoxic activities against A549 and HepG2 cell lines with the IC50 values of 0.86 and 0.81 μM, respectively. Conclusion Compound 16 is a potential anticancer lead compound. |
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