新型羽扇豆烷衍生物的合成、表征及抗肝癌活性。
Synthesis, Characterization and Anti-hepatoma Activity of New Hederagenin Derivatives.
机构信息
Department of Pharmacy Engineering, School of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, China.
Xinjiang Institute of Materia Medica, Urumuqi 830001, China.
出版信息
Mini Rev Med Chem. 2020;20(3):252-257. doi: 10.2174/1389557519666191010091612.
BACKGROUND
Based on the biological significance of hederagenin-type saponins found in our previous investigation, a series of new hederagenin derivatives were designed and synthesized.
METHODS
Their in vitro antiproliferative activities were evaluated against the HepG2 liver cancer cell line and normal cell line L929 by MTT assay.
RESULTS
The preliminary bioassay results demonstrated that all the tested compounds 1-7 showed potent anti-hepatoma activities, and some compounds exhibited better effects than 5-fluorouracil against human hepatocellular carcinoma HepG2 cell line. Furthermore, compound 5 showed a significant antihepatoma activity against HepG2 cells with an IC50 value of 1.88 µM. Besides, all of the tested compounds showed a low cytotoxic effect against the normal cell line L929.
CONCLUSION
All the compounds 1-7 displayed superior selectivity against human hepatocellular carcinoma HepG2 cell line, and the results suggest that the structural modifications of C ring on the hederagenin backbone are vital for modulating anti-hepatoma activities.
背景
基于我们之前的研究中发现的皂皮酸型甾体皂苷的生物学意义，设计并合成了一系列新的皂皮酸衍生物。
方法
通过 MTT 法测定它们对 HepG2 肝癌细胞系和正常细胞系 L929 的体外增殖活性。
结果
初步的生物测定结果表明，所有测试的化合物 1-7 均表现出很强的抗肝癌活性，一些化合物对人肝癌 HepG2 细胞系的作用优于 5-氟尿嘧啶。此外，化合物 5 对 HepG2 细胞表现出显著的抗癌活性，IC50 值为 1.88µM。此外，所有测试的化合物对正常细胞系 L929 的细胞毒性作用都较低。
结论
所有化合物 1-7 对人肝癌 HepG2 细胞系均表现出较高的选择性，结果表明皂皮酸主链 C 环的结构修饰对于调节抗癌活性至关重要。
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