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Mini-Reviews in Medicinal Chemistry

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ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

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Research Article

Synthesis, Characterization and Anti-hepatoma Activity of New Hederagenin Derivatives

Author(s): Xiao Liu, Lu Sun, Qing-Hua Liu, Bao-Quan Chen* and Yu-Ming Liu*

Volume 20, Issue 3, 2020

Page: [252 - 257] Pages: 6

DOI: 10.2174/1389557519666191010091612

Price: $65

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Abstract

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.

Keywords: Nigella glandulifera, hederagenin-type saponin, hederagenin, structural modification, anti-hepatoma, cytotoxicity.

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