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Updated: Mar 15, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis and biological evaluation of Hederacolchiside A1 derivatives as anticancer agents
Yuanying Fang1, Zunhua Yang2, Hui Ouyang1
1National Engineering Research Center for Manufacturing Technology of TCM Solid Preparation, Jiangxi University of Traditional Chinese Medicine, 56 Yangming Road, Nanchang 330006, China.
Abstract:
Modification of Hederacolchiside A1 (HA1) on 28-COOH gave a series of novel triterpenoid saponin compounds containing ester or amide group. Comparing with natural product HA1, several derivatives showed decreased toxicity in the mice acute toxicity trial and increased the anticancer activity in vitro. Especially compound 1 exhibited the strongest antiproliferative activities against human cancer cell lines tested (IC50=1.1-4.6μM) and potent tumor inhibition rate in vivo (46.8%).
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