Synthesis and biological evaluation of Hederacolchiside A1 derivatives as anticancer agents

Bioorg Med Chem Lett. 2016 Oct 1;26(19):4576-4579. doi: 10.1016/j.bmcl.2016.08.077.

Yuanying Fang ¹, Zunhua Yang ², Hui Ouyang ¹, Rikang Wang ¹, Jun Li ¹, Hesong Huang ¹, Yi Jin ¹, Yulin Feng ¹, Shilin Yang ²

Affiliations

1 National Engineering Research Center for Manufacturing Technology of TCM Solid Preparation, Jiangxi University of Traditional Chinese Medicine, 56 Yangming Road, Nanchang 330006, China.
2 College of Pharmacy, Jiangxi University of Traditional Chinese Medicine, 818 Xingwan Road, Nanchang 330004, China.

PMID: 27592134 DOI: 10.1016/j.bmcl.2016.08.077

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%).

Keywords

Anticancer activity; Derivatives; Hederacolchiside A(1); Triterpenoid saponins.

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