Nitric oxide-donating derivatives of hederacolchiside A1: Synthesis and biological evaluation in vitro and in vivo as potential anticancer agents

Bioorg Med Chem Lett. 2017 Jan 1;27(1):98-101. doi: 10.1016/j.bmcl.2016.11.021.

Yuanying Fang ¹, Rikang Wang ¹, Mingzhen He ¹, Hesong Huang ¹, Qi Wang ¹, Zunhua Yang ², Yan Li ¹, Shilin Yang ³, Yi Jin ⁴

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. Electronic address: joshyyy@126.com.
3 College of Pharmacy, Jiangxi University of Traditional Chinese Medicine, 818 Xingwan Road, Nanchang 330004, China.
4 National Engineering Research Center for Manufacturing Technology of TCM Solid Preparation, Jiangxi University of Traditional Chinese Medicine, 56 Yangming Road, Nanchang 330006, China. Electronic address: yinghua616909@hotmail.com.

PMID: 27866816 DOI: 10.1016/j.bmcl.2016.11.021

Abstract

A series of nitric oxide (NO) donating derivatives of hederacolchiside A₁ bearing triterpenoid saponin motif were designed, synthesized and evaluated for their Anticancer activity. All of the tested furoxan-based NO releasing compounds showed significant proliferation inhibitory activities. Especially compound 6a exhibited strong cytotoxicity (IC₅₀=1.6-6.5μM) against four human tumor cell lines (SMMC-7721, NCI-H460, U251, HCT-116) in vitro and the highest level of NO releasing. Furthermore, compound 6a was revealed low acute toxicity to mice and weak haemolytic activity with potent tumor growth inhibition against mice H22 hepatocellular cells in vivo (51.5%).

Keywords

Anticancer activity; Furoxan; Hederacolchiside A(1); Nitric oxide; Triterpenoid saponin.

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