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

作者：Fang, Yuanying; Wang, Rikang; He, Mingzhen; Huang, Hesong; Wang, Qi; Yang, Zunhua^*; Li, Yan; Yang, Shilin; Jin, Yi^*

来源：Bioorganic & Medicinal Chemistry Letters, 2017, 27(1): 98-101.

DOI：10.1016/j.bmcl.2016.11.021

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

A series of nitric oxide (NO) donating derivatives of hederacolchiside A(1) 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 = 1.6-6.5 mu M) 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%).

• 出版日期2017-1-1
• 单位江西中医药大学