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

被引:18
作者
Fang, Yuanying [1 ]
Wang, Rikang [1 ]
He, Mingzhen [1 ]
Huang, Hesong [1 ]
Wang, Qi [1 ]
Yang, Zunhua [2 ]
Li, Yan [1 ]
Yang, Shilin [2 ]
Jin, Yi [1 ]
机构
[1] Jiangxi Univ Tradit Chinese Med, Natl Engn Res Ctr Mfg Technol TCM Solid Preparat, 56 Yangming Rd, Nanchang 330006, Jiangxi, Peoples R China
[2] Jiangxi Univ Tradit Chinese Med, Coll Pharm, 818 Xingwan Rd, Nanchang 330004, Jiangxi, Peoples R China
关键词
Nitric oxide; Hederacolchiside A(1); Furoxan; Triterpenoid saponin; Anticancer activity; TRITERPENOID SAPONINS; 1,2,4-TRIAZOLE/OXIME HYBRIDS; HEMOLYTIC-ACTIVITY; CARCINOMA; ACID; DESIGN;
D O I
10.1016/j.bmcl.2016.11.021
中图分类号
R914 [药物化学];
学科分类号
100705 [微生物与生化药学];
摘要
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%). (C) 2016 Elsevier Ltd. All rights reserved.
引用
收藏
页码:98 / 101
页数:4
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