Synthesis and biological evaluation of Hederacolchiside A1 derivatives as anticancer agents

被引：14

作者：

Fang, Yuanying ^{[1
]}

Yang, Zunhua ^{[2
]}

Ouyang, Hui ^{[1
]}

Wang, Rikang ^{[1
]}

Li, Jun ^{[1
]}

Huang, Hesong ^{[1
]}

Jin, Yi ^{[1
]}

Feng, Yulin ^{[1
]}

Yang, Shilin ^{[2
]}

机构：

[1] Jiangxi Univ Tradit Chinese Med, Natl Engn Res Ctr Mfg Technol TCM Solid Preparat, 56 Yangming Rd, Nanchang 330006, Peoples R China

[2] Jiangxi Univ Tradit Chinese Med, Coll Pharm, 818 Xingwan Rd, Nanchang 330004, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2016年 / 26卷 / 19期

关键词：

Hederacolchiside A(1); Triterpenoid saponins; Derivatives; Anticancer activity; CHINENSIS BUNGE REGEL; ANTITUMOR-ACTIVITY; PULSATILLA; SAPONINS;

D O I：

10.1016/j.bmcl.2016.08.077

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：

Modification of Hederacolchiside A(1) (HA(1)) on 28-COOH gave a series of novel triterpenoid saponin compounds containing ester or amide group. Comparing with natural product HA(1), 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 = 1.1-4.6 mu M) and potent tumor inhibition rate in vivo (46.8%). (C) 2016 Elsevier Ltd. All rights reserved.

引用

收藏

页码：4576 / 4579

页数：4

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