Synthesis, cytotoxicity and haemolytic activity of Pulsatilla saponin A, D derivatives

被引:30
作者
Chen, Zhong [1 ]
Duan, Huaqing [1 ]
Wang, Minglei [1 ]
Han, Li [2 ]
Liu, Yanli [1 ]
Zhu, Yongming [1 ]
Yang, Shilin [1 ]
机构
[1] Soochow Univ, Coll Pharmaceut Sci, Suzhou 215123, Peoples R China
[2] Nanyang Inst Technol, Zhang Zhongjing Coll Chinese Med, Nanyang, Peoples R China
基金
中国国家自然科学基金;
关键词
Cytotoxicity; Haemolytic activity; Pulsatilla saponin A; Pulsatilla saponin D; Derivatives; CHINENSIS BUNGE REGEL; ANTITUMOR PRINCIPLE; APOPTOSIS; TRITERPENOIDS;
D O I
10.1016/j.bmcl.2015.04.049
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
The strong haemolytic activity of Pulsatilla saponin A (PSA), D (PSD) hampered their clinical development of antitumor agents. In order to solve this problem, C-28 position modification derivatives of PSA/PSD were synthesized. The cytotoxicity and haemolytic activity of these compounds were evaluated. Structure-activity relationship and structure-toxicity relationship had been observed. The mice acute toxicity of compound 11 was reduced greatly than that of PSA. This study indicates that compound 11 may represent an interesting class of potent antitumor agents from triterpenoid saponins avoiding the haemolysis problem. The present study has important significance for the development of antitumor saponins. (C) 2015 Elsevier Ltd. All rights reserved.
引用
收藏
页码:2550 / 2554
页数:5
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