1. Academic Validation
  2. Synthesis, cytotoxicity and haemolytic activity of Pulsatilla saponin A, D derivatives

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

  • Bioorg Med Chem Lett. 2015 Jun 15;25(12):2550-4. doi: 10.1016/j.bmcl.2015.04.049.
Zhong Chen 1 Huaqing Duan 1 Minglei Wang 1 Li Han 2 Yanli Liu 1 Yongming Zhu 3 Shilin Yang 4
Affiliations

Affiliations

  • 1 College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, China.
  • 2 Zhang Zhongjing College of Chinese Medicine, Nanyang Institute of Technology, 80 Chang Jiang Road, Nanyang, China.
  • 3 College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, China. Electronic address: zhuyongming@suda.edu.cn.
  • 4 College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, China. Electronic address: yangshilin@suda.edu.cn.
Abstract

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.

Keywords

Cytotoxicity; Derivatives; Haemolytic activity; Pulsatilla saponin A; Pulsatilla saponin D.

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