title: Synthesis, cytotoxicity and haemolytic activity of Pulsatilla saponin A, D derivatives.
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.
authors.affiliation: College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, China.
authors.forename: Zhong
authors.initials: Z
authors.lastname: Chen
authors.affiliation: College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, China.
authors.forename: Huaqing
authors.initials: H
authors.lastname: Duan
authors.affiliation: College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, China.
authors.forename: Minglei
authors.initials: M
authors.lastname: Wang
authors.affiliation: Zhang Zhongjing College of Chinese Medicine, Nanyang Institute of Technology, 80 Chang Jiang Road, Nanyang, China.
authors.forename: Li
authors.initials: L
authors.lastname: Han
authors.affiliation: College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, China.
authors.forename: Yanli
authors.initials: Y
authors.lastname: Liu
authors.affiliation: College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, China. Electronic address: zhuyongming@suda.edu.cn.
authors.forename: Yongming
authors.initials: Y
authors.lastname: Zhu
authors.affiliation: College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, China. Electronic address: yangshilin@suda.edu.cn.
authors.forename: Shilin
authors.initials: S
authors.lastname: Yang
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D051379:Mice; D012503:Saponins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; C000601508:Pulsatilla saponin D; D012503:Saponins; C000588664:Pulsatilla saponin A
keywords: Cytotoxicity; Derivatives; Haemolytic activity; Pulsatilla saponin A; Pulsatilla saponin D