2. Academic Validation
  3. The derivatives of Pulsatilla saponin A, a bioactive compound from Pulsatilla chinensis: Their synthesis, cytotoxicity, haemolytic toxicity and mechanism of action

The derivatives of Pulsatilla saponin A, a bioactive compound from Pulsatilla chinensis: Their synthesis, cytotoxicity, haemolytic toxicity and mechanism of action

  • Eur J Med Chem. 2017 Mar 31:129:325-336. doi: 10.1016/j.ejmech.2017.02.025.
Xiaohang Tong 1,  Li Han 2,  Huaqing Duan 3,  Yaru Cui 4,  Yulin Feng 4,  Yongming Zhu 3,  Zhong Chen 5,  Shilin Yang 6
Affiliations

Affiliations

  • 1 College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, China; College of Pharmaceutical Science, Guizhou University, 242Hua Xi Avenue, Guiyang 550025, China.
  • 2 Zhang Zhongjing College of Chinese Medicine, Nanyang Institute of Technology, 80 Chang Jiang Road, Nanyang 473000, China.
  • 3 College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, China.
  • 4 Jiangxi University of Traditional Chinese Medicine, Nanchang, 56 Yang Ming Road, Nanchang 330006, China.
  • 5 College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, China. Electronic address: chinacczz0720@gmail.com.
  • 6 College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, China; College of Pharmaceutical Science, Guizhou University, 242Hua Xi Avenue, Guiyang 550025, China; Jiangxi University of Traditional Chinese Medicine, Nanchang, 56 Yang Ming Road, Nanchang 330006, China.
PMID: 28237662 DOI: 10.1016/j.ejmech.2017.02.025
Abstract

The strong haemolytic toxicity of Pulsatilla saponin A (PSA) has hampered its clinical development as an injectable Anticancer agent. To circumvent this challenge, twenty PSA derivatives with C ring or C-28 or C-3 modifications were synthesized and evaluated for cytotoxicity against seven selected human tumor lines, as well as for haemolytic toxicity. Structure-activity relationship (SAR) and structure-toxicity relationship (STR) correlations were also elucidated. Compared with PSA, compound 22 showed a better balance between haemolytic toxicity (HD50 > 500 μM) and cytotoxicity toward lung Cancer cells A549 (IC50 = 4.68 μM). Molecular studies indicated that 22 was liked to lead to G1 cell cycle arrest and therefore, 22 may be a potent antitumor drug candidate.

Keywords

Cell cycle arrest; Cytotoxicity; Haemolytic activity; Pulsatilla saponin A; Structure–activity relationship (SAR).

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