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  2. A novel method for synthesis of α-spinasterol and its antibacterial activities in combination with ceftiofur

A novel method for synthesis of α-spinasterol and its antibacterial activities in combination with ceftiofur

  • Fitoterapia. 2017 Jun;119:12-19. doi: 10.1016/j.fitote.2017.03.011.
Xiaomin Yang 1 Jianyu Zhou 1 Tao Wang 2 Ling Zhao 1 Gang Ye 1 Fei Shi 1 Yinglun Li 3 Huaqiao Tang 1 Qi Dong 1 Xuerong Zhou 1 Min Xu 1 Qian Rong 1 Helin Chen 1 Xiaoyu Yang 1 Yu Cai 1
Affiliations

Affiliations

  • 1 Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, Sichuan 611130, China.
  • 2 Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu 610041, China.
  • 3 Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, Sichuan 611130, China. Electronic address: liyinglun01@163.com.
Abstract

In this study, we designed a novel method of the synthesis of α-spinasterol from commercially available stigmasterol and explored the combinational effect of the α-spinasterol with ceftiofur in vitro against S. pullorum cvcc533, S. pneumoniae CAU0070, E. coli, and S. aureus. α-Spinasterol was obtained by a key reaction of Bamford-Stevens reaction with a desirable yield for five steps. The combination of α-spinasterol and ceftiofur showed stronger synergetic effect against the four pathogenic strains compared with that of stigmasterol and ceftiofur alone. In time-kill analyses, at concentrations above the MICs, ceftiofur in combination with α-spinasterol exhibited time-dependency and concentration-dependency comparing to time dependency with ceftiofur alone. We conclude that the combination usage of α-spinasterol and ceftiofur is an effective and promising strategy against the four pathogenic Bacterial strains in vitro.

Keywords

Antibacterial activity; Ceftiofur; Stigmasterol; α-Spinasterol.

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