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

作者：Yang, Xiaomin; Zhou, Jianyu; Wang, Tao; Zhao, Ling; Ye, Gang; Shi, Fei; Li, Yinglun^*; Tang, Huaqiao; Dong, Qi; Zhou, Xuerong; Xu, Min; Rong, Qian; Chen, Helin; Yang, Xiaoyu; Cai, Yu

来源：Fitoterapia, 2017, 119: 12-19.

DOI：10.1016/j.fitote.2017.03.011

• Ceftiofur
• alpha-Spinasterol
• Stigmasterol
• Antibacterial activity

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

• 出版日期2017-6
• 单位四川农业大学; 中国科学院成都生物研究所