title: A novel method for synthesis of α-spinasterol and its antibacterial activities in combination with ceftiofur.
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.
authors.affiliation: Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, Sichuan 611130, China.
authors.forename: Xiaomin
authors.initials: X
authors.lastname: Yang
authors.affiliation: Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, Sichuan 611130, China.
authors.forename: Jianyu
authors.initials: J
authors.lastname: Zhou
authors.affiliation: Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu 610041, China.
authors.forename: Tao
authors.initials: T
authors.lastname: Wang
authors.affiliation: Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, Sichuan 611130, China.
authors.forename: Ling
authors.initials: L
authors.lastname: Zhao
authors.affiliation: Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, Sichuan 611130, China.
authors.forename: Gang
authors.initials: G
authors.lastname: Ye
authors.affiliation: Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, Sichuan 611130, China.
authors.forename: Fei
authors.initials: F
authors.lastname: Shi
authors.affiliation: Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, Sichuan 611130, China. Electronic address: liyinglun01@163.com.
authors.forename: Yinglun
authors.initials: Y
authors.lastname: Li
authors.affiliation: Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, Sichuan 611130, China.
authors.forename: Huaqiao
authors.initials: H
authors.lastname: Tang
authors.affiliation: Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, Sichuan 611130, China.
authors.forename: Qi
authors.initials: Q
authors.lastname: Dong
authors.affiliation: Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, Sichuan 611130, China.
authors.forename: Xuerong
authors.initials: X
authors.lastname: Zhou
authors.affiliation: Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, Sichuan 611130, China.
authors.forename: Min
authors.initials: M
authors.lastname: Xu
authors.affiliation: Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, Sichuan 611130, China.
authors.forename: Qian
authors.initials: Q
authors.lastname: Rong
authors.affiliation: Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, Sichuan 611130, China.
authors.forename: Helin
authors.initials: H
authors.lastname: Chen
authors.affiliation: Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, Sichuan 611130, China.
authors.forename: Xiaoyu
authors.initials: X
authors.lastname: Yang
authors.affiliation: Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, Sichuan 611130, China.
authors.forename: Yu
authors.initials: Y
authors.lastname: Cai
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002511:Cephalosporins / Q000494:pharmacology*; D004357:Drug Synergism; D004926:Escherichia coli / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013210:Staphylococcus / Q000187:drug effects; D013265:Stigmasterol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D002511:Cephalosporins; C031312:spinasterol; C053503:ceftiofur; D013265:Stigmasterol
keywords: Antibacterial activity; Ceftiofur; Stigmasterol; α-Spinasterol