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

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.

1.A novel method was constructed for the synthesis of α-spinasterol from commercially available stigmasterol.2.The synergistic antibacterial activities α-spinasterol and ceftiofur in vitro against Escherichia coli, Streptococcus pneumoniae, Salmonella pullorum, and Staphylococcus aureus showed intriguing results.3.The combination of ceftiofur and α-spinasterol exhibited time-dependency and concentration-dependency comparing to time dependency with ceftiofur alone.155