Research of screening of azole antifungal drugs and antibacterial mechanism
Objective In order to obtain drugs with good antibacterial activity in vitro,the antifungal activity of 14 kinds of azole chemical synthetic drugs(A1-A7 and B1-B7)was screened.The antifungal mechanism of Candida albicans was discussed.Methods The minimum inhibitory concentration(MIC)and minimum fungicidal concentration(MFC)of the drug were measured by microliquid dilution method.Time sterilization curve was measured by AGAR plate counting method.The checkerboard dilution method was used to determine the antibacterial effect of the compound in vitro,and the highly effective antifungal compound was screened.Based on compound B7,the morphological changes of Candida albicans were observed through the induction of liquid mycelia,the inhibition of biofilm formation was measured by XTT method,and the in vitro antifungal activity of the compound against Candida albicans and its mechanism of action were preliminarily investigated by the primary fluorescence determination of oxidative stress reactive oxygen species in fungal cells.Results In this study,compound B7 was screened from 14 azole compounds with good antifungal effects in vitro,represented by Candida albicans ATCC SC5314,whose MIC was 0.062 5 μg·mL-1,and MFC was 0.25 μg·mL-1,and its bactericidal activity was dose-dependent.The combination with fluconazole has additive effect.The mycelium induction experiment showed that B7 had obvious inhibitory effect on mycelium growth,and the XTT experiment showed that compound B7 had certain inhibitory effect on biofilm.The primary fluorescence determination of oxidative stress reactive oxygen species in fungal cells showed that compound B7 could increase the oxidative stress reactive oxygen species of Candida albicans with increasing concentration and was always higher than that of miconazole positive control group.Conclusion Compound B7 has good antifungal effect in vitro,and can inhibit mycelium growth and biofilm formation.
candida albicanspathogenic mechanismantibacterial in vitro
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