五环三萜类柴胡皂苷单体对白念珠菌伊曲康唑耐药株活性研究

Effect of monomers(pentaeyclic triterpennoids of saikosaponines) from Buplerum kunmingense against itraconazole-resistant Candida albicans strains

目的从柴胡中提取具有抗真菌活性的五环三萜类单体Bp3,研究该单体对伊曲康唑耐药白念珠菌菌株的作用及其与伊曲康唑的相互作用。方法参照CLSI标准,采用棋盘微量稀释法,测定单用Bp3、伊曲康唑及两者联合使用时对20株伊曲康唑耐药白念珠菌菌株的MIC,计算部分抑菌浓度指数(FIC),判定两药相互作用。结果单独用药时Bp3及伊曲康唑对伊曲康唑耐药白念珠菌菌株MIC的几何均数值(GM值)分别为1.941μg/mL和1.008μg/mL。联合用药时Bp3和伊曲康唑的GM值分别降低为1.189μg/mL和0.346μg/mL。2种药物单用和联合使用时MIC值差异均有统计学意义(P<0.05),联用时在20株耐药株均表现为协同或相加作用。结论五环三萜类单体Bp3对白念珠菌伊曲康唑耐药株有一定的抑制作用,且与伊曲康唑有协同或相加作用。

Objective To study the antifungal activity of the monomer Bp3（saikosaponins） isolated from Bupleurum kunmingense with chemical structure of Pentaeyclic triterpennoids.Methods According to the Standard of Clinical and Laboratory Standards Institute（CLSI）,the microdilution method and checkerboard microdilution method were used to determine the antifungal activities of Bp3,itraconazole and their combination to itraconazole-resistant C.albicans strains respectively.Results The minimal inhibitory concentrations（MIC） of Bp3 and itraconazole alone were 1.941 μg/mL and 1.008 μg/mL,respectively.In the combination,the MIC of Bp3 and itraconazole were 1.189 μg/mL and 0.346 μg/mL respectively.The geometric mean（MG） of Bp3 and itraconazole were significant reduce in MIC.The interaction analysis showed that synergistic and additive effects were showed in these isolates.Conclusion Comparing with any single agent,the combination of Bp3 and itraconazole was significantly more active to itraconazole-resistant C.albicans strains.