小檗碱和鱼腥草素钠离子对化合物体外抗菌活性评价

Antimicrobial activity evaluation on ion-pair compounds of berberine and sodium houttuyfonate in vitro

目的研究鱼腥草素、新鱼腥草素经碳链修饰并与盐酸小檗碱离子配对后的6种离子对化合物的体外抗菌活性。方法采用琼脂打孔扩散法测定化合物对标准菌的抑菌圈大小;二倍稀释法测定化合物和抗菌药物对标准菌及临床分离耐药菌株的最低抑菌浓度(MIC)和最低杀菌浓度(MBC、MFC);微量稀释棋盘法测定化合物与抗菌药物联用的部分抑菌浓度指数(FICI),评价其与抗菌药物联用的效果。结果己酰乙醛亚硫酸氢钠、庚酰乙醛亚硫酸氢钠、癸酰乙醛亚硫酸氢钠小檗碱离子对化合物显示出比对照品化合物更显著的抗菌活性,但抗菌活性弱于临床常用抗菌药物;合成的离子对化合物对实验所用临床分离耐甲氧西林金黄色葡萄球菌(MRSA)的活性比临床常用抗菌药物更好;联合抑菌实验表明离子对化合物与抗菌药物之间的协同作用较弱。实验中离子对化合物在抗菌药物中的添加多数情况降低了测试抗菌药物对病原菌的MIC值。结论合成的离子对化合物对MRSA有很好的抗微生物活性,其在临床上的应用具有潜在价值。

Objective To determine the antimicrobial activity in vitro of six ion-pair compounds synthesized by carbon chain modification of houttuynia and neohouttuynia and pairing with berberine hydrochloride ions.Methods The diameter of inhibition zone of compounds against standard microbes was determined by AGAR diffusion method.The minimum inhibitory concentration(MIC),minimum bactericidal concentration(MBC),and minimum fungicidal concentration(MFC)of compounds and antibiotics against standard microbes and clinical isolates were determined by double dilution method.The fractional inhibitory concentration index(FICI)of the compounds combined with antibiotics was determined by microdilution checkerboard.Results The ion-pair compounds of hexanoyl,heptanoyl and decanoyl acetaldehyde sodium bisulfite showed more significant antimicrobial activity than the control compounds,but the antimicrobial activity was weaker than that of commonly used clinical antibiotics.The activity of synthesized ion-pair compounds against the clinical isolation of Methicillin-resistant Staphylococcus aureus(MRSA)was better than that of commonly used clinical antibiotics.The combined antimicrobial experiments showed weak synergistic effect between ion-pair compounds and antibiotics.Addition of ion-pair compounds to antibiotics in most cases reduced the MIC value of tested antibiotics against pathogens.Conclusion Synthesized ion-pair compounds have good antimicrobial activity against MRSA,and potential value in clinical application.