为了逆转由β-内酰胺酶引起的细菌耐药性,采用紫外分光光度法从天然化合物中筛选出能够抑制β-内酰胺酶的7种天然化合物,并应用"棋盘法"分别测定它们与抗生素联用对产超广谱β-内酰胺酶(ESBLs)大肠杆菌的抗菌活性。结果表明:芦荟大黄素、槲皮素、香紫苏醇、木犀草素、苦参碱、大蒜素和五味子甲素对β-内酰胺酶有不同程度的抑制作用,均可增加抗生素对产ESBLs大肠杆菌敏感性,且其增加程度与其对β-内酰胺酶的抑制作用强度呈正相关,表明此7种天然化合物增加抗生素对产ESBLs大肠杆菌敏感性的机制是通过抑制大肠杆菌产生的β-内酰胺酶,使抗生素免于水解而发挥作用的。该研究为解决由β-内酰胺酶引起的细菌耐药性问题提供了新的思路和途径。
To reverse bacterial drug resistance induced by β-lactamase,seven natural compounds inhibiting β-lactamase were screened out from natural compounds by the method of ultraviolet spectrophotometry,and their effects of increasing the antibiotics sensitization on producing ESBLs Escherichia coli were measured by checker-board method. The results showed that β-lactamase was inhibited by aloe emodin,quercetin,sclareol,matrine,allicin and luteolin at different degrees. There existed a good correlation between the increasing antimicrobial activity against producing ESBLs E. coli and their inhibitory effect on β-lactamase. The results suggest that the increased susceptibility of antibiotics against producing ESBLs E. coli by these natural compounds is due to the inhibition to β- lactamase produced by E. coli. This study provides a new way to take precautions against the bacterial resistance caused by β-lactamase.