AcrB-IN-6

AcrB-IN-6 is an effective inhibitor of AcrB and suppresses the function of bacterial multidrug efflux pumps. AcrB-IN-6 significantly enhances the antibacterial activity of multiple antibiotics and produces 32-fold reductions in minimum inhibitory concentration (MIC) values in wild-type Escherichia coli BW25113. AcrB-IN-6 exhibits strong synergistic antibacterial effects together with low cytotoxicity and hemolytic properties. AcrB-IN-6 is utilized in research focused on antimicrobial resistance mechanisms, bacterial efflux systems, and strategies designed to restore antibiotic susceptibility in multidrug-resistant bacterial strains.

Method: The post-antibiotic effects of azithromycin and linezolid against Escherichia coli BW25113 were evaluated in the presence of AcrB-IN-6.
Rresult: AcrB-IN-6 extended the post-antibiotic effects of azithromycin and linezolid by 2 h and 1.5 h, respectively.[1]
Method: Hemolytic activity and mammalian-cell cytotoxicity were evaluated using murine erythrocytes and HEK293 cells exposed to AcrB-IN-6.
Rresult: AcrB-IN-6 caused no appreciable hemolysis at 2–256 μg/mL and showed relatively low cytotoxicity toward HEK293 cells.[1]

Method: Male SPF Kunming mice infected with Escherichia coli BW25113 received a single intraperitoneal dose of AcrB-IN-6 alone at 25 mg/kg or AcrB-IN-6 at 5 or 15 mg/kg in combination with tetracycline.
Rresult: AcrB-IN-6 monotherapy reduced the bacterial burden by approximately 0.5 log10 CFU, while combination treatment produced a more pronounced, dose-dependent enhancement of tetracycline efficacy.[1]
Method: The biosafety of a single hemocoel injection of AcrB-IN-6 at 250–1000 mg/kg was evaluated in Galleria mellonella larvae.
Rresult: AcrB-IN-6 showed favorable biosafety in Galleria mellonella larvae even at the highest tested dose.[1]