Phenylboronic Acid-Modified Gold Nanoclusters as a Nanoantibiotic to Treat Vancomycin-Resistant Enterococcus faecalis-Caused Infections

Vancomycin is one of the last lines of defense against certain drug-resistant bacteria-caused infections. However, the high susceptibility to drug resistance and high toxicity seriously limit the application of vancomycin. Nanoantibiotics provide opportunities to solve these problems. Herein, we present mercaptophenylboronic acid (MBA)-modified gold nanoclusters with well-defined molecular formulas and structure (Au₄₄(MBA)₁₈) and excellent antibacterial activities against various drug-resistant bacteria such as vancomycin-resistant Enterococcus faecalis (VRE). Au₄₄(MBA)₁₈ interacts with bacteria by first attaching to teichoic-acid and destroying the cell wall and subsequently binding to the bacterial DNA. Au₄₄(MBA)₁₈ could be administered via multiple routes and has a high biosafety (500 mg/kg, no ototoxicity), overcoming the two major shortcomings of vancomycin (sole administration route and high ototoxicity). Our study is insightful for curing infections caused by multidrug-resistant bacteria using nanoantibiotics with high biosafety.