小檗碱及其衍生物抗菌作用研究进展OA

The widespread dissemination of multidrug-resistant bacteria worldwide has exacerbated the antibiotic resistance crisis.The diminished efficacy of conventional antibacterial agents and insufficient development of novel drugs have driven intensive research on natural antimicrobial active substances.Berberine,a major isoquinoline alkaloid derived from traditional Chinese medicines such as Coptis chinensis Franch.,exhibits low toxicity,low mutagenicity,multi-target effects,and low risk of inducing drug resistance,showing promising application prospects in the field of anti-infective therapy.This study systematically elaborated on the physicochemical properties and broad-spectrum pharmacological activities of berberine,focusing on its six major antibacterial mechanisms.It reviewed the inhibitory effects of berberine on gram-positive bacteria,including Staphylococcus aureus,Enterococcus faecalis and Clostridioides difficile,and on gram-negative bacteria,such as Escherichia coli,Pseudomonas aeruginosa,Klebsiella pneumoniae,Acinetobacter baumannii,and Helicobacter pylori.Notably,berberine retains favorable activity against multi drug-resistant strains,and its structurally modified derivatives can significantly enhance its antibacterial efficacy.Furthermore,as a natural efflux pump inhibitor,berberine exerts synergistic effects when combined with various antibiotics and can reverse bacterial resistance.It also exhibits broad-spectrum inhibitory activity against fungi,including Candida albicans and Cryptococcus neoformans.Despite limitations,such as poor water solubility and low bioavailability,novel formulation and delivery strategies have effectively improved its application constraints.This review provides a reference for the research and clinical translation of berberine and its derivatives in combating multidrug-resistant bacteria,and offers insights from traditional Chinese medicine to address the global antibiotic resistance crisis.