This invention relates to the field of
biomedical technology, and in particular to the application of TarA inhibitors in the preparation of antibacterial potentiators for enhancing the
efficacy of β-
lactam antibiotics against methicillin-resistant
Staphylococcus aureus (MRSA) infections. Through
virtual screening, target validation, and
in vitro and
in vivo pharmacodynamic experiments, this invention confirms that the
natural product norzelamin is an effective TarA inhibitor and antibacterial
potentiator. Experiments show that norzelamin has a synergistic effect when used in combination with various β-
lactam antibiotics. In a mouse model of MRSA-infected pneumonia, the combination of norzelamin and
cefotaxime sodium significantly reduced pulmonary bacterial load, alleviated systemic
inflammatory response, and improved
lung tissue
pathological damage compared to monotherapy. This invention provides a novel synergistic
treatment strategy and candidate compound for overcoming MRSA resistance in clinical practice, and has significant development value and application prospects.