Identification of a Novel Antagonist of BRS-3 from Natural Products and Its Protective Effects Against H₂O₂-Induced Cardiomyocyte Injury.

ABSTRACT: The identification of exogenous ligands from natural products is an alternative strategy to explore the unrevealed physiological functions of orphan G-protein-coupled receptors (GPCRs). In this study, we have successfully identified and pharmacologically characterized licoisoflavone A (LIA) as a novel selective antagonist of BRS-3, an orphan GPCR. Functional studies showed that pretreatment with LIA ameliorated hydrogen peroxide (H₂O₂)-induced cardiomyocyte injury. Furthermore, LIA pretreatment significantly restored the activities of malondialdehyde (MDA), superoxide dismutase (SOD), and catalase (CAT), as well as lactate dehydrogenase (LDH) levels, in H9c2 cells following H₂O₂ exposure. The protective effect of LIA was also evident in primary c

SUBMITTER: Lu J 

PROVIDER: S-EPMC11943355 | biostudies-literature | 2025 Mar

REPOSITORIES: biostudies-literature