Exploring the Bioactive Metabolites Behind the Medicinal Functions of Garcinia oblongifolia Champ. ex Benth....

Garcinia oblongifolia, used by the Li ethnic group native to southern China, is valued for its anti-inflammatory, antimicrobial, and wound-healing properties, yet its bioactive metabolites remain poorly characterized. This study aimed to elucidate tissue-specific metabolic mechanisms underlying the pharmacological effects of G. oblongifolia through untargeted metabolite profiling combined with bioactivity correlation analysis. Untargeted UHPLC-QE-MS metabolomics mapped phytochemical variations across leaves, twigs, bark, and fruits, while antioxidant (ABTS/DPPH), antitumor (CCK-8, apoptosis staining), anti-inflammatory (LPS-triggered cytokine assay), and antibacterial assays evaluated functional activities. Metabolomic analysis identified 402 tissue-specific metabolites, with flavonoids and xanthones as major bioactive candidates. Functional assays revealed tissue-dependent efficacy: leaves exhibited superior ABTS radical scavenging, bark showed the strongest DPPH inhibition, and fruits demonstrated potent antitumor/anti-inflammatory effects. All tissues displayed antibacterial activity against Gram-positive pathogens. Correlation analysis highlighted kaempferol-3-O-rutinoside, marucoflavone, and isovitexin as key contributors to antioxidant activity, while daidzin, kaempferol, and cirsimarin were primarily associated with antitumor, anti-inflammatory, and antibacterial activities. Integrated metabolomic-functional profiling demonstrates that tissue-specific bioactivity profiles of G. oblongifolia arise from differential accumulation of key flavonoid/xanthone metabolites. This metabolite-activity matrix provides a scientific basis for optimizing medicinal utilization, quality standardization, and drug discovery from this ethnopharmacological resource. This study characterized tissue-specific metabolites and bioactivities of Garcinia oblongifolia, an ethnomedicine. Untargeted metabolomics (UHPLC-QE-MS) identified 402 metabolites, predominantly flavonoids/xanthones. Bioassays showed leaves excelled in ABTS scavenging, bark in DPPH inhibition, fruits in antitumor/anti-inflammatory effects, and all tissues had antibacterial activity. Key correlated metabolites included kaempferol-3-O-rutinoside (antioxidant), daidzin (antitumor), and kaempferol (anti-inflammatory/antibacterial). This metabolite-activity matrix guides optimized medicinal use and quality control.