Study on chemical composition, plasma-absorbed components, and anti-inflammatory and antibacterial activity of Hypericum patulum.

This study investigated the chemical composition of Hypericum patulum and its plasma metabolites in rats using ultra-high-performance liquid chromatography coupled to a Q-Exactive Plus Orbitrap mass spectrometer (UPLC-Q Exactive Plus Orbitrap MS). A total of 162 compounds were identified in the plant extract of H. patulum, encompassing 50 flavonoids, 32 organic acids, 26 xanthones, 12 polycyclic polyprenylated acylphloroglucinols (PPAPs), 10 amino acids, 8 coumarins, 5 alkaloids, 3 sugars, 2 terpenoids, 3 aldehydes, and 11 others. Analysis of rat plasma revealed 48 compounds, consisting of 20 prototypes (predominantly xanthones, organic acids, and flavonoids) and 28 metabolites generated via glucuronidation, methylation, and sulfation. In LPS-induced RAW 264.7 macrophages, H. patulum extract significantly inhibited NO release and suppressed the expression of pro-inflammatory mediators, including IL-6, TNF-α, COX-2, iNOS, and IL-1β. In vivo, quercetin and shikimic acid attenuated xylene-induced ear edema and inflammatory infiltration in mice, and also lowered serum levels of the pro-inflammatory cytokines TNF-α, IL-6, and IL-1β. Antibacterial testing revealed that shikimic acid demonstrated activity against a panel of pathogens, with minimum inhibitory concentration (MIC) of 13.00, 6.50, and 20.08 mg/mL against Staphylococcus aureus, Escherichia coli, and β-hemolytic Streptococcus, respectively. Vanillic acid showed MICs of 6.50 mg/mL against S. aureus and 3.25 mg/mL against E. coli, whereas quercetin inhibited S. aureus at a concentration of 3.25 mg/mL. These findings characterize the pharmacologically active components of H. patulum, thereby validating its traditional use and laying a foundation for future investigations into its therapeutic mechanisms.