The hepatoprotective activity and chemical constituents of Helicteres hirsuta water extract

Introduction: Many species belonging to the genus Helicteres are used in the traditional medicine of Asian countries. Helicteres hirsuta (雁婆麻) is widely distributed and cultivated in China but not used for medicinal purposes. However, the decoction of H. hirsuta has long been employed in Vietnamese folk medicine for managing hepatic disorders. The systematic pharmacological validation and phytochemical characterization of this plant remain inadequate. This study sought to elucidate the chemical constituents of the H. hirsuta water extract (HWE) and to assess its hepatoprotective efficacy through in vitro and in vivo models. The findings are expected to not only provide scientific evidence for its traditional use in Vietnam but also highlight the potential of H. hirsuta as a new, untapped therapeutic resource for Traditional Chinese Medicine. Methods: HWE was fractionated by column chromatography, and isolated constituents were identified using spectroscopic techniques. Hepatoprotective activity was examined against paracetamol-induced cytotoxicity in HepG2 cells, while antioxidant capacity with DPPH radical scavenging and lipid peroxidation assays were assessed. Main bioactive constituents identified by UPLC–MS were quantified in HWE which was further investigated in vivo. Hepatoprotective effects of HWE (412.5 and 825 mg/kg) were evaluated in mice with paracetamol-induced hepatotoxicity (400 mg/kg). Serum biomarkers (ALT, AST, ALP, bilirubin), oxidative stress parameters (GSH, MDA), and histopathology were analyzed, using silymarin (100 mg/kg) as positive control. Results: HWE exhibited pronounced hepatoprotective activity in vitro (EC₅₀ = 20.12 ± 0.15 µg/mL) with strong antioxidant potential (DPPH, IC₅₀ = 33.91 ± 0.48 µg/mL; MDA, IC₅₀ = 165.07 ± 8.60 µg/mL). Nine compounds were identified, including danshensu (>2 % w/w) as predominant constituent, rosmarinic acid, tiliroside, isoacteoside, forsythoside B, and four flavonoid glucuronides. In vivo, HWE significantly ameliorated biochemical and oxidative stress markers, with greater efficacy at 825 mg/kg. Conclusion: HWE, particularly at 825 mg/kg, demonstrated significant hepatoprotective activity, attributable to polyphenolic constituents, notably danshensu. These findings scientifically substantiate traditional use and provide a foundation for therapeutic development.