Oxymatrine is a quinolizidine alkaloid extracted from the roots of Sophora flavescens[1]. Oxymatrine possesses a wide range of pharmacological activities and exerts anti-inflammatory, anti-fibrotic, and anti-tumor effects mainly by inhibiting iNOS expression and regulating signaling pathways such as TGF-β/Smad and TLR4[2]. Oxymatrine is commonly used in research on liver fibrosis, neuroprotection, and the proliferation and apoptosis mechanisms of various tumor cells[3,4].
In vitro, pretreatment of HUVEC cells with Oxymatrine (2, 4, 8μM) for 1h, followed by continued treatment with oxidized low-density lipoprotein (ox-LDL, 100μg/mL) for 24h, significantly reversed the ox-LDL-induced decrease in cell viability[5]. Treatment of high glucose (55mM glucose)-induced HepG2 cells with Oxymatrine (0.1, 1μM) for 24h dose-dependently reduced glucose production[6].
In vivo, intraperitoneal injection of Oxymatrine (25, 50, 100mg/kg; once daily) for 30 days in C57BL/6J mice infected with Echinococcus multilocularis significantly reduced the wet weight of abdominal cysts[7]. Administration of Oxymatrine (30, 60, 120mg/kg; i.p.) once at 1h before and once at 12h after LPS induction in mice with LPS-induced mastitis significantly reduced the LPS-induced increase in myeloperoxidase (MPO) activity and distribution in mammary tissue at 24h[8].
References:[1] Chen X, Yi C, Yang X, et al. Liquid chromatography of active principles in Sophora flavescens root[J]. Journal of Chromatography B, 2004, 812(1-2): 149-163.
[2] Wang Y, Hua C, Zhang H, et al. Alkaloids as emerging therapeutics against pulmonary fibrosis: classification, mechanisms, and translational potential[J]. Chemistry & Biodiversity, 2025, 22(12): e01495.
[3] Chai N L, Fu Q, Shi H, et al. Oxymatrine liposome attenuates hepatic fibrosis via targeting hepatic stellate cells[J]. World Journal of Gastroenterology: WJG, 2012, 18(31): 4199.
[4] Dhurandhar Y, Tomar S, Das A, et al. Unlocking the potential of oxymatrine: a comprehensive review of its neuroprotective mechanisms and therapeutic prospects in neurological disorders[J]. ACS Chemical Neuroscience, 2024, 15(23): 4245-4257.
[5] Jin X, Fu W, Zhou J, et al. Oxymatrine attenuates oxidized low-density lipoprotein-induced HUVEC injury by inhibiting NLRP3 inflammasome-mediated pyroptosis via the activation of the SIRT1/Nrf2 signaling pathway[J]. International journal of molecular medicine, 2021, 48(4): 187.
[6] Zhu Y X, Hu H Q, Zuo M L, et al. Effect of oxymatrine on liver gluconeogenesis is associated with the regulation of PEPCK and G6Pase expression and AKT phosphorylation[J]. Biomedical reports, 2021, 15(1): 56.
[7] Zhu Y, Wu P, Wen R, et al. Oxymatrine alleviates Echinococcus multilocularis infection by remodeling the liver immune microenvironment and intestinal flora homeostasis[J]. Frontiers in Cellular and Infection Microbiology, 2025, 15: 1658336.
[8] Yang Z, Yin R, Cong Y, et al. Oxymatrine lightened the inflammatory response of LPS-induced mastitis in mice through affecting NF-κB and MAPKs signaling pathways[J]. Inflammation, 2014, 37(6): 2047-2055.