Wogonoside is a naturally occurring flavone glucuronide that inhibits α-glucosidase with an IC50 value of 18.25nM[1]. Wogonoside suppresses inflammatory responses by inhibiting macrophage pyroptosis through blockade of the NOD-like receptor family pyrin domain containing 3 (NLRP3)/caspase-1/gasdermin D signaling cascade and modulation of purinergic signaling[2]. Wogonoside exhibits a variety of biological activities, such as anti-inflammatory, lipid-lowering and cardiac function improvement effects, and is widely used to mitigate atherosclerosis[3].
In vitro, Wogonoside treatment for 48 hours significantly inhibited the viability of U251MG, SHG44, A172 and U87MG cells, with IC50 values of 193.44μM, 305.08μM, 269.54μM and 199.83μM, respectively[4]. Incubation of RAW264.7 cells with 50μM Wogonoside for 24 hours reduced lipopolysaccharides (LPS)-induced the production of NO and PGE2, and decreased the levels of TNF-α and IL-6[5].
In vivo, Wogonoside treatment via oral administration at a dose of 8mg/kg daily for 4 weeks alleviated CCl4-elicited liver fibrosis in rats, and effectively restored the levels of superoxide dismutase, glutathione and IL-10[6]. Oral administration of Wogonoside (50mg/kg/day) for 10 consecutive days alleviated the dextran sulfate sodium (DSS)-caused colitis in mice, improved intestinal barrier function and regulated bacterial translocation[7]. Intragastric administration of Wogonoside at a dose of 40mg/kg daily for 8 weeks inhibited the progression of osteoarthritis in a mouse model of destabilization of the medial meniscus (DMM), reduced proteoglycan loss, and attenuated cartilage calcification[8].
References:
[1] Zeng X, Zhao M, Yao H. Anti-lung cancer, anti-microbial, anti-α-glucosidase, anti-sorbitol dehydrogenase, and in silico studies of wogonoside and isoliquiritigenin as natural compounds[J]. Journal of Oleo Science, 2023, 72(10): 919-927.
[2] Ni H T N, Huan D Q, Vu H D, et al. Wogonoside: Chemistry, pharmacology, and pharmacokinetics[J]. Fitoterapia, 2026: 107354.
[3] Gong Z, Yang H, Gao L, et al. Mechanisms of wogonoside in the treatment of atherosclerosis based on network pharmacology, molecular docking, and experimental validation[J]. BMC Complementary Medicine and Therapies, 2025, 25(1): 28.
[4] Zhang L, Wang H, Cong Z, et al. Wogonoside induces autophagy-related apoptosis in human glioblastoma cells[J]. Oncology Reports, 2014, 32(3): 1179-1187.
[5] Yang Y Z, Tang Y Z, Liu Y H. Wogonoside displays anti-inflammatory effects through modulating inflammatory mediator expression using RAW264. 7 cells[J]. Journal of Ethnopharmacology, 2013, 148(1): 271-276.
[6] Wang Q, Wen R, Lin Q, et al. Wogonoside shows antifibrotic effects in an experimental regression model of hepatic fibrosis[J]. Digestive Diseases and Sciences, 2015, 60(11): 3329-3339.
[7] Huang S, Fu Y, Xu B, et al. Wogonoside alleviates colitis by improving intestinal epithelial barrier function via the MLCK/pMLC2 pathway[J]. Phytomedicine, 2020, 68: 153179.
[8] Tang Q, Zheng G, Feng Z, et al. Wogonoside inhibits IL-1β induced catabolism and hypertrophy in mouse chondrocyte and ameliorates murine osteoarthritis[J]. Oncotarget, 2017, 8(37): 61440.