Oxyberberine

Oxyberberine (Oxyberberin; Berlambine) is an orally effective heme oxygenase HO-1 agonist that can activate antioxidant mechanisms by regulating the PI3K/Akt/AMPK signaling pathway. Oxyberberine induces HO-1 expression, increases SOD and GSH-Px activity, inhibits NF-κB-mediated inflammatory responses, and improves insulin sensitivity and glucose metabolism. Oxyberberine has anti-diabetic, neuroprotective, anti-inflammatory and antioxidant effects, and can be used to study type 2 diabetes, traumatic brain injury (TBI) and inflammatory bowel disease^[1][2][3]. In Vitro: Oxyberberine (5-20 μM; 24-48 h) promotes glucose-stimulated insulin secretion in INS-1 cells, reduces intracellular reactive oxygen species (ROS) and malondialdehyde (MDA) levels, and increases superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) activities^[1].
Oxyberberine (10-40 μM; 24 h) enhances glucose consumption, upregulates phosphorylated Akt (p-Akt) and GSK-3β (p-GSK-3β) expressions, and downregulates glucose-6-phosphatase (G6Pase) and phosphoenolpyruvate carboxykinase (PEPCK) levels in insulin-resistant HepG2 cells^[1].
In Vivo: Oxyberberine (50, 100 mg/kg; gavage; once a day; 6 weeks) significantly reduces fasting blood glucose, glycosylated serum protein (GSP) and blood lipid levels in the HFD/STZ-induced rat type 2 diabetes model, and improves insulin resistance and pancreatic tissue pathological damage^[1].
Oxyberberine can significantly alleviate DSS-induced ulcerative colitis in mice, which may be related to the inhibition of TLR4/Myd88/NF-κB pathway excitation and regulation of intestinal flora. LD₅₀ >5000 mg/kg. Oxyberberine (12.5-50 mg/kg; intraperitoneal injection; once daily; 21 days) significantly improves colon tissue pathological damage in the TNBS-induced rat colitis model, reduces the proinflammatory markers TNF-α, IL-2, IL-8 and IL-22, and increases the levels of IL-4 and IL-13^[2].
Oxyberberine (25, 50 mg/kg; intraperitoneal injection; once daily; 21 days) alleviates neurological deficits, improves anxiety-like behaviors and cognitive impairment in the traumatic brain injury (TBI) model of male C57BL/6 mice, and inhibits the HMGB1-mediated TLR4/NF-κB inflammatory pathway in brain tissue^[3].