Gamma-Mangostin

Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptor antagonist and potent epoxidase 2 (COX-2) inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer^[2]. Gamma-Mangostin inhibits [3^H] spiperone binding to cultured rat aortic myocytes (IC₅₀=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC₅₀=0.32 μM). Gamma-Mangostin has anti-inflammatory, antibacterial, antioxidant and anticancer activities, and can be used in the study of metabolic disorders such as diabetes^{[1][2][3][4][5]}. IC50 & Target:5-hydroxytryptamine 2A (5-HT2A) receptors^[1] In Vitro:Gamma-Mangostin (0.5, 2.5, 5 μM; 2 hours) as an insulin sensitizer, alleviates hyperglycemia and is nontoxic to both vascular smoothing cells isolated from the external carotid artery in SD rats and FL83B mouse hepatocytes^[5].
In Vivo:Gamma-Mangostin (0.5, 1, 2 mg/kg; Oral gavage (p.o.); 14 days) significantly reduces fasting blood glucose, cholesterol, serum glutamic oxaloacetic transaminase (SGOT), serum glutamic pyruvic transaminase (SGPT), and ameliorates damaged hepatocytes, primarily swelling, hydropic changes, and necrotic cells in the streptozotocin (STZ) (HY-13753) (30 mg/kg) induced diabetic BALB/C mouse model^[3].
Gamma-Mangostin (1, 2, 4 mg/kg; Oral gavage (p.o.); 14 days) significantly reduces blood urea nitrogen (BUN) and creatinine in plasma, and ameliorates the damage to renal proximal tubular cells in BALB/C mice with streptozotocin (STZ) (HY-13753) (30 mg/kg) induced diabetes^[4].
Gamma-Mangostin (0.1, 0.2, 0.4 mg; Oral gavage (p.o.); 4 weeks) can reduce fasting blood glucose levels and oral glucose tolerance tests in diabetic ICR mice^[5].