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CAS No. : 1617-90-9
MCE 国际站:Vincamine
产品活性:Vincamine 是从马达加斯加长春花中提取的一种单萜类吲哚生物碱。Vincamine 可以作为一种外周血管扩张剂 (Vasodilator),对脑微血管循环有选择性的血管调节作用。Vincamine 是一种 GPR40 激动剂,通过改善 β 细胞功能障碍和促进葡萄糖刺激型胰岛素分泌 (GSIS) 发挥 β 细胞保护作用。Vincamine 可改善体内葡萄糖稳态,对 2 型糖尿病 (T2DM) 的研究具有潜力。
研究领域:GPCR/G Protein
作用靶点:Free Fatty Acid Receptor
结构分类:生物碱 | 吲哚类生物碱
来源:植物 | 夹竹桃科 | 长春花
In Vitro: Vincamine (20, 40 and 80 μM; 24 hours) exerts a significant, concentration-dependent protective effect in LPS-treated human corneal epithelial cells (HCECs) cells.Vincamine (20, 40 and 80 μM; 24 hours) significantly reduces ROS level in a dose-dependent manner in LPS-treated human corneal epithelial cells (HCECs)cells. Additionally, after Vincamine administration, the levels of MDA is also significantly reduced while the levels of T-AOC, and SOD are increased in a dose-dependent manner.Vincamine (20, 40 and 80 μM; 24 hours) rescues TrxR activity in a dose-dependent manner in HCECs. However, the intracellular activities of Trx, GR and GPx are neither inhibited nor activated by both LPS and Vincaminer.Vincamine could activate GPR40 (EC50=6.28 µM) with DHA (GPR40 ligand) as a positive control (EC50=3.85 µM) in hGPR40-CHO cells.
In Vivo: Vincamine (intraperitoneal injection; 15 and 30 mg/kg/day; 6 weeks) improves glucose tolerance in type 2 diabetic model mice. It effectively lowers the levels of fasting blood glucose and glycated hemoglobin. At the same time, it ameliorates oral glucose tolerance and elevated glucose-induced plasma insulin concentration without influence on basal insulin secretion in vivo.<.br>
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