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Vincamine

CAS No. : 1617-90-9

MCE 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：GPR40

In Vitro: Vincamine (20, 40 and 80 μM; 24 hours) exerts a signi?cant, 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??M) with DHA (GPR40 ligand) as a positive control (EC₅₀=3.85??M) 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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