产品
编 号:F356496
分子式:C22H26N2O2
分子量:350.45
产品类型
结构图
CAS No: 42971-09-5
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生物活性:
Vinpocetine (Ethyl apovincaminate) is a derivative of the alkaloid Vincamine that blocks voltage-gated Na+ channels. The IC50 value of Vinpocetine on direct IKK inhibition in the cell-free system is 17.17 μM. Vinpocetine is a phosphodiesterase (PDE) inhibitor and inhibits NF-κB-dependent inflammatory responses by directly targeting IκB kinase complex (IKK), and has been widely used for the treatment of cerebrovascular disorders.
体内研究:
Vinpocetine (2.5-10 mg/kg;腹膜内注射;C57BL/6 小鼠) 有效抑制 TNF-α 或 LPS 诱导的促炎介质上调,包括 TNF-α、IL-1β 和 MIP-2,并降低TNF-α 或 LPS 诱导的肺部炎症小鼠模型中多形核白细胞的间质浸润。Animal Model:C57BL/6 mice (8 weeks of age)
Dosage:2.5 mg/kg, 5 mg/kg, and 10 mg/kg
Administration:Intraperitoneal injection
Result:Inhibited TNF-α- or LPS-induced up-regulation of proinflammatory mediators, including TNF-α, IL-1β, and MIP-2, and decreased interstitial infiltration of polymorphonuclear leukocytes in a mouse model of TNF-α- or LPS-induced lung inflammation.
体外研究:
Vinpocetine (5-50 μM;7 小时;VSMC、HUVEC、A549 细胞和 RAW264.7 细胞) 以剂量依赖性方式有效抑制 TNF-α 诱导的 NF-κB 依赖性转录活性,具有近似的 IC50 值为 25 μM。Vinpocetine 对细胞活力没有显著影响。 Vinpocetine (50 μM;7 小时;VSMC、HUVEC、A549 细胞和 RAW264.7 细胞) 有效抑制 TNF-α-诱导多种细胞类型中 TNF-α、IL-1β、IL-8、MCP-1、VCAM-1、ICAM-1 和 MIP-2 转录本的上调。