Vinpocetine is a selective inhibitor for PDE1 with IC50 of 21 μM, it also blocks voltage-gated Na+ channels. It's a natural product isolated and purified from the herbs of Catharanthus roseus (L.) G. Don.
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[3]. Vinp inhibits mitogen-activated protein kinase (MAPK) and nuclear factor-κB (NF-κB)-dependent inflammatory responses and oxidative damage in which osteoclasts are often involved[4]. In both in vivo and in vitro experiments, vinpocetine can confer protection of rat renal cells by inhibiting the NF-κB signaling pathway and activating the Nrf2/ARE signaling pathway[5]. Vinpocetine potently suppressed tumor necrosis factor-α-induced nuclear factor kappa-light-chain-enhancer of activated B cells activation and proinflammatory mediator expression in primary cultured macrophages in vitro, as well as in the aorta wall in vivo, suggesting vinpocetine conferred anti-AAA (Abdominal aortic aneurysm) effect at least partially via the inhibition of inflammation[6]. Vinpocetine treatment may exhibit anti-inflammatory activity and alleviate cognitive impairment[7]. The effects of vinpocetine might be attributed not only to its antioxidant and anti-inflammatory properties, but also to its suppressing effect on GSK3β (Glycogen synthase kinase-3β) activity and its downstream BACE1(β-secretase) [8].
United States, California
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Stanford University
Recruiting
Palo Alto, California, United States, 94304
Contact: Jordan Seliger 650-468-8740 jseliger@stanford.edu
Principal Investigator: Kimford J Meador, MD 收起 <<
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