白藜芦醇抑制II型磷脂酰肌醇4激酶：磷酸肌醇代谢途径中的关键成分。
Resveratrol inhibits type II phosphatidylinositol 4-kinase: a key component in pathways of phosphoinositide turn over.
作者信息
Srivastava Rupa, Ratheesh Aparna, Gude Rajiv K, Rao K V K, Panda Dulal, Subrahmanyam Gosukonda
机构信息
Biotechnology group, School of Bioscience and Bioengineering, Indian Institute of Technology Bombay, Powai, Mumbai 400076, India.
出版信息
Biochem Pharmacol. 2005 Oct 1;70(7):1048-55. doi: 10.1016/j.bcp.2005.07.003.
Resveratrol has anti-inflammatory, cardio protective and cancer chemopreventive properties. The molecular targets for resveratrol in early signaling cascades are not well understood. Resveratrol inhibits type II PtdIns 4-kinase but not PtdIns 3-kinase activity in vitro. Resveratrol directly binds to the enzyme with a Kd of 7.2 microM. Kinetic studies show that resveratrol competes with PtdIns binding. Inhibition of PtdIns 4-kinase activity by resveratrol/phenylarsine oxide reduces Jurkat cell adhesion to matrigel/fibronectin coated surfaces, suggesting a role for type II PtdIns 4-kinase in lymphocyte infiltration to the sites of inflammation.
白藜芦醇具有抗炎、心脏保护和癌症化学预防特性。白藜芦醇在早期信号级联反应中的分子靶点尚未完全明确。在体外，白藜芦醇可抑制II型磷脂酰肌醇4激酶（PtdIns 4-kinase）的活性，但不影响磷脂酰肌醇3激酶（PtdIns 3-kinase）的活性。白藜芦醇以7.2微摩尔的解离常数（Kd）直接与该酶结合。动力学研究表明，白藜芦醇与磷脂酰肌醇（PtdIns）的结合存在竞争。白藜芦醇/苯胂氧化物对PtdIns 4激酶活性的抑制作用可降低Jurkat细胞与基质胶/纤连蛋白包被表面的黏附，提示II型PtdIns 4激酶在淋巴细胞向炎症部位浸润过程中发挥作用。
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