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目的:研究血管扩张药肼酞嗪和KRN2391对蛋白激酶的直接作用以探讨其作用机制.方法:采用层析纯化的蛋白激酶进行体外活性测定.结果:肼酞嗪可以抑制PKA和PKG的活性(0.01-10 mmol·L~(-1)),其IC_(50)分别为1.2和2.5 mmol·L~(-1),而对PKC作用很小.KRN2391(1—1000μmol·L~(-1))对PKA,PKG和PKC活性均无明显影响.结论:肼酞嗪对PKA和PKG的直接作用可能是其扩张血管的机制之一.
OBJECTIVE: To study the direct effect of vinfluidazine and KRN2391 on protein kinases in order to explore its mechanism.Methods: The purified kinases were used for in vitro activity determination.Results: Hydralazine could inhibit the activity of PKA and PKG (IC50) of 1.2 and 2.5 mmol·L -1, respectively, while the effect on PKC was very little.KRN2391 (1-1000 μmol·L -1) )) Had no significant effect on PKA, PKG and PKC activity.Conclusion: The direct effect of hydralazine on PKA and PKG may be one of the mechanisms of dilating blood vessels.