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目的:研究钙/钙调素依赖性蛋白激酶Ⅱ抑制剂KN-62对谷氨酸介导皮质神经元损伤及CCDPK Ⅱ活性下降的影响。方法:LDH释放代表神经元损伤,~(32)P掺入法测CCDPK Ⅱ活性,放射自显影显示后磷酸化水平变化。结果:只有在谷氨酸(100μmol·L~(-1),10min)作用前加KN-62可部分保护神经元损伤,明显拮抗CCDPK Ⅱ活性下降,活性由48.0％恢复到90.6％,显著抑制内源蛋白后磷酸化水平下降。结论:KN-62对CCDPK Ⅱ活性的保护作用是通过抑制CCDPK Ⅱ的自身磷酸化而实现的。
AIM: To investigate the effect of calcineurin / calmodulin-dependent protein kinase Ⅱ inhibitor KN-62 on glutamate-mediated cortical neuron injury and CCDPK Ⅱ activity decline. Methods: LDH release represented neuronal injury, CCDPK Ⅱ activity was measured by ~ (32) P incorporation method, and autophosphorylation was detected by autoradiography. Results: Neuron injury was partially protected by glutamate (100μmol·L -1, 10min), and the activity of CCDPK Ⅱ was obviously inhibited. The activity of CCDPK Ⅱ was reduced from 48.0% to 90.6%, which was significantly inhibited Phosphorylation of endogenous protein decreased. Conclusion: The protective effect of KN-62 on CCDPK Ⅱ activity is achieved by inhibiting the autophosphorylation of CCDPK Ⅱ.