Liu Y, Tsuchida A, Cohen M V, Downey J M
Department of Physiology, College of Medicine, University of South Alabama, Mobile 36688-0002, USA.
J Mol Cell Cardiol. 1995 Mar;27(3):883-92. doi: 10.1016/0022-2828(95)90038-1.
We have proposed that ischemic preconditioning in the rabbit heart is initiated by adenosine A1 receptor stimulation which results in an upregulation of protein kinase C (PKC). Subsequent sustained ischemia then causes renewed stimulation of adenosine A1 receptors with rapid reactivation of PKC and phosphorylation of a target protein(s) which mediates the protection. If the above theory is correct then angiotensin II (AII) receptor stimulation, which is known to activate PKC, should also protect the heart. Isolated rabbit hearts were subjected to 30 min of regional ischemia and 2 h of reperfusion. Infarct size was determined by tetrazolium staining. Pretreating hearts with 100 mM AII for 5 min, followed by 10 min of drug-free perfusion prior to the prolonged ischemia limited infarction (7.2 +/- 2.0% of the risk area v 31.1 +/- 3.4% in control animals, P < 0.01). This protection could be blocked by the AT1 receptor blocker losartan (10 microM), but not by the AT2 receptor blocker PD 123319 (10 microM). Polymyxin B (50 microM), a PKC inhibitor, also blocked the protective effect of AII. These observations demonstrated that activation of PKC by AT1 receptor stimulation prior to ischemia does mimic ischemic preconditioning. Following AII infusion, administration, during the 30 min ischemic period, of either SPT [8-(p-sulfophenyl)theophylline] (an adenosine receptor blocker) or losartan failed to block AII's protective effect. However, co-administration of SPT and losartan did abort AII's protection suggesting that AII may not be completely washed out during the 10 min drug-free perfusion allowing residual agonist to reactivate PKC during the 30 min ischemia even when adenosine receptors are blocked. Thus, if only one of the receptors (AT1 or adenosine) were activated during the ischemic period, protection would occur. We conclude that activation of PKC by AII, prior to ischemia, can limit myocardial infarction. While PKC must be reactivated during ischemia to realize protection, the specific receptor type initiating reactivation is not crucial.
我们提出,兔心脏的缺血预处理是由腺苷A1受体刺激引发的,这会导致蛋白激酶C(PKC)上调。随后的持续性缺血会再次刺激腺苷A1受体,使PKC快速重新激活,并使介导保护作用的一种或多种靶蛋白磷酸化。如果上述理论正确,那么已知可激活PKC的血管紧张素II(AII)受体刺激也应能保护心脏。将离体兔心脏进行30分钟的局部缺血和2小时的再灌注。通过四氮唑染色确定梗死面积。在长时间缺血前,用100 mM AII预处理心脏5分钟,随后进行10分钟的无药灌注,可限制梗死(危险区域的7.2±2.0%,而对照动物为31.1±3.4%,P<0.01)。这种保护作用可被AT1受体阻滞剂氯沙坦(10 μM)阻断,但不能被AT2受体阻滞剂PD 123319(10 μM)阻断。PKC抑制剂多粘菌素B(50 μM)也可阻断AII的保护作用。这些观察结果表明,缺血前通过AT1受体刺激激活PKC确实模拟了缺血预处理。在输注AII后,在30分钟缺血期给予SPT [8-(对磺基苯基)茶碱](一种腺苷受体阻滞剂)或氯沙坦均未能阻断AII的保护作用。然而,联合给予SPT和氯沙坦确实消除了AII的保护作用,这表明在10分钟的无药灌注期间,AII可能未被完全清除,从而使残留的激动剂在30分钟缺血期间重新激活PKC,即使腺苷受体被阻断。因此,如果在缺血期仅激活其中一种受体(AT1或腺苷),就会产生保护作用。我们得出结论,缺血前AII激活PKC可限制心肌梗死。虽然缺血期间PKC必须重新激活才能实现保护作用,但启动重新激活的具体受体类型并不关键。