Bolli R, Jeroudi M O, Patel B S, Aruoma O I, Halliwell B, Lai E K, McCay P B
Department of Medicine, Baylor College of Medicine, Houston, TX 77030.
Circ Res. 1989 Sep;65(3):607-22. doi: 10.1161/01.res.65.3.607.
Recent evidence suggests that postischemic myocardial dysfunction ("stunning") may be mediated by oxygen free radicals, but the exact time window during which the critical radical-mediated damage develops remains unknown. Furthermore, the evidence for the oxyradical hypothesis is indirect and, therefore, inconclusive. Thus, the potent and cell-permeable antioxidant N-(2-mercaptopropionyl)-glycine (MPG) was administered as an intra-coronary infusion (8 mg/kg/hr) to three groups of open-chest dogs undergoing a 15-minute coronary occlusion followed by 4 hours of reperfusion. In group I (n = 8), the infusion of MPG was started 15 minutes before occlusion and ended 2 hours after reperfusion; in group II (n = 9), MPG was started 1 minute before reperfusion and ended 2 hours thereafter; in group III (n = 10), MPG was started 1 minute after reperfusion and ended 2 hours and 15 minutes thereafter. Control dogs (group IV) (n = 10) received vehicle. Recovery of contractile function (assessed as systolic wall thickening) was equivalent in groups I and II, and in both groups it was substantially greater than in controls (p less than 0.005 at 4 hours). In contrast, in group III recovery of function was indistinguishable from controls. To determine whether the protection afforded by MPG was due to inhibition of free radical reactions, myocardial production of free radicals was directly assessed by intracoronary infusion of the spin trap alpha-phenyl N-tert-butyl nitrone (PBN). In control dogs (group VII, n = 6), radical adducts of PBN were released in the coronary venous blood after reperfusion, with a burst occurring in the first 5 minutes. MPG given as in group II (group V, n = 5) markedly suppressed myocardial production of PBN adducts (delta = -98% over 3 hours, p less than 0.01 vs. controls); this effect was evident immediately after reperfusion. MPG given as in group III (group VI, n = 5) also suppressed PBN adduct production (delta = -83% over 3 hours, p less than 0.025 vs. controls), but this effect was delayed. Hence, the radicals important in myocardial stunning appear to be those generated immediately after reperfusion. In vitro studies demonstrated that MPG is an exceptionally powerful scavenger of .OH (rate constant = 8.1 x 10(9) M-1 sec-1 by pulse radiolysis) but has no significant effect on .O2- (rate constant less than 10(3) M-1 sec-1), H2O2 (rate constant = 1.6 M-1 sec-1), or non-.OH-initiated lipid peroxidation, suggesting that removal of .OH is the major mechanism of the beneficial effects of MPG.(ABSTRACT TRUNCATED AT 400 WORDS)
近期证据表明,缺血后心肌功能障碍(“心肌顿抑”)可能由氧自由基介导,但关键的自由基介导损伤发生的确切时间窗仍不清楚。此外,氧自由基假说的证据是间接的,因此尚无定论。因此,将强效且可透过细胞的抗氧化剂N-(2-巯基丙酰基)-甘氨酸(MPG)以冠状动脉内输注(8毫克/千克/小时)的方式给予三组开胸犬,这些犬经历15分钟的冠状动脉闭塞,随后再灌注4小时。在第一组(n = 8)中,MPG输注在闭塞前15分钟开始,在再灌注后2小时结束;在第二组(n = 9)中,MPG在再灌注前1分钟开始,并在其后2小时结束;在第三组(n = 10)中,MPG在再灌注后1分钟开始,并在其后2小时15分钟结束。对照组犬(第四组)(n = 10)给予赋形剂。收缩功能的恢复(以收缩期室壁增厚评估)在第一组和第二组中相当,且两组均显著大于对照组(4小时时p < 0.005)。相比之下,第三组的功能恢复与对照组无差异。为确定MPG提供的保护是否归因于对自由基反应的抑制,通过冠状动脉内输注自旋捕捉剂α-苯基N-叔丁基硝酮(PBN)直接评估心肌自由基的产生。在对照组犬(第七组,n = 6)中,再灌注后PBN的自由基加合物在冠状静脉血中释放,在前5分钟出现一个峰值。以第二组的方式给予MPG(第五组,n = 5)显著抑制心肌PBN加合物的产生(3小时内Δ = -98%,与对照组相比p < 0.01);这种效应在再灌注后立即明显。以第三组的方式给予MPG(第六组,n = 5)也抑制PBN加合物的产生(3小时内Δ = -83%,与对照组相比p < 0.025),但这种效应延迟出现。因此,在心肌顿抑中起重要作用的自由基似乎是再灌注后立即产生的那些。体外研究表明,MPG是·OH的一种异常强大的清除剂(脉冲辐射分解法测得速率常数 = 8.1×10⁹ M⁻¹秒⁻¹),但对超氧阴离子(速率常数 < 10³ M⁻¹秒⁻¹)、过氧化氢(速率常数 = 1.6 M⁻¹秒⁻¹)或非·OH引发的脂质过氧化没有显著影响,这表明清除·OH是MPG产生有益作用的主要机制。(摘要截断于400字)