Dzurba A, Ziegelhoeffer A, Breier A, Vrbjar N, Szekeres L
Institute for Heart Research, Slovak Academy of Sciences, Bratislava, Czechoslovakia.
Cardioscience. 1991 Jun;2(2):105-8.
The delayed effects of 7-oxo-prostacyclin, protecting the heart against extrasystoles, ventricular fibrillation, and cardiac arrest induced by high doses of ouabain or in ischemia and postischemic reperfusion, have already been described; but little is known about the molecular mechanisms involved. In this study, 50 micrograms.kg-1 7-oxo-prostacyclin administered intramuscularly significantly stimulated the activity of (Na+K+)-ATPase in rat heart sarcolemma 24 and 48 hours after application (p less than 0.01 and p less than 0.001, respectively). Kinetic analysis revealed a mixed type of stimulation of ATPase activity, with increased Vmax and decreased Km values. Cycloheximide (1 mg.kg-1) applied together with 7-oxo-prostacyclin, significantly antagonized the stimulatory effect of 7-oxo-prostacyclin, and had a modulatory effect on the kinetics of the (Na+K+)-ATPase both 24 and 48 hours after administration. The results show that protein synthesis is involved in the mechanism of the increase in enzyme activity.
7-氧代前列环素对心脏具有保护作用,可防止高剂量哇巴因或在缺血及缺血后再灌注过程中诱发的早搏、心室颤动和心脏骤停,其延迟效应已有相关描述;但对于其中涉及的分子机制却知之甚少。在本研究中,肌肉注射50微克·千克⁻¹的7-氧代前列环素,在给药后24小时和48小时可显著刺激大鼠心肌肌膜中(钠钾)-ATP酶的活性(分别为p<0.01和p<0.001)。动力学分析显示,ATP酶活性受到混合型刺激,Vmax增加而Km值降低。与7-氧代前列环素一起应用的环己酰亚胺(1毫克·千克⁻¹)可显著拮抗7-氧代前列环素的刺激作用,并在给药后24小时和48小时对(钠钾)-ATP酶的动力学产生调节作用。结果表明,蛋白质合成参与了酶活性增加的机制。