Yamashita Y, Miyake Y, Mitsuhiro S, Furukawa T
Department of Biochemistry, Faculty of Pharmaceutical Science, Kinki University, Osaka, Japan.
Nihon Yakurigaku Zasshi. 1992 Jul;100(1):11-20. doi: 10.1254/fpj.100.11.
The effects of ifenprodil on adenosine triphosphatase (ATPase) activity were examined using guinea pig liver mitochondria. 1) Intact mitochondrial ATPase activity was stimulated by ifenprodil in a concentration-dependent manner, this effect being further potentiated with dinitrophenol. The stimulation by ifenprodil appeared with only ATP among four nucleotides as substrate. Mg2+ and Ca2+ attenuated the effect of ifenprodil. Ifenprodil abolished the KCN-induced inhibition. 2) Heat-treated mitochondrial ATPase activity, kept for 60 min at 50 degrees C, was decreased in a concentration-dependent manner by ifenprodil. The inhibitory effect of ifenprodil was abolished by Mg2+ and Ca2+. These results indicate that ifenprodil has two behaviors, acceleration of a latent ATPase and inhibition of an activated ATPase. These findings, together with our previous data, suggest that ifenprodil seems to affect the actions of Mg2+ and Ca2+ on mitochondrial ATPase by directly affecting the membrane, and these mechanisms may be involved in its anti-cyanide effect.
使用豚鼠肝脏线粒体研究了艾芬地尔对三磷酸腺苷酶(ATP酶)活性的影响。1)艾芬地尔以浓度依赖的方式刺激完整线粒体的ATP酶活性,用二硝基苯酚可进一步增强这种作用。在四种核苷酸作为底物中,仅ATP存在时艾芬地尔才有刺激作用。镁离子(Mg2+)和钙离子(Ca2+)减弱了艾芬地尔的作用。艾芬地尔消除了氰化钾(KCN)诱导的抑制作用。2)在50摄氏度下保持60分钟的热处理线粒体ATP酶活性,艾芬地尔以浓度依赖的方式使其降低。镁离子和钙离子消除了艾芬地尔的抑制作用。这些结果表明,艾芬地尔有两种作用,即加速潜在的ATP酶活性和抑制活化的ATP酶活性。这些发现与我们之前的数据一起表明,艾芬地尔似乎通过直接影响膜来影响镁离子和钙离子对线粒体ATP酶的作用,并且这些机制可能与其抗氰化物作用有关。