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黄绿青霉素,一种线粒体腺苷三磷酸酶的特异性抑制剂。

Citreoviridin, a specific inhibitor of the mitochondiral adenosine triphosphatase.

作者信息

Linnett P E, Mitchell A D, Osselton M D, Mulheirn L J, Beechey R B

出版信息

Biochem J. 1978 Mar 15;170(3):503-10. doi: 10.1042/bj1700503.

Abstract
  1. Citreoviridin was a potent inhibitor of the soluble mitochondrial ATPase (adenosine triphosphatase) similar to the closely related aurovertins B and D. 2. Citreoviridin inhibited the following mitochondrial energy-linked reactions also: ADP-stimulated respiration in whole mitochondria from ox heart and rat liver; ATP-driven reduction of NAD+ by succinate; ATP-driven NAD transhydrogenase and ATPase from ox heart submitochondrial particles. 3. The dissociation constant (KD) calculated by a simple law-of-mass-action treatment for the citreoviridin--ATPase complex was 0.5--4.2micron for ox-heart mitochondrial preparations and 0.15micron for rat liver mitochondria. 4. Monoacetylation of citreoviridin decreased its inhibitory potency (KD=2--25micron, ox heart; KD=0.7micron, rat liver). Diacetylation greatly decreased the inhibitory potency (KD=60--215micron, ox heart). 5. Hydrogenation of citreoviridin monoacetate diminished its inhibitory potency considerably. 6. No significant enhancement of fluorescence was observed when citreoviridin interacted with the mitochondrial ATPase.
摘要
  1. 黄绿青霉素是可溶性线粒体ATP酶(腺苷三磷酸酶)的强效抑制剂,与密切相关的金轮霉素B和D类似。2. 黄绿青霉素还抑制以下线粒体能量相关反应:牛心和大鼠肝脏完整线粒体中ADP刺激的呼吸作用;ATP驱动的琥珀酸对NAD⁺的还原作用;牛心亚线粒体颗粒中ATP驱动的NAD转氢酶和ATP酶。3. 对黄绿青霉素 - ATP酶复合物采用简单的质量作用定律处理计算得到的解离常数(KD),牛心线粒体制剂为0.5 - 4.2微米,大鼠肝脏线粒体为0.15微米。4. 黄绿青霉素的单乙酰化降低了其抑制效力(牛心:KD = 2 - 25微米;大鼠肝脏:KD = 0.7微米)。双乙酰化极大地降低了抑制效力(牛心:KD = 60 - 215微米)。5. 黄绿青霉素单乙酸酯的氢化作用显著降低了其抑制效力。6. 黄绿青霉素与线粒体ATP酶相互作用时,未观察到荧光有明显增强。

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