RHODAMINE-123 INHIBITS BIOENERGETIC FUNCTION IN ISOLATED RAT-LIVER MITOCHONDRIA
RHODAMINE-123 INHIBITS BIOENERGETIC FUNCTION IN ISOLATED RAT-LIVER MITOCHONDRIA
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DOI：
10.1016/0006-291x(84)91453-0
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发表时间：
1984-01-01
影响因子：
3.1
通讯作者：
APRILLE, JR
中科院分区：
文献类型：
--
作者：
MODICANAPOLITANO, JS;WEISS, MJ;APRILLE, JR
罗丹明123在活细胞的线粒体中积累，并表现出选择性抗癌活性。通过测试染料对离体大鼠肝线粒体的影响，研究了毒性的生化基础。低得多的浓度的罗丹明123所需的抑制ADP刺激的呼吸和ATP的合成，以及耦合通电线粒体比所需的抑制解偶联呼吸和解偶联刺激的ATP水解。与线粒体相关的罗丹明123的量是几倍，在通电条件下比在非通电条件下，这可能解释了为什么耦合功能似乎是更敏感的抑制比非耦合功能在低浓度的罗丹明123。显然，罗丹明123抑制的位点最有可能是F0F1 ATP酶复合物，也可能是电子转移反应。
Rhodamine 123 accumulates in the mitochondria of living cells and exhibits selective anticarcinoma activity. The biochemical basis of toxicity was investigated by testing the effect of the dye on isolated rat liver mitochondria. Much lower concentrations of rhodamine 123 were required to inhibit ADP-stimulated respiration and ATP synthesis in well-coupled energized mitochondria than were required to inhibit uncoupled respiration and uncoupler-stimulated ATP hydrolysis. The amount of rhodamine 123 associated with the mitochondria was severalfold greater under energized than under nonenergized conditions, which may explain why coupled functions appeared to be more sensitive than uncoupled functions to inhibition at low concentrations of rhodamine 123. Apparently, the site of rhodamine 123 inhibition is most likely the F0F1 ATPase complex and possibly electron transfer reactions as well.