Petzinger E, Frimmer M
Naunyn Schmiedebergs Arch Pharmacol. 1982 Apr;319(1):87-92. doi: 10.1007/BF00491484.
Isolated hepatocytes accumulate demethylphalloin (DMP) under aerobic conditions. In the absence of oxygen the initial rate of the DMP uptake is reduced to less than 20%, while reoxygenation restores the transport. Liver cells release previously accumulated phallotoxin when the oxygen supply is interrupted. DMP uptake is blocked by oligomycin, antimycin A, carbonylcyano-chlorophenylhydrazon (CCCP) or dinitrophenol and is partially inhibited by carboxyatractyloside. Depletion of ATP in hepatocytes by replacement of glucose by fructose reduces the accumulation of toxin too. Below 22 degrees C no uptake was measurable. Between 22 degrees and 37 degrees C an apparent activation energy of 76.6 kJ/mol toxin and a Q10 of 2.6 was calculated for the carrier mediated uptake of DMP. The results suggest that the uptake of demethylphalloin is an energy dependent substrate transfer very similar to that of cholate.
分离的肝细胞在有氧条件下会积累去甲基鬼笔环肽(DMP)。在无氧条件下,DMP摄取的初始速率降低至20%以下,而复氧可恢复转运。当氧气供应中断时,肝细胞会释放先前积累的鬼笔毒素。寡霉素、抗霉素A、羰基氰氯苯腙(CCCP)或二硝基苯酚可阻断DMP摄取,而羧基苍术苷可部分抑制其摄取。用果糖替代葡萄糖使肝细胞中的ATP耗竭也会降低毒素的积累。在22℃以下无法检测到摄取。在22℃至37℃之间,计算出载体介导的DMP摄取的表观活化能为76.6 kJ/mol毒素,Q10为2.6。结果表明,去甲基鬼笔环肽的摄取是一种能量依赖性的底物转运,与胆酸盐的转运非常相似。