Baláz S, Sturdík E, Durcová E, Antalík M, Sulo P
Biochim Biophys Acta. 1986 Aug 13;851(1):93-8. doi: 10.1016/0005-2728(86)90252-5.
The dependence of the uncoupling activity in the series of 16 carbonylcyanide phenylhydrazones on their physico-chemical properties (partition coefficient, dissociation constant and rate constant for reaction with thiols) is investigated using two physiologically based models, one for protonophoric mechanism of uncoupling and the other assuming the covalent modification of a membrane constituent to be the key step in this process. As indicated by uptake experiments, at the given conditions a lipophilic-hydrophilic equilibrium is attained without any loss of the compounds via chemical reactions. Using this fact to reduce the number of adjustable parameters, a better fit to the data on stimulation of respiration is obtained with the former (protonophoric) model.
利用两种基于生理的模型,研究了16种羰基氰化物苯腙系列中解偶联活性对其物理化学性质(分配系数、解离常数和与硫醇反应的速率常数)的依赖性,一种模型用于解偶联的质子载体机制,另一种模型假设膜成分的共价修饰是该过程的关键步骤。摄取实验表明,在给定条件下,可达到亲脂-亲水平衡,且化合物不会因化学反应而损失。利用这一事实减少可调参数的数量,使用前一种(质子载体)模型能更好地拟合呼吸刺激数据。