Transport of Organic Compounds through Biological Membranes.I.Accumulative Uptake of S-Benzoylthiamine by Human Erythrocytes

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The accumulative uptake of S-benzoylthiamme (SBT) by human red cells was demonstrated and the detail of the transport mechanism was investigated. From the studies on i) the transport of SBT into the red cells and into the ghosts, ii) the decomposition of SBT in the red cell homogenate and in an aqueous medium, iii) the effect of the concentration gradient on the uptake, and iv) the effect of the extracellular pH on the uptake, it was concluded that the penetration of SBT into the red cells proceeds through two steps ; the first, a passive diffusion of SBT through the cell membrane, and the second, a rapid decomposition of SBT to undiffusible thiamine and the resultant its accumulation in the cell. In a series of substituted S-benzoylthiamines, the rate of their decomposition to thiamine in the red cell was found to be a predominant factor determining the rate of the penetration into the red cells, both being a linear function to Hammett's σ-constants of the substituents. An important role of SBT in the intestinal absorption of S-benzoylthiamine monophosphate and the followed high blood thiamine concentration and its duration was pointed out.
社団法人日本薬学会の論文
1967-03-25