Mitomycinと血清Albuminの結合(第1報)ウサギ血清中での抗菌活性とタンパク結合の関係について

概要

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The time-dependent changes in biological activities of mitomycin derivatives, demethoxymitomycin A (DMMA, 7-amino-N-methyl-isomitomycin B (NMMB), mitomycin C (MMC), decarbamoylmitomycin C (DCMC), 10-acethoxydecarbamoylmitomycin C (ADCMC), in rabbit blood serum and in 0.4% bovine serum albumin (BSA) aqueous solution at 37° were investigated in order to clarify the reason for difference in biological activities of these compounds in vitro and in vivo. In these compounds, both in rabbit blood serum and in 0.4% BSA aqueous solution, remarkable decrease in their biological activities were found for DCMC and ADCMC, the carbamoyl group at C-10 having been removed from Mitomycin or replaced by an acyl group. The observed effects were assumed to be due to the binding of these compounds with BSA. Further, to elucidate the thermodynamic mechanism of the binding of mitomycin derivatives with BSA, some stoichiometric investigations were made on the interaction between these compounds and BSA by an equilibrium dialysis procedure at 25° and 5°. All the compounds were found to be bound with BSA according to the Langmuir type interaction. The free energy changes of binding of both DCMC and ADCMC were larger than the others and these large values of energy changes were found to be due to large entropy changes. The possible mechanism of the interaction is discussed.
公益社団法人日本薬学会の論文
1972-10-25