Initial Intraorgan Formation of Mercapturic Acid

概要

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The disposition of S-benzyl-glutathione (BSG) in male Wister rats was evaluated by the HPLC method to examine whether the kidney and liver contributed independently to the biosynthesis of S-benzyl-N-acetylcysteine (BNAc), a mercapturic acid (Chart 1). After intravenous injection, BSG was rapidly transported in both the kidney and the liver at a ratio of about 7:3. Simultaneously, a large amount of BNAc was found in both the kidney and the liver. In the kidney, S-benzyl-cysteine (BCys) reached a maximum concentration (C_<max>) at 2 min after BSG injection, whereas BNAc reached C_<max> within 3 to 5 min. The generation of BNAc was also observed in the liver. While renal BNAc reached C_<max> within 3 to 5 min, hepatic BNAc reached C_<max> around 5 min after BSG injection. Moreover, the elimination half-life of the BNAc after intravenous injection of the BSG was equivalent to that observed after intravenous injection of the BNAc itself. These results demonstrate that the kidney contributes to the initial intraorgan generation of BNAc and that this mercapturic acid is also synthesized in the liver and preferentially excreted into urine.
公益社団法人日本薬学会の論文
2001-11-01