Abstract

Glucosaccharo-1:4-lactone, the specific and potent inhibitor of β-glucuronidase, was orally administered to mice, rats, and guinea pigs. The results indicate that glucosaccharo-1:4-lactone is absorbed from the intestinal tract and distributed throughout the body. The glucuronidase activity of liver and kidney was inhibited for at least 2 hr after administration of the lactone and recovered gradually to the initial activity within several hours. Ten to twenty per cent of the lactone orally administered to rats was recovered in the urine afterward. These experiments indicate that there is no enzymatic ring opening of glucosaccharo-1:4-lactone in rat liver and kidney. Administration of glucosaccharate, glucuronate, glucuronolactone, and gluconolactone showed little or no effect on the tissue glucuronidase activities.

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