Studies on Glucosaccharolactones

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Abstract
Inhibition of β-glucuronidase by glucosaccharate and its lactones were studied by administering these compounds to mice and measuring β-glucuronidase activity of the liver. The blood was also tested for its inhibitory action on partially purified preparations of rat liver β-glucuronidase. When these compounds were orally given to mice and β-glucuronidase activities of the fresh liver homogenates were measured, their inhibitory activities were found in the following order. SDL>SL 1:4>SL 3:6>SA. SDL, intravenously given, was taken up by the liver more readily than SL 1:4. Saccharate had no effect within the dose range applied in the experiment. Thus, the 3:6-lactonization caused an increase of the effect of the free sugar acid or its 1:4-monolactone and this result was quite contrary to that of the in vitro test reported previously. The intensified inhibitory effect of the 3:6-lactonized hydroxy acids shown in the in vivo experiment was explained by the enhanced intestinal absorption and cell membrance penetration due to an electrically less charged state of the lactones than the corresponding acids.