C. Sacco et Ej. Calabrese, SELECTIVE-INHIBITION OF GASTROINTESTINAL BETA-GLUCURONIDASE BY POLY(VINYLBENZYL D-GLUCARO(1,4)LACTONATE) .2. POLY(VINYLBENZYL D-GLUCARO(1,4) LACTONATE) IN-VITRO INHIBITION STUDIES, Human & experimental toxicology, 13(11), 1994, pp. 759-763
In vitro inhibition studies with beta-glucuronidase from purified E. c
oli and mouse intestinal contents indicated that the polymer, poly(vin
ylbenzyl D-glucaro(1,4)lactonate, is an effective beta-glucuronidase i
nhibitor. Purified E. coli beta-glucuronidase was inhibited by 99.6% w
ith 177 mM D-glucaro(1,4)lactone using the polymer-inhibitor. Similarl
y, 95% inhibition of beta-glucuronidase activity of mouse intestinal c
ontents was obtained with 177 mM and 50% inhibition was obtained with
31.5 mM D-glucaro(1,4)lactone based on the modified polymer. The struc
tural requirements of an effective beta glucuronidase inhibitor based
on the structure of the polymer-inhibitor are also discussed.