Selective Inhibition of Gastrointestinal β-Glucuronidase by Poly(vinylbenzyl D-glucaro(1,4)lactonate). Part 2. Poly(vinylbenzyl D-Glucaro(1,4) lactonate) In vitro Inhibition Studies

Abstract

In vitro inhibition studies with β-glucuronidase from purified E. coli and mouse intestinal contents indicated that the polymer, poly(vinylbenzyl D-glucaro(1,4)lactonate, is an effective β-glucuronidase inhibitor. Purified E. coli β-glucuronidase was inhibited by 99.6% with 1 77 mM D-glucaro(1,4)lactone using the polymer-inhibitor. Similarly, 95% inhibition of β-glucuronidase activity of mouse intestinal contents 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 structural requirements of an effective β-glucuronidase inhibitor based on the structure of the polymer-inhibitor are also discussed.