P-Glucuronidase inhibitors

OioHioOg 258.184 p-Glucuronidase inhibitor, antiinflammatory action. Use experimentally to facilitate glucuronodation of carcinogens and inhibit neoplasm formation. Insol. H2O. Mp 185-186°. Log P -1.04 (calc). 

Glycoprotein. Isol. from Micromonospora sp. BR-1613. P-Glucuronidase inhibitor. Vax 280 (e 359) (H2O) (Berdy). 

C. L. Joyce, S. R. Mack, R. A. Anderson, and L. J. D. Zaneveld. Effect of hyaluronidase, p-glucuronidase and P-N-acetylglucosaminidase inhibitors on sperm penetration of the mouse oocyte. Biol. Reprod. 35 336 (1986). 

S-Carboxy-3/ ,4/ ,55 -trihydroxy-piperidine from Baphia racemosa (Leguminosae) seeds is an inhibitor of human P-D-glucuronidase and a-L-iduronidase [147]. The all trans-dihydroxyproline, (25, 3/ ,4f )-2-carboxy-3,4-dihydroxypyrrolidine, from Amanita virasa is structurally analogous at C(2), C(3) and C(4) to O-glucuronic acid and it is also a moderate inhibitor of human P-D-glucuronidase [148]. 

S,31, 47 ,55 )-3,4,5-Trihydroxypipecolic acid (1) was isolated from the seeds of legume Baphia racemosa Bak. It is a specific inhibitor of human fiver 3-D-glucuronidase and idouronidase but it has no effect on a- and p-glucosidases or mannosidases. (2S,4S,5S)-... 

To investigate the intrinsic GUS levels of plants, extracts were prepared from sterile vegetative tissues and seeds and assayed for beta-glucuronidase activity, initially by using the convenient spectrophotometric assays employing p-nitrophenol, and later with extremely sensitive fluorometric methods. In no case was any significant beta-glucuronidase activity found. Plants assayed included tobacco, potato, Brassica napus. Petunia hybrida, tomato, wheat, barley, maize, and Arabidopsis thaliana. Reconstruction experiments with purified GUS added to tobacco and potato extracts indicated that there were no intrinsic inhibitors present in the extracts that would pose a potential problem for... 

All except 374 showed modest inhibitory activity toward various galactosi-dases. The novel synthetic p-methoxybenzyl analog (—)-377 was a reasonably effective inhibitor of (3-glucuronidase from E. coli, but poorly active toward several other glycosidases. 

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