Silymarin and its components are inhibitors of beta-glucuronidase.
Silymarin, a commercial crude drug used as a hepatoprotective, was found to inhibit 53% of beta-glucuronidase activity at a final concentration of 0.8 mg/ml. Of three compounds A, silybin and C, which were isolated from silymarin, A and silybin potently inhibited the enzyme activity, followed by C. beta-Glucuronidases of intestinal bacteria, HGU-1 and HGU-2, and E. coli HB101 were noncompetitively inhibited by silybin. beta-Glucuronidase of the feces of a healthy human and of a human with colon cancer were also inhibited by silybin, silymarin and saccharic acid 1,4-lactone at 0.03-0.15 mg/ml. Silymarin and silybin protected the increase in enzyme activity in the serum of the rats treated with CCl4.
Kim
D H
DH
College of Pharmacy, Kyunghee University, Seoul, Korea.
Jin
Y H
YH
Park
J B
JB
Kobashi
K
K
D000818:Animals; D001419:Bacteria / Q000187:drug effects / Q000201:enzymology; D002252:Carbon Tetrachloride Poisoning / Q000201:enzymology; D002855:Chromatography, Thin Layer; D003110:Colonic Neoplasms / Q000201:enzymology; D005243:Feces / Q000382:microbiology; D005966:Glucuronidase / Q000037:antagonists & inhibitors*; D006801:Humans; D007422:Intestines / Q000382:microbiology; D008099:Liver / Q000187:drug effects / Q000201:enzymology; D008297:Male; D008862:Microsomes, Liver / Q000187:drug effects / Q000201:enzymology; D051381:Rats; D017208:Rats, Wistar; D012838:Silymarin / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*
D012838:Silymarin; D005966:Glucuronidase