Inhibition of some hepatic lysosomal glycosidases by ethanolamines and phenyl 6-deoxy-6-(morpholin-4-yl)-beta-D-glucopyranoside.
The hepatic lysosomal glycosidases alpha-glucosidase and beta-glucuronidase were inhibited in vitro and in vivo by mono- and diethanolamines. The in vivo inhibition is dose dependent and occurs at a value less than LD50. Phenyl 6-deoxy-6-(morpholin-4-yl)-beta-D-glucopyranoside inhibited alpha-glucosidase both in vitro and in vivo. The treatment of the enzymes in vitro by ethanolamine exhibited a reversible inhibition of the mixed and competitive types for alpha-glucosidase and beta-glucuronidase, respectively. Diethanolamine showed a reversible inhibition of the competitive type for both enzymes. It is a potent inhibitor for beta-glucuronidase, in vitro, whose inhibition constant (Ki) is 5 x 10(-5) M. Phenyl 6-deoxy-6-(morpholin-4-yl)-beta-D-glucopyranoside is a potent inhibitor only for hepatic alpha-glucosidase with a Ki value of 1.6 x 10(-5) M. The pattern of the pH dependence of enzymic activity was not affected by ethanolamine inhibition. The magnitude of the inhibition of enzymes is dependent on the structure of the inhibitor.
Balbaa
M
M
Department of Biochemistry, Faculty of Science, Alexandria University, Egypt.
Abdel-Hady
N
N
el-Rashidy
F
F
Awad
L
L
el-Ashry el-S
H
H
Schmidt
R R
RR
D000818:Animals; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D004983:Ethanolamines / Q000737:chemistry / Q000494:pharmacology*; D005960:Glucosides / Q000737:chemistry / Q000494:pharmacology*; D005966:Glucuronidase / Q000037:antagonists & inhibitors* / Q000302:isolation & purification; D065089:Glycoside Hydrolase Inhibitors; D006863:Hydrogen-Ion Concentration; D007700:Kinetics; D008099:Liver / Q000201:enzymology*; D008247:Lysosomes / Q000201:enzymology*; D051379:Mice; D009025:Morpholines / Q000737:chemistry / Q000494:pharmacology*; D000520:alpha-Glucosidases / Q000302:isolation & purification
D004791:Enzyme Inhibitors; D004983:Ethanolamines; D005960:Glucosides; D065089:Glycoside Hydrolase Inhibitors; D009025:Morpholines; C121205:phenyl-6-deoxy-6-(morpholin-4-yl)glucopyranoside; D000520:alpha-Glucosidases; D005966:Glucuronidase