Inhibition of some hepatic glycosidases by the diseco nucleoside, 4-amino-3-(D-glucopentitol-1-yl)-5-mercapto-1,2,4-triazole and its 3-methyl analog.
The in vivo and in vitro effects of 4-amino-3-(D-glucopentitol-1-yl)-5-mercapto-1,2,4-triazole and its 3-methyl analogue on alpha- and beta-glucosidases, beta-glucuronidase as well as alpha-amylase have been investigated. alpha-Glucosidase is the enzyme that is markedly affected in vivo and in vitro in a dose-dependent manner. The compounds showed a reversible inhibition of a competitive type for alpha-glucosidase. Moreover, they exert a relatively potent inhibition on alpha-glucosidase with a Ki magnitude of 3.6 x 10(-4), 9.5 x 10(-5) M.
Balbaa
Mahmoud
M
Department of Biochemistry, Faculty of Science, Alexandria University, Alexandria, Egypt.
Mansour
Hamdi
H
El-Sawy
Hany
H
El-Ashry
El-Sayed H
el-SH
D000818:Animals; D001667:Binding, Competitive; D004305:Dose-Response Relationship, Drug; D004591:Electrophoresis, Polyacrylamide Gel; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D005966:Glucuronidase / Q000037:antagonists & inhibitors; D065089:Glycoside Hydrolase Inhibitors; D006026:Glycoside Hydrolases / Q000302:isolation & purification / Q000378:metabolism; D008099:Liver / Q000201:enzymology*; D051379:Mice; D009705:Nucleosides / Q000737:chemistry / Q000494:pharmacology*; D013438:Sulfhydryl Compounds / Q000737:chemistry / Q000494:pharmacology*; D014230:Triazoles / Q000737:chemistry / Q000494:pharmacology*; D000516:alpha-Amylases / Q000037:antagonists & inhibitors; D001617:beta-Glucosidase / Q000037:antagonists & inhibitors*
D004791:Enzyme Inhibitors; D065089:Glycoside Hydrolase Inhibitors; D009705:Nucleosides; D013438:Sulfhydryl Compounds; D014230:Triazoles; D006026:Glycoside Hydrolases; D000516:alpha-Amylases; D001617:beta-Glucosidase; D005966:Glucuronidase