Biological Effect of Glycosyl-Oxadiazolinethione and Glycosyl-sulfanyloxadiazole Derivatives through their in vitro Inhibition of Glycosidases from Bacteria and Normal or Diabetic Rats
Ahmed T. A. Boraei,
El Sayed H. El Ashry.
The inhibition of glycosidases from bacteria and the liver of normal and diabetic rats by 2-(tetra-O-acetyl-β-Dglucopyranosylsulfanyl)-
5-(1-benzyl-1H-indol-2-yl)-1,3,4-oxadiazole BnM-3B; 3-(2,3,4,6-tetra-O-acetyl-β-D-galactopyranosyl)-
5-(1H-indol-2-yl)-1,3,4-oxadiazole- 2(3H)-thione MTB-4A; 3-(2-acetamido-3,4,6-tri-O-acetyl-2-deoxy-β-Dglucopyranosyl)-
5-(1-benzyl-1H-indol-2-yl)-1,3,4-oxadiazole-2(3H)-thione BnN-5A has been investigated. In vitro treatment
of hepatic α-amylase and β-glucuronidase from control and streptozotocin-induced diabetic rats by S- and Nglycosyl
analogues from oxadiazolinethione derivatives exhibited a significant dose-dependent decrease on the specific
activity of both α-amylase and β-glucuronidase. Moreover, these compounds also exhibited a significant decrease on the
specific activity of α-amylase and α-glucosidase produced by Bacillus subtilis AH. The observed IC50 values of these
compounds are much lower than that of ethanolamines, higher for α-glucosidase than α-amylase from bacteria and significantly
lower for hepatic α-amylase and β-glucuronidase from diabetic rats. The obtained results suggest that these compounds
are good inhibitors that act on glycosidases from bacteria and normal / diabetic rats in different mechanisms.
Keywords: Enzyme inhibitors, ethanolamines, glycosidases, glycosyl-sulfanyl-oxadiazole, oxadiazolinethione.
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