Title:Biological Effect of Glycosyl-Oxadiazolinethione and Glycosyl-sulfanyloxadiazole Derivatives through their in vitro Inhibition of Glycosidases from Bacteria and Normal or Diabetic Rats
Volume: 12
Issue: 3
Author(s): Mahmoud Balbaa, Aseel Shibli, Riham Hosna, Hoda Yusef, Ahmed T. A. Boraei and El Sayed H. El Ashry
Affiliation:
Keywords:
Enzyme inhibitors, ethanolamines, glycosidases, glycosyl-sulfanyl-oxadiazole, oxadiazolinethione.
Abstract: 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.
