Biological Effect of Glycosyl-Oxadiazolinethione and Glycosyl-sulfanyl-oxadiazole Derivatives through their in Vitro Inhibition of Glycosidases from Bacteria and Normal or Diabetic Rats
Abstract
The inhibition of glycosidases from bacteria and the liver of normal and diabetic rats
by2-(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.
Author(s)
Balbaa M., Shibli A., Hosna R., Yusef H., Boraei A., El Ashry S.
Journal/Conference Information
Letters in Drug Design and Discovery ,12(3): 211-218