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- Title
Hypoglycemic, hepatoprotective and molecular docking studies of 5-[(4-chlorophenoxy) methyl]-1,3,4-oxadiazole-2-thiol.
- Authors
Shehzadi, Naureen; Hussain, Khalid; Bukhari, Nadeem Irfan; Islam, Muhammad; Khan, Muhammad Tanveer; Salman, Muhammad; Siddiqui, Sabahat Zahra; Aziz-Ur-Rehman; Abbasi, Muhammad Athar
- Abstract
The present study aimed at the evaluation of anti-hyperglycemic and hepatoprotective potential of a new drug candidate, 5-[(4-chlorophenoxy) methyl]-1,3,4-oxadiazole-2-thiol (OXCPM) through in vitro and in vivo assays, respectively. The compound displayed excellent dose-dependent α-amylase (28.0-92.0%), α-glucosidase (40.3-93.1%) and hemoglobin glycosylation (9.0%- 54.9%) inhibitory effects and promoted the uptake of glucose by the yeast cells (0.2 to 26.3%). The treatment of the isoniazid- and rifampicin- (p.o., 50 mg/kg of each) intoxicated rats with OXCPM (100 mg/kg, p.o.) resulted in restoring the normal serum levels of the non-enzymatic (total bilirubin, total protein and albumin) and bringing about a remarkable decrease in the levels of enzymatic (alanine transaminases, aspartate transaminases and alkaline phosphatase) biomarkers. The molecular docking studies indicated high binding affinity of the compound for hyperglycemia-related protein targets; fructose-1,6-bisphosphatase, beta2-adrenergic receptors and glucokinase. The results indicate that OXCPM may not only reduce hyperglycemia by enzyme inhibition but also the disease complications through protection of hemoglobin glycosylation and hepatic injury.
- Subjects
HYPOGLYCEMIC agents; HEMOGLOBINS; GLYCOSYLATION; GLUCOSE; ENZYMES
- Publication
Bangladesh Journal of Pharmacology, 2018, Vol 13, Issue 2, p149
- ISSN
1991-007X
- Publication type
Academic Journal
- DOI
10.3329/bjp.v13i2.35514