Hypoglycemic, hepatoprotective and molecular docking studies of 5-[(4-chlorophenoxy) methyl]-1, 3, 4-oxadiazole-2-thiol

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 ɑ-amylase (28.0-92....

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Main Authors: Naureen Shehzadi (Author), Khalid Hussain (Author), Nadeem Irfan Bukhari (Author), Muhammad Islam (Author), Muhammad Tanveer Khan (Author), Muhammad Salman (Author), Sabahat Zahra Siddiqui (Author), Aziz Ur Rehman (Author), Muhammad Athar Abbasi (Author)
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Published: Bangladesh Pharmacological Society, 2018-05-01T00:00:00Z.
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100 1 0 |a Naureen Shehzadi  |e author 
700 1 0 |a Khalid Hussain  |e author 
700 1 0 |a Nadeem Irfan Bukhari  |e author 
700 1 0 |a Muhammad Islam  |e author 
700 1 0 |a Muhammad Tanveer Khan  |e author 
700 1 0 |a Muhammad Salman  |e author 
700 1 0 |a Sabahat Zahra Siddiqui  |e author 
700 1 0 |a Aziz Ur Rehman  |e author 
700 1 0 |a Muhammad Athar Abbasi  |e author 
245 0 0 |a Hypoglycemic, hepatoprotective and molecular docking studies of 5-[(4-chlorophenoxy) methyl]-1, 3, 4-oxadiazole-2-thiol 
260 |b Bangladesh Pharmacological Society,   |c 2018-05-01T00:00:00Z. 
500 |a 10.3329/bjp.v13i2.35514 
500 |a 1991-0088 
520 |a 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 ɑ-amylase (28.0-92.0%), ɑ-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. Video Clip of Methodology: Glucose uptake by yeast cells:   4 min 51 sec   Full Screen   Alternate 
546 |a EN 
690 |a Anti-hyperglycemic 
690 |a Hepatoprotective 
690 |a Molecular docking 
690 |a 5-[(4-chlorophenoxy) methyl]-1 
690 |a 3 
690 |a 4-oxadiazole-2-thiol 
690 |a Therapeutics. Pharmacology 
690 |a RM1-950 
655 7 |a article  |2 local 
786 0 |n Bangladesh Journal of Pharmacology, Vol 13, Iss 2 (2018) 
787 0 |n https://www.banglajol.info/index.php/BJP/article/view/35514 
787 0 |n https://doaj.org/toc/1991-0088 
856 4 1 |u https://doaj.org/article/0320f3927c4d4da281b1d2b42b5aa98c  |z Connect to this object online.