Abstract
Purpose: To evaluate 5-Benzyl-1,3,4-oxadiazole-2-thiol (OXPA) for antidiabetic and antioxidant properties.
 Methods: Antidiabetic activity was evaluated using three in vitro models, glucose uptake by yeast cells, alpha amylase inhibition assay and hemoglobin glycosylation inhibition assays. Antioxidant potential was determined by DPPH radical scavenging, reducing power and lipid peroxidation assays.
 Results: OXPA showed antidiabetic activity in all the three models. The activity of the compound was comparable with that of metronidazole in glucose uptake by yeast cells, but the alpha amylase inhibition activity of the compound was slightly lower than that of acarbose, whereas the hemoglobin glycosylation inhibition activity of the compound was higher than that of vitamin E. DPPH free radical and hydrogen peroxide scavenging activity of the compound was comparable with that of vitamin C. In reducing power assay, the activity of the compound was lower than that of vitamin C (p > 0.05).
 Conclusion: The results of antidiabetic and antioxidant activity indicate that OXPA may be a drugcandidate for treating both diabetes and its associated oxidative stress.
Highlights
The compound under investigation, 5-Benzyl1,3,4-oxadiazole-2-thiol (OXPA), is a derivative of 1,3,4-oxadiazole having benzyl and thiol at positions 5 and 2, respectively (Figure 1)
It is reported that thiol containing compounds act as antioxidants due to proton donating potential [35], while oxadiazole ring is a pharmacophore possessing a number of pharmacological activities including antidiabetic activity [3,4,5]
These results showed that the compound facilitated the transport of glucose in the yeast cells in all the three glucose solutions (5, 10 and 25 mM)
Summary
The compound under investigation, 5-Benzyl1,3,4-oxadiazole-2-thiol (OXPA), is a derivative of 1,3,4-oxadiazole having benzyl and thiol at positions 5 and 2, respectively (Figure 1). It is reported that thiol containing compounds act as antioxidants due to proton donating potential [35], while oxadiazole ring is a pharmacophore possessing a number of pharmacological activities including antidiabetic activity [3,4,5]. The advanced glycation end products being the source of free radicals further aggravate oxidative stress [9] Such complications can be reduced using antioxidants or compounds having both antidiabetic and antioxidant activities [10]. The sample/standard solution (3.4 mL) and 43 mM H2O2 (0.6 mL), prepared in phosphate buffer (pH 7.4), were mixed and kept at room temperature at dark for 50 min. One milliliter solution of sample, potato starch, alpha amylase (0.025 %, W/V) were mixed with 1 mL of sodium phosphate buffer (pH 6.9) and incubated at 37 °C for 30 min. The absorbance of the mixture was measured at 540 nm to calculate the alpha amylase inhibition activity
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