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image of Synthesis of (E)-3-(aryl)-1-phenylprop-2-en-1-one Chalcone Derivatives for Hyperglycemic Effect in Diabetes: In-vitro, In-vivo and In-silico Approach

Abstract

Background

Diabetes mellitus (DM) is a chronic metabolic disorder that seeks treatment instead of available mitigative therapy.

Methods

Six ()-3-(aryl)-1-phenylprop-2-en-1-one chalcones were synthesized and characterized through various spectroscopic techniques. Their anti-diabetic potential was examined through (α-glucosidase and α-amylase inhibition assays), (alloxan-induced hyperglycemia), and studies.

Results

All the chalcones derivatives significantly inhibited α-glucosidase and α-amylase. Compounds (IC = 1.10 ± 0.02) and (IC = 3.25 ± 0.10 µM) exhibited the most potent activity against α-glucosidase. The effect of compounds and was also significant against α-amylase with IC of 13.2 ± 0.50 and 10.2 ± 0.4 µM, respectively. In alloxan-induced hyperglycemic model, a significant (<0.001) reduction in blood glucose level (BGL) was observed by compounds , and with maximum percent inhibition of 47.48, 47.22 and 47.55, respectively. In the oral glucose tolerance test, a continuous reduction in BGL was noted at 60 minutes. No negative effect was seen on lipid profile, and in liver and renal function tests. However, a slight gain in body weight was noted. Moreover, docking result indicates good interaction of these molecules with the target enzymes, α-glucosidase and α-amylase.

Conclusion

These results demonstrate that all these molecules have significant anti-diabetic potential.

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2025-06-24
2025-09-09

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Synthesis of (E)-3-(aryl)-1-phenylprop-2-en-1-one Chalcone Derivatives for Hyperglycemic Effect in Diabetes: In-vitro, In-vivo and In-silico Approach
Bentham Science Publishers ; https://doi.org/10.2174/0109298673343058250127103657
/content/journals/cmc/10.2174/0109298673343058250127103657
/content/journals/cmc/10.2174/0109298673343058250127103657
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  • Article Type:     Research Article
Keywords: α-glucosidase inhibition ; α-amylase ; B-cells ; Synthesis ; anti-diabetic activities ; chalcone derivatives

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