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Objectives <p>The in vivo assay is a key step in the development of a new compound as a drug. In the present work, bis-4-aminocoumarin derivative 3,3'-(p-tolylmethylene)bis(4-amino-2H-chromen-2-one) (<b>PTBAC</b>) and bis-4-hydroxycoumarin derivative 3,3'-((4-((1-(2-chlorobenzyl)-1H-1,2,3-triazol-4-yl)methoxy)phenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) (<b>2CTMBHC</b>) that showed high anti-α-glucosidase activity on the yeast form of this enzyme were selected for in vivo anti-hyperglycemic assay.</p> Methods <p>The in vivo anti-hyperglycemic effect of <b>PTBAC</b> and <b>2CTMBHC</b> was assessed using oral starch tolerance test in streptozotocin-induced diabetic albino mouse model, and the results were compared with acarbose as a representative inhibitor of intestinal α-glucosidase enzyme. Toxicity of the selected compounds was also evaluated in vivo.</p> Results <p>The obtained results revealed that both selected compounds, <b>PTBAC</b> and <b>2CTMBHC</b>, showed more anti-diabetic effects when compared with acarbose as a standard drug. In vivo anti-diabetic assays also demonstrated that bis-4-hydroxycoumarin derivative <b>2CTMBHC</b> was more potent than bis-4-aminocoumarin derivative <b>PTBAC</b>. In vivo results were also confirmed by in vitro and in silico studies. Moreover, there was not any apparent signs of toxicity and mortality in in vivo toxicity assay.</p> Conclusions <p>In summary,&#xa0;in vivo anti-hyperglycemic effects of two synthetic compounds <b>PTBAC</b> and <b>2CTMBHC</b> was confirmed in this study. Given that these compounds exhibited no evidences of toxicity and mortality in mice, therefore, they are good candidates for further investigations.</p> Graphical Abstract <p></p>

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In vivo anti-hyperglycemic activity and toxicity evaluation of two bis-coumarin derivative as potential α-glucosidase inhibitors

  • 期刊论文

  • 发表日期：

    2025年2月13日

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  • Maryam Mohammadi-Khanaposhtani,
  • Tayebeh Bahrami,
  • Fatemeh Bandarian,
  • Ensieh Nasli-Esfahani,
  • Davoud Roostaei,
  • Ehsan Zamani,
  • Forough Aghajani,
  • Mohammad Mahdavi,
  • Nematollah Ahangar

摘要

Objectives

The in vivo assay is a key step in the development of a new compound as a drug. In the present work, bis-4-aminocoumarin derivative 3,3'-(p-tolylmethylene)bis(4-amino-2H-chromen-2-one) (PTBAC) and bis-4-hydroxycoumarin derivative 3,3'-((4-((1-(2-chlorobenzyl)-1H-1,2,3-triazol-4-yl)methoxy)phenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) (2CTMBHC) that showed high anti-α-glucosidase activity on the yeast form of this enzyme were selected for in vivo anti-hyperglycemic assay.

Methods

The in vivo anti-hyperglycemic effect of PTBAC and 2CTMBHC was assessed using oral starch tolerance test in streptozotocin-induced diabetic albino mouse model, and the results were compared with acarbose as a representative inhibitor of intestinal α-glucosidase enzyme. Toxicity of the selected compounds was also evaluated in vivo.

Results

The obtained results revealed that both selected compounds, PTBAC and 2CTMBHC, showed more anti-diabetic effects when compared with acarbose as a standard drug. In vivo anti-diabetic assays also demonstrated that bis-4-hydroxycoumarin derivative 2CTMBHC was more potent than bis-4-aminocoumarin derivative PTBAC. In vivo results were also confirmed by in vitro and in silico studies. Moreover, there was not any apparent signs of toxicity and mortality in in vivo toxicity assay.

Conclusions

In summary, in vivo anti-hyperglycemic effects of two synthetic compounds PTBAC and 2CTMBHC was confirmed in this study. Given that these compounds exhibited no evidences of toxicity and mortality in mice, therefore, they are good candidates for further investigations.

Graphical Abstract