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<p>Prolonged hyperglycemia exacerbates diabetes through the formation of early Amadori-glycoxidation, intermediate reactive dicarbonyl species and advanced cross-linked aggregates. The study utilizes multi-spectroscopies based biophysical analyses to encompass an early to advanced stage inhibition of fructose (Fru) and methylglyoxal mediated bovine serum albumin (BSA) glycation (Fru-gBSA and methylglyoxal-gBSA) by introducing dansyl labelled molecular probe in the privileged scaffold <i>pseudo C</i><sub><i>2</i></sub>‒symmetric <i>transoid</i> aldazines (<i>bis</i>-aldimine) framework. The study thus explores the pharmacophoric role of aldazine moiety through the conformational-binding selection of s-<i>trans</i> dansylated-<i>bis</i>-vanillin aldimines (DVBA-<b>1</b>) to investigate the inhibition mechanism of BSA glycation from early Amadori-glycoxidation to advanced cross-linking. Conformational studies in association with molecular docking and dynamic simulation reflects a distinctive binding between IIA and IIIA sub-domain of BSA of a specific rotameric <i>transoid</i> conformation of DVBA-<b>1</b>, among all <i>transoid</i> conformers, which causes secondary structural perturbation and glycation micro-environment alteration. This strategy supports the primary interactions of aldazine pharmacophore of DVBA-<b>1</b> near sugar-binding domain of BSA resulting inhibition of glycation.</p> Graphical abstract <p></p>

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Labeling dansyl molecular probe in aldazines to decipher conformational selected inhibition pathway from early to advanced glycation

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2026年7月4日

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  • Santu Bhunia,
  • Arindam Bankura,
  • Charu Chand Hansda,
  • Subhodeep Das,
  • Sudipta Sasmal,
  • Sansa Dutta,
  • Ranjan Jana,
  • Koushik Chandra

摘要

Prolonged hyperglycemia exacerbates diabetes through the formation of early Amadori-glycoxidation, intermediate reactive dicarbonyl species and advanced cross-linked aggregates. The study utilizes multi-spectroscopies based biophysical analyses to encompass an early to advanced stage inhibition of fructose (Fru) and methylglyoxal mediated bovine serum albumin (BSA) glycation (Fru-gBSA and methylglyoxal-gBSA) by introducing dansyl labelled molecular probe in the privileged scaffold pseudo C2‒symmetric transoid aldazines (bis-aldimine) framework. The study thus explores the pharmacophoric role of aldazine moiety through the conformational-binding selection of s-trans dansylated-bis-vanillin aldimines (DVBA-1) to investigate the inhibition mechanism of BSA glycation from early Amadori-glycoxidation to advanced cross-linking. Conformational studies in association with molecular docking and dynamic simulation reflects a distinctive binding between IIA and IIIA sub-domain of BSA of a specific rotameric transoid conformation of DVBA-1, among all transoid conformers, which causes secondary structural perturbation and glycation micro-environment alteration. This strategy supports the primary interactions of aldazine pharmacophore of DVBA-1 near sugar-binding domain of BSA resulting inhibition of glycation.

Graphical abstract