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Structural Bases for Hesperetin Derivatives: Inhibition of Protein Tyrosine Phosphatase 1B, Kinetics Mechanism and Molecular Docking Study. | LitMetric

AI Article Synopsis

  • The study focused on how different forms of hesperetin affect the inhibition of diabetes-related enzymes, specifically PTP1B and α-glycosidase.
  • Hesperetin 5-glucoside, a derivative with a sugar molecule, was found to significantly inhibit PTP1B more effectively than regular hesperetin, which has no sugar.
  • The presence, position, and number of sugar moieties in hesperetin variants influence their ability to inhibit PTP1B, suggesting that hesperetin 5-glucoside might be a promising candidate for new diabetes treatments.

Article Abstract

In the present study, we investigated the structure-activity relationship of naturally occurring hesperetin derivatives, as well as the effects of their glycosylation on the inhibition of diabetes-related enzyme systems, protein tyrosine phosphatase 1B (PTP1B) and α-glycosidase. Among the tested hesperetin derivatives, hesperetin 5--glucoside, a single-glucose-containing flavanone glycoside, significantly inhibited PTP1B with an IC value of 37.14 ± 0.07 µM. Hesperetin, which lacks a sugar molecule, was the weakest inhibitor compared to the reference compound, ursolic acid (IC = 9.65 ± 0.01 µM). The most active flavanone hesperetin 5--glucoside suggested that the position of a sugar moiety at the C-5-position influences the PTP1B inhibition. It was observed that the ability to inhibit PTP1B is dependent on the nature, position, and number of sugar moieties in the flavonoid structure, as well as conjugation. In the kinetic study of PTP1B enzyme inhibition, hesperetin 5--glucoside led to mixed-type inhibition. Molecular docking studies revealed that hesperetin 5--glucoside had a higher binding affinity with key amino residues, suggesting that this molecule best fits the PTP1B allosteric site cavity. The data reported here support hesperetin 5--glucoside as a hit for the design of more potent and selective inhibitors against PTP1B in the search for a new anti-diabetic treatment.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8705904PMC
http://dx.doi.org/10.3390/molecules26247433DOI Listing

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