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Quercetin based derivatives as sirtuin inhibitors.

Vladimír Heger1, Jonna Tyni2, Attila Hunyadi3

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Summary

Two quercetin derivatives, diquercetin and 2-chloro-1,4-naphtoquinone-quercetin, show promise as SIRT6 inhibitors. These compounds target sirtuins, offering potential new treatments for age-related diseases.

Keywords:
DeacetylationQuercetin derivativesSIRT2 inhibitorSIRT6 inhibitorSirtuin

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Area of Science:

  • Biochemistry
  • Pharmacology
  • Molecular Biology

Background:

  • Polyphenols exhibit diverse pharmacological effects and modulate sirtuins, enzymes crucial for aging, metabolism, and disease.
  • Sirtuin 6 (SIRT6) is vital for genomic stability and glucose metabolism, making it a key target for therapeutic intervention.
  • Quercetin and its derivatives are known to interact with sirtuins and offer protection against chronic illnesses.

Purpose of the Study:

  • To identify and characterize novel SIRT6 inhibitors from quercetin derivatives.
  • To elucidate the mechanism of inhibition for identified compounds using in vitro and molecular modeling approaches.
  • To explore the therapeutic potential of these polyphenolic compounds in age-related diseases.

Main Methods:

  • In vitro enzyme inhibition assays to determine IC50 values against SIRT6 and SIRT2.
  • Kinetic analysis to understand the mode of inhibition (e.g., competitive, non-competitive).
  • Molecular docking simulations to predict binding interactions within the SIRT6 catalytic site.

Main Results:

  • Diquercetin and 2-chloro-1,4-naphtoquinone-quercetin were identified as SIRT6 inhibitors with IC50 values of 130 μM and 55 μM, respectively.
  • 2-Chloro-1,4-naphtoquinone-quercetin also inhibited SIRT2 (IC50 = 14 μM).
  • Kinetic studies revealed diquercetin competes with NAD+, while 2-chloro-1,4-naphtoquinone-quercetin competes with the acetylated substrate, suggesting distinct binding mechanisms.

Conclusions:

  • Diquercetin and 2-chloro-1,4-naphtoquinone-quercetin are effective SIRT6 inhibitors with different modes of action.
  • These findings highlight the potential of natural polyphenols as a novel therapeutic strategy for age-related conditions.
  • Further research into these compounds could lead to the development of new treatments targeting sirtuin pathways.