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Natural Polyphenols Inhibit Lysine-Specific Demethylase-1 in vitro.

Arian Abdulla1, Xiaoping Zhao, Fajun Yang

  • 1Department of Medicine, Developmental and Molecular Biology, Diabetes Research and Training Center, Albert Einstein College of Medicine, 1301 Morris Park Avenue, Bronx NY 10461, USA.

Journal of Biochemical and Pharmacological Research
|May 11, 2013
PubMed
Summary

Natural polyphenols like resveratrol and curcumin inhibit the enzyme LSD1, crucial for cell processes. This discovery reveals a new therapeutic target for diseases linked to LSD1 activity.

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Natural polyphenols, including resveratrol, exhibit health benefits against major diseases.
  • These compounds can act as antioxidants and target proteins to modulate biological pathways.
  • Lysine-specific histone demethylase 1 (LSD1) is vital for cell growth, differentiation, and metabolism.

Purpose of the Study:

  • To investigate the effects of natural polyphenols (resveratrol, curcumin, quercetin) and analogs on LSD1 activity.
  • To identify if LSD1 is a novel molecular target for these bioactive natural compounds.

Main Methods:

  • In vitro enzymatic assays were used to measure LSD1 inhibition.
  • Comparison of polyphenol inhibitory effects against a known LSD1 inhibitor (TCP).
Keywords:
LSD1curcumindemethylationmyogenesispolyphenolquercetinresveratrol

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  • Assessment of polyphenol effects on myogenic expression and differentiation in C2C12 fibroblasts.

    • Main Results:

    • Resveratrol, curcumin, and quercetin potently inhibited LSD1 activity in vitro.
    • These polyphenols were more effective LSD1 inhibitors than trans-2-phenylcyclopropylamine (TCP).
    • Inhibition of LSD1 by resveratrol and curcumin suppressed myogenic expression and differentiation in fibroblasts.

    Conclusions:

    • LSD1 is identified as a novel molecular target for resveratrol, curcumin, and quercetin.
    • The observed inhibitory effects are independent of the antioxidant properties of these polyphenols.
    • LSD1 inhibition by these natural compounds may contribute to their previously documented health benefits.