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Updated: Jun 3, 2026
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Deacetylation Assays to Unravel the Interplay between Sirtuins (SIRT2) and Specific Protein-substrates
Published on: February 27, 2016
Identification and evaluation of citrus peel-derived polymethoxyflavonoids as natural SIRT1 activators
Jung Ko1, Dwina Juliana Warman1, Peng Lu1
1Department of Applied Biological Chemistry, Graduate School of Agricultural and Life Science, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-8657, Japan.
Food Chemistry
|June 1, 2026
Summary
Citrus peels contain polymethoxyflavonoids (PMFs) that activate Sirtuin 1 (SIRT1), an enzyme linked to aging and disease. Heptamethoxyflavone (HMF) from kara mandarin showed the strongest SIRT1 activation, suggesting potential health benefits.
Area of Science:
- Biochemistry
- Pharmacology
- Nutraceuticals
Background:
- Sirtuin 1 (SIRT1) is a key regulator of aging and metabolic health.
- Citrus peel-derived polymethoxyflavonoids (PMFs) possess diverse bioactivities.
- The SIRT1-activating potential of PMFs is largely unexplored.
Purpose of the Study:
- To screen citrus peel extracts for SIRT1 activation.
- To identify specific PMFs that activate SIRT1.
- To elucidate the mechanism of SIRT1 activation by PMFs.
Main Methods:
- Non-fluorescence-based SIRT1 deacetylase assay.
- Electrospray ionization time-of-flight mass spectrometry (ESI-TOF-MS) for compound identification.
- Kinetic analysis and molecular docking simulations.
Main Results:
- Kara mandarin, shiikuwasha, and dekopon extracts significantly enhanced SIRT1 activity.
- Five PMFs, including heptamethoxyflavone (HMF), were identified as potent SIRT1 activators.
- HMF demonstrated the strongest activation, surpassing resveratrol, by decreasing substrate Km.
Conclusions:
- Citrus peels are a valuable natural source of SIRT1 activators.
- HMF's interaction with the SIRT1 N-terminal domain was computationally modeled.
- These findings support the use of citrus peels in functional foods for health promotion.
