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Article Abstract
The natural flavonoid macakurzin C () exhibited adiponectin biosynthesis-inducing activity during adipogenesis in human bone marrow mesenchymal stem cells and its molecular mechanism was directly associated with a pan-peroxisome proliferator-activated receptor (PPAR) modulator affecting all three PPAR subtypes α, γ, and δ. In this study, increases in adiponectin biosynthesis-inducing activity by macakurzin C derivatives () were studied. The most potent adiponectin biosynthesis-inducing compound , macakurzin C 3,5-dimethylether, was elucidated as a dual PPARα/γ modulator. Compound may exhibit the most potent activity because of the antagonistic relationship between PPARδ and PPARγ. Docking studies revealed that the -methylation of macakurzin C to generate compound significantly disrupted PPARδ binding. Compound has therapeutic potential in hypoadiponectinemia-related metabolic diseases.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10129854 | PMC |
| http://dx.doi.org/10.4062/biomolther.2022.097 | DOI Listing |
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Macakurzin C Derivatives as a Novel Pharmacophore for Pan-Peroxisome Proliferator-Activated Receptor Modulator.
Biomol Ther (Seoul)
May 2023
College of Pharmacy, Natural Products Research Institute, Seoul National University, Seoul 08826, Republic of Korea.
Article Synopsis
- - Macakurzin C, a natural flavonoid, boosts adiponectin production in human stem cells by activating all three PPAR subtypes (α, γ, δ) during adipogenesis.
- - The most effective derivative, macakurzin C 3,5-dimethylether, acts as a dual modulator for PPARα and PPARγ, potentially because it disrupts the binding of PPARδ, which has an antagonistic effect on PPARγ.
- - This research suggests that macakurzin C and its derivatives may offer new therapeutic options for metabolic issues linked to low adiponectin levels.