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Phenolic Compounds Inhibit 3T3-L1 Adipogenesis Depending on the Stage of Differentiation and Their Binding Affinity to PPARγ
- Source :
- Molecules, Dadun. Depósito Académico Digital de la Universidad de Navarra, instname, Molecules, Vol 24, Iss 6, p 1045 (2019), Volume 24, Issue 6
- Publication Year :
- 2019
- Publisher :
- MDPI, 2019.
-
Abstract
- Phenolic compounds might modulate adiposity. Here, we report our observation that polyphenols and phenolic acids inhibit adipogenesis in 3T3-L1 with different intensity depending on the family and the stage of differentiation. While quercetin and resveratrol inhibited lipid accumulation along the whole process of differentiation, apigenin and myricetin were active during the early and latest stages, but not intermediate, contrary to hesperidin. The activity of phenolic acids was limited to the early stages of the differentiation process, except p-coumaric and ellagic acids. This anti-adipogenic effect was accompanied by down-regulation of Scd1 and Lpl. Molecular docking analysis revealed that the inhibitory activity of these phenolic compounds over the early stages of adipogenesis exhibits a significant correlation (r = 0.7034<br />p = 0.005) with their binding affinity to the ligand-binding domain of PPAR&gamma<br />Results show that polyphenols and phenolic acids would interact with specific residues of the receptor, which could determine their potential anti-adipogenic activity during the early stages of the differentiation. Residues Phe264, His266, Ile281, Cys285 and Met348 are the most frequently involved in these interactions, which might suggest a crucial role for these amino acids modulating the activity of the receptor. These data contribute to elucidate the possible mechanisms of phenolic compounds in the control of adipogenesis.
- Subjects :
- PPARγ
Pharmaceutical Science
Resveratrol
Nile Red
Analytical Chemistry
chemistry.chemical_compound
Mice
0302 clinical medicine
Drug Discovery
Apigenin
chemistry.chemical_classification
0303 health sciences
Adipocyte
Phenolic acid
Adipogenesis
phenolic acid
Nile red
Gene Expression Regulation, Developmental
Cell Differentiation
Amino acid
Molecular Docking Simulation
Biochemistry
Chemistry (miscellaneous)
030220 oncology & carcinogenesis
Molecular Medicine
Myricetin
Quercetin
Stearoyl-CoA Desaturase
Polyphenol
adipocyte
Article
lcsh:QD241-441
03 medical and health sciences
lcsh:Organic chemistry
Phenols
3T3-L1 Cells
Animals
Physical and Theoretical Chemistry
030304 developmental biology
3T3-L1
Flavonoids
Hesperidin
Organic Chemistry
Lipid Metabolism
PPAR gamma
polyphenol
chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 14203049
- Volume :
- 24
- Issue :
- 6
- Database :
- OpenAIRE
- Journal :
- Molecules
- Accession number :
- edsair.doi.dedup.....41e175d552dff1b97da8f73fa9ed37ec