Nutraceuticals as Ligands of PPAR𝜸

Table 1

Potential dietary PPAR𝛾 ligands.

Ligand	Binding affinity	Type of assay	Reference
Linoleic acid	Ki > 1 μM	Competitive radio-labeled binding assay	[22]
Nitrolinoleic acid	Ki = 133 nM
9-Hydroxyoctadecadienoic acid (9-HODE)
13-Hydroxyoctadecadienoic acid (13-HODE)
9/10-NO2-linoleic acid	IC50 = 0.6 μM	Scintillation proximity	[23]
12-NO2-linoleic acid	IC50 = 0.41 μM	Competitive binding assay
13-NO2-linoleic acid	IC50 = 0.44 μM
Azelaoyl phosphatidylcholine (in oxidized LDL)	40 nm	Radiolabeled binding assay	[24]
Docosahexaenoic acid (DHA)	EC50 > 10 μm	Dual luciferase reporter system	[25]
4-Hydroxy docosahexaenoic acid (4-HDHA)	EC50 = 3.7 μm
4-Oxodocosahexaenoic acid (4-oxo-DHA)	EC50 = 0.4 μM
Conjugated linoleic acid isomers (CLA)	IC50 = 3.2–7.4 μM	Competitive scintillation proximity assays	[26]
Isoflavones:
Genistein	Ki = 5.7 μM	Membrane-bound competitive PPAR𝛾 binding assay	[27]
Daidzein	20 μM	Luciferase reporter assay in 3T3-L1 cells	[28]
	EC50 = 73 μM	Luciferase reporter assay in HeLa cells	[29]
Equol	20 μM	Luciferase reporter assay in 3T3-L1 cells	[28]
Biochanin A	EC50 = 3.7 μm	Luciferase reporter assay in HeLa cells	[29]
	EC50 < 1 μM	Luciferase reporter assay in HepG2 cells	[29]
Flavonoids:
Psi-baptigenin	EC50 = 2.9 μM	Transcriptional factor activity assay in ThP-1 cells	[30]
Hesperidin	EC50 = 6.6 μM
Quercetin (from dill, bay leaves, and oregano)	EC50 = 2.8 μM	Ligand screening assay	[31]
2^′-Hydroxy chalcone (cinnamon in polymeric form)	EC50 = 3.8 μM	Ligand screening assay	[31]
Rosmarinic acid (marjoram)	EC50 = 16 μM	Ligand screening assay	[31]