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. 2012 Jun 20;2012:858352. doi: 10.1155/2012/858352

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]