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] |