Experimental IC₅₀ values and transactivation activity of the selected compounds.

A competitive binding assay was used to assess the ability of experimental compounds, FMOC or rosiglitazone to displace a fluorescent PPARγ ligand from a human-derived recombinant PPARγ ligand-binding domain. The concentration of the test compound that results in a half-maximal shift in the polarization value is defined as IC50. This value is a measure of the relative affinity of the test compound for the PPAR ligand-binding domain. The transactivation capacity of selected compounds was also determined in HepG2 cells as described in Materials and Methods. Results represent the mean ± SD of at least three separate experiments performed in triplicate. Results are expressed as arbitrary firefly luciferase units relative to arbitrary renilla luciferase units. For compounds C2, C3 and C6, no binding was observed when assayed at concentrations up to 8 mM. Compounds C4 and C10 were not assayed because of solubility problems. For Rosiglitazone and FMOC, gene reporter activity at 500 and 1000 μM were not assayed because of solubility problems. **p<0.001 and * p<0.05 when compared to the control (DMSO) in an ANOVA test.