Receptor activation of curcumin on human peroxisome proliferators-activated receptors γ1 / 中草药

ABSTRACT

Objective: To determine whether curcumin is a natural ligand for human peroxisome proliferators-activated receptors γ1 (hPPARγ1) by measuring the combination ability and internal activity. Methods: The combination ability was determined by radioactively labeled ligand binding experiment (RBCA), and the internal activity was estimated by trans-activation reporter gene test. Results: The combination ability of curcumin on hPPARγ1 showed that IC50 was (8.82 ± 0.74) μmol/L, and Ki was 0.72 μmol/L. The internal activity showed that EC50 was 7.3 μmol/L and Emax was 43.3. Conclusion: Curcumin has affinity and intrinsic activity with hPPARγ1, which suggests that curcumin may be a natural ligand of hPPARγ1.