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

Xue-Mei YANG.
Artículo en Zh | WPRIM | ID: wpr-852620

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.
Biblioteca responsable: WPRO