【摘要】 目的测定姜黄素（CUR）与人过氧化物酶体增殖物激活受体γ₁（h PPARγ₁）的亲和力和内在活性,确定CUR是否为h PPARγ₁的天然配体。方法通过放射性标记配基竞争结合实验和反式激活报告基因分别检测CUR与h PPARγ₁的结合活性和功能活性。结果 CUR与h PPARγ₁结合的半数抑制浓度(IC₅₀)为（8.82±0.74）μmol/L,抑制常数（Ki）为0.72μmol/L;CUR对h PPARγ₁的半数有效浓度(EC₅₀)为7.3μmol/L,最大活性倍数(E_max)为43.3。结论 CUR不仅能与h PPARγ₁受体结合,而且能激活h PPARγ₁,可能是h PPARγ₁的天然配体。更多还原

【Abstract】 Objective To determine whether curcumin is a natural ligand for human peroxisome proliferators-activated receptors γ1(h PPARγ1) 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 h PPARγ1 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 h PPARγ1, which suggests that curcumin may be a natural ligand of h PPARγ1.更多还原