论文部分内容阅读
目的测定姜黄素(CUR)与人过氧化物酶体增殖物激活受体γ_1(h PPARγ_1)的亲和力和内在活性,确定CUR是否为h PPARγ_1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 PPARγ_1的结合活性和功能活性。结果 CUR与h PPARγ_1结合的半数抑制浓度(IC_(50))为(8.82±0.74)μmol/L,抑制常数(Ki)为0.72μmol/L;CUR对h PPARγ_1的半数有效浓度(EC_(50))为7.3μmol/L,最大活性倍数(E_(max))为43.3。结论 CUR不仅能与h PPARγ_1受体结合,而且能激活h PPARγ_1,可能是h PPARγ_1的天然配体。
Objective To determine the affinity and intrinsic activity of curcumin against human peroxisome proliferator activated receptor γ_1 (h PPARγ_1) and to determine whether CUR is a natural ligand for h PPARγ_1. Methods The binding activity and functional activity of CUR and hPPARγ_1 were detected by radiolabeled ligand binding assay and transactivation reporter gene respectively. RESULTS: The half inhibitory concentration (IC 50) of CUR and h PPARγ 1 was (8.82 ± 0.74) μmol / L and the inhibition constant (Ki) was 0.72 μmol / ) Was 7.3μmol / L, the maximum activity fold (E max) was 43.3. Conclusion CUR can not only bind to h PPARγ_1 receptor, but also activate h PPARγ_1, which may be a natural ligand of h PPARγ_1.