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[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(hPPARγ1)的亲和力和内在活性,确定CUR是否为hPPARγ1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hPPARγ1的结合活性和功能活性。结果 CUR与hPPARγ1结合的半数抑制浓度(IC50)为(8.82±0.74)μmol/L,抑制常数(Ki)为0.72 μmol/L;CUR对hPPARγ1的半数有效浓度(EC50)为7.3 μmol/L,最大活性倍数(Emax)为43.3。结论 CUR不仅能与hPPARγ1受体结合,而且能激活hPPARγ1,可能是hPPARγ1的天然配体。
[Key word]
[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.
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[基金项目]
国家自然科学基金资助项目(30572353);重庆市医学科研计划项目(2013-2-116)