Narala Venkata R, Smith Monica R, Adapala Ravi K, Ranga Rajesh, Panati Kalpana, Moore Bethany B, Leff Todd, Reddy Vudem D, Kondapi Anand K, Reddy Raju C
Department of Internal Medicine, Division of Pulmonary and Critical Care Medicine, University of Michigan Medical Center, Ann Arbor, MI 48109.
Gene Ther Mol Biol. 2009 Apr 1;13(1):20-25.
Curcumin, a compound found in the spice turmeric, has been shown to possess a number of beneficial biological activities exerted through a variety of different mechanisms. Some curcumin effects have been reported to involve activation of the nuclear transcription factor peroxisome proliferator-activated receptor-γ (PPAR-γ), but the concept that curcumin might be a PPAR-γ ligand remains controversial. Results reported here demonstrate that, in contrast to the PPAR-γ ligands ciglitazone and rosiglitazone, curcumin is inactive in five different reporter or DNA-binding assays, does not displace [(3)H]rosiglitazone from the PPAR-γ ligand-binding site, and does not induce PPAR-γ-dependent differentiation of preadipocytes, while its ability to inhibit fibroblast-to-myofibroblast differentiation is not affected by any of four PPAR-γ antagonists. These multiple lines of evidence conclusively demonstrate that curcumin is not a PPAR-γ ligand and indicate the need for further investigation of the mechanisms through which the compound acts.
姜黄素是一种存在于香料姜黄中的化合物，已被证明具有多种有益的生物活性，这些活性通过多种不同机制发挥作用。据报道，姜黄素的一些作用涉及核转录因子过氧化物酶体增殖物激活受体-γ（PPAR-γ）的激活，但姜黄素可能是一种PPAR-γ配体这一概念仍存在争议。此处报道的结果表明，与PPAR-γ配体环格列酮和罗格列酮不同，姜黄素在五种不同的报告基因或DNA结合试验中无活性，不能从PPAR-γ配体结合位点取代[³H]罗格列酮，也不能诱导前脂肪细胞的PPAR-γ依赖性分化，而其抑制成纤维细胞向肌成纤维细胞分化的能力不受四种PPAR-γ拮抗剂中任何一种的影响。这些多方面的证据确凿地证明姜黄素不是PPAR-γ配体，并表明需要进一步研究该化合物发挥作用的机制。
