Curcumin is not a ligand for peroxisome proliferator-activated receptor-γ
Curcumin is not a ligand for peroxisome proliferator-activated receptor-γ
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发表时间：
2009-04
影响因子：
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通讯作者：
V. Narala;Monica R. Smith;R. K. Adapala;Rajesh Ranga;K. Panati;B. Moore;T. Leff;V. D. Reddy;A. K. Kondapi;Raju C Reddy
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作者：
V. Narala;Monica R. Smith;R. K. Adapala;Rajesh Ranga;K. Panati;B. Moore;T. Leff;V. D. Reddy;A. K. Kondapi;Raju C Reddy
姜黄素是在香料姜黄中发现的一种化合物，已被证明具有通过各种不同机制发挥的许多有益的生物活性。一些姜黄素的作用已被报道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PPAR-γ配体的概念仍然存在争议。本文报道的结果表明，与PPAR-γ配体环格列酮和罗格列酮相比，姜黄素在5种不同的报告基因或DNA结合试验中无活性，不会从PPAR-γ配体结合位点取代[（3）H]罗格列酮，也不会诱导前脂肪细胞的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4种PPAR-γ拮抗剂中任何一种的影响。这些多条证据最终证明姜黄素不是PPAR-γ配体，并表明需要进一步研究该化合物的作用机制。
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.