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Curcumin is not a ligand for peroxisomeproliferator-activated receptor-γ Research Article

机译:姜黄素不是过氧化物酶体增殖物激活受体γ的配体-研究文章

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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 [3H]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.
机译:姜黄素是香料姜黄中的一种化合物,已显示具有通过多种不同机制发挥的许多有益生物活性。据报道,姜黄素的某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,但是姜黄素可能是PPAR-γ配体的概念仍存在争议。此处报道的结果表明,与PPAR-γ配体西格列酮和罗格列酮相比,姜黄素在五种不同的报道分子或DNA结合试验中均无活性,不会从PPAR-γ配体结合位点置换[3H] rosiglitazone,并且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成肌纤维细胞分化的能力不受任何四种PPAR-γ拮抗剂的影响。这些多方面的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理。

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