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鉴定一种具有胰岛素增敏作用的 PPARγ 天然配体的油树脂,该配体来源于饮食诱导肥胖的 C57Bl/6J 小鼠模型,并检测其在. 中的抗氧化活性。

Characterization of an Oleoresin Containing PPARγ Natural Ligands with Insulin-Sensitizing Effects in a C57Bl/6J Mouse Model of Diet-Induced Obesity and Antioxidant Activity in .

机构信息

Postgraduate Department, Faculty of Veterinary Sciences, Universidad Austral de Chile, Valdivia 5110566, Chile.

Center for Aging and Regeneration (CARE), Department of Cellular and Molecular Biology, Faculty of Biological Sciences, Pontificia Universidad Católica de Chile, Santiago 8320000, Chile.

出版信息

Nutrients. 2021 May 27;13(6):1828. doi: 10.3390/nu13061828.

Abstract

The biomedical potential of the edible red seaweed (formerly ) has not been explored. Red seaweeds are enriched in polyunsaturated fatty acids and eicosanoids, which are known natural ligands of the PPARγ nuclear receptor. PPARγ is the molecular target of thiazolidinediones (TZDs), drugs used as insulin sensitizers to treat type 2 diabetes mellitus. Medical use of TZDs is limited due to undesired side effects, a problem that has triggered the search for selective PPARγ modulators (SPPARMs) without the TZD side effects. We produced oleoresin (Gracilex), which induces PPARγ activation without inducing adipocyte differentiation, similar to SPPARMs. In a diet-induced obesity model of male mice, we showed that treatment with Gracilex improves insulin sensitivity by normalizing altered glucose and insulin parameters. Gracilex is enriched in palmitic acid, arachidonic acid, oleic acid, and lipophilic antioxidants such as tocopherols and β-carotene. Accordingly, Gracilex possesses antioxidant activity in vitro and increased antioxidant capacity in vivo in These findings support the idea that Gracilex represents a good source of natural PPARγ ligands and antioxidants with the potential to mitigate metabolic disorders. Thus, its nutraceutical value in humans warrants further investigation.

摘要

(以前)被认为可食用的红海藻的生物医学潜力尚未得到探索。红海藻富含多不饱和脂肪酸和二十烷酸,这些都是众所周知的过氧化物酶体增殖物激活受体γ(PPARγ)核受体的天然配体。PPARγ 是噻唑烷二酮类(TZDs)的分子靶点,TZDs 类药物被用作治疗 2 型糖尿病的胰岛素增敏剂。由于存在不良副作用,TZDs 的医学用途受到限制,这一问题促使人们寻找没有 TZD 副作用的选择性 PPARγ 调节剂(SPPARMs)。我们生产了一种油树脂(Gracilex),它可诱导 PPARγ 激活而不诱导脂肪细胞分化,类似于 SPPARMs。在雄性肥胖症模型中,我们发现 Gracilex 通过使葡萄糖和胰岛素参数正常化来改善胰岛素敏感性。Gracilex 富含棕榈酸、花生四烯酸、油酸和脂溶性抗氧化剂,如生育酚和β-胡萝卜素。因此,Gracilex 在体外具有抗氧化活性,并在体内增加了抗氧化能力。这些发现支持这样一种观点,即 Gracilex 是天然 PPARγ 配体和抗氧化剂的良好来源,具有减轻代谢紊乱的潜力。因此,其在人类中的营养保健品价值值得进一步研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba5a/8227508/92710e2431c7/nutrients-13-01828-g001.jpg

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