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从[植物名称未给出]叶片中分离出的内生真菌的代谢产物具有抗氧化活性以及对过氧化物酶体增殖物激活受体α、β/δ和γ的激动剂活性。

Metabolites of endophytic fungi isolated from leaves of exhibit antioxidant activity and agonist activity on peroxisome proliferator-activated receptors α, β/δ and γ.

作者信息

Mesquita Pedro Góes, de Araujo Laiza Magalhaes, Neves Francisco de Assis Rocha, Borin Maria de Fátima

机构信息

Laboratory of Molecular Pharmacology, Department of Pharmacy, Faculty of Sciences Health, University of Brasilia, Brasilia, Brazil.

出版信息

Front Fungal Biol. 2022 Dec 8;3:1049690. doi: 10.3389/ffunb.2022.1049690. eCollection 2022.

Abstract

is a metabolic disorder that affects millions of people worldwide and is linked to oxidative stress and inflammation. Thiazolidinediones (TZD) improve insulin sensitization and glucose homeostasis mediated by the activation of peroxisome proliferator-activated receptors γ (PPARγ) in patients with type 2 diabetes. However, their use is associated with severe adverse effects such as loss of bone mass, retention of body fluids, liver and heart problems, and increased risk of bladder cancer. Partial PPARγ agonists can promote the beneficial effects of thiazolidinediones with fewer adverse effects. Endophytic fungi colonize plant tissues and have a particularly active metabolism caused by the interaction with them, which leads to the production of natural products with significant biological effects that may be like that of the colonized plant. Here, we identify seven endophytic fungi isolated from leaves that have antioxidant activities. Also, one of the extracts presented pan-agonist activity on PPAR, and another showed activity in PPARα and PPARβ/δ. A better understanding of this relationship could help to comprehend the mechanism of action of antioxidants in treating diabetes and its complications. Moreover, compounds with these capabilities to reduce oxidative stress and activate the receptor that promotes glucose homeostasis are promising candidates in treatment of diabetes.

摘要

是一种影响全球数百万人的代谢紊乱疾病,与氧化应激和炎症有关。噻唑烷二酮类药物(TZD)可改善2型糖尿病患者因过氧化物酶体增殖物激活受体γ(PPARγ)激活介导的胰岛素敏感性和葡萄糖稳态。然而,它们的使用与严重的不良反应有关,如骨质流失、体液潴留、肝脏和心脏问题以及膀胱癌风险增加。部分PPARγ激动剂可以在产生较少不良反应的情况下促进噻唑烷二酮类药物的有益作用。内生真菌定殖于植物组织中,并因其与植物的相互作用而具有特别活跃的代谢,这导致产生具有显著生物学效应的天然产物,这些效应可能与被定殖植物的效应相似。在此,我们鉴定了从叶片中分离出的七种具有抗氧化活性的内生真菌。此外,其中一种提取物对PPAR具有泛激动剂活性,另一种在PPARα和PPARβ/δ中显示出活性。更好地理解这种关系有助于理解抗氧化剂在治疗糖尿病及其并发症中的作用机制。此外,具有这些降低氧化应激和激活促进葡萄糖稳态受体能力的化合物是治疗糖尿病的有前途的候选药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8166/10512301/942e0c73db5c/ffunb-03-1049690-g001.jpg

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