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从[具体来源1]和[具体来源2]中鉴定植物酚类物质作为新型过氧化物酶体增殖物激活受体γ(PPARγ)部分激动剂和降血糖剂。

Identification of Plant Phenolics from and as Novel PPARγ Partial Agonists and Hypoglycemic Agents.

作者信息

Treml Jakub, Václavík Jiří, Molčanová Lenka, Čulenová Marie, Hummelbrunner Scarlet, Neuhauser Cathrina, Dirsch Verena M, Weghuber Julian, Šmejkal Karel

机构信息

Department of Molecular Pharmacy, Masaryk University, 612 00 Brno, Czech Republic.

Department of Natural Drugs, Masaryk University, 612 00 Brno, Czech Republic.

出版信息

J Agric Food Chem. 2025 Jun 4;73(22):13960-13972. doi: 10.1021/acs.jafc.4c11398. Epub 2025 May 20.


DOI:10.1021/acs.jafc.4c11398
PMID:40392982
Abstract

The aim of our study was to determine the PPARγ agonism and hypoglycemic activity of natural phenolics isolated from and . We started with a molecular docking preselection, followed by cell culture assays, such as PPARγ luciferase reporter gene assay and PPARγ protein expression by Western blot analysis. The ability of the selected compounds to induce GLUT4 translocation in cell culture and lower blood glucose levels in chicken embryos was also determined. Among the thirty-six plant phenolic compounds, moracin M showed the highest hypoglycemic effect in an experiment (7.33 ± 2.37%), followed by mulberrofuran Y (3.84 ± 1.34%) and diplacone (3.69 ± 1.37%). Neither moracin M nor mulberrofuran Y showed a clear effect on the enhancement of GLUT4 translocation or agonism on PPARγ, while diplacone succeeded in both (3.62 ± 0.16% and 2.4-fold ± 0.2, respectively). Thus, we believe that the compounds moracin M, mulberrofuran Y, and diplacone are suitable for further experiments to elucidate their mechanisms of action.

摘要

我们研究的目的是确定从[具体植物1]和[具体植物2]中分离出的天然酚类化合物的过氧化物酶体增殖物激活受体γ(PPARγ)激动活性和降血糖活性。我们首先进行了分子对接预选,随后进行了细胞培养实验,如PPARγ荧光素酶报告基因实验以及通过蛋白质免疫印迹分析检测PPARγ蛋白表达。还测定了所选化合物在细胞培养中诱导葡萄糖转运蛋白4(GLUT4)转位以及降低鸡胚血糖水平的能力。在36种植物酚类化合物中,桑辛素M在鸡胚实验中显示出最高的降血糖效果(7.33±2.37%),其次是桑呋喃Y(3.84±1.34%)和双苯吡酮(3.69±1.37%)。桑辛素M和桑呋喃Y对增强GLUT4转位或对PPARγ的激动作用均未显示出明显效果,而双苯吡酮在这两方面均取得成功(分别为3.62±0.16%和2.4倍±0.2)。因此,我们认为桑辛素M、桑呋喃Y和双苯吡酮这些化合物适合进一步实验以阐明其作用机制。

相似文献

[1]
Identification of Plant Phenolics from and as Novel PPARγ Partial Agonists and Hypoglycemic Agents.

J Agric Food Chem. 2025-6-4

[2]
In vivo hypoglycemic effects of phenolics from the root bark of Morus alba.

Fitoterapia. 2009-6-21

[3]
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[4]
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[5]
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J Agric Food Chem. 2018-7-17

[6]
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[7]
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[8]
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[9]
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Eur J Pharmacol. 2014-12-15

[10]
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本文引用的文献

[1]
Moracin E and M isolated from Morus alba Linné induced the skeletal muscle cell proliferation via PI3K-Akt-mTOR signaling pathway.

Sci Rep. 2023-11-23

[2]
Management of Hyperglycemia in Type 2 Diabetes, 2022. A Consensus Report by the American Diabetes Association (ADA) and the European Association for the Study of Diabetes (EASD).

Diabetes Care. 2022-11-1

[3]
C-geranylated flavonoids from Paulownia tomentosa Steud. fruit as potential anti-inflammatory agents.

J Ethnopharmacol. 2022-10-5

[4]
Anti-Hyperglycemic Effects of Oils and Extracts Derived from Sea Buckthorn - A Comprehensive Analysis Utilizing In Vitro and In Vivo Models.

Mol Nutr Food Res. 2022-6

[5]
Inhibition Mechanism of Components Isolated from Branches on Diabetes and Diabetic Complications via Experimental and Molecular Docking Analyses.

Antioxidants (Basel). 2022-2-14

[6]
Phenolic Bioactives From Plant-Based Foods for Glycemic Control.

Front Endocrinol (Lausanne). 2021

[7]
Fluorescence microscopy-based quantitation of GLUT4 translocation.

Methods Appl Fluoresc. 2022-1-21

[8]
Avens Root ( L.) Extract Discovered by Target-Based Screening Exhibits Antidiabetic Activity in the Hen's Egg Test Model and .

Front Pharmacol. 2021-12-15

[9]
Moracin D induces apoptosis in prostate cancer cells via activation of PPAR gamma/PKC delta and inhibition of PKC alpha.

Phytother Res. 2021-12

[10]
Antidiabetic potential of dietary polyphenols: A mechanistic review.

Food Res Int. 2021-7

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