Treml Jakub, Václavík Jiří, Molčanová Lenka, Čulenová Marie, Hummelbrunner Scarlet, Neuhauser Cathrina, Dirsch Verena M, Weghuber Julian, Šmejkal Karel
Department of Molecular Pharmacy, Masaryk University, 612 00 Brno, Czech Republic.
Department of Natural Drugs, Masaryk University, 612 00 Brno, Czech Republic.
J Agric Food Chem. 2025 Jun 4;73(22):13960-13972. doi: 10.1021/acs.jafc.4c11398. Epub 2025 May 20.
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.
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。
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