The aim of our study was to determine the PPARγ agonism and hypoglycemic activity of natural phenolics isolated from Paulownia tomentosa and Morus alba. We started with a molecular docking preselection, followed by in vitro 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 in ovo 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.

• Klíčová slova
• PPARγ, diabetes mellitus, hypoglycemic, natural products, plant phenolics,
• MeSH
• fenoly * chemie   farmakologie   izolace a purifikace   MeSH
• hypoglykemika * chemie   farmakologie   izolace a purifikace   MeSH
• kuřecí embryo MeSH
• lidé MeSH
• Morus * chemie   MeSH
• myši MeSH
• PPAR gama * agonisté   metabolismus   genetika   chemie   MeSH
• přenašeč glukosy typ 4 metabolismus   genetika   MeSH
• rostlinné extrakty * chemie   farmakologie   izolace a purifikace   MeSH
• simulace molekulového dockingu MeSH
• zvířata MeSH
• Check Tag
• kuřecí embryo MeSH
• lidé MeSH
• myši MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• fenoly * MeSH
• hypoglykemika * MeSH
• PPAR gama * MeSH
• přenašeč glukosy typ 4 MeSH
• rostlinné extrakty * MeSH

Background: Oxidative stress is a key factor in the pathophysiology of many diseases. This study aimed to verify the antioxidant activity of selected plant phenolics in cell-based assays and determine their direct or indirect effects. Methods: The cellular antioxidant assay (CAA) assay was employed for direct scavenging assays. In the indirect approach, the influence of each test substance on the gene and protein expression and activity of selected antioxidant enzymes was observed. One assay also dealt with activation of the Nrf2-ARE pathway. The overall effect of each compound was measured using a glucose oxidative stress protection assay. Results: Among the test compounds, acteoside showed the highest direct scavenging activity and no effect on the expression of antioxidant enzymes. It increased only the activity of catalase. Diplacone was less active in direct antioxidant assays but positively affected enzyme expression and catalase activity. Morusin showed no antioxidant activity in the CAA assay. Similarly, pomiferin had only mild antioxidant activity and proved rather cytotoxic. Conclusions: Of the four selected phenolics, only acteoside and diplacone demonstrated antioxidant effects in cell-based assays.

• Klíčová slova
• CAA, Nrf2-ARE, antioxidants, catalase, glucose toxicity, plant phenolics, superoxide dismutase,
• MeSH
• antioxidační responzivní elementy MeSH
• antioxidancia chemie   farmakologie   MeSH
• biologické markery MeSH
• exprese genu MeSH
• faktor 2 související s NF-E2 genetika   metabolismus   MeSH
• fenoly chemie   farmakologie   MeSH
• glukosa MeSH
• lidé MeSH
• molekulární struktura MeSH
• oxidační stres MeSH
• protinádorové látky chemie   farmakologie   MeSH
• rostlinné extrakty chemie   farmakologie   MeSH
• superoxiddismutasa 1 genetika   metabolismus   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• antioxidancia MeSH
• biologické markery MeSH
• faktor 2 související s NF-E2 MeSH
• fenoly MeSH
• glukosa MeSH
• NFE2L2 protein, human MeSH Prohlížeč
• protinádorové látky MeSH
• rostlinné extrakty MeSH
• SOD1 protein, human MeSH Prohlížeč
• superoxiddismutasa 1 MeSH