Most cited article - PubMed ID 20877208
Antiradical and cytoprotective activities of several C-geranyl-substituted flavanones from Paulownia tomentosa fruit
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.
- Keywords
- PPARγ, diabetes mellitus, hypoglycemic, natural products, plant phenolics,
- MeSH
- Phenols * chemistry pharmacology isolation & purification MeSH
- Hypoglycemic Agents * chemistry pharmacology isolation & purification MeSH
- Chick Embryo MeSH
- Humans MeSH
- Morus * chemistry MeSH
- Mice MeSH
- PPAR gamma * agonists metabolism genetics chemistry MeSH
- Glucose Transporter Type 4 metabolism genetics MeSH
- Plant Extracts * chemistry pharmacology isolation & purification MeSH
- Molecular Docking Simulation MeSH
- Animals MeSH
- Check Tag
- Chick Embryo MeSH
- Humans MeSH
- Mice MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Names of Substances
- Phenols * MeSH
- Hypoglycemic Agents * MeSH
- PPAR gamma * MeSH
- Glucose Transporter Type 4 MeSH
- Plant Extracts * MeSH
The review presents prenylated flavonoids as potential therapeutic agents for the treatment of topical skin infections and wounds, as they can restore the balance in the wound microenvironment. A thorough two-stage search of scientific papers published between 2000 and 2022 was conducted, with independent assessment of results by two reviewers. The main criteria were an MIC (minimum inhibitory concentration) of up to 32 µg/mL, a microdilution/macrodilution broth method according to CLSI (Clinical and Laboratory Standards Institute) or EUCAST (European Committee on Antimicrobial Susceptibility Testing), pathogens responsible for skin infections, and additional antioxidant, anti-inflammatory, and low cytotoxic effects. A total of 127 structurally diverse flavonoids showed promising antimicrobial activity against pathogens affecting wound healing, predominantly Staphylococcus aureus strains, but only artocarpin, diplacone, isobavachalcone, licochalcone A, sophoraflavanone G, and xanthohumol showed multiple activity, including antimicrobial, antioxidant, and anti-inflammatory along with low cytotoxicity important for wound healing. Although prenylated flavonoids appear to be promising in wound therapy of humans, and also animals, their activity was measured only in vitro and in vivo. Future studies are, therefore, needed to establish rational dosing according to MIC and MBC (minimum bactericidal concentration) values, test potential toxicity to human cells, measure healing kinetics, and consider formulation in smart drug release systems and/or delivery technologies to increase their bioavailability.
- Keywords
- MRSA, S. aureus, anti-inflammatory, antibacterial, antioxidant, cytotoxicity, mastitis, nanotechnology, prenylated flavonoids, skin, wound healing,
- MeSH
- Anti-Bacterial Agents pharmacology MeSH
- Anti-Infective Agents * pharmacology MeSH
- Antioxidants * pharmacology MeSH
- Flavonoids pharmacology MeSH
- Wound Healing MeSH
- Humans MeSH
- Microbial Sensitivity Tests MeSH
- Animals MeSH
- Check Tag
- Humans MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Review MeSH
- Names of Substances
- Anti-Bacterial Agents MeSH
- Anti-Infective Agents * MeSH
- Antioxidants * MeSH
- Flavonoids 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.
- Keywords
- CAA, Nrf2-ARE, antioxidants, catalase, glucose toxicity, plant phenolics, superoxide dismutase,
- MeSH
- Antioxidant Response Elements MeSH
- Antioxidants chemistry pharmacology MeSH
- Biomarkers MeSH
- Gene Expression MeSH
- NF-E2-Related Factor 2 genetics metabolism MeSH
- Phenols chemistry pharmacology MeSH
- Glucose MeSH
- Humans MeSH
- Molecular Structure MeSH
- Oxidative Stress MeSH
- Antineoplastic Agents chemistry pharmacology MeSH
- Plant Extracts chemistry pharmacology MeSH
- Superoxide Dismutase-1 genetics metabolism MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Names of Substances
- Antioxidants MeSH
- Biomarkers MeSH
- NF-E2-Related Factor 2 MeSH
- Phenols MeSH
- Glucose MeSH
- NFE2L2 protein, human MeSH Browser
- Antineoplastic Agents MeSH
- Plant Extracts MeSH
- SOD1 protein, human MeSH Browser
- Superoxide Dismutase-1 MeSH
Paulownia tomentosa, a member of the plant family Paulowniaceae and a rich source of biologically active secondary metabolites, is traditionally used in Chinese herbal medicine. Flavonoids, lignans, phenolic glycosides, quinones, terpenoids, glycerides, phenolic acids, and miscellaneous other compounds have been isolated from different parts of P. tomentosa plant. Recent interest in this species has focused on isolating and identifying of prenylated flavonoids, that exhibit potent antioxidant, antibacterial, and antiphlogistic activities and inhibit severe acute respiratory syndrome coronavirus papain-like protease. They show cytotoxic activity against various human cancer cell lines and inhibit the effects of human cholinesterase, butyrylcholinesterase, and bacterial neuraminidases. Most of the compounds considered here have never been isolated from any other species of plant. This review summarizes the information about the isolated compounds that are active, their bioactivities, and the structure-activity relationships that have been worked out for them.
- Keywords
- Bignonia tomentosa, Flavonoid, Lignan, Paulownia tomentosa, Paulowniaceae, Phenolic glycosides,
- Publication type
- Journal Article MeSH
- Review MeSH
The aim of this study was to describe behaviour, kinetics, time courses and limitations of the six different fully automated spectrometric methods--DPPH, TEAC, FRAP, DMPD, Free Radicals and Blue CrO5. Absorption curves were measured and absorbance maxima were found. All methods were calibrated using the standard compounds Trolox® and/or gallic acid. Calibration curves were determined (relative standard deviation was within the range from 1.5 to 2.5%). The obtained characteristics were compared and discussed. Moreover, the data obtained were applied to optimize and to automate all mentioned protocols. Automatic analyzer allowed us to analyse simultaneously larger set of samples, to decrease the measurement time, to eliminate the errors and to provide data of higher quality in comparison to manual analysis. The total time of analysis for one sample was decreased to 10 min for all six methods. In contrary, the total time of manual spectrometric determination was approximately 120 min. The obtained data provided good correlations between studied methods (R=0.97-0.99).
- MeSH
- Antioxidants analysis MeSH
- Time Factors MeSH
- Chromans analysis MeSH
- Gallic Acid analysis MeSH
- Automation, Laboratory instrumentation methods standards MeSH
- Reference Standards MeSH
- Spectrum Analysis instrumentation methods standards MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- 6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid MeSH Browser
- Antioxidants MeSH
- Chromans MeSH
- Gallic Acid MeSH