Most cited article - PubMed ID 20653997
Effect of diplacone on LPS-induced inflammatory gene expression in macrophages
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
This study was done to identify the content compounds of Achillea wilhelmsii (A. wilhelmsii) and to evaluate its hypoglycemic and anti-hypercholesterolemic activity and effect on inflammatory mediators. The extracts and fractions of A. wilhelmsii were thoroughly analyzed using high performance liquid chromatography (HPLC), and the total content of phenols and flavonoids was determined. The hypoglycemic activity was evaluated in vivo using alloxan-induced diabetic mice. The effect upon inflammatory mediators was evaluated in vitro using the human monocytic leukemia cell line (THP-1). The anti-hypercholesterolemic activity was evaluated in vitro using the 3-hydroxy-3-methylglutaryl-CoA (HMG-CoA) reductase assay kit. The water extract (WE)-treated group showed the highest reduction in the fasting blood glucose levels (FBGL). The chloroform fraction (CF) and ethyl acetate fraction (EAF) both showed a significant ability to reduce the secretion of tumor necrosis factor alpha (TNF-α). The EAF, however, also attenuated the levels of matrix metalloproteinase-2 (MMP-2) and matrix metalloproteinase-9 (MMP-9). The CF showed the most significant 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) inhibition activity. The five main compounds in the CF were isolated and identified. Out of the five compounds in the CF, 1β,10β-epoxydesacetoxymatricarin (CP1) and leucodin (CP2) showed the highest anti-hypercholesterolemic potential. A molecular docking study provided corresponding results.
- Keywords
- 3-hydroxy-3-methylglutaryl-CoA reductase, Achillea wilhelmsii, anti-hypercholesterolemic, cardiometabolic disease, docking, flavonoids, hypoglycemic, inflammation,
- MeSH
- Acyl Coenzyme A chemistry MeSH
- Antioxidants administration & dosage chemistry MeSH
- Cell Line MeSH
- Diabetes Mellitus, Experimental drug therapy MeSH
- Phenols administration & dosage chemistry isolation & purification MeSH
- Flavonoids administration & dosage chemistry isolation & purification MeSH
- Hypercholesterolemia drug therapy MeSH
- Hyperglycemia drug therapy MeSH
- Humans MeSH
- Inflammation Mediators chemistry MeSH
- Mice, Inbred NOD MeSH
- Mice MeSH
- Achillea chemistry MeSH
- Risk Factors MeSH
- Plant Extracts administration & dosage chemistry MeSH
- Molecular Docking Simulation MeSH
- Chromatography, High Pressure Liquid MeSH
- Inflammation drug therapy MeSH
- Animals MeSH
- Check Tag
- Humans MeSH
- Mice MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- 3-hydroxy-3-methylglutaryl-coenzyme A MeSH Browser
- Acyl Coenzyme A MeSH
- Antioxidants MeSH
- Phenols MeSH
- Flavonoids MeSH
- Inflammation Mediators MeSH
- Plant Extracts 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