chrysin and quercitrin

Microsomal aromatase enzymes of humans and rats have been used in antiaromatase assays, but enzyme activity is species-specific. The current study extracted hepatic microsomes of Nile tilapia (Oreochromis niloticus) to investigate and compare the antiaromatase activity of chrysin, quercetin, and quercitrin. This activity was evaluated using a dibenzylfluorescein (DBF) assay. Results revealed that the age and body weight of Nile tilapia affected the yield of extracted microsomes. Extraction of hepatic microsomes of Nile tilapia was most effective when using a reaction medium with a pH of 8.0. A DBF assay using Nile tilapia microsomes revealed significant differences in levels of antiaromatase activity for chrysin, quercetin, and quercitrin. Chrysin was the most potent aromatase inhibitor, with an IC50 of 0.25 mg/mL. In addition, chrysin is an aromatase inhibitor that also inhibits the proliferation of cancer cells. Hepatic microsomes of Nile tilapia can be used to investigate and compare the antiaromatase activity of different compounds.

Topics: Animals; Antioxidants; Aromatase Inhibitors; Cell Proliferation; Cichlids; Flavonoids; Hep G2 Cells; Humans; Hydrogen-Ion Concentration; MCF-7 Cells; Microscopy, Electron, Scanning; Microsomes, Liver; Quercetin

Flavonoids are natural phenolic compounds with antioxidant, anti-inflammatory, and antimicrobial capacity. This study aims to investigate the effects of different flavonoids for potential use in periodontal applications.. Cultures of Staphylococcus epidermidis or primary human gingival fibroblasts (HGFs) were treated with different doses of chrysin, diosmetin, galangin, quercitrin, and taxifolin. The effect of these molecules was evaluated on S. epidermidis growth rate and HGF viability, gene expression, collagen production, reactive oxygen species (ROS) levels, wound healing, and production of matrix metalloproteinase (MMP)-1 and tissue inhibitor of MMP-1 (TIMP1).. Among all the screened flavonoids, quercitrin showed the most promising biologic effects, in both HGFs and S. epidermidis. Thus, quercitrin was not toxic for HGFs; increased collagen IIIα1 and decorin levels; downregulated interleukin-6 messenger RNA levels; decreased the expression of profibrotic markers during wound healing; decreased ROS levels in basal and stimulated conditions; and decreased the MMP1/TIMP1 ratio. Quercitrin also decreased the bacterial growth rate.. RESULTS suggest that quercitrin could contribute to protect and recover the integrity of gingival tissues, thus displaying a potential use for periodontal disease treatment or to functionalize dental implant abutments to improve soft tissue integration. Further studies are required to confirm the role of quercitrin in gingival tissues.

Topics: Adult; Anti-Bacterial Agents; Antioxidants; Cell Culture Techniques; Cell Survival; Cells, Cultured; Collagen; Collagen Type III; Decorin; Female; Fibroblasts; Flavonoids; Gingiva; Humans; Interleukin-6; Male; Matrix Metalloproteinase 1; Middle Aged; Quercetin; Reactive Oxygen Species; Staphylococcus epidermidis; Tissue Inhibitor of Metalloproteinase-1; Wound Healing; Young Adult

Flavonoids are natural antioxidants that positively influence bone metabolism. The present study screened among different flavonoids to identify biomolecules for potential use in bone regeneration. For this purpose, we used MC3T3-E1 and RAW264.7 cells to evaluate their effect on cell viability and cell differentiation. First, different doses of chrysin, diosmetin, galangin, quercitrin and taxifolin were analyzed to determine the optimum concentration to induce osteoblast differentiation. After 48h of treatment, doses ≥100μM of diosmetin and galangin and also 500μM taxifolin revealed a toxic effect on cells. The same effect was observed in cells treated with doses ≥100μM of chrysin after 14 days of treatment. However, the safe doses of quercitrin (200 and 500μM) and taxifolin (100 and 200μM) induced bone sialoprotein and osteocalcin mRNA expression. Also higher osteocalcin secreted levels were determined in 100μM taxifolin osteoblast treated samples when compared with the control ones. On the other hand, quercitrin and taxifolin decreased Rankl gene expression in osteoblasts, suggesting an inhibition of osteoclast formation. Indeed, osteoclastogenesis suppression by quercitrin and taxifolin treatment was observed in RAW264.7 cells. Based on these findings, the present study demonstrates that quercitrin and taxifolin promote osteoblast differentiation in MC3T3-E1 cells and also inhibit osteoclastogenesis in RAW264.7 cells, showing a positive effect of these flavonoids on bone metabolism.

Topics: Animals; Biomarkers; Cell Differentiation; Cell Line; Cell Survival; Flavonoids; Gene Expression; Integrin-Binding Sialoprotein; Macrophages; Mice; Osteoblasts; Osteocalcin; Osteoclasts; Osteogenesis; Quercetin