baohuoside-i and icaritin

This study aimed to identify the osteogenesis effect of icariside II (ICSII) and icaritin (ICT) in vitro. Bone marrow mesenchymal stem cells (BMSCs) were treated with ICSII and ICT in order to detect the proliferation and differentiation of BMSCs, the expression of the osteogenesis-related proteins with or without osteogenic medium (OM) and genes, Runt-related transcription factor 2 (Runx-2), osteocalcin (OCN), osteopontin (OPN), osterix, and basic fibroblast growth factor (bFGF), and the phosphorylation levels of mitogen-activated protein kinase (MAPK). We found that the optical density increased and alkaline phosphatase decreased after the BMSCs were treated with different concentrations of ICSII; however, ICT showed an opposing effect. The formation of calcium nodules was observed after the BMSCs were treated with ICSII and ICT. The expression level of osteogenesis-related proteins was enhanced following treatment with both ICSII or ICT, while the expression level of the osteogenesis-related genes Runx-2, OCN, OPN, osterix, and bFGF significantly increased with ICSII treatment (P < 0.05), and only Runx-2 and bFGF significantly increased (P < 0.01) with ICT. The expression of osteogenic differentiation-related proteins (except OPN) following treatment with ICSII + OM or ICT + OM was not notably increased. Both ICSII and ICT elevated the phosphorylation levels of MAPK/ERK, which was attenuated by GDC-0994 (an inhibitor of MAPK/ERK). Collectively, these data indicate that ICSII and ICT facilitate orientation osteogenic differentiation of BMSCs, which is most likely via the MAPK/ERK pathway. OM did not synergistically enhance the osteogenesis effect of ICSII and ICT.

Topics: Animals; Calcium; Cell Differentiation; Cell Proliferation; Cell Shape; Cells, Cultured; Dogs; Flavonoids; Gene Expression Regulation; MAP Kinase Signaling System; Mesenchymal Stem Cells; Osteogenesis

Topics: Antineoplastic Agents; Apoptosis; ATP Binding Cassette Transporter, Subfamily B; Cell Line, Tumor; Cell Survival; Dose-Response Relationship, Drug; Doxorubicin; Drug Resistance, Multiple; Drug Resistance, Neoplasm; Flavonoids; Gene Expression Regulation, Neoplastic; Humans; Multidrug Resistance-Associated Proteins; Osteosarcoma; Phosphorylation; Rhodamine 123; STAT3 Transcription Factor; Triterpenes

Increasing evidence shows the therapeutic superiority of herbal extracts in comparison to isolated single constituents. One of the reasons may be attributed to the synergy effect of compound combinations. Flavonoids from Herba Epimedii have been shown to have therapeutic effect against bone loss. Our previous study showed that Icariside II inhibited pre-osteoclast RAW264.7 growth. The aim of this study was to investigate whether the activity of Icariside II is synergized by other components of Herba Epimedii. The inhibitory activity of Icariside II was significantly enhanced in the presence of the extract of Herba Epimedii (EHE) at the ratio of 1:1, 1:5 and 1:10. Icaritin, another flavonoid constituent, was shown here to inhibit RAW264.7 growth in a dose-dependent manner. Further, we found that Icariside II, together with Icaritin, synergistically inhibited RAW264.7 growth. The synergistic effect is significant when the ratio of Icariside II and Icaritin was 10:1, 5:1, 1:1, 1:2, and 1:5, respectively. In conclusion, Icaritin were an active component. The inhibitory activity of Icariside II on pre-osteoclast RAW264.7 growth was synergized by Icaritin, which maybe contribute to the efficiency of Herba Epimedii extract on curing bone-related diseases, such as osteoporosis.

Topics: Animals; Cell Line; Cell Proliferation; Drug Synergism; Epimedium; Flavonoids; Mice; Osteoclasts; Plant Extracts

Three kinds of prenylated flavonols, icariside I, icariside II, and icaritin, were isolated from an icariin hydrolysate and their effects on melanogenesis evaluated based on mushroom tyrosinase inhibition and quantifying the melanin contents in melanocytes. Although none of the compounds had an effect on tyrosinase activity, icariside II and icaritin both effectively inhibited the melanin contents with an IC50 of 10.53 and 11.13 MM, respectively. Whereas icariside II was obtained from a reaction with beta-glucosidase and cellulase, the icariin was not completely converted into icariside II. Thus, for the high-purity production of icariside II, the reaction was optimized using the response surface methodology, where an enzyme concentration of 5.0 mg/ml, pH 7, 37.5 degrees C;, and 8 h reaction time were selected as the central conditions for the central composite design (CCD) for the enzymatic hydrolysis of icariin into icariside II using cellulase. Empirical models were developed to describe the relationships between the operating factors and the response (icariside II yield). A statistical analysis indicated that all four factors had a significant effect (p<0.01) on the icariside II production. The coefficient of determination (R2) was good for the model (0.9853), and the optimum production conditions for icariside II was an enzyme concentration of 7.5 mg/ml, pH 5, 50 degrees C, and 12 h reaction time. A good agreement between the predicted and experimental data under the designed optimal conditions confirmed the usefulness of the model. A laboratory pilot scale was also successful.

Topics: Animals; Biotechnology; Cell Line, Tumor; Chromatography, High Pressure Liquid; Epimedium; Flavones; Flavonoids; Hydrogen-Ion Concentration; Hydrolysis; Mass Spectrometry; Melanins; Melanocytes; Mice; Mice, Inbred C57BL; Monophenol Monooxygenase; Umbelliferones