P104 Icariin Attenuates Intestinal Inflammation through Inhibition of the Nuclear Factor-ĸB signaling
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Abstract Background Icariin is a natural flavonoid glucoside from plants in Epimedium family, known to have anti-oxidative and anti-inflammatory activities. This study investigated the effects of Icariin on nuclear factor-kappa B (NF-ĸB) signaling pathway in intestinal epithelial cells (IEC) and macrophages, and in acute and chronic murine colitis models. Methods Human IEC line COLO 205 and murine macrophage cell line RAW 264.7 were pretreated with Icariin and then stimulated with tumor necrosis factor-α (TNF-α) and lipopolysaccharide respectively for in vitro studies. The expression of pro- and anti-inflammatory cytokines were evaluated by real-time RT-PCR (TNF- α, IL-6, IL-8, IL-12, and IL-10), and the effect of Icariin on NF-ĸB signaling pathway was examined by immunoblot analysis to detect IĸBα phosphorylation and degradation. Dextran sulfate sodium (DSS)-induced acute colitis in C57BL/6 wild-type mice and chronic colitis in IL-10-/- mice were treated with or without Icariin for in vivo studies. The severity of colitis was evaluated by daily body weight change, colon length, and colonic tissue histopathology. Results Icariin significantly attenuated the production of pro-inflammatory cytokines and degeneration of anti-inflammatory cytokines, and alleviated IĸBα phosphorylation and degradation in both IEC and murine macrophages stimulated by TNF-α and LPS, respectively. Icariin also significantly reduced the severity of colitis in both DSS-induced acute colitis model and chronic colitis in IL-10-/- mice models. Conclusion Icariin inhibits NF-ĸB signaling in both IECs and macrophages, and attenuates experimental murine colitis. These results suggest that Icariin may be a potential novel therapeutic agent for inflammatory bowel disease.Keywords:
Icariin
Epimedium
Proinflammatory cytokine
IκBα
Epimedium has beneficial effects in nourishing and building up the body and is widely used in practical production of Epimedium preparations. As one of the major active compounds in Epimedium preparations, icariin is be used as a quality control index of industrial manufacture. However, content of icariin was observed to increase to uncertain extent in pharmaceutical production, which might bring difficulties in quality control. The content fluctuation mainly occurred in high-temperature extraction process. The aim of this study is to investigate what happen to flavonol-glycosides in Epimedium under heating treatment. Ultra-Performance Liquid Chromatography-Linear Ion Trap Mass Spectrometer was applied to profile the transformation rule of flavonol-glycosides in Epimedium and search for an explanation for the increase in icariin content under heating treatment. 56 compounds were found to have significantly changed and their structures were identified, among which 15 flavonol-glycosides were proposed to play a role in icariin content variation. Further studies were conducted based on 8 flavonol-glycosides standard substances to obtain more credible data. Finally, Baohuoside II, 2"-o-rhamnosylicariside II, Epimedin A1, Epimedin A, Epimedin B, Epimedin C, Baohuoside I and Anhydroicaritin were found to transform into icariin during the heating process. This study provides an evidence for the quality control study of Epimedium preparation, as well as reference for chemical researches in natural pharmacy.
Icariin
Epimedium
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In this study, epimedins A-, B-, and C-, and icariin-rich extracts were simultaneously isolated from Epimedium brevicornu Maxim. through a convenient four-stage process consisting of solvent extraction, macroporous resin column pre-concentration, extraction fractionation, and reversed-phase (RP) silica gel column chromatography. Single factor experiments and response surface methodology (RSM) were used to optimize the preparation conditions. In the final products, the purities of epimedins A - C and icariin were 23.04%, 64.50%, 54.92%, and 77.54%, respectively, which will lay a foundation for the further purification of epimedin monomers and full utilization of Epimedium resources. Meanwhile, the osteogenic effects of epimedins A - C were investigated for the first time and compared with that of icariin, which will provide guidance for the clinical applications of Epimedium in the treatment of osteoporosis.
Icariin
Epimedium
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Icariin
Epimedium
Berberidaceae
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The mass fraction of icariin from Epimedium koreanum Nakai.in different harvest periods,producing areas and altitudes was determined by using HPLC.There are excellent linear correlation in ranges 0.1～1.4g/L with this quantitative method.The mass fraction of icariin from leaf in different harvest periods is 0.31446%～3.68099%.The mass fraction of icariin of Epimedium koreanum Nakai.in Linjiang was the highest.The highest mass fraction of icarlin is distributed at 629m.The mass fraction distribution of icariin in the same Epimedium koreanum Nakai.is leafpart over groundstem.
Icariin
Epimedium
Fraction (chemistry)
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Objective To determine the content of rouhuoside and icariin in Epimedium wushanense,and compare the content variety of these 2 compounds in different growing seasons.MethodsSamples were dealt with by HPLC with beckmancoulter_(TM)-C_(18) analytical column.The mobile phase was consisted of acetonitrilewater(25: 75).The flow rate was 1.0 ml·min~(-1).The UV detection was set at 270 nm.ResultsThe linear response range from (0.196 42) ～ 1.964 2μg of rouhuoside(r=(0.999) 12,n=10);0.193 35 ～ 1.933 5 μg of icariin(r=0.999 00,n=10).In the whole growing seasons of Epimedium wushanense,the content of icariin is less than 0.5% except for in May,while the content of rouhuoside is more than 1.710%.ConclusionAs far as rouhuoside and icariin to be concerned,the content of rouhuoside is much higher than that of icariin in each month of the growing seasons of Epimedium wushanense,and rouhuoside is the main component in Epimedium wushanense.
Icariin
Epimedium
Content determination
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OBJECTIVE To compare the pharmacokinetics of icariin and icarisideⅡin Wistar rats after administration of icariin monomer and Epimedium flavonoids.METHODS 16 Wistar rats were divided into two groups randomly and received an intragastric administration of 50 mg·kg-1 icariin monomer(5 mL·kg-1) and 0.2 g Epimedium flavonoids(containing 50 mg icariin) kg-1 body weight,respectively.The plasma samples were collected as scheduled,and icariin and icarisideⅡwere analyzed by HPLC-MS/MS.The pharmacokinetic parameters of icariin and icarisideⅡwere calculated and evaluated by non-compartment model.RESULTS The plasma concentration of icariin and icarisideⅡafter administration of icariin monomer were all higher than that after Epimedium flavonoids.The main parameters of icariin after icariin monomer and Epimedium flavonoids were shown as follows:t1/2(3.6±1.1)h and(6.0±3.4)h,tmax(1.0±0.7)h and(1.2±1.1)h,Cmax(21.0±9.1)ng·mL-1and(14.9±4.5)ng·mL-1,AUC0-12(78.5±42.6)ng·mL-1·h and(42.5±13.8)ng·mL-1·h,AUC0-∞(87.0±45.4)ng·mL-1 ·h and(51.2±13.0)ng·mL-1·h.The main parameters of icarisideⅡafter icariin monomer and Epimedium flavonoids were shown as follows: t1/2(3.0±1.4)h and(17.2±10.2)h,tmax(3.9±2.3)h and(0.9±0.5)h,Cmax(20.9±8.6)ng·mL-1 and(5.4±2.4)ng·mL-1,AUC0-12(87.1±24.8)ng·mL-1·h and(18.8±10.2)ng·mL-1·h,AUC0-∞(96.3±22.9)ng·mL-1 ·h and(35.2±8.4)ng·mL-1·h.CONCLUSION The plasma concentration of icariin and icarisideⅡafter administration of icariin monomer were all higher than that after Epimedium flavonoids.Statistical analysis of main pharmacokinetic parameters of icariin showed that AUC0-12 and AUC0-∞ have statistical significance,while all of the main pharmacokinetic parameters of icarisideⅡhave statistical significance.
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Epimedium
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To research on the variation regularity of the five main flavonoids contents in Epimedium and processed Epimedium.The contents of Epimedin A, Epimedin B, Epimedin C, Icariin and Baohuoside I in Epimedium and processed Epimedium were determined, respectively.There were varieties in the contents of Epimedin A, Epimedin B, Epimedin C, Icariin and Baohuoside in Epimedium and processed Epimedium. There were different variety tendencies in different species and different batches.The variety tendencies of the contents of five main flavonoids depend on the processing technology and the flavonoids proportion in Epimedium and processed Epimedium.
Icariin
Epimedium
Berberidaceae
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RP-HPLC Determination of Rouhuoside and Icariin in Herba Epimedii of Different Species and Part Used
Objective: In order to determinate the content of rouhuoside and icariin in Chinese traditional medicine-Herba Epimedii, several samples from different species and their different parts were examined. Methods: Nineteen samples from 3 species and their different parts were dealt with by HPLC with BECKMAN COULTER TMC_(18) analytical column. The mobile phase consisted of acetonitrile-water(25: 75). The flow rate was 1. 0mL·min~(-1). The UV detection was set at 270nm. Results: The linear response range from 0. 19642-1. 9642μg of rouhuoside(r=0. 99912, n=10);0. 19335-1. 9335μg of icariin(r=0. 99900, n=10). The content of rouhuoside is higher than that of icariin in Epimedium wushanense, while the content of rouhuoside is lower than that of icariin in Epimedium brevicornum and Epimedium sagittatum. Conclusion: As far as both the contents of rouhuoside and icariin in Epimedium wushanense to be concerned, it was obviously different in different parts used(leave, root and stem)of one whole plant. Rouhuoside was the main component in Epimedium wushanense, and icariin was the main component in Epimedium brevicornum and Epimedium sagittatum.
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Epimedium
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Icariin
Epimedium
Glucosyltransferases
Berberidaceae
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