epimedin-c and icariin

Topics: alpha-Glucosidases; Diabetes Mellitus, Type 2; Drugs, Chinese Herbal; Ferric Compounds; Flavonoids; Glycoside Hydrolase Inhibitors; Humans; Ligands; Magnetic Iron Oxide Nanoparticles; Tandem Mass Spectrometry

Bone nonunion remains a challenge during the treatment of bone defect accompanied with infection. Epimedii herba is a widely used medicine in clinic to enhance bone healing. Epimedin C and icariin are the major flavonoid glycosides from Epimedii herba. Although the effects of these compounds have been reported, their different absorption and utilisation by osteoblasts remain unclear. In the present study, lipopolysaccharide (LPS)-induced osteoblast was adopted as the model cell to evaluate the effects of epimedin C and icariin. The intracellular and extracellular drug concentrations within 24 h were assayed by pipette tip solid-phase extraction and high-performance liquid chromatography, respectively. MTT, alkaline phosphatase (ALP) and calcified nodule staining were performed to identify and evaluate the effects of epimedin C and icariin on LPS-induced osteoblasts. The regulatory roles of epimedin C and icariin in the bone morphogenetic protein-2 (BMP-2)/Runt-related transcription factor 2 (Runx2) signalling pathway were investigated. The results revealed that epimedin C and icariin were not efficiently absorbed by LPS-induced osteoblasts. Nevertheless, they still had high utilisation efficiency after entering the cells. ALP activity, mineralisation and osteoblasts proliferation were enhanced by a high concentration of epimedin C and icariin. The suppressed expression of BMP-2 and Runx2 in LPS-induced osteoblasts was up-regulated significantly after treatment with epimedin C and icariin. These findings firstly illustrated the behavior of epimedin C and icariin from Epimedii herba on LPS-induced osteoblasts and the regulatory property on the expression of key genes and proteins of the BMP-2/Runx2 signalling pathway, which might be helpful for better understanding flavonoids' mechanism to enhance bone repair and improving their future application.

Topics: Animals; Bone Morphogenetic Protein 2; Core Binding Factor Alpha 1 Subunit; Flavonoids; Lipopolysaccharides; Male; Osteoblasts; Rats, Sprague-Dawley; RNA, Messenger; Signal Transduction

A novel icariin type flavonoid glycoside with a malonaldehydic acid intramolecular ester and two known flavonoid glycosides were isolated from

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Drug Evaluation, Preclinical; Epimedium; Flavonoids; Lipopolysaccharides; Mice; Molecular Structure; RAW 264.7 Cells; Tumor Necrosis Factor-alpha

Herba Epimedii is a traditional Chinese herbal medicine that contains a mixture of bioactive flavonoid glycosides. Among them, icariin has the most outstanding bioactive functions, while epimedin C exhibits substantial toxicity. A recombinant α-L-rhamnosidase (

Topics: Aspergillus nidulans; Chromatography, High Pressure Liquid; Drugs, Chinese Herbal; Flavonoids; Glycoside Hydrolases

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.

Topics: 3T3 Cells; Animals; Cell Differentiation; Dose-Response Relationship, Drug; Epimedium; Flavonoids; Mice; Molecular Conformation; Osteogenesis; Plant Extracts; Structure-Activity Relationship

Topics: Amino Acid Sequence; Bacteroides Infections; Bacteroides thetaiotaomicron; Flavonoids; Glycoside Hydrolases; Glycosides; Hesperidin; Hydrolysis; Rutin; Substrate Specificity

The therapeutic properties of

Topics: alpha-Glucosidases; Diabetes Mellitus, Type 2; Enzyme Inhibitors; Epimedium; Flavonoids; Glycoside Hydrolase Inhibitors; Hypoglycemic Agents; Molecular Docking Simulation; Plant Extracts; Protein Tyrosine Phosphatase, Non-Receptor Type 1

To study the metabolic products of main compounds of Chuankezhi injection in rat, 12 Sprague\ Dawley rats were classed into 2 groups, a blank control group and an intermuscular administration group,\ respectively. Rat feces and urine samples were collected from 0−24 h and 24−48 h after administration. All\ the samples were ultrasonically treated with methanol and then analyzed using LC-LTQ Orbitrap MSn. By\ comparison with the total ion chromatogram of samples from the blank control group, the metabolites in the\ samples of drug-treated group were screened. These metabolites were further analyzed by multistage product\ ion scanning and comparison of retention time with reference substances. As a result, a total of 12 flavonoid\ metabolites were tentatively identified from the rat feces and no metabolite was discovered in the rat urine.\ Epimedin C and icariin were detected in the rat blood samples after 30 min of administration, but their\ metabolites and other original flavones were not detected. Furthermore, no original flavones and their\ metabolites were detected in rat blood samples after 2 and 4 h of administration. The potential metabolism\ paths were further characterized and the principal in vivo transformation of flavones from Chuankezhi injection\ were deglycosylation, dehydration, methylation, oxidation and isomerization in rats.

Topics: Administration, Oral; Animals; Chromatography, High Pressure Liquid; Drugs, Chinese Herbal; Feces; Flavones; Flavonoids; Injections; Rats; Rats, Sprague-Dawley; Urine

In this work, near infrared (NIR) spectroscopy was used in combination with chemometrics to determine the epimedin A, epimedin B, epimedin C, icariin, and moisture contents of Herba Epimedii. The variable selection method genetic algorithm (GA) and regression tool support vector machine (SVM) were used to improve the model performance. Four different calibration models, namely Full-PLS, GA-PLS, Full-SVM, and GA-SVM, were established, and their performances in terms of prediction accuracy and model robustness were systemically studied and compared. In conclusion, the performances of the models based on the efficient variables selected through GA were better than those based on full spectra, and the nonlinear models were superior over the linear models. In addition, the GA-SVM model demonstrated the optimal performance in predicting five quality parameters (viz. epimedin A, epimedin B, epimedin C, icariin, and moisture). For GA-SVM, the determination coefficient (R

Topics: Calibration; Chromatography, High Pressure Liquid; Drugs, Chinese Herbal; Flavonoids; Humidity; Least-Squares Analysis; Multivariate Analysis; Nonlinear Dynamics; Reference Standards; Solutions; Spectroscopy, Near-Infrared

To study pharmacokinetic characteristics of epimedin A, B, C and icariin after intermuscular administration of Chuankezhi injection to rat. The established RRLC-MS/MS method was applied for simultaneous determination of four analytes in rat plasma and calculating their pharmacokinetic parameters. As a result, each analyte showed a good linear relationship in the concentration range of 1-1 000 μg•L⁻¹.The intra-day precise was 96.9%-107.5% with RSD<5.99%, inter-day precise was 92.3%-105.0% with RSD<10.16%. The relative recovery of four analytes was 88.1%-101.1% with RSD<7.9% and their absolute recovery was 72.0%-86.6% with RSD<6.3%. After intermuscular administration of Chuankezhi injection, the plasma concentration of four flavonoid glycosides rapidly arose to peaks at about 10 min, and then quickly declined in rat. Tmax of epimedin A, B, C and icariin was 0.21, 0.19, 0.16 and 0.49 h, respectively, and their mean elimination half-life(t1/2z) was 0.60, 0.62, 0.47 and 0.49 h. The established method was validated to be sensitive, rapid and specific for determination of the four analytes. Serum concentration of 4 species of epimedium flavonoids in Chuankezhi injection was low, and their absorption and elimination seem quickly, displaying similar pharmacokinetic characteristics in this study.

Topics: Animals; Drugs, Chinese Herbal; Epimedium; Flavonoids; Injections; Male; Rats; Rats, Sprague-Dawley; Tandem Mass Spectrometry

The genus Epimedium is rich in terms of flavonoids, of which icariin, epimedin A, epimedin B and epimedin C are known especially to be biologically active. Therefore, it is important to quantify these compounds. In this study, a HPLC method coupled with DAD detection was developed and validated for the determination of icariin, epimedin A, epimedin B and epimedin C in Epimedium species growing in Turkey. The chromatographic separation was performed using a gradient system with a mobile phase of 0.1% formic acid (A) and acetonitrile (B) applied at a flow rate of 1 mL/min using.a diode array detector. The highest values were, respectively, icariin 0.65%, epimedin A 0.13%, epimedin B 0.11%, epimedin C 0.06%. The highest values were obtained from the materials collected in Uzungol (Trabzon-Turkey).

Topics: Chromatography, High Pressure Liquid; Epimedium; Flavonoids; Turkey

An efficient, feasible enrichment and separation method of epimedins A, B, C and icariin from Herba Epimedii was developed by the combination of microwave-assisted extraction, macroporous resins and preparative HPLC. WDX-5 macroporous resin shows better recoveries at 96.2%, 97.0%, 98.2% and 97.1% for epimedins A, B, C and icariin than other macroporous resins used in the experiments. As a result, epimedins A (5.1 mg), B (15.3 mg), C (7.6 mg) and icariin (14.3 mg) were obtained from 6.0 g crude Herba Epimedii with the recoveries at 70.8%, 68.9%, 66.7% and 95.3%, respectively. The method developed in this study may provide scientific references for the enrichment and separation of flavonoids from Herba Epimedii.

Topics: Chromatography, High Pressure Liquid; Epimedium; Flavonoids; Molecular Structure

The aim of this study is to evaluate the medicinal values of different parts of Epimedium brevicornu Maxim. and the effect of processing on major pharmaceutical ingredients in it. The contents of icariin and epimedin C in different parts and processed medicinal material of E. brevicornu in Taihang Mountain were determined with ultrasonic extraction and RP-HPLC. The results indicated that the contents of icariin and epimedin C, respectively 3.4524% and 0.5485%, in the leaf are higher than that in other parts. The contents of icariin and epimedin C, respectively 0.1942 % and 0.1342%, in the stem (include petiole) are the lowest. The contents of these ingredients in the root (include rhizome) are close to that in the leaf. The icariin and epimedin C in all parts of E. brevicornu reduced after processing. The content of icariin in the processed leaf is about 59.5% of that in unprocessed leaves. The effect of prossing on the content of icariin in the stem is unobvious. The content of epimedin C in the processed leaf is about 33.7% of that in unprocessed leaf. The content of epimedin C in the processed stem (include petiole) is about 36.9% of that in unprocessed stem. It is worth to exploit the stem and petiole of E. brevicornu because there are certain contents of pharmaceutical ingredients in them. The firepower should be paid attention to and the temperature should not be very high to avoid the damage on pharmaceutical ingredients in E. brevicornu when process it.. Este estudio pretende evaluar los valores medicinales de diferentes partes de la Epimedium brevicornu Maxim y el efecto de su procesamiento sobre sus principales componentes farmacéuticos. El contenido de icariina y epimedin C en diferentes partes y en material medicinal procesado de Epimedium brevicornu en la montaña de Taihang fue determinado mediante extracción ultrasónica y RP-HPLC. Los resultados indicaron que el contenido de icariina y epimedin C, respectivamente 3,4524% y 0,5485%, en la hoja son mayores que en otras partes. El contenido de icariina y epimedin C, respectivamente 0,1942% y 0,1342%, en el tallo (peciolo incluido) es más bajo. El contenido de estos componentes en la raíz (rizoma incluido) es similar al de la hoja. El contenido de icariina y epimedin C en todas las partes de E. brevicornu se vio reducido después del procesado. El contenido de icariina en la hoja procesada es aproximadamente el 59,5% del de la hoja sin procesar. El efecto del procesado sobre el contenido de icariina en el tallo no es evidente. El contenido de epimedin C en el tallo procesado es de aproximadamente el 33,7% del de la hoja sin procesar. El contenido de epimedin C en el tallo procesado (peciolo incluido) es de aproximadamente el 36,9% de aquel del tallo sin procesar. Vale la pena aprovechar el tallo y peciolo de la E. brevicornu porque hay cierto contenido de componentes farmacéuticos en ellos. Hay que controlar la potencia de fuego y la temperatura no debe ser muy alta para evitar dañar los componentes farmacéuticos de la E. brevicornu.

Topics: China; Chromatography, High Pressure Liquid; Drugs, Chinese Herbal; Epimedium; Flavonoids; Humans

The concentration variations of main flavonoids, epimedins A-C and icariin, among ten representative populations of Epimedium brevicornu Maxim. were assessed by HPLC. The populations were collected during the flowering stage and included 419 individual samples. Remarkable variations within and among populations were detected. SXXA Population (see Fig. 1) was an outlier due to its significant low concentrations (<1.00-4.46 mg/g). But even without SXXA, significant concentration differences among populations were still observed in epimedin A (2.31-8.42 mg/g), epimedin B (6.67-55.7 mg/g), epimedin C (5.39-23.0 mg/g), icariin (8.50-39.9 mg/g), and their total (29.1-123 mg/g). All populations except SXXA showed much higher concentrations than the recommended standards (i.e. 5 mg/g for icariin and 13 mg/g for the total). A high-concentration-population structure, estimated both by principal component analysis (PCA) and unweighted pair group method with averaging (UPGMA) cluster analysis, based on Euclidean distances, was observed. Both methods allowed separation of the populations in four groups defined by the concentrations of four main flavonoids. The populations (SXLC and SXQS) located in north of Yellow River were clustered together and characterized by highest concentrations of epimedin B, icariin, and their total. Considering of the high concentrations of main flavonoids and abundant resources, E. brevicornu could be exploited as a good medical resource for Herba Epimedii and would offer a tremendous potential for commercial development, but SXXA population should be paid special attention, and further study is needed.

Topics: China; Chromatography, High Pressure Liquid; Cluster Analysis; Epimedium; Flavonoids; Phylogeny; Principal Component Analysis

This study characterizes the correlation between the chemical fingerprint and estrogenic activity of an Epimedium koreanum extract. The estrogenic activity of 31 E. koreanum extract samples was evaluated by a luciferase reporter gene assay, and the samples were classified into 3 groups based on their bioactivity. A chemical fingerprint analysis was performed on each sample by high-performance liquid chromatography (HPLC), and 44 common peaks were selected from the chromatogram and used as a dataset for a pattern recognition analysis. A canonical discriminant analysis performed on this dataset determined a distinct distribution of the samples according to their estrogenic activity on the scoring plot. The classification results showed that 90.3% of the original grouped cases had been correctly classified. The total content of the 4 major extract compounds, epimedin A, epimedin B, epimedin C, and icariin, exhibited good correlation (r=0.784) with the estrogenic activities of the respective extracts. This chromatographic fingerprint-chemometric analysis system could be useful for predicting the E. koreanum pharmacological activity and consequent biological activity-relevant quality control assessment.

Topics: Cell Line, Tumor; Chromatography, High Pressure Liquid; Discriminant Analysis; Epimedium; Estrogens; Flavonoids; Genes, Reporter; Humans; Luciferases; Plant Extracts; Plant Leaves

This study was to comprehensively evaluate the chemical quality of main species of epimedium planted in China. The contents of 5 marker compounds, epimedin A, epimedin B, epimedin C, icariin and baohuoside I, as well as total flavonoids of 22 samples of 8 officinal species of Epimedium were determined by HPLC and UV, separately. Some physical and chemical tests (H2O, total ash, acid-insoluble ash and EtOH extract) were also carried out to investigate their chemical qualities. There were significant differences in types and contents of prenyl-flavonoid glycosides such as epimedin A, epimedin B, epimedin C, icariin and baohuoside I in different species, meanwhile, the physical and chemical parameters results also showed that there were obvious differences in chemical quality among different species of epimedium herb. The results provide theoretical and experimental basis for the establishment of comprehensive quality assessment system of epimedium in China.

Topics: Chromatography, High Pressure Liquid; Drugs, Chinese Herbal; Epimedium; Flavonoids; Plants, Medicinal; Quality Control; Species Specificity; Spectrophotometry, Ultraviolet

Herbal Epimedium species have been widely in Traditional Chinese Medicine for sexual enhancement, immunity improvement, anticancer and anti-aging treatment, with flavonoids and polysaccharides being the major active components. However, exhaustive depletion of wild sources warrants germplasm evaluation and quality resource exploration. A preliminarily analysis had previously indicated that a specific local geographic accession of Epimedium sagittatum found in Luotian (LT) county of Hubei Province (China) had a much higher content of total flavonoids and polysaccharides. In this study, we further investigated the medicinal component variation in the LT type under different light intensities and in different regions by the common-garden experiment. The results indicated a light intensity range of 40-160 μmol/m²/s was the most suitable for the synthesis and accumulation of total flavonoids, while polysaccharide accumulation was negatively correlated with the light intensity. Icariin was the component displaying the highest content among flavonoids, and the content of major flavonoid bioactive components was relatively stable in the third year after cultivation. There was significant correlation between the major flavonol glycoside constituents and the geographic location, and Central China followed by Northern China were the highly suitable regions for cultivation of LT type E. sagittatum. The results revealed that there was a functional balance between flavonoids and polysaccharides at different developmental stages, and the best harvesting stage should consider the primary contents of interest. This study provides important information on the exploration of quality resources, further breeding approaches and cultivation practices of E. sagittatum, and thus the important insights to enhance our understanding of quality control of traditional medicinal plants.

Topics: China; Epimedium; Flavonoids; Light; Medicine, Chinese Traditional; Plants, Medicinal; Polysaccharides; Seasons

Flavonoids isolated from Herba Epimedii such as icaritin, icariin and epimedin C have been suggested as potential bone anabolic compounds. However, the "specific localized effects" of these flavonoids in bone, in vivo, and the metabolism of these flavonoids in zebrafish larvae have never been demonstrated. In this study, we used multiple methods including in vivo imaging, drug metabolites profiling, transcriptomic and proteomic approaches to determine the mechanisms involved in the distribution and metabolism of the flavonoids in zebrafish larvae by measuring the fluorescence emission, in vivo, of icaritin and its glycoside derivatives. The fluorescence emission mechanism of icaritin in vitro was identified by spectrophotometric analysis, and the fluorescent property of icaritin was used as a probe to visualize the metabolism and distribution of icaritin and its glycoside derivatives in zebrafish larvae. Phase I and phase II metabolism of icaritin and its derivatives were identified in zebrafish by mass spectrometry. The combined transcriptomics and proteomics demonstrate a high degree of conservation of phase I and phase II drug metabolic enzymes between zebrafish larvae and mammals. Icaritin and its glycoside derivatives were demonstrated using combined approaches of in vivo imaging, drug metabolites identification, and transcriptomic and proteomic profiling to illustrate phase I and phase II metabolism of the flavonoids and their distribution in bone of zebrafish larvae. This study provides a new methodological model for use of the zebrafish larvae to examine drug metabolism.

Topics: Amino Acid Sequence; Animals; Bone and Bones; Calcification, Physiologic; Calcium; Cattle; Chromatography, Liquid; Flavonoids; Fluorescence; Gene Expression Profiling; Glycosides; Imaging, Three-Dimensional; Inactivation, Metabolic; Larva; Mass Spectrometry; Molecular Sequence Data; Organ Specificity; Peptides; Proteomics; Serum Albumin, Bovine; Spectrophotometry; Time Factors; Zebrafish

Icariin and epimedins A, B, C are a series of active flavonol glycoside in Epimedium brevicornum Maxim. A pilot-scale preparative high performance liquid chromatographic (HPLC) method was developed to purify the four flavonol glycosides as reference standards from the crude extract of Epimedium brevicornum Maxim. After the crude extract containing approximately 20% flavonols was enriched using macropore resin, the obtained target fractions were subjected to pilot-scale preparative HPLC purification. With the aid of a self-packed pilot-scale preparative column (220 mm x 77 mm, 10 microm), the 4 target compounds were separated well within 35 min in a single chromatographic run by the elution with acetonitrile-water (26:74 or 30:70, v/v). By repetitive injection of the enriched target fraction onto the preparative column, 33 g icariin as well as 4.6 g epimedin C, 3.7 g epimedin B, and 0.6 g epimedin A were obtained from 300 g crude extract. The purities of all products were greater than 98%. This pilot-scale preparative HPLC technique and the two step separation technology for 4 target compounds are quite useful for the production of the reference standard series with good purity like icariin, epimedins A, B, C standards due to its high performance, rapid separation and more amounts of products obtained.

Topics: Chromatography, High Pressure Liquid; Epimedium; Flavonoids; Glycosides; Pilot Projects; Reference Standards; Reproducibility of Results

To establish a new method and validate its feasibilities for quality evaluation of Fructus Epimedii.. Four main effective flavones, epimedin A, epimedin B, epimedin C and icariin were selected as analytes to evaluate the quality of Fructus Epimedii. The relative correction factors (RCF) of icariin to the other three flavones were calculated. The method was evaluated by comparison of the quantitative results between external standard method and QAMS method.. No significant differences were found in the quantitative results of three flavones by external standard method and QAMS method.. It is feasible and accurate to evaluate the quality of Fructus Epimedii.

Topics: Chromatography, High Pressure Liquid; Drugs, Chinese Herbal; Flavonoids; Reproducibility of Results; Statistics as Topic; Time Factors

An ultrasonic-assisted extraction (UAE) procedure of epimedin A, epimedin B, epimedin C and icariin from Herba Epimedii was developed. The effects of ethanol concentration, ratio of liquid to solid, UAE time, extraction temperature and number of extraction cycles on the extraction yields of the four flavonoids from Herba Epimedii were investigated. The optimal UAE condition was found using orthogonal test: 50% (v/v) ethanol solution, liquid:solid ratio of 30 ml/g, ultrasonication duration 30 min, extraction temperature 50 degrees C and three extraction cycles. The UAE method showed a high reproducibility. Epimedin A, B, C and icariin in the crude extract exhibited photodegradation under ultraviolet irradiation. This UAE method was shown to be highly efficient compared with the conventional Soxhlet extraction and boiling extraction. The effect of ultrasound on cell destruction was examined by scanning electron microscopy. The contents of epimedin A, B, C and icariin in the leaves of 20 Epimedium species were determined using high-performance liquid chromatographic method following UAE method.

Topics: Chromatography, High Pressure Liquid; Epimedium; Flavonoids; Indicators and Reagents; Microscopy, Electron, Scanning; Photochemistry; Plant Extracts; Reproducibility of Results; Ultrasonics

The purpose is to determine absorption mechanism of five bioactive prenylated flavonoids (baohuoside I, icariin, epimedine A, B, and C) present in heat-processed Epimedium koreanum Nakai (Yin Yanghuo).. Transport of five prenylated flavonoids present in heat-processed herbs were studied in the human intestinal Caco-2 model and the perfused rat intestinal model.. In the perfused rat intestinal model, prenylated flavonoids with a monoglucosidic bond (e.g., icariin) was rapidly hydrolyzed into corresponding metabolites (e.g., baohuoside I). In the Caco-2 model, apical to basolateral permeability of a monoglycoside baohuoside I (1.46 x 10(-6) cm/sec) was more than 2 folds greater than four prenylated flavonoids with 2 or more sugar moieties (<0.6 x 10(-6) cm/sec). The slow apical to basolateral transport of baohuoside I was the result of efflux. This efflux was carrier-mediated and active since its transport was vectorial, concentration- and temperature-dependent with activation energies greater than 15 kcal/mol. Efflux of baohuoside I was significantly suppressed by inhibitors of BCRP and MRP2, whereas efflux of icariin was significantly inhibited only by p-glycoprotein inhibitor verapamil. Because YHH is often heat-processed for better efficacy, we determined and found the optimal condition for increasing contents of more bioavailable flavonoids (i.e., baohuoside I) to be 160-170 degrees C for 5-7 min.. Poor bioavailability of prenylated flavonoids results from their poor intrinsic permeation and transporter-mediated efflux. Heat processing parameters may be optimized to preserve the herb's bioavailable flavonoids, which help retain and improve its efficacy during processing.

Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; ATP Binding Cassette Transporter, Subfamily G, Member 2; ATP-Binding Cassette Transporters; Biological Availability; Caco-2 Cells; Epimedium; Flavonoids; Hot Temperature; Humans; Hydrolysis; Intestinal Absorption; Intestine, Small; Male; Multidrug Resistance-Associated Protein 2; Multidrug Resistance-Associated Proteins; Neoplasm Proteins; Perfusion; Permeability; Prenylation; Rats; Rats, Sprague-Dawley; Time Factors

Herba Epimedii (family Berberidaceae), Yinyanghuo in Chinese, is one of the commonly used Chinese medicines. Flavonoids are considered as its active components. In this study, a reliable pressurized liquid extraction (PLE) and HPLC method was developed for simultaneous determination of 15 flavonoids, namely hexandraside E, kaempferol-3-O-rhamnoside, hexandraside F, epimedin A, epimedin B, epimedin C, icariin, epimedoside C, baohuoside II, caohuoside C, baohuoside VII, sagittatoside A, sagittatoside B, 2''-O-rhamnosyl icariside II and baohuoside I in different species of Epimedium. The analysis was performed by using a Zorbax SB-C18 analytical column (250 mm x 4.6 mm I.D., 5 microm) at gradient elution of water and acetonitrile with diode-array detection (270 nm). All calibration curves showed good linearity (r(2)>0.9997) within test ranges. The LOD and LOQ were lower than 1.31 ng and 2.62 ng on column, respectively. The RSD for intra- and inter-day of 15 analytes was less than 3.8% at three levels, and the recoveries were 90.5-106.8%. The validated method was successfully applied for the analysis of 15 flavonoids in different species of Epimedium which had great variation on the contents of investigated flavonoids. Hierarchical clustering analysis based on the characteristics of 15 investigated compound peaks in HPLC profiles showed that 26 samples were divided into three main clusters, which were in accordance with their flavonoid contents. Four flavonoids including epimedin A, B, C and icariin were optimized as markers for quality control of the species of Epimedium used as Yinyanghuo.

Topics: Chromatography, High Pressure Liquid; Epimedium; Flavonoids; Reproducibility of Results

To review the quality of Epimedium extract in the market.. The contents of icariin, epimedin C, sagittatoside B and total flavonoids in Epimedium extracts sold in the market were assayed by the methods of HPLC and UV respectively. HPLC fingerprintings were obtained at the same time.. The contents of icariin in most of the extracts are closely similar with the ones labeled by the companies. 3 type chromatograms were classified in all the HPLC fingerprintings, and were corresponded with their raw materials. The contents of epimedin C, sagittatoside B and total flavonoids were different in the samples with the same content of icariin.. We can primarily confirm the origin of raw materials by comparing the HPLC fingerprinting of extracts with the ones of materials. The difference of extracts quality mainly comes from the difference of materials. So we suggest that Epimedium extract product should be labeled the origin of materials, and assayed with more compound contents, to ensure the quality stabilization.

Topics: China; Chromatography, High Pressure Liquid; Ecosystem; Epimedium; Flavonoids; Plant Extracts; Plants, Medicinal; Quality Control; Species Specificity

To achieve the quality control of Herba Epimedii, and to evaluate the quality of medical materials of the 8 official species including the 5 species recorded in 'Chinese Pharmacopoeia' including Epimedium brevicornum, E. sagittatum, E. pubescens, E. koreanum and E. wushanense, and the 3 other species (E. acuminatum, E. myrianthum, E. leptorrhizum) recorded in 'Guizhou Quality Criteria for Traditional Chinese Medical Material and Nationality Medical Material', and E. pseudowushanuse (new species) which is used as E. wushanense for a long time.. The contents of icariin and total flavonoids of 102 samples of 9 officinal species of Herba Epimedii were determined by HPLC and UV, respectively.. The contents of icariin in about 30% of the samples of the 5 species recorded in 'Chinese Pharmacopoeia' were lower than 0.5%, which is acceptable quality recorded in 'Chinese Pharmacopoeia'. Refering the literatures, we suggested the total contents of epimedin A, B, C and icariin (epi-medium multi-glycosides, ABCI) should be established as a new standard instead of the content of icariin. The content of total flavonoids, not less than 5.0%, and ABCI, not less than 1.3%, could be used to evaluate the quality of the above medical materials efficiently.

Topics: Drugs, Chinese Herbal; Epimedium; Flavonoids; Flavonols; Pharmacognosy; Plants, Medicinal; Quality Control; Reproducibility of Results; Seasons; Species Specificity

To investigate the chemical constituents of Epimedium brevicornum.. The chemical constituents were isolated by using silica gel column chromatography and preparative TLC. The structures were identified on the basis of physical-chemical constants and spectral data.. Five compounds were isolated and identified as hyperoside, icariin, epimedin B, epimedin C, inositol.. Compound I and III - V were isolated from the plant for the first time.

Topics: Epimedium; Flavonoids; Plant Components, Aerial; Plants, Medicinal; Quercetin

To comment on main resource species of Herba Epimedii.. Taxonomy, resource investigation and quality evaluation of flavonoid contents were made.. 7 species of Herba Epimedii having broad distribution were summarized. According the area of their distribution, they were named Epimedium sagittatum, E. brevicornu, E. acuminatum, E. koreanum, E. pubescens, E. leptorrhizum and E. wushanense. Each distribution in detail and icariin and likewise compounds contents of these 7 species were provided. Other 8 Epimedium species much used were proposed. Medicinal characters 15 species were provided in this paper.. On the basis of distribution character, resource quantity and growing with other species mingled, it is suggested that 4 main production or purchasing districts in China be divided. The most important district is northeastern district, where only E. koreanum grows there, with the best guality. Northwestern and northern district is the second one, where E. brevicornu, mainly grows with much stable guality. Then it is eastern and southern district, where E. sagittatum grows with the largest quantity but unstable quality. Southwestern district is the last one, mingle species complex and identification important. In Sichuan province, E. acuminatum and E. pubescens are main species, with other 12 species growing there. In Guizhou province, E. acuminatum, E. leptorrhizum and E. wushanense are main species, other 7 species growing there and E. leptorrhizum with poor quality. It is suggested that E. acuminatum be recorded in Chinese Pharmacopoeia.

Topics: China; Conservation of Natural Resources; Drugs, Chinese Herbal; Ecosystem; Epimedium; Flavonoids; Pharmacognosy; Plants, Medicinal; Quality Control

To establish a RP-HPLC method for the determination of epimedin C and icariin in Herba Epimedii.. Chromatographic conditions: Hypersil BDS-C18 column, acetonitrice and water containing 0.05% phosphoric acid as gradient eluents, G1315A photodiode array detector at 272 nm.. The average recovery rate of epimedin C was 99.7%, RSD 1.5% (n = 9), icariin 102.5%, RSD 1.1% (n=9).. The method is reliable, stable and well repeatable. It provides the useful information for quality evaluation.

Topics: China; Drugs, Chinese Herbal; Ecosystem; Epimedium; Flavonoids; Plant Components, Aerial; Plants, Medicinal; Quality Control; Species Specificity

A micellar electrokinetic capillary chromatographic (MEKC) method with diode-array detection is developed for the characterization of pharmacologically active flavonoids in extracts prepared from Epimedium brevicornum, E. humanense, E. coactum, and E. truncatum. The pK(a) values of icarin, epimedin B, and epimedin C are determined by spectrophotometry. Optimal separation of icarin, epimedin B and C, and eight other compounds is achieved by determining pK(a) values and by systematically optimizing electrolytic and instrumental parameters. The repeatability of analyses and the reliability of identification are evaluated by the marker technique. Calculated for relative migration times of flavonoids in the extracts, the repeatability of the analyses varies from 0.7 to 6.4% (nine replicates). For migration indices calculated with two markers, however, the repeatability almost falls below 0.5%. The distribution of the flavonoids is found to differ both qualitatively and quantitatively among the four species. The MEKC technique appears to provide a powerful tool for the identification and quality control of plant drugs and for phytotaxonomic investigations.

Topics: Cardiovascular Agents; Chromatography; Drugs, Chinese Herbal; Electrophoresis, Capillary; Flavonoids; Hydrogen-Ion Concentration; Plant Extracts; Plants, Medicinal; Reproducibility of Results; Spectrophotometry, Ultraviolet