forsythiaside and phillyrin

Topics: Forsythia; Gene Expression Profiling; Glucosides; Glycosides

Topics: Chemical Fractionation; Forsythia; Fruit; Glucosides; Glycosides; Plant Extracts; Rutin; Solvents; Ultrasonics

In order to obtain the optimum method for content determination of Forsythia Fructus (FF), a variety methods for the sample preparation of FF were evaluated by the content determination methods of Chinese Pharmacopoeia. And an optimum method was screened and as follows: 30 times with 70% ethanol solution in ultrasonic extractor for half an hour. The method can achieve the best effect of simultaneously extracting forsythoside A and forsythin. Then, a HPLC method for simultaneous determination of forsythoside A and forsythin was established by methodology. The HPLC chromatographic conditions: the mobile phase consisted of acetonitrile (A)-0.4% acetic acid solution (B) with gradient elution [0-33 min，15%A，33-43 min，15%-25%A，43-60 min，25% A] was at the flow rate of 1 mL·min⁻¹, the column temperature was 25 °C, and the detection wavelength was 330 and 277 nm. Moreover, the contents of forsythoside A and forsythin for 10 Green Forsythia Fructus (GF) and 5 Old Forsythia Fructus (OF) were determined by this method and Chinese Pharmacopoeia. The result not only displayed that the established method is effective, rapid, and simple, but also showed that the contents of forsythoside A and forsythin for GF and OF were significantly different. Which implied that the forsythoside A and forsythin limit standard for GF and OF should be controled by different values. This studies provide an important basis for the establishment of the content determination of FF and the quality control standard for GF and OF.

Topics: Chromatography, High Pressure Liquid; Drugs, Chinese Herbal; Forsythia; Fruit; Glucosides; Glycosides; Phytochemicals; Quality Control

1. Phillyrin and forsythoside A are two important active ingredients in Forsythia suspensa. However, the effects of phillyrin and forsythoside A on the activities of cytochrome P450 (CYP450) remain unclear. 2. This study aimed to investigate the effects of phillyrin and forsythoside A on the activities of CYP1A2, CYP2C11, CYP2D1 and CYP3A1/2 by cocktail probe drugs in rats both in vivo and in vitro. 3. Many pharmacokinetic parameters of caffeine and metoprolol in phillyrin pretreatment group, caffeine and tolbutamide in forsythoside A pretreatment group were affected significantly. In rat liver microsomal incubation system, the concentrations of acetaminophen and dextrophan in the phillyrin pretreatment group are higher than blank control group by 207.69% and 125.00%, however, the concentrations of 4-hydroxytolbutamide and 6β-hydroxytestosterone were not significantly altered. The concentrations of acetaminophen and 4-hydroxytolbutamide in the forsythoside A pretreatment group are higher than blank control group by 223.07% and 154.16%, whereas the concentrations of dextrophan and 6β-hydroxytestosterone were not significantly altered. 4. These results indicated that Phillyrin had potential inductive effects on rat CYP1A2 and CYP2D1 activities, without affecting CYP2C11 and CYP3A1/2 activities. Moreover, forsythoside A had inductive effects on the activities of CYP1A2 and CYP2C11, without affecting CYP2D1 and CYP3A1/2 activities.

Topics: Animals; Cytochrome P-450 Enzyme System; Glucosides; Glycosides; Male; Rats

Forsythiae Fructus (FF), the dried fruit of Forsythia suspensa, has been widely used as a heat-clearing and detoxifying herbal medicine in China. Green FF (GF) and ripe FF (RF) are fruits of Forsythia suspensa at different maturity stages collected about a month apart. FF undergoes a complex series of physical and biochemical changes during fruit ripening. However, the clinical uses of GF and RF have not been distinguished to date. In order to comprehensively compare the chemical compositions of GF and RF, NMR-based metabolomics coupled with HPLC and UV spectrophotometry methods were adopted in this study. Furthermore, the in vitro antioxidant and antibacterial activities of 50% methanol extracts of GF and RF were also evaluated. A total of 27 metabolites were identified based on NMR data, and eight of them were found to be different between the GF and RF groups. The GF group contained higher levels of forsythoside A, forsythoside C, cornoside, rutin, phillyrin and gallic acid and lower levels of rengyol and β-glucose compared with the RF group. The antioxidant activity of GF was higher than that of RF, but no significant difference was observed between the antibacterial activities of GF and RF. Given our results showing their distinct chemical compositions, we propose that NMR-based metabolic profiling can be used to discriminate between GF and RF. Differences in the chemical and biological activities of GF and RF, as well as their clinical efficacies in traditional Chinese medicine should be systematically investigated in future studies.

Topics: Anti-Bacterial Agents; Antioxidants; Bacillus subtilis; Biphenyl Compounds; Cyclohexanones; Drugs, Chinese Herbal; Escherichia coli; Forsythia; Fruit; Gallic Acid; Glucose; Glucosides; Glycosides; Hydroxyl Radical; Picrates; Plant Extracts; Proton Magnetic Resonance Spectroscopy; Pseudomonas aeruginosa; Rutin; Staphylococcus aureus

An optimized microwave-assisted extraction (MAE) method and RP-HPLC method were developed for the simultaneous extraction and determination of rutin, forsythiaside A, and phillyrin in the fruits of Forsythia suspensa. The key parameters of the open-vessel MAE process were optimized. A mixed solvent of methanol and water (70:30, v/v) was most suitable for the simultaneous extraction of the three components. The sample was soaked for 10 min before extraction. The optimized conditions were: microwave power 400 W, temperature 70°C, solvent-to-material ratio 30 mL/g, and extraction time 1 min. Compared to conventional extraction methods, the proposed method can simultaneously extract the three components in high yields and was proved to be a more rapid method with a lower solvent consumption. The optimized HPLC-photodiode array detection analysis was validated to have good linearity, precision, accuracy, and sensitivity. The developed MAE followed by RP-HPLC is a fast and appropriate method for the simultaneous extraction and determination of rutin, forsythiaside A, and phillyrin in the fruits of F. suspensa.

Topics: Chemical Fractionation; Chromatography, High Pressure Liquid; Forsythia; Fruit; Glucosides; Glycosides; Microwaves; Plant Extracts; Rutin

This paper aims to establish a new method of calibration and positioning in quantitative analysis of multicomponents by single marker (QAMS), using Shuanghuanglian oral liquid as the research object. Establishing relative correction factors with reference chlorogenic acid to other 11 active components (neochlorogenic acid, cryptochlorogenic acid, cafferic acid, forsythoside A, scutellarin, isochlorogenic acid B, isochlorogenic acid A, isochlorogenic acid C, baicalin and phillyrin wogonoside) in Shuanghuanglian oral liquid by 3 correction methods (multipoint correction, slope correction and quantitative factor correction). At the same time chromatographic peak was positioned by linear regression method. Only one standard uas used to determine the content of 12 components in Shuanghuanglian oral liquid, in stead of needing too many reference substance in quality control. The results showed that within the linear ranges, no significant differences were found in the quantitative results of 12 active constituents in 3 batches of Shuanghuanglian oral liquid determined by 3 correction methods and external standard method (ESM) or standard curve method (SCM). And this method is simpler and quicker than literature methods. The results were accurate and reliable, and had good reproducibility. While the positioning chromatographic peaks by linear regression method was more accurate than relative retention time in literature. The slope and the quantitative factor correction controlling the quality of Chinese traditional medicine is feasible and accurate.

Topics: Apigenin; Calibration; Chlorogenic Acid; Chromatography, High Pressure Liquid; Drugs, Chinese Herbal; Flavanones; Flavonoids; Glucosides; Glucuronates; Glycosides; Reproducibility of Results

In the present study, an in situ rat model was employed to systemically investigate the absorption of phillyrin and forsythiaisde. Three concentrations of phillyrin (0.2, 0.4 and 1.5 mg) were tested and the results showed that phillyrin cannot be absorbed in the digestive tract. The absorption rates of forsythiaside in stomach were 7.773, 7.228 and 6.751% h(-1) for 0.5, 1 and 2.5 mg, and no significant difference was found in different concentrations. The absorptions of forsythiaside in intestine were investigated in different concentrations and different absorption sites. The mean P% were 6.618, 7.199, 9.210 and 9.747% h(-1) of forsythiaside in intestine for 0.25, 0.5, 1, 2.5 mg dosage, and the statistical analysis showed that the absorption had no relation with concentration. In addition, in different digestive segments, the mean P% were 7.528, 8.382, 8.191, 9.109 and 6.908% h(-1) for the gastric, duodenum, jejunum, ileum and colon, respectively. No statistical differences of absorption were found for forsythiaside among different digestive segments indicated no specific absorption site was found.

Topics: Algorithms; Animals; Anti-Infective Agents; Gastric Mucosa; Glucosides; Glycosides; In Vitro Techniques; Intestinal Absorption; Male; Perfusion; Permeability; Rats; Rats, Sprague-Dawley; Rats, Wistar

To study the intestinal absorption kinetics characteristic of the main four active ingredients in Shuanghuanglian oral liquid (SHL) and to investigate the influence of herbal compatibility in SHL on absorption of main effective ingredients.. The in situ rat circulation model was used to investigate the concentration change differences of the four active components in SHL during perfusion.. The absorption quantity of different concentrations of baicalin, chlorogenic acid, phillyrin and forsythoside A ranging from 40-160, 6-24, 3-12, 2.6-10.4 mg x L(-1) respectively was linear with concentration and showed no saturation at high concentration. The absorption rate constant K(a) and the hourly absorption percentages A were essentially unchanged. The pH changing from 5.0-7.43 had little influence on the absorption of phillyrin except baicalin, chlorogenic acid and forsythoside A. The calculated K(a) and A of the four active ingredients had no significant differences from that obtained after perfusing via duodenum, jejunum, ileum and colon; The calculated K(a) and A of baicalin in Scutellariae Radix (SR), chlorogenic acid in Lonicerae Japonicae Flos (LJF) and phillyrin in Forsythiae Fructus (FF) had no significant differences compared with that in SHL, but the calculated K(a) and A of forsythoside A in FF were obviously superior to that in SHL.. The intestinal absorption of the four active ingredients in SHL was mainly passive diffusion and had no difference in different segments of rat intestine; the compatibility of SHL compounds changed the absorption of forsythoside A in FF obviously.

Topics: Administration, Oral; Animals; Chlorogenic Acid; Drugs, Chinese Herbal; Flavonoids; Glucosides; Glycosides; Hydrogen-Ion Concentration; Intestinal Absorption; Intestinal Mucosa; Intestines; Male; Rats; Rats, Sprague-Dawley

To investigate the habitat processing method of Forsythiae Fructus based on the different indexes, and to choose the best habitat producing process.. The habitat producing process was researched by the L9(3(4)) orthogonal and the single factor test. The contents of phillyrin and forsythiaside A were determined by HPLC.. The contents of phillyrin and forsythiaside A from Forsythiae Fructus processed by evaporating were 1.33-3.05, and 9.71-44.82 mg x g(-1), respectively. The contents of phillyrin and forsythiaside A from Forsythiae Fructus processed by cooking were 4.63-5.46 mg x g(-1), and 40.20-64.84 mg x g(-1), respectively.. With phillyrin and forsythiaside A as evaluation indexes, cooking method is superior to evaporate method while it is superior to dry method. It is conductive to the preservation and stability of phillyrin and forsythiaside A that add 4 times water of material volum and boil 10 min.

Topics: Chromatography, High Pressure Liquid; Drug Compounding; Drugs, Chinese Herbal; Ecosystem; Forsythia; Glucosides; Glycosides

A simple and reproducible HPLC-photodiode array detector method has been described for evaluating and controlling quality of Forsythia suspensa extract (FSE). First, by analysis of chromatographic fingerprints, the similarities of chromatograms of FSE samples from the same pharmaceutical company exceeded 0.999, 0.997 and 0.960, respectively, although they were much lower from different pharmaceutical companies. Second, by further comparing many batches of extract chromatograph charts with the corresponding reference herb materials, the "common peaks" 3, 5, 7 and 10 were defined as "marker peaks", which were identified as (+)-pinoresinol-beta-D-glucoside, forsythiaside, phillyrin and phillygenin, respectively. Third, four "marker peaks" were simultaneously determined based on fingerprint chromatogram for further controlling the quality of FSE quantitatively. Namely, the newly developed method was successfully applied to analyze 38 batches of FSE samples supplied by three pharmaceutical factories, which showed acceptable linearity, intra-day precision (RSD<2.76%), inter-day precision (RSD<3.43%) and the average recovery rates in the range of (95.38+/-2.96)% to (101.60+/-3.08)%. At last, hierarchical clustering analysis and Bayes discriminant analysis statistical methods were used to classify and differentiate the 38 FSE samples to provide the basis for guiding reasonable use of FSE and controlling its quality better.

Topics: Chromatography, High Pressure Liquid; Drugs, Chinese Herbal; Forsythia; Glucosides; Glycosides; Lignans; Magnetic Resonance Spectroscopy; Plant Extracts; Plants, Medicinal; Quality Control

To establish methods for the determination of phillyrin and forsythoside A in Lianqiao Bingdu Qing capsule by RP-HPLC.. The determination of phillyrin was carried out on YWG-C18 column (4.6 mm x 250 mm, 10 microm), using acetonitrile-water (25:75) as mobile phase at a flow rate of 0.8 mL x min(-1) and detected at the wavelength 277 nm. The determination of forsythoside A was carried out with YWG-C18 column(4.6 mm x 250 mm,10 microm), using acetonitrile-water-Acetic acid (17:83:0.4) as mobile phase at a flow rate of 1.0 mL x min(-1) and detected at the wavelength 280 nm.. The average recovery of phillyrin was 99.6%, RSD = 1.9% (n = 5). The average recovery of forsythoside A was 101.3%, RSD = 2.5% ( n = 5).. The methods were simple and accurate and could be used to control the quality of the Lianqiao Bingdu Qing capsule.

Topics: Capsules; Chromatography, High Pressure Liquid; Drugs, Chinese Herbal; Forsythia; Fruit; Glucosides; Glycosides; Plants, Medicinal

To study the chemical constituents with antiviral action from Yinqiaosan on influenza virus.. Constituents were isolated by different kinds of column chromatography and their structures were elucidated with chemical and spectral methods.. Eleven chemical constituents were isolated and elucidated as arctiin, phillyrin, forsythiaside, liquiritigenin, liquiritin, genistein, formononetin, daidzein, glycitrin, 3,3',4-tri-omethlellagic acid and chlorogenic acid.. Genistein, daidzein, glycitrin and 3,3',4-tri-omethlellagic acid were isolated from Yinqiaosan for the first time.

Topics: Antiviral Agents; Arctium; Drug Combinations; Drugs, Chinese Herbal; Forsythia; Furans; Genistein; Glucosides; Glycosides; Isoflavones; Plants, Medicinal