In order to find potential therapeutic agents on lung inflammatory conditions, the extracts of Acanthopanax divaricatus var. albeofructus were prepared and its constituents were isolated. They include lignans such as (+)-syringaresinol (1), acanthoside B (2), salvadoraside (3) and acanthoside D (4), lariciresinol-9-O-beta-D-glucopyranoside (5) and phenylpropanoids such as 4-[(1E)-3-methoxy-1-propenyl]phenol (6), coniferin (7), and methyl caffeate (8). The extracts and several constituents such as compound 1, 6 and 8 inhibited the production of inflammatory markers, IL-6 and nitric oxide, from IL-1beta-treated lung epithelial cells and lipopolysaccharide (LPS)-treated alveolar macrophages. Furthermore, the extracts and compound 4 significantly inhibited lung inflammation in lipolysaccharide-treated acute lung injury in mice by oral administration. Thus it is suggested that A. divaricatus var. albeofructus and its several constituents may be effective against lung inflammation.
Eleutherococcus* ; Acute Lung Injury ; Administration, Oral ; Animals ; Epithelial Cells ; Interleukin-6 ; Lignans ; Lung* ; Macrophages ; Macrophages, Alveolar ; Mice ; Nitric Oxide ; Pneumonia*

To compare the pharmacokinetics of syringin, eleutheroside E and isofraxidin after intravenous administration of each monomer and Ciwujia injection. Twenty-four Sprague-Dawley rats were randomly divided into four groups and intravenously administrated with syringin, eleutheroside E, isofraxidin, and Ciwujia injection, respectively. The concentrations of the three components in rat plasma were determined by LC-MS/MS. DAS 2.0 software was applied to calculate the pharmacokinetic parameters while the SPSS 17.0 software was used for statistical analysis. Significant difference (P < 0.05) was found between each monomer and the injection on the main pharmacokinetic parameters such as AUC, CL and t1,/2. Compared with the injection, the group treated with the syringin has obvious decrease in AUC, and increase in CL while the group treated with eleutheroside E has obvious increase in AUC, and decrease in CL The t1/2 of isofraxidin was prolonged in Ciwujia injection. Pharmacokinetic characters of the ingredients in the injection varied greatly from the monomer. Other constituents in the injection may have an impact on the pharmacokinetic profiles of these three components.
Administration, Intravenous ; Animals ; Coumarins ; administration & dosage ; blood ; pharmacokinetics ; Drugs, Chinese Herbal ; administration & dosage ; pharmacokinetics ; Glucosides ; administration & dosage ; blood ; pharmacokinetics ; Lignans ; administration & dosage ; blood ; pharmacokinetics ; Male ; Phenylpropionates ; administration & dosage ; blood ; pharmacokinetics ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo determine the concentration of schisandrin in Shengmaiyin with HPLC.

METHODThe sample was extracted with ethyl acetate through supersonic wave. The solution was filtrated and evaporated. The residue was resolved with methanol and determined by HPLC using PHENOMENEX C18 (4.6 mm x 250 mm, 5 microns) chromatographic column, methanol-acetonitrile-water (15:15:10) as mobile phase. The wavelength for detection was 254 nm.

RESULTThe peak of schizandrin appears on about 7.10 minutes. The standard curves of schizandrin were linear in the concentration range of 0.2-2.0 micrograms, r = 0.9996. The average recovery of schizandrin were 100.5% (RSD 2.84%).

CONCLUSIONThis method was found to be sensitive, quick and accurate for the measurement of schizandrin concentrations in Shengmaiyin.

Administration, Oral ; Chromatography, High Pressure Liquid ; Cyclooctanes ; analysis ; Drug Combinations ; Drugs, Chinese Herbal ; administration & dosage ; chemistry ; isolation & purification ; Lignans ; analysis ; Plants, Medicinal ; chemistry ; Polycyclic Compounds ; analysis ; Schisandra ; chemistry

OBJECTIVETo study the lignans components in rat serum after oral administration of Fuzheng Huayu decoction (FZHY), and to investigate the active ingredients in vivo.

METHODA rapid, sensitive and selective method using liquid chromatography-electrospray ionization tandem mass spectrometry (HPLC-ESI-MSn) was established. The serum samples were extracted with ethyl acetate (EtOAc)for three times. The chromatographic separation was achieved on a Waters Atlantis T3 column by gradient elution using methanol and water containing 5 mmol x L(-1) ammonium acetate as mobile phase, at a flow rate of 0.2 mL x min(-1). Mass spectra were acquired in positive ion mode. Identification and structural elucidation of the components in FZHY and dosed serum were performed by comparing their retention time and MSn spectra with those of reference compounds and reported data in the literatures.

RESULTSchisandrin, schisandrol B, schisantherin A and schisandrin B were found in FZHY and dosed serum, but schisandrin C and deoxyschizandrin were only found in FZHY.

CONCLUSIONSchisandrin, schisandrol B, schisantherin A and schisandrin B can be directly absorbed into the blood after oral administration of FZHY, and the four lignans components from Schisandra chineisis might play a key role as the ingredient basement of FZHY for anti-liver fibrosis.

Administration, Oral ; Animals ; Blood Chemical Analysis ; methods ; Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; administration & dosage ; chemistry ; Lignans ; blood ; Male ; Mass Spectrometry ; methods ; Rats ; Rats, Wistar

OBJECTIVETo investigate the pharmacokinetic interaction among three major bioactive compounds of Shengmai formula.

METHODSAfter oral administration of ginsenoside Rg(1), ginsenoside Rb(1) and schisandrin with the same dose(100 mg.kg(-1)) individually or in combination, rat serum samples were extracted, then these three compounds were determined by liquid chromatography-mass spectrometry(LC-MS). The pharmacokinetic parameters of three compounds in single or combination form were calculated by WinNonLinu6.0 using non-compartment model.

RESULTSCompared with single drug group, the peak concentration of ginsenoside Rg(1) in combined group increased from(0.476 ±0.238) μg.ml(-1) to (1.946 ±1.432) μg.ml(-1), AUC(0-∞) increased from(0.523 ±0.238) μg.h.ml(-1) to (1.908 ±1.319) μg.h.ml(-1), CL decreased from(226311 ± 96819) ml.h(-1).kg(-1) to(90650 ±73684) ml.h(-1).kg(-1) and Vd decreased from(317110 ±154009) ml.kg(-1) to(130967 ±78306) ml.kg(-1). While the pharmacokinetic parameters of ginsenoside Rb(1) and schisandrin showed no significant change.

CONCLUSIONCombined oral administration of three compounds of Shengmai formula can improve the bioavailability of ginsenoside RgRg(1), however it does not change the pharmacokinetic behavior of ginsenoside RbRg(1) and schisandrin.

Animals ; Biological Availability ; Chromatography, Liquid ; Cyclooctanes ; administration & dosage ; blood ; pharmacokinetics ; Drug Synergism ; Ginsenosides ; administration & dosage ; blood ; pharmacokinetics ; Lignans ; administration & dosage ; blood ; pharmacokinetics ; Male ; Polycyclic Compounds ; administration & dosage ; blood ; pharmacokinetics ; Rats ; Rats, Sprague-Dawley ; Tandem Mass Spectrometry

OBJECTIVETo develop a UPLC method for the simultaneous determination of liquiritin, narirutin, hesperidin, ammonium glycyrrhetate, honokiol and magnolol in Huoxiang Zhengqi oral liquid.

METHODA Zorbax Eclipse C18 column was used with the mobile phase of acetonitrile and 0. 05% phosphate acid by gradient elution at the detection wavelength of 220 nm. The flow rate was 0.42 mL x min(-1) and the column temperature was 30 degrees C.

RESULTThe calibration curves were linear in the ranges of 0.001 7-0.034, 0.003 4-0.068, 0.006 4-0.128, 0.012 8-0.256, 0.003 2-0.064, 0.006 4-0.128 microg, respectively. The average recoveries were 103.3%, 98.39%, 98.29%, 102.1%, 98.45%, 102.2% with RSDs of 2.1%,1.0%, 0.50%, 2.3%, 0.9%, 2.0%, respectively.

CONCLUSIONThe UPLC method was simple, rapid and accurate, it could be used for quality control of Huoxiang Zhengqi oral liquid.

Administration, Oral ; Biphenyl Compounds ; chemistry ; Chromatography, High Pressure Liquid ; methods ; Disaccharides ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Flavanones ; chemistry ; Glucosides ; chemistry ; Hesperidin ; chemistry ; Lignans ; chemistry ; Pharmaceutical Solutions ; chemistry

To study the preparation method of Schisandra total lignanoids enteric (SLE) nanoparticles and evaluate its pharmacokinetics in rats, SLE nanoparticles were prepared by modified emulsion solvent diffusion method. The properties of SLE nanoparticles were evaluated of morphology, mean diameter and entrapment efficiency. An HPLC method was employed to determine the concentration of deoxyschisandrin (QS) and schisantherin A (SA) in plasma, which were used as an index of Schisandra total lignanoids, and the bioavailability of the nanoparticles was compared with the reference group by oral administration using SD rats. The nanoparticles observed by transmission electronmicroscopy were round, and the mean particle sizes of SLE were (36.7 +/- 4.4) nm. Entrapment efficiency of QS and SA were (97.5 +/- 0.7)% and (91.3 +/- 0.8)%, respectively. Its pharmacokinetic process calculated with 3p97 software was fitted to a one-compartment model. The pharmacokinetic parameters showed sustained-release property. Compared with reference formulation, the AUCs of SLE nanoparticles were 2.3 and 5.8 times separately. These results suggested that the incorporation into Eudragit S100 of Schisandra total lignanoids can improve the bioavailability.
Animals ; Area Under Curve ; Biological Availability ; Cyclooctanes ; administration & dosage ; chemical synthesis ; pharmacokinetics ; Female ; Lignans ; administration & dosage ; chemical synthesis ; pharmacokinetics ; Male ; Nanoparticles ; Particle Size ; Polycyclic Compounds ; administration & dosage ; chemical synthesis ; pharmacokinetics ; Rats ; Rats, Sprague-Dawley ; Schisandra

The paper aims to study the pharmacokinetic parameters of gastrodin in rats effected by compound compatibilitiy and different doses of Tiangou Jiangya capsule. The extracts from Gastrodiae Rhizoma( equivalent to gastrodin 16.82 mg x kg(-1) and Tiangou jiangya capsule (equivalent to gastrodin 8.410, 16.82, 33.64 mg x kg(-1)) were oral administrated to rats respectively. The plasma were taken at various time points and treated with acetonitrile to measure the contents of gastrodin by HPLC method. The mean plasma concentration-time data were analyzed by 3P97 pharmacokinetic software and the pharmacokinetic parameters between groups were treated by SPSS 16.0. The results showed that gastrodin in rat was fitted to one-compartment model, Cmax and AUC of Tiangou Jiangya capsule were in direct proportion to oral administration, and t1/2Ka had nothing to do with doses, which indicated that gastrodin was fitted first-order rate transfter process in vivo. Morever, comparison with the Gastrodiae Rhizoma extract, isodose gastrodin in Tiangou Jiangya capsule showed a significant decrease for Cmax, Ke and increase for t1/2Ke, V/Fc, this indicated that compound compatibility can delay the absorbtion of gastrodin, prolong the resident time and promote the distribution in vivo, but its bioavailability is not significantly effected.
Administration, Oral ; Animals ; Benzyl Alcohols ; administration & dosage ; chemistry ; pharmacokinetics ; pharmacology ; Blood Pressure ; drug effects ; Female ; Flavonoids ; chemistry ; pharmacology ; Furans ; chemistry ; pharmacology ; Gastrodia ; chemistry ; Glucosides ; administration & dosage ; chemistry ; pharmacokinetics ; pharmacology ; Lignans ; chemistry ; pharmacology ; Male ; Rats ; Rats, Sprague-Dawley ; Software

OBJECTIVETo investigate the effect of prescription compatibility on the pharmacokinetics of components from Dachengqi Decoction (DCQD, ) in rats.

METHODSTwenty-four male rats were randomly and equally divided into the DCQD group, Dahuang (Radix et Rhizoma Rhei, Polygonaceae) group, Houpo (Magnolia officinalis Rehd., Magnoliaceae) group, and Zhishi (Fructus Aurantii Immaturus, Rutaceae) group. The blood samples were collected before dosing and subsequently at 10, 15, 20, 30, 45 min, 1, 2, 4, 8, and 12 h following gavage. The levels of aloe-emodin, rhein, emodin, chrysophanol, honokiol, magnolol, hesperidin, and naringin in rat serum were quantified using a liquid chromatography tandem mass spectrometry (LC-MS/MS) method for pharmacokinetic study.

RESULTSThe area under the curve (AUC), mean retention time (MRT), the peak concentration (C(max)) of aloe-emodin, rhein, emodin, and chrysophanol in the DCQD group were significantly different compared with the Dahuang group (P <0.05, respectively). The mean plasma concentration, C(max), and the absorption of Dahuang's component in the DCQD group were obviously lower at each time point than those in the Dahuang group, while the elimination process of Dahuang's component was obviously delayed (P <0.05). Half-lives of aloe-emodin, chrysophanol, and rhein were also extended in the DCQD group (P <0.05, respectively). In the DCQD group, the mean plasma concentration, AUC, C(max) and absorption of honokiol, and magnolol were significantly lower (P <0.01, respectively) at each time point than those in the Houpo group, while the drug distribution half-life time (T(1/2α)), the drug eliminated half-life time (T(1/2β)), MRT, and time of peak concentration (T(max)) were significantly delayed (P <0.05, respectively). Pharmacokinetic parameters of hesperidin and naringin in the Zhishi group were not significantly different as compared with the DCQD group (P >0.05, respectively), while the MRT of naringin was significantly longer.

CONCLUSIONSThe compatibility in Chinese medicine could affect the drug's pharmacokinetics in DCQD, which proves that the prescription compatibility principle of Chinese medicine formulations has its own pharmacokinetic basis.

Administration, Oral ; Animals ; Anthraquinones ; administration & dosage ; blood ; pharmacokinetics ; Biphenyl Compounds ; administration & dosage ; blood ; pharmacokinetics ; Drug Incompatibility ; Emodin ; administration & dosage ; blood ; pharmacokinetics ; Flavanones ; administration & dosage ; blood ; pharmacokinetics ; Hesperidin ; administration & dosage ; blood ; pharmacokinetics ; Lignans ; administration & dosage ; blood ; pharmacokinetics ; Male ; Plant Extracts ; administration & dosage ; blood ; chemistry ; pharmacokinetics ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo study the acute and chronic toxicity of Tiangou Jiangya capsule.

METHODTiangou Jiangya capsule was intragastrically administered to mice twice a day. The appearance, behavior, mental status, respiratory changes of mice and the number of poisoned and dead mice in each group were noted daily for 14 consecutive days. The amount of weight and feed of survived mice were recorded every day. The mice were divided into four groups: the treatment groups (minimum, middle, maximum dose of Tiangou Jiangya capsule) and the control group. After continuously orally administrated for 6 months, the rats' behavior, weight gain, food consumption, indications for hematology, blood biochemistry, urine analysis, electrocardiogram, systematic autopsy and histopathology were observed. The above physiological indexes were inspected again 1 month after cease of administration.

RESULTThe oral acute toxicity study of Tiangou Jiangya capsule in mice revealed that the maximum dose is 534.86 g x kg(-1), which was 534.86 times the recommended human maximum dose in clinical practice. Compared with normal control group, no significant differences were observed in rats' behaviors, food-intake, electrocardiogram and relative examination indexes among the treatment groups. There was no difference of hematology, biochemistry test, urine and histopathology.

CONCLUSIONThe minimum dosage of Tiangou Jiangya capsule is relatively safe. It caused weight loss by administrated with the middle and maximum dose for 6 months, which should be paid attention in clinical studies.

Animals ; Antihypertensive Agents ; administration & dosage ; toxicity ; Behavior, Animal ; drug effects ; Benzyl Alcohols ; administration & dosage ; toxicity ; Body Weight ; drug effects ; Drugs, Chinese Herbal ; administration & dosage ; toxicity ; Eating ; drug effects ; Electrocardiography ; drug effects ; Female ; Flavonoids ; administration & dosage ; toxicity ; Furans ; administration & dosage ; toxicity ; Glucosides ; administration & dosage ; toxicity ; Lignans ; administration & dosage ; toxicity ; Male ; Mice ; Mice, Inbred ICR ; Rats ; Rats, Wistar