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1.
Article in Chinese | WPRIM | ID: wpr-862668

ABSTRACT

Objective::To study the pharmacokinetics of sinapic acid from stir-fried Raphani Semen in normal rats and the correlation between pharmacokinetics-pharmacodynamics (PK-PD) in asthma rats. Method::Normal rats received 4.5, 9, 18 g·kg-1 of stir-fried Raphani Semen by oral administration, respectively. Blood was taken from ophthalmic venous plexus at different time points according to the experimental design, the plasma concentration of sinapic acid was analyzed by UHPLC-MS/MS, and data analysis was performed using DAS 3.2.8 software to obtain the pharmacokinetic parameters. Rat asthma model was established by intraperitoneal injection of ovalbumin with aluminum hydroxide, and treated with ethanol extract of stir-fried Raphani Semen (low and high doses of 4.5, 9 g·kg-1). After treatment for 3 weeks, taking blood at different time points, plasma and serum were separated. UHPLC-MS/MS was established for the determination of plasma concentration of sinapic acid, contents of interleukin-5 (IL-5), immunoglobuin E (IgE), tumor necrosis factor-α (TNF-α) in serum at different time points were detected by enzyme-linked immunosorbent assay (ELISA), DAS 3.2.8 software was used for PK-PD model fitting and data analysis. Result::After normal rats were administrated with low, medium and high doses of stir-fried Raphani Semen, the peak concentration (Cmax) of sinapic acid in plasma were (29.35±10.32), (62.70±27.47), (137.33±40.95) μg·L-1, its area under the curve (AUC0-t) were (92.83±27.16), (240.74±75.09), (633.95±195.88) μg·L-1·h, its peak time (Tmax) were (2.58±0.80), (3.00±0), (5.50±1.23) h, respectively. Compared with the low dose group, AUC0-t and mean retention time (MRT0-t) were all increased in the medium and high dose groups, showing statistical differences (P<0.05, P<0.01). The linear relationship of AUC0-t in sinapic acid was good within the dose range of 4.5-18 g·kg-1. After treating with ethanol extract of stir-fried Raphani Semen for 0.083, 0.167 h, compared with the model group of asthmatic rats, serum levels of IL-5, IgE, TNF-α of the medication groups were decreased to different degrees (P<0.05, P<0.01). Cmax of sinapic acid in the low and high dose groups were (58.43±29.94), (61.16±18.79) μg·L-1, its AUC0-t were (188.75±37.07), (247.90±36.89) μg·L-1·h, respectively. AUC0-t, apparent volume of distribution (Vz/F) and clearance rate (CLz/F) all increased significantly with the increase of dose. The best pharmacokinetic model of sinapic acid was fitted as a one-compartment model for extravascular administration, PK-PD model may be applicable to indirect connection model. Conclusion::The plasma concentration of sinapic acid is correlated with contents of IL-5, IgE and TNF-α, dosage and functional state (pathological or physiological state) can affect the pharmacokinetic behavior of sinapic acid from stir-fried Raphani Semen in rats, and it has a certain correlation with the anti-asthmatic effect.

2.
Article in Chinese | WPRIM | ID: wpr-350178

ABSTRACT

To observe the protective effect of scutellarin ethyl ester on focal cerebral ischemia injury induced by middle cerebral artery occlusion in rats(MCAOR), and explore its mechanism. Totally 84 male SD rats were randomly divided into seven groups: sham-operated group, model group,positive drug group(niomdipine,12 mg•kg⁻¹), Brevisapin tablets group(48 mg•kg⁻¹), and high, middle and low-dose scutellarin ethyl ester groups(100, 50, 25 mg•kg⁻¹). The MCAOR model was prepared by using thread embolism method to observe the neurological function of rats, the area of cerebral infarction was measured with TTC, and the levels of MDA, SOD and NO in serum were detected with semiautomatic biochemistry analyzer.Ox-LDL and TNF-α cell injury models was established by treating HUVECs with 200 mg•L⁻¹ ox-LDL and 100 μg•L⁻¹ TNF-α,and the levels of MDA, SOD, NO, ET, 6-keto-PGF1α,TXB2, IL-1, IL-6, IL-8, ICAM-1 and PECAM-1 in the cell supernatant were determined. The results showed that scutellarin ethyl ester could effectively improve the neurological function of MCAOR rats, and significantly reduce the area of cerebral infarction. Compared with the model group, activities of SOD and NO in serum increased, while content of MDA decreased. In the cell supernatant, activities of SOD, 6-keto-PGF1α and NO increased, content of IL-1, IL-6, IL-8, ICAM-1, PECAM-1, TXB2, ET and MDA decreased, which indicated that scutellarin ethyl ester has a certain protective effect on focal cerebral ischemia injury induced by middle cerebral artery occlusion in rats, and its mechanism may be related to antioxidative stress, improvement of endothelial function and reduction in inflammatory reaction.

3.
Article in Chinese | WPRIM | ID: wpr-338220

ABSTRACT

To estabish ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method for simultaneous determination of quercetin(QCT), isorhamnetin(ISR), kaempferol(KMF), ginkgolide A(GA), ginkgolide B(GB), ginkgolide C(GC) and bilobalide(BB) in rat plasma and investigate the pharmacokinetic process of seven compounds after oral administration of Yindan Xinnaotong Ruanjiaonang, The results indicated that all calibrations curves showed good linearity (r≥0.997 1). RSD of intra-day and inter-day precisions were all within 11%. The matrix effects and extraction recovery were in the range of 93.28%-103.6% and 72.43%-95.77% respectively. The peak concentration (Cmax) of QCT, ISR, KMF, GA, GB, GC and BB were (45.02±11.28), (49.90±13.82), (27.85±8.38), (76.31±18.19), (76.54±15.43), (35.35±10.28), (48.70±12.34) μg•L⁻¹, respectively. The peak time (tmax) of seven constituents were (0.33±0.11), (0.50±0.23), (0.33±0.14), (0.75±0.29), (1.0±0.35), (1.5±0.23), (0.75±0.50) h, respectively. UPLC-MS/MS method established in this research was proved to be so rapid and sensitive that it can be applied to the pharmacokinetic study of seven bioactive constituents in Yindan Xinnaotong Ruanjiaonang.

4.
Article in Chinese | WPRIM | ID: wpr-272680

ABSTRACT

To explore the anti-atherosclerotic mechanism of active component compatibility of Danshen and Shanzha (SC121) based on network pharmacology and in vitro research validation with cell model. On one hand, according to the chemical structures and pharmacological activities of the compounds reported in Danshen and Shanzha, 5 compounds, i.e., salvianolic acid B, tanshinone ⅡA, tanshinol, epicatechin and procyanidin B2 were chosen and used for network pharmacology analysis. Then the TCMSP(http://lsp.nwsuaf.edu.cn/tcmsp.php)was used for finding the network targets for 5 compounds from SC121. The signaling pathway associated with cardiovascular disease was analyzed by KEGG mapping, the biological process associated with cardiovascular disease was analyzed by Uniprot. And, the mechanism of SC121 was predicted by network pharmacology. In vitro cell model was subsequently performed for validation. HUVEC and RAW264.7 cell injuries and foam cell formation were constructed by ox-LDL, and the intervention effects of SC121 were assayed. The result showed that SC121 not only alleviated the damage of HUVEC and RAW264.7, lowered the ROS level, but also decreased the area of foam cell in a dose-dependent manner, which indicated that SC121 could inhibit the damage of endothelial cells and lower the oxidative stress. The experimental data validated the prediction of network pharmacology, and elucidated the mechanism of SC121's effect on AS.

5.
Article in Chinese | WPRIM | ID: wpr-246097

ABSTRACT

The UHPLC-LTQ-Orbitrap high resolution mass spectrometer was used to explore the chemical compositions in safflower. The rapid separation of the compositions was conducted by the UHPLC, following by high resolution full scan and MS2 scan, under the positive and negative ion mode. The chemical formula of compositions were deduced by full scan data in less than 5, then the potential structures were confirmed by the MS2 data. Forty-nine compounds were detected, of which 26 was identified, and 5 compounds was validated by the standard substances.


Subject(s)
Carthamus tinctorius , Chemistry , Chromatography, High Pressure Liquid , Methods , Drugs, Chinese Herbal , Chemistry , Molecular Structure , Tandem Mass Spectrometry , Methods
6.
Article in Chinese | WPRIM | ID: wpr-299775

ABSTRACT

To explore the prevention effect of the joint combination of Yindanxinnaotong soft capsule (YDXNT) and exercise (swimming) on atherosclerotic rats. The method of 3 x 3 factorial design, including two factors (YDXNT and swimming) and three levels (0, 1, 2 g x kg(-1) YDXNT; 0, 0.5, 1 h swimming), was mainly adopted. The atherosclerotic rat model was established by ligating their left common carotid arteries and feeding high-fat diet. After 8 weeks, blood samples were collected from their thoracic aorta to determine blood viscosity, plasma viscosity, fibrinogen (FIB), nitric oxide (NO), 6-keto-PGF(1alpha) endothelin (ET) and thromboxane B2 (TXB2). The tissues of left common carotid arteries of the rats were collected to detect the positive expression of SM22alpha and determine the semi-quantitation through the immunohistochemical staining. The result showed that the combination of YDXNT and swimming can significantly decrease the plasma viscosity (F = 3.241, P = 0.017), the high and low shear blood viscosity (F = 6.444, P = 0.001; F = 3.002, P = 0.024) and FIB (F = 4.046, P = 0.005). The increased NO and 6-keto-PGF(1alpha) and the decreased ET and TXB2 indicated a significant interaction (P < 0.05). The swimming showed an obvious main effect in the expression of up-regulated protein SM22alpha (F = 8.088, P = 0.001). The study suggested that the combined administration of YDXNT and swimming could improve the hemorheological parameters of atherosclerotic rats, protect the vascular endothelium, inhibit the vascular remodeling in atherosclerosis and positively prevent the atherosclerosis.


Subject(s)
Animals , Atherosclerosis , Drug Therapy , Genetics , Metabolism , Blood Viscosity , Combined Modality Therapy , Drugs, Chinese Herbal , Exercise Therapy , Humans , Male , Microfilament Proteins , Genetics , Metabolism , Muscle Proteins , Genetics , Metabolism , Rats , Rats, Sprague-Dawley , Swimming
7.
Article in Chinese | WPRIM | ID: wpr-300204

ABSTRACT

<p><b>OBJECTIVE</b>To study the protected effect of Yindan Xinnaotong capsule (YDXNTC) and main components compatibility on myocardium ischemia/reperfusion injury.</p><p><b>METHOD</b>Global ischemia/reperfusion was adopted to induce myocardial ischemia/reperfusion injury (MIRI) in isolated rat heart. Sprague-Dawley (SD) rats were divided into control, model, YDXNTC, Ginkgo biloba extract (GBE) group, ethanol extract of Salvia miltiorrhiza (SM-E) group, aqueous extract of Salvia miltiorrhiza (SM-H) group, mixed compatibility of other components in YDXNTC (MC), GBE and SM-E compatibility (GSEC), GBE and SM-H compatibility (GSHC), and SM-E and SM-H compatibility (SEHC). During the experiment, electrocardiogram was recorded to observe cardiac arrest time, heart resuscitation time, regaining normal rhythm time, the incidence and duration of arrhythmias (VT/VF). At the end of reperfusion, hearts were arrested and homogenated to assay the activity of superoxide dismutase (SOD), and the content of malondialdehyde (MDA), lactate dehydrogenase (LDH), creatine kinase-MB (CK-MB), cardiac troponin I.</p><p><b>RESULT</b>(1) YDXNTC, SM-E, SM-H and MC elevated cardiac arrest time, also reduced rebeating time, restoring normal rhythm time as well as the duration of arrhythmia, but no remarkable impact on VT/VF occurrence. GBE was effective for incidence of VT/VF, also achieved good effect on shortening rebeating time, restoring normal rhythm time and arrhythmia duration. Likewise, obviously reduced rebeating time, restoring normal rhythm time and arrhythmia duration, and evaluated cardiac arrest time were also exhibited in compatibility groups except that no lengthened cardiac arrest time was detected in GSHC. And the incidence of VT/VF was decreased by GSEC. (2) YDXNT, ginkgo biloba extract (GBE), ethanol extract of salvia miltiorrhiza (SM-E), GBE and SM-E compatibility (GSEC), and SM-E and aqueous extract of salvia miltiorrhiza (SM-H) compatibility (SEHC) could improved SOD and decreased MDA level SM-H, mixed compatibility of other elements in YDXNTC (MC) and GBE and SM-H compatibility (GSHC) showed a role on MDA reduction. (3) LDH was declined by YDXNT and SM-H. CK-MB was reduced by GBE, SM-E, SM-H, and GSEC. (4) The release of cTnI was only inhibited by GSEC.</p><p><b>CONCLUSION</b>YDXNTC, primary materials and main components compatibility has a certain protection effect on MIRI, its mechanism may be related to antioxidant and calcium overload reduction.</p>


Subject(s)
Animals , Arrhythmias, Cardiac , Capsules , Creatine Kinase, MB Form , Metabolism , Drugs, Chinese Herbal , Pharmacology , Electrocardiography , Ginkgo biloba , Chemistry , Heart , In Vitro Techniques , L-Lactate Dehydrogenase , Metabolism , Male , Malondialdehyde , Metabolism , Myocardial Reperfusion Injury , Metabolism , Myocardium , Metabolism , Pathology , Phytotherapy , Plant Extracts , Pharmacology , Protective Agents , Pharmacology , Rats , Rats, Sprague-Dawley , Salvia miltiorrhiza , Chemistry , Superoxide Dismutase , Metabolism , Troponin I , Metabolism
8.
Acta Pharmaceutica Sinica ; (12): 917-924, 2013.
Article in Chinese | WPRIM | ID: wpr-259529

ABSTRACT

The current study aims to investigate the pharmacokinetic properties of Huangqin Tang on different oral doses. An LC-MS method for simultaneous determination of flavonoids and terpenoids in rat plasma was developed and validated. Plasma samples were treated with hydrochloric acid (containing 1% ascorbic acid), precipitated with acetonitrile, separated on a Zorbax SB-C18 column, detected by single quadruple mass spectrometry with an electrospray ionization interface, and quantified using selected ion monitoring mode. All pharmacokinetic parameters were processed by non-compartmental analysis using WinNonlin software. The results of specificity, linearity, intra-day and inter-day precisions, accuracy, and stability for LC-MS assay were suitable for the quantification of paeoniflorin, baicalin, wogonoside, baicalein, wogonin, oroxylin A, glycyrrhizic acid and glycyrrhetinic acid in rat plasma. The concentration-time profiles of baicalin, wogonoside, baicalein, wogonin, oroxylin A and glycyrrhizic acid showed double-peak phenomenon after Huangqin Tang was orally administered at 40 g x kg(-1) dose; all eight constituents in rat plasma showed good dose-exposure relationship within the dosage of 10-40 g x kg(-1); although plasma concentrations were different, the flavonoids with the same backbone showed the similar fate in the body with the corresponding dosage. In conclusion, the LC-MS assay was successfully applied for the pharmacokinetic study of multi-constituents of Huangqin Tang with different doses. Additionally, these constituents demonstrated good pharmacokinetic properties in the body.


Subject(s)
Administration, Oral , Animals , Chromatography, Liquid , Dose-Response Relationship, Drug , Drugs, Chinese Herbal , Chemistry , Flavanones , Blood , Pharmacokinetics , Flavonoids , Blood , Pharmacokinetics , Glucosides , Blood , Pharmacokinetics , Glycyrrhetinic Acid , Blood , Pharmacokinetics , Glycyrrhizic Acid , Blood , Pharmacokinetics , Male , Monoterpenes , Blood , Pharmacokinetics , Pentacyclic Triterpenes , Blood , Pharmacokinetics , Rats , Rats, Wistar , Spectrometry, Mass, Electrospray Ionization
9.
Article in Chinese | WPRIM | ID: wpr-346458

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the effect of active components of Danshen and Shanzha of different matching proportions on atherosclerosis (AS), in the expectation of obtaining the optimum combination method.</p><p><b>METHOD</b>Atherosclerotic rats were fed with high fat diet, and injected with vitamin D3 and ovalbumin. Aqueous extracts of Danshen (DSA) and Shanzha (SZA) and lipophilic extracts of danshen (DSL) were adopted for a low, medium and high-dose orthogonal experiment, to observe the effect of their different matching proportions on lipid level, oxidative stress, endothelial function and inflammatory reaction. The principal component analysis and cluster analysis were adopted for the multi-objective optimization of experimental results.</p><p><b>RESULT</b>Compared with the model group, all of samples with different proportions of DSA, DSL and SZA showed effect in lowering lipid level, scavenging free radicals, reducing endothelial dysfunction and inhibiting inflammation. According to the variance analysis, DSA2-SZA2-DSL1, DSA3-SZA2-DSL1, DSA3-SZA3 -DSL3 and DSA3-SZA1-DSL1 were the optimal proportions for lowering lipid level, scavenging free radicals, reducing endothelial dysfunction and inhibiting inflammation, respectively. According to the results of the multi-objective optimization, DSA2-SZA1-DSL2 was the optimal proportions of anti-AS.</p><p><b>CONCLUSION</b>All of active components of Danshen and Shanzha of different matching proportions show the anti-AS effect in rats to varying degrees, but with different focus in different matching proportions.</p>


Subject(s)
Animals , Anti-Inflammatory Agents , Pharmacology , Antioxidants , Pharmacology , Atherosclerosis , Drug Therapy , Drugs, Chinese Herbal , Therapeutic Uses , Endothelium, Vascular , Lipids , Blood , Male , Phenanthrolines , Therapeutic Uses , Phytotherapy , Rats , Salvia miltiorrhiza , Chemistry
10.
Article in Chinese | WPRIM | ID: wpr-350693

ABSTRACT

<p><b>OBJECTIVE</b>To establish a method to determine underivatized endogenous amino acids in brain tissues after cerebral ischemia based on RRLC-QQQ.</p><p><b>METHOD</b>Diamonsil chromatographic column C18 (4.6 mm x 250 mm, 5 microm) was adopted to determine 12 amino acids in 15 min, with acetonitrile-0.1% formic acid for gradient elution. The flow rate was set at 0.5 mL x min(-1). With ESI as the ion source, positive ion scanning mode was adopted for multi-reaction monitoring.</p><p><b>RESULT</b>Each amino acid standard curve (AAs) showed good linear relationship within the detection range (r > 0.996), with the limit of detection of less than 11%, the limit of quantitation of less than 3.09 microg x L(-1). The RSD of intra- and inter-day precisions at high, middle and low concentrations were less than 11%.</p><p><b>CONCLUSION</b>The determination results of actual samples showed that compared with the levels of AAs of the sham operation group, all of the remaining amino acids apart from N-acetyl-aspartate increased in brain tissues. Some amino acids showed significant changes in a time-dependent manner after the operation. The method is so simple, rapid and sensitive that it can be used for finding biological metabolite markers of cerebral ischemia, and exploring cerebral ischemia molecular mechanisms and synergistic mechanism of combined administration of multi-component traditional Chinese medicines.</p>


Subject(s)
Amino Acids , Metabolism , Animals , Brain , Metabolism , Brain Ischemia , Metabolism , Chromatography, High Pressure Liquid , Methods , Male , Rats , Rats, Sprague-Dawley , Reproducibility of Results , Tandem Mass Spectrometry , Methods
11.
Journal of Medical Biomechanics ; (6): E344-E349, 2013.
Article in Chinese | WPRIM | ID: wpr-804307

ABSTRACT

Objective To study effects of flow shear stress combined with salvianolic acid B (Sla B) on anti-platelet aggregation and its possible mechanism under the theoretical framework of biomechanopharmacology. Methods 2×4 factor experimental design was employed. By using Bioflux 1000 microfluidic system, shear stresses of 0.02 Pa and 1.5 Pa were applied together with four levels of Sla B concentration treatment on human vascular endothelial cells (HUVECs) for 20 hours. Then the cell supernatant was collected to detect concentration of 6-keto-PGF1α and vWF by ELISA and their effects on ADP-induced platelet aggregation were tested. Immunofluorescence method was used to detect vWF in endothelial cell cytoplasm. Results Physical shear stress of 1.5 Pa combined with Sla B of 100 μg/mL could significantly promote the endothelial secretion of 6-keto-PGF1α as compared to low shear stress condition (P<0.05). The endothelial cell supernatant under shear stress of 1.5 Pa showed an obvious anti-platelet aggregation effect. As the single factor, shear stresses significantly influenced vWF secretion (P<0.01), but Sla B had no obvious effects on vWF secretion. Conclusions Sla B inhibited ADP-induced platelet aggregation by increasing endothelial secretion of PGI2 under physical shear stresses. From the view of biomechaopharmacology (interaction between blood flow, blood vessel and blood), the physical flow shear stress is beneficial for the anti-thrombosis effect of Sla B.

12.
Article in Chinese | WPRIM | ID: wpr-346891

ABSTRACT

<p><b>OBJECTIVE</b>To establish a LC-MS/MS method for determining the concentration of tanshinone IIA, salvianolic acid B and paeoniflorin of refined coronary cataplasm in rabbit plasma, in order to determine the concentration of the three main ingredients in blood after transdermal administration and calculate their pharmacokinetic parameters.</p><p><b>METHOD</b>Rabbits were given refined coronary cataplasm on the basis of 15 g x kg(-1) by transdermal administration to detect the plasma concentration of the three main ingredients using LC-MS/MS. Winnonlin software was used to calculate their major pharmacokinetic parameters.</p><p><b>RESULT</b>Tanshinone IIA, salvianolic acid B and paeoniflorin showed good linearity (r>0.999) at 1-100, 50-1 000, 10-1 000 microg x L(-1) respectively in plasma, with average recovery rate of 96.57%, 91.90%, 95.93%, respectively. The RSD within day were less than 15%. After transdermal administration of refined coronary cataplasm in rabbits, the main pharmacokinetic parameters of tanshinone IIA, salvianolic acid B or paeoniflorin were as follows: Cmax (20.85 +/- 12.68), (636.25 +/- 386.91), (787.80 +/- 395.64) microg x L(-1); Tmax (0.49 +/- 0.28), (0.44 +/- 0.27), (0.46 +/- 0.30) h.</p><p><b>CONCLUSION</b>The LC-MS/MS method is highly selective and sensitive to determine the concentration of samples in rabbit plasma. The pharmacokinetic characteristics of tanshinone IIA, salvianolic acid B and paeoniflorin are suitable to assess the percutaneous absorption of refined coronary cataplasm.</p>


Subject(s)
Animals , Benzoates , Pharmacokinetics , Benzofurans , Pharmacokinetics , Bridged-Ring Compounds , Pharmacokinetics , Chromatography, Liquid , Methods , Coronary Disease , Drug Therapy , Abietanes , Pharmacokinetics , Drugs, Chinese Herbal , Pharmacokinetics , Glucosides , Pharmacokinetics , Humans , Male , Monoterpenes , Rabbits , Tandem Mass Spectrometry , Methods
13.
Article in Chinese | WPRIM | ID: wpr-308666

ABSTRACT

<p><b>OBJECTIVE</b>To establish an absorption-metabolic model suitable for studying the complex traditional Chinese medicine (TCM) system, with the classic Jinlingzi Powder formula as the example, in order to explore the correlation among absorption behavior and absorption-metabolism behavior of different Jinlingzi Powder formulas and their compound compatibility.</p><p><b>METHOD</b>An absorption-metabolic model suitable for TCM study was established according to in vivo characteristics of drugs, to combine the intestinal absorption model with the liver microsomal metabolism model. A quantitative analysis was conduced for absorbable components of Jinlingzi Powder and its absorption-metabolism components by HPLC.</p><p><b>RESULT</b>The model could be used for studies on the absorption-metabolism process of TCM. Among the 15 main components which were derived from Jinlingzi Powder extracts, 10 could be absorbed by intestinal tract. A new component peak was shown after metabolism with the A-M model. The absorbable components of Jinlingzi Powder were related to its compatibility. Toosendan was found to be the major factor impacting the main component-absorption ratio (Ar) and absorption-metabolism ratio (Mr), followed by Rhizoma Corydalis.</p><p><b>CONCLUSION</b>The absorption-metabolism model suitable for studying the complex traditional Chinese medicine system was established and used for the study on compound compatibility of Jinglingzi Powder. The compatibility of the formula has an impact on absorbable component ratio of Jinlingzi Powder, which helps interpret the theory of formula compatibility from the angle of in vitro compound pharmacokinetics (the difference between absorption and metabolism). Toosendan is the main factor impacting overall absorption and absorption-metabolism, while Rhizoma Corydalis is the minor factor.</p>


Subject(s)
Animals , Corydalis , Chemistry , Drugs, Chinese Herbal , Metabolism , Pharmacokinetics , Humans , Intestinal Absorption , Intestines , Metabolism , Male , Melia , Chemistry , Models, Animal , Powders , Pharmacokinetics , Rats , Rats, Wistar
14.
Article in Chinese | WPRIM | ID: wpr-284418

ABSTRACT

<p><b>OBJECTIVE</b>To research the expectorant components in volatile oil from the root and rhizome of Aster tataricus.</p><p><b>METHOD</b>GC-MS was applied to isolate and identify the compounds. In addition, TLC was used to isolate compound, and its structure was elucidated on the basis of spectral data analysis. At the same time, its expectorant effect was observed by method of the excretion quantity of phenol red in trachea of mice.</p><p><b>RESULT</b>Seven compounds were isolated and identified by GC-MS, they were (R)(-)-p-menth-1-en-4-ol (1), 2-undecanone (2), n-decanoic acid (3), (-)-spathulenol (4), hexahydrofamrnesyl acetone (5), hexadecanoic acid (6), and cis-9, cis-12-octaecadienoic acid (7). A known compound 1-acetoxy-2-ene(E)-4,6- decandiyne was isolated from the root and rhizome of A. tataricus, and it was shown to have expectorant effect.</p><p><b>CONCLUSION</b>1-Acetoxy-2-ene(E) -4,6- decandiyne, a main compound in volatile oil, had been found to have expectorant effect.</p>


Subject(s)
Animals , Aster Plant , Chemistry , Drugs, Chinese Herbal , Chemistry , Pharmacology , Expectorants , Chemistry , Pharmacology , Gas Chromatography-Mass Spectrometry , Magnetic Resonance Spectroscopy , Male , Mice , Oils, Volatile , Chemistry , Plant Roots , Chemistry , Rhizome , Chemistry
15.
Article in Chinese | WPRIM | ID: wpr-284387

ABSTRACT

<p><b>OBJECTIVE</b>To observe the protective effects of catechin morphon (GCG and EGCG) on hypoxia-reoxygenation induced injury in myocardial cells and to explore the mechanisms.</p><p><b>METHOD</b>In cultured neonatal rat cardiomyocytes, we investigated the preconditioning protection by GCG and EGCG on the spontaneous beating, the survival rate, the release of LDH, MDA, SOD, GSH-Px and the ATP enzyme activity of cardiomyocyte cellular membrane in cultured rat cardiomyocytes treated during the reoxygenation 1h following hypoxia 3 h. The blocking agent of protien kinase C staurosporine (10 nmol x L(-1)) or the deactivator of Gi/o protein pertussis toxin (PTX, 200 microg x mL(-1)) were added before the catechin treatment.</p><p><b>RESULTS</b>Preconditioning by GCG and EGCG increased the spontaneous beating and the survival rate, and decreased the release of LDH and MDA with the rise of SOD and ATP enzyme activity. Inhibition of PKC by staurosporine and Gi/o protein by PTX abolished the protection by catechin with the reduction of the beating, survival rate and activity of SOD, and the increase of the release of LDH and MDA. The results indicated that the activation of signal transduction pathway from PKC and Gi/o protein seemed to be involved in the cardioprotection of preconditioning by GCG and EGCG.</p><p><b>CONCLUSION</b>The protection by GCG and EGCG on hypoxia-reoxygenation injury in cultured neonatal rat cardiomyocytes is found, which is related with scavenging of free radicals, and PKC Gi/o signal transduction pathway.</p>


Subject(s)
Animals , Cardiotonic Agents , Chemistry , Pharmacology , Catechin , Chemistry , Pharmacology , Female , Free Radicals , Metabolism , Hypoxia , Myocytes, Cardiac , Metabolism , Pathology , Oxygen , Metabolism , Protein Kinase C , Metabolism , Proteins , Metabolism , Rats , Signal Transduction , Survival Rate
16.
Article in Chinese | WPRIM | ID: wpr-283849

ABSTRACT

<p><b>OBJECTIVE</b>To observe the antioxidant effects of water extract of Carthamus tinctorius on ox-LDL induced injury in rat cardiac microvascular endothelial cell and detecting oxygen derived free radicals (OFR) to explore the antioxidant mechanisms.</p><p><b>METHOD</b>By using the third generation of rat cardiac microvascular endothelial cells (rCMEC), the protection of water extract of C. tinctorius was investigated after ox-LDL (100 mg x L(-1) induced damage. The supernatant was collected for detecting lactate dehydrogenase (LDH), malondialdehyde (MDA), superoxide dismutase (SOD), xanthine oxidase (XOD), glutathione peroxidase (GSH-Px), nitric oxide (NO), nitric oxide synthase (NOS) activity, and cell suspension was collected for detecting reactive oxygen species (ROS) by electron spin resonance (ESR).</p><p><b>RESULT</b>Water extract of C. tinctorius increased the rCMEC survival rate, reduced LDH, MDA and XOD levels, and improved SOD, GSH-Px and NOS activity, while in the cell suspension ROS signal decreased significantly.</p><p><b>CONCLUSION</b>Water extract of C. tinctorius has antioxidation. The mechanisms are likely related with scavenging of free radicals, enhancing its clearance, enhancing endogenous antioxidant activity.</p>


Subject(s)
Animals , Carthamus tinctorius , Chemistry , Drugs, Chinese Herbal , Chemistry , Pharmacology , Electron Spin Resonance Spectroscopy , Methods , Endothelial Cells , Metabolism , Enzyme Activation , Glutathione Peroxidase , Metabolism , L-Lactate Dehydrogenase , Metabolism , Lipoproteins, LDL , Pharmacology , Microvessels , Cell Biology , Nitric Oxide Synthase , Metabolism , Rats , Rats, Wistar , Reactive Oxygen Species , Metabolism , Superoxide Dismutase , Metabolism , Water , Chemistry , Xanthine Oxidase , Metabolism
17.
Article in Chinese | WPRIM | ID: wpr-295465

ABSTRACT

<p><b>OBJECTIVE</b>To study on the chemical stability of Salvia miltirrhiza hairy root.</p><p><b>METHOD</b>The rolA gene was detected by PCR in DNA and the chemical contituent variances were detected by HPLC.</p><p><b>RESULT</b>The rolA gene was found in all the 10 batches of the culfured hairy root. The similarities of the chromatographic fingerprints of the 10 batches are higher than 0. 95.</p><p><b>CONCLUSION</b>There are no significant differences of the chemical constituents in 10 hairy root samples.</p>


Subject(s)
Chromatography, High Pressure Liquid , DNA, Plant , Genetics , Drugs, Chinese Herbal , Chemistry , Genes, Plant , Plant Roots , Chemistry , Genetics , Polymerase Chain Reaction , Reproducibility of Results , Salvia miltiorrhiza , Chemistry , Genetics , Sensitivity and Specificity
18.
Article in Chinese | WPRIM | ID: wpr-252176

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the effect of prim-O-glucosylcimifugin and 4'-O-p-D-glucosyl-5-O-methylvisa-mminol con on the proliferation of smooth muscle cell stimulated by TNF-alpha.</p><p><b>METHOD</b>The primary cell culture method of smooth muscle cell (SMC) was established by attachment-block. The SMC was identificated by immunochemistry method, and the growth curve was drawn by cytometry. The third generation of SMC was adopted in the experiment. The effect of prim-O-glucosylcimif-ugin and 4'-O-beta-D-glucosyl-5-O-methylvisamminol con on the proliferation and cell cycle of SMC was investigated by MTT and flow cytometry respectively.</p><p><b>RESULT</b>TNF-alpha of 5 micro g x L(-1) can stimulate the proliferation of SMC and increase the proportion of G2 phase and S phase in cell cycle which has great significant difference (P < 0.01) compared with control. The three dose groups of prim-O-glucosylcimifugin and 4'-O-beta-D-glucosyl-5-O-methylvisammin-ol con can inhibit the proliferation of SMC and increase the proportion of G0/G1 phase, which has great significant difference (P < 0.01) compared with model group.</p><p><b>CONCLUSION</b>Prim-O-glucosylcimifugin and 4'-O-beta-D-glucosyl-5-O-methylvisamminol con can inhibit the proliferation of SMC stimulated by TNF-alpha.</p>


Subject(s)
Animals , Cell Proliferation , Cells, Cultured , Drugs, Chinese Herbal , Pharmacology , Female , Male , Monosaccharides , Pharmacology , Myocytes, Smooth Muscle , Cell Biology , Rats , Rats, Wistar , Tumor Necrosis Factor-alpha , Pharmacology , Xanthenes , Pharmacology
19.
Article in Chinese | WPRIM | ID: wpr-252147

ABSTRACT

<p><b>OBJECTIVE</b>To study the relationship between the antioxidant activities and the contents of active ingredients in Radix Scutellaria.</p><p><b>METHOD</b>The antioxidant activities of extracts and active ingredients of Radix Scutellaria in NADPH-dependent lipid peroxidation in rat liver microsome were assayed.</p><p><b>RESULT</b>Extracts of Radix Scutellaria showed a 50% inhibition of lipid peroxidation in the concentration range of 2.72-18.27 mg x L(-1).</p><p><b>CONCLUSION</b>The antioxidant activities of extracts of Radix Scutellaria are not only related with the contents but also the ratio of the active ingredients.</p>


Subject(s)
Animals , Antioxidants , Chemistry , Pharmacology , Drugs, Chinese Herbal , Pharmacology , Lipid Peroxidation , Microsomes, Liver , Metabolism , Rats , Rats, Wistar , Scutellaria , Chemistry
20.
Article in Chinese | WPRIM | ID: wpr-269080

ABSTRACT

Gushukang is a compound Chinese herbal preparation. Pharmacological studies indicated that Gushukang can increase bone density, inhibit bone resorption, promote bone formation, and restore bone microstructure, as well as improve bone biomechanical parameters and promote healing of bone fracture. Clinical observations demonstrated that it has favorable efficacy in preventing and treating osteoporosis.


Subject(s)
Bone Density , Bone Resorption , Drugs, Chinese Herbal , Therapeutic Uses , Humans , Osteogenesis , Osteoporosis , Drug Therapy , Phytotherapy
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