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1.
Article in Chinese | WPRIM | ID: wpr-888165

ABSTRACT

The efficacy of gastrodin as a Chinese herbal medicine extract in the treatment of tension-type headache has been confirmed. This paper systematically reviewed the efficacy and safety of gastrodin in the treatment of tension-type headache, aiming to provide a new choice for the treatment of this disease. In this study, four Chinese databases, four English databases and two trial registries were searched from the date of establishment to September 2020. The related randomized controlled trials(RCTs) were screened out according to the predetermined criteria. The bias risk assessment tool developed by Cochrane collaboration was used to evaluate the quality of the reports. RevMan 5.4.1 was used for Meta-analysis, and GRADE system for the evidence-based evaluation on the quality of outcome indicators. A total of 177 articles were retrieved and 8 articles were finally included for analysis, with a total sample size of 1 091 cases, which included 565 cases in the treatment group and 526 cases in the control group. The overall quality of included stu-dies was not high. The results of Meta-analysis are as follows:(1)In terms of headache frequency, gastrodin group was better than wes-tern medicine group(MD=-2.90, 95%CI[-3.76,-2.03], P<0.000 01).(2)In terms of number of abnormal blood vessels in TCD, gastrodin group was better than western medicine group(MD=-88.96, 95%CI[-102.36,-75.55], P<0.000 01).(3)In terms of effective rate, gastrodin group was better than western medicine group(RR=1.47, 95%CI[1.29, 1.68], P<0.000 01). The results of subgroup analysis are as follows:(1)Effective rate based on age, for the patients upper age limit 40-46 years old, gastro-din group was better than western medicine group(RR=1.69, 95%CI[1.50, 1.90], P<0.000 01); for the patients upper age limit 55-60 years old, gastrodin group was better than western medicine group(RR=1.27, 95%CI[1.16, 1.38], P<0.000 01).(2)Effective rate based on dosage form, both the gastrodin capsules and injection groups were better than western medicine group(RR_(capsules)=1.42, 95%CI[1.08, 1.88], P=0.01; RR_(injection)=1.50, 95%CI[1.26, 1.77], P<0.000 01). GRADE evaluation showed that the above outcomes had low quality of evidence. Only one article detailed the occurrence of adverse reactions and thus the present study cannot make a positive conclusion on the safety of gastrodin in the treatment of tension-type headache. The small number and low quality of the included reports affected the reliability of the results. In the future, more high-quality randomized controlled trails are needed to improve the evaluation on the efficacy and safety of gastrodin in the treatment of tension-type headache.


Subject(s)
Adult , Benzyl Alcohols/therapeutic use , Drugs, Chinese Herbal/adverse effects , Glucosides , Humans , Middle Aged , Reproducibility of Results , Tension-Type Headache
2.
Article in Chinese | WPRIM | ID: wpr-878990

ABSTRACT

Gastrodiae Rhizoma-Uncariae Ramulus cum Uncis is the most frequently used herbal pair in the treatment of Parkinson's disease(PD). Gastrodin and isorhynchophylline are important components of Gastrodiae Rhizoma-Uncariae Ramulus cum Uncis herb pair with anti-Parkinson mechanism. This study aimed to investigate the effect of gastrodin combined with isorhynchophylline on 1-methyl-4-phenylpyridinium(MPP~+)-induced apoptosis of PC12 cells and their antioxidant mechanism. The leakage of lactate dehydrogenase(LDH) from cells to media was analyzed by spectrophotometry. Apoptotic cells were labeled with Annexin V-fluorescein isothiocyanate(FITC) and propidium iodide(PI) and analyzed by flow cytometry. The cell cycle was analyzed using propidium iodide(PI) staining. Lipid peroxidation(LPO) level was analyzed by spectrophotometry. The mRNA expression of caspase-3 was examined by Real-time RT-PCR. The protein expressions of heme oxygenase 1(HO-1) and NADPH: quinoneoxidore-ductase 1(NQO-1) were determined by Western blot. Gastrodin combined with isorhynchophylline reduced the percentage of Annexin V-positive cells and cell cycle arrest in MPP~+-induced PC12 cells. Gastrodin combined with isorhynchophylline down-regulated the mRNA expression of caspase-3, up-regulated the protein expressions of HO-1 and NQO-1, and reduced LPO content in MPP~+-induced PC12 cells. PD98059, LY294002 or LiCl could partially reverse these changes pretreated with gastrodin combined with isorhynchophylline, suggesting that gastrodin combined with isorhynchophylline inhibited MPP~+-induced apoptosis of PC12 cells and oxidative stress through ERK1/2 and PI3 K/GSK-3β signal pathways. Our experiments showed that gastrodin combined with isorhynchophylline could down-re-gulate the mRNA expression of caspase-3 and up-regulate the protein expressions of HO-1 and NQO-1, so as to reduce oxidative stress and inhibit apoptosis.


Subject(s)
1-Methyl-4-phenylpyridinium/toxicity , Animals , Antioxidants , Apoptosis , Benzyl Alcohols , Cell Survival , Glucosides , Glycogen Synthase Kinase 3 beta , Oxindoles , PC12 Cells , Rats
3.
Neuroscience Bulletin ; (6): 461-470, 2019.
Article in English | WPRIM | ID: wpr-775428

ABSTRACT

Gastrodin is a phenolic glycoside that has been demonstrated to provide neuroprotection in preclinical models of central nervous system disease, but its effect in subarachnoid hemorrhage (SAH) remains unclear. In this study, we showed that intraperitoneal administration of gastrodin (100 mg/kg per day) significantly attenuated the SAH-induced neurological deficit, brain edema, and increased blood-brain barrier permeability in rats. Meanwhile, gastrodin treatment significantly reduced the SAH-induced elevation of glutamate concentration in the cerebrospinal fluid and the intracellular Ca overload. Moreover, gastrodin suppressed the SAH-induced microglial activation, astrocyte activation, and neuronal apoptosis. Mechanistically, gastrodin significantly reduced the oxidative stress and inflammatory response, up-regulated the expression of nuclear factor erythroid 2-related factor 2, heme oxygenase-1, phospho-Akt and B-cell lymphoma 2, and down-regulated the expression of BCL2-associated X protein and cleaved caspase-3. Our results suggested that the administration of gastrodin provides neuroprotection against early brain injury after experimental SAH.


Subject(s)
Animals , Apoptosis , Astrocytes , Metabolism , Benzyl Alcohols , Blood-Brain Barrier , Metabolism , Brain , Metabolism , Brain Edema , Calcium , Metabolism , Glucosides , Glutamic Acid , Metabolism , Male , Microglia , Metabolism , Neurons , Neuroprotective Agents , Oxidative Stress , Rats, Sprague-Dawley , Subarachnoid Hemorrhage , Metabolism
4.
Article in Chinese | WPRIM | ID: wpr-771476

ABSTRACT

OBJECTIVE@#To explore the role of mitochondrial permeability transition pore (mPTP) in mediating the protective effect of gastrodin against oxidative stress damage in H9c2 cardiac myocytes.@*METHODS@#H9c2 cardiac myocytes were treated with HO, gastrodin, gastrodin+HO, cyclosporin A (CsA), or CsA+gas+HO group. MTT assay was used to detect the survival ratio of H9c2 cells, and flow cytometry with Annexin V-FITC/PI double staining was used to analyze the early apoptosis rate after the treatments. The concentration of ATP and level of reactive oxygen species (ROS) in the cells were detected using commercial kits. The mitochondrial membrane potential of the cells was detected with laser confocal microscopy. The expression of cytochrome C was detected with Western blotting, and the activity of caspase-3 was also assessed in the cells.@*RESULTS@#Gastrodin pretreatment could prevent oxidative stress-induced reduction of mitochondrial membrane potential, and this effect was inhibited by the application of CsA. Gastrodin significantly lowered the levels of ROS and apoptosis-related factors in HO-exposed cells, and such effects were reversed by CsA. CsA significantly antagonized the protective effect of gastrodin against apoptosis in HO-exposed cells.@*CONCLUSIONS@#Gastrodin prevents oxidative stress-induced injury in H9c2 cells by inhibiting mPTP opening to reduce the cell apoptosis.


Subject(s)
Adenosine Triphosphate , Apoptosis , Benzyl Alcohols , Pharmacology , Caspase 3 , Cell Line , Cell Survival , Cyclosporine , Pharmacology , Cytochromes c , Glucosides , Pharmacology , Humans , Hydrogen Peroxide , Pharmacology , Membrane Potential, Mitochondrial , Mitochondrial Membrane Transport Proteins , Physiology , Myocytes, Cardiac , Metabolism , Oxidative Stress , Reactive Oxygen Species
5.
Braz. oral res. (Online) ; 32: e104, 2018. tab, graf
Article in English | LILACS | ID: biblio-974458

ABSTRACT

Abstract This study evaluated the three-year lifespan of the bond to dentin of experimental self-etch adhesives containing benzodioxole derivatives - 1,3-benzodioxole (BDO) and piperonyl alcohol (PA) - as co-initiator alternative to amines. Adhesive resins were formulated using Bis-GMA, TEGDMA, HEMA, camphorquinone and different co-initiators: BDO, PA or ethyl 4-dimethylamino benzoate (EDAB - amine). An experimental self-etch primer was used to complete the two-step, self-etch adhesive system. Clearfil SE Bond (CSE) was used as commercial reference. Bond strength to human dentin was assessed by microtensile bond strength (µTBS) test, and failure mode was classified. Morphology of the dentin bonding interface was assessed via scanning electron microscopy (SEM). Irrespective of the dental adhesives evaluated, µTBS was higher after 24 hours compared with that after 1.5 and 3 years (p ≤ 0.001). However, adhesives with BDO and PA as co-initiators showed significantly higher bond strength than the bonding resin with EDAB (p ≤ 0.002), independent of the time evaluated. The commercial adhesive CSE showed similar bond strength compared with the other groups (p ≥ 0.05). Mixed failures were mainly observed after 24 hours, while adhesive failures were more frequently observed after 1.5 and 3 years. No notable differences in homogeneity and continuity along the bonded interfaces were detected among the materials in the SEM analysis. In conclusion, benzodioxole derivatives are feasible alternative co-initiators to tertiary amine in camphorquinone-based self-etching dental adhesive formulations.


Subject(s)
Humans , Benzyl Alcohols/chemistry , Dentin-Bonding Agents/chemistry , Resin Cements/chemistry , Dentin/drug effects , Dioxoles/chemistry , Benzodioxoles/chemistry , para-Aminobenzoates/chemistry , Polyethylene Glycols/chemistry , Polymethacrylic Acids/chemistry , Surface Properties , Tensile Strength , Time Factors , Materials Testing , Camphor/analogs & derivatives , Camphor/chemistry , Microscopy, Electron, Scanning , Reproducibility of Results , Dental Bonding/methods , Bisphenol A-Glycidyl Methacrylate/chemistry , Dentin/chemistry , Methacrylates/chemistry
6.
Braz. j. med. biol. res ; 51(10): e7439, 2018. graf
Article in English | LILACS | ID: biblio-951707

ABSTRACT

Nuclear factor erythroid-related factor 2 (Nrf2) has been implicated in several detoxifying and antioxidant defense processes. Nrf2-mediated heme oxygenase-1 (HO-1) expression was demonstrated to play a key role against oxidative stress. Gastrodin (GSTD) is a well-known active compound isolated from the roots of Rhizoma gastrodiae, a plant used in ancient Chinese traditional medicine. The aim of this work was to investigate whether GSTD could alleviate H2O2-induced oxidative stress in mouse liver sinusoidal endothelial cells (LSECs). In LSECs exposed to 1 mM H2O2, treatment with GSTD (1, 10, or 50 µM) resulted in higher cell viability than the untreated control. Treated cells maintained a higher Bcl2/Bax ratio and suppressed caspase-9 expression compared with untreated cells, reducing cell apoptosis. GSTD was protective for H2O2-induced oxidative injury by reducing the generation of intracellular reactive oxygen species and malondialdehyde. HO-1 and Nrf2 expressions were synergistically upregulated by GSTD. Inhibition of HO-1 by 10 µM zinc protoporphyrin resulted in less protective effects on cell viability and malondialdehyde reduction by GSTD treatment in H2O2-exposed LSECs. Additionally, phosphorylated p38 in LSECs exposed to H2O2 was elevated by GSTD. Inhibition of p38 phosphorylation by SB203580 did not induce Nrf2 and HO-1 expression after 1 or 10 µM GSTD treatment and the protective effect on cell viability and malondialdehyde reduction in H2O2-exposed LSECs was reduced. The data conclusively demonstrated that GSTD-induced HO-1 and Nrf2 expression is involved in protection of LSECs from H2O2-induced oxidative injury, which may be regulated by p38 phosphorylation.


Subject(s)
Animals , Rabbits , Benzyl Alcohols/pharmacology , Endothelial Cells/drug effects , p38 Mitogen-Activated Protein Kinases/metabolism , Heme Oxygenase-1/metabolism , Glucosides/pharmacology , Hydrogen Peroxide/pharmacology , Up-Regulation/drug effects , Cell Survival/drug effects , Apoptosis/drug effects , Liver/cytology , Liver/drug effects , Malondialdehyde/metabolism , Models, Theoretical
7.
Article in Chinese | WPRIM | ID: wpr-351218

ABSTRACT

With patients' general situation, medication use, occurrence time of adverse drug reaction/event (ADR/ADE), clinical manifestations and prognosis as reference items, a retrospective study was made for 315 cases with ADR/ADE induced by Gastrodin in Chongqing from January 2008 to June 2014, in order to analyze the characteristics of ADR/ADE and provide reference for rational clinical medication. The results showed that among the 315 cases with ADR/ADE, 143 cases (45.4%) were males and 172 cases (54.6%) were females, most of them (74.9%) were aged above 45; 60 cases (19.0%) with ADE were caused by off-label indications and 66 cases (21.0%) with ADE were caused by over dosage; ADR/ADE cases induced by intravenous drip mainly happened within 30 min (85.5%), ADR/ADE cases induced by oral administration mainly happened within 2 h (74.4%), and all of ADR/ ADE cases induced by intramuscular injection happened within 10 min. Totally 593 ADR/ADE cases were reported, which were mainly damages in gastrointestinal system, skin and its adnexa; And 61.9% of ADR/ADE cases were newly reported. It is suggested that medical workers shall learn about the regularity and characteristics of ADR/ADE induced by gastrodin, apply it in clinic with standards, pay close attention to changes of patients' situations and attach importance to the monitoring of ADR/ADE, so as to enhance the safety of medication.


Subject(s)
Adolescent , Adult , Aged , Benzyl Alcohols , Child , Child, Preschool , China , Epidemiology , Drug-Related Side Effects and Adverse Reactions , Epidemiology , Drugs, Chinese Herbal , Female , Gastrointestinal Tract , Glucosides , Humans , Male , Middle Aged , Retrospective Studies , Skin , Young Adult
8.
Article in Chinese | WPRIM | ID: wpr-246129

ABSTRACT

To establish a HPLC method for simultaneously determining plasma concentrations of gastrodin (Gas) and its metabolites hydroxybenzyl alcohol (HBA), puerarin (Pur) and internal standard (IS) p-hydroxyphenylethanol (Tyr) in rats and studying the pharmacokinetic process and interactions of gastrodin and puerarin after single and combined intravenous injection and oral administration. With Tyr as the internal standard, plasma samples were processed with methanol for protein precipitation, supernatant was dried with N2, and residues were re-dissolved with acetonitrile-0.05% phosphoric acid (20: 80). Chromatography was carried out on an Agilent ZORBAX SB-Aq C18 column (4.6 mm x 250 mm, 5 μm), with acetonitrile-0.05% phosphoric acid as the gradient mobile phase for the gradient elution. The UV detector wavelength was set at 221 nm for Gas HBA and IS and 250 nm for Pur. After the single or combined administration of Gas and Pur, their plasma concentrations in rats were detected. WinNonlin 5.2 pharmacokinetic software and SPSS 17. 0 software were used to respectively calculate pharmacokinetic parameters of each group, make a statistical analysis and compare the pharmacokinetic processes of Gas and Pur after the single or combined administration. According to the results, the absolute recoveries between low, media and high concentrations of Gas, HBA and Pur and IS as well as Tyr were more than 77.20%, with a good linearity (r > 0.999 6, n = 5) for Gas, HBA and Pur within concentration ranges of 0.10-101, 0.03-7.58 and 0.05-5.98 mg xL ('1) respectively. The lower limits of quantification for Gas, HBA and Pur were 0.10, 0.03, 0.05 mg x L(-1), respectively. Their in-ra-day and inter-day precisions were less than 12% with the accuracy between 85. 1% -1 10. %. All of the three substances and IS were stable during the whole analysis process. The findings showed significant differences in the main in vivo pharmacokinetic parame-ers in rats (AUC, C.(max) T,½ T.(max) MRT) after the single and combined administration of Gas and Pur. Either after the oral adminis-ration or after the intravenous injection, parameters showed a lower clearance rate ( L) longer mean residence time ( RT) and higher relative bioavailability, especially after the oral administration. Specifically, the relative bioavailability of the combined oral ad-inistration of Pur was 10. 7 times of that of the single administration, while that of Gas was 1. times of that of the single administra-ion. The combined administration of Gas and Pur can promote the absorption, decrease the elimination rate and prolong the mean resi-ence time. The method is simple and accurate and can be applied in the simultaneous determination of plasma concentrations of Gas, HBA and Pur in rats and the pharmacokinetic studies.


Subject(s)
Administration, Oral , Animals , Benzyl Alcohols , Blood , Pharmacokinetics , Chromatography, High Pressure Liquid , Drugs, Chinese Herbal , Pharmacokinetics , Glucosides , Blood , Pharmacokinetics , Isoflavones , Blood , Pharmacokinetics , Male , Rats , Rats, Wistar
9.
Article in English | WPRIM | ID: wpr-287153

ABSTRACT

<p><b>OBJECTIVE</b>To study the effect of gastrodin on isolated thoracic aorta rings of rats and to investigate the potential mechanism.</p><p><b>METHODS</b>A perfusion model of isolated thoracic aorta rings of rats was applied. The effect of cumulative gastrodin (5, 50, 100,150, 200, and 250 μmol/L) on endothelium-intact aorta rings was investigated. The same procedure was applied to observe the effect of gastrodin on endothelium-intact/denuded aorta rings pre-contracted with 10(-6) mol/L phenylephrine hydrochloride (PE). The aorta rings incubated by 200 mmol/L gastrodin in the Ca(2+)-free (K-H) solution was contracted by using PE. The effect of 200 mmol/L gastrodin on endothelium-denuded aorta rings pre-contracted with 60 mmol/L KCl was also observed.</p><p><b>RESULTS</b>Compared with the denuded gastrodin group, the intact gastrodin group could significantly relax the PE-contracted aorta rings (P<0.01). In Ca(2+)-free (K-H) solution KHS, the PE-induced contraction rate of aorta rings pre-incubated by gastrodin was 6.5%±0.7%, which was significantly less than the control group (11.8%±0.9%,P<0.01). However, after 3 mmol/L CaCl2 was added, the Ca(2+)-induced contraction in the gastrodin group (51.7%±2.4%) was similar to that in the control group (49.8%±2.8%). The contractile rate of rings in the KCl-contracted gastrodin group (96.3%±0.6%) was not significantly different from that in the control group (96.8%±1.2%).</p><p><b>CONCLUSIONS</b>Gastrodin has the effect of vasorelaxation on isolated thoracic aorta rings of rats. The mechanism of the vasorelaxation of gastrodin may mainly work through the inhibition of inositol 1, 4, 5-trisphosphosphate receptor on the sarcoplasmic reticulum of the arterial smooth muscle, which leads to the reduction of the Ca(2+) released from the sarcoplasmic reticulum.</p>


Subject(s)
Animals , Aorta, Thoracic , Physiology , Benzyl Alcohols , Pharmacology , Calcium , Metabolism , Endothelium, Vascular , Physiology , Female , Glucosides , Pharmacology , In Vitro Techniques , Male , Phenylephrine , Pharmacology , Rats , Rats, Wistar , Vasodilation
10.
Braz. j. microbiol ; 45(4): 1139-1144, Oct.-Dec. 2014. ilus
Article in English | LILACS | ID: lil-741263

ABSTRACT

Bacteria have evolved various mechanisms to extract utilizable substrates from available resources and consequently acquire fitness advantage over competitors. One of the strategies is the exploitation of cryptic cellular functions encoded by genetic systems that are silent under laboratory conditions, such as the bgl (β-glucoside) operon of E. coli. The bgl operon of Escherichia coli, involved in the uptake and utilization of aromatic β-glucosides salicin and arbutin, is maintained in a silent state in the wild type organism by the presence of structural elements in the regulatory region. This operon can be activated by mutations that disrupt these negative elements. The fact that the silent bgl operon is retained without accumulating deleterious mutations seems paradoxical from an evolutionary view point. Although this operon appears to be silent, specific physiological conditions might be able to regulate its expression and/or the operon might be carrying out function(s) apart from the utilization of aromatic β-glucosides. This is consistent with the observations that the activated operon confers a Growth Advantage in Stationary Phase (GASP) phenotype to Bgl+ cells and exerts its regulation on at least twelve downstream target genes.


Subject(s)
Escherichia coli/enzymology , Escherichia coli/genetics , Gene Expression Regulation , beta-Glucosidase/genetics , beta-Glucosidase/metabolism , Arbutin/metabolism , Benzyl Alcohols/metabolism , Escherichia coli/growth & development , Escherichia coli/metabolism , Glucosides/metabolism , Operon
11.
Article in Chinese | WPRIM | ID: wpr-321345

ABSTRACT

Nineteen compounds were isolated from the whole plants of Aconitum tanguticum by various of chromatographic techniques and their structures were determined through spectral analysis (1D, 2D-NMR and MS) and comparison with the literature data. These compounds were identified as 5-hydroxymethy furfural (1), 5-acetoxymethyl furfural (2), pyrrolezanthine [5-hydroxymethyl-1-[2-(4-hydroxyphenyl) -ethyl] -1H-pyrrole-2-carbaldehyde] (3), lichiol B (4), phthalic acid dibutyl ester (5), 3, 4-dihydroxy phenylethanol (6), 3, 4-dihydroxy phenylethanol glucoside (7), salidroside (8), p-hydroxy phenylethanol (9), p-hydroxybenzoie acid glucoside (10), p-hydroxybenzoic acid (11), gastrodin (12), 1-(3, 4-dimethoxyphenyl) -1, 2-ethanediol (13), p-hydroxy benzaldehyde (14), p-hydroxy acetophenone (15), 3, 4-dihydroxy phenyl ethyl acetate (16), syringic aldehyde (17), ethyl beta-D-fructopyranoside (18), and p-hydroxybenzoic acid methyl ester (19). Compounds 3 and 4 were isolated from the Ranunculaceae family for the first time, and compounds 2, 6 and 9-19 were isolated from the Aconitum genus for the first time, and compounds 1 and 5 were isolated from the species for the first time.


Subject(s)
Aconitum , Chemistry , Benzyl Alcohols , Chemistry , Furaldehyde , Chemistry , Glucosides , Chemistry , Molecular Structure , Phenols , Chemistry , Plant Extracts , Chemistry , Spectrometry, Mass, Electrospray Ionization
12.
Article in Chinese | WPRIM | ID: wpr-327859

ABSTRACT

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.


Subject(s)
Administration, Oral , Animals , Benzyl Alcohols , Chemistry , Pharmacokinetics , Pharmacology , Blood Pressure , Female , Flavonoids , Chemistry , Pharmacology , Furans , Chemistry , Pharmacology , Gastrodia , Chemistry , Glucosides , Chemistry , Pharmacokinetics , Pharmacology , Lignans , Chemistry , Pharmacology , Male , Rats , Rats, Sprague-Dawley , Software
13.
Article in Chinese | WPRIM | ID: wpr-310986

ABSTRACT

This study aims to establish an HPLC method for simultaneous determination of gastrodin and eight nucleosides and nucleobases components in Gastrodia elata. The separation was carried out on an Agilent Zorbax Bonus-RP (4.6 mm x 250 mm, 5 μm) column with a methanol-(0.04% acetic acid) water solution gradient elution program at a flow rate of 1.0 mL x min(-1). The column temperature was 36 degrees C, and the detection wavelength was 254 nm. The volume of injection was 20 μL. The nine components including gastrodin, cytosine, uracil, cytosine, adenine, thymine, uridine, guanosine and adenosine were well separated. The calibration curve was well linear in the range of 2.04-262.00 mg x L(-1), 0.20-24.67 mg x L(-1), 0.18-23.75 mg x L(-1), 0.20-25.83 mg x L(-1), 0.20-26.67 mg x L(-1), 0.16-20.00 mg x L(-1), 0.22-27.71 mg x L(-1), 0.20-24.29 mg x L(-1), 0.24-30.58 mg x L(-1), respectively, and the correlation coefficient was between 0.998 9-0.999 9. The average recovery of gastrodin and eight nucleosides and nucleobases were 96.4%-99.6%, RSD less than 2.7% (n = 6). The contents of gastrodin in all the seven Tibet cultured Gastrodia elata samples were over 2 mg x g(-1). Further, all samples contain higher contents of adenosine, guanosine, uridine and cytidine compared to low contents of cytosine, uracil, adenine and thymine. The established method is accurate, reproducible and suitable for the determination of gastrodin and eight nucleosides and nucleobases comppnents in Gastrodia elata.


Subject(s)
Benzyl Alcohols , Chromatography, High Pressure Liquid , Methods , Drugs, Chinese Herbal , Gastrodia , Chemistry , Glucosides , Nucleosides , Nucleotides
14.
Chinese Medical Journal ; (24): 3926-3931, 2014.
Article in English | WPRIM | ID: wpr-240657

ABSTRACT

<p><b>BACKGROUND</b>Gastrodin, as one of the major components extracted from the Chinese herb Gastrodia elata Bl., has many biologic effects, one of which is anti-apoptosis. Apoptosis is considered to be one of the pathogenetic mechanisms in steroid-induced osteonecrosis of the femoral head (ONFH). Therefore, we performed this study to investigate whether gastrodin has the potential to prevent steroid-induced ONFH.</p><p><b>METHODS</b>All 18 male adult Wistar rats were divided equally into three groups: the steroid group, the gastrodin+steroid group, and the control group. Osteonecrosis was induced by low-dose lipopolysaccharide and subsequent high-dose methylprednisolone. Histomorphometric method was used to determine the incidence of osteonecrosis. Terminal deoxynucleotidyl transferase-mediated dUTP nick end-labeling (TUNEL) assay was performed to detect apoptotic index of osteocytes and osteoblasts. Real-time PCR and Western blotting were performed to detect mRNA and protein expression of Bax, Bcl-2, and Caspase-3. Fisher's exact probability test and one-way analysis of variance (ANOVA) with Turkey's post hoc test were used to examine significant differences between groups.</p><p><b>RESULTS</b>The incidence of osteonecrosis in the gastrodin+steroid group (16.7%) was significantly lower than that in the steroid group (83.3%). According to TUNEL assay, the apoptotic indices in the steroid group, the gastrodin+steroid group, and the control group were 91.1%, 27.1%, and 5.4%, respectively, and the differences were significant between groups. Compared with the control group and the gastrodin+steroid group, the mRNA and protein expression levels of Bax and Caspase-3 were significantly higher in the steroid group, but the Bcl-2 mRNA and protein expression levels were significantly lower.</p><p><b>CONCLUSION</b>Gastrodin could prevent steroid-induced ONFH by anti-apoptosis.</p>


Subject(s)
Animals , Apoptosis , Benzyl Alcohols , Therapeutic Uses , Femur Head Necrosis , Drug Therapy , Glucosides , Therapeutic Uses , Lipopolysaccharides , Pharmacology , Male , Rats , Rats, Wistar , Steroids , Pharmacology
15.
Acta Pharmaceutica Sinica ; (12): 800-806, 2014.
Article in Chinese | WPRIM | ID: wpr-245012

ABSTRACT

This study is to screen the Chinese herbal compounds which could inhibit the production of Abeta and investigate the underlying mechanism. Ten types of compounds which have potential value in the treatment of AD were selected as initial screening trial. The cell models which used could overexpress Abeta and beta-secretases or Abeta and gamma-secretases. Extracellular Abeta was determined by ELISA after the cell models treated with different concentrations of compounds (0.5-100 micromol x L(-1)), separately. Then the compounds were selected which could inhibit extracellular Abeta and their best concentration ranges were decided, too. Furthermore, the cell viability and apoptosis rate, the level of intracellular Abeta, beta and gamma-secretases were determined after the cell models treated with different concentrations of selected compounds. The results showed that 4 of the 10 compounds could reduce the level of extracellular Abeta; they were cryptotanshinone, astragalosides, gastrodin and paeoniflorin, and their best concentration ranges were 0.5-5.0, 0.5-5.0, 5.0-50, 1.0-25 micromol x L(-1), respectively. Further study indicated that the 4 selected compounds were nontoxic to the cellular models and lowering intracellular Abeta were more effective compared with extracellular; of which astragalosides and gastrodin showed dose-dependent inhibition to the activities of beta and gamma-secretases, with the maximum inhibiting rates of 78.2% and 80.3%, respectively. In conclusion, cryptotanshinone, astragalosides, gastrodin and paeoniflorin could inhibit the expression and secretion of Abeta, and the underlying inhibiting mechanism of astragalosides and gastrodin were related with the reduction of the beta and gamma-secretase activities, respectively.


Subject(s)
Amyloid Precursor Protein Secretases , Metabolism , Amyloid beta-Peptides , Apoptosis , Benzyl Alcohols , Pharmacology , Cell Line , Dose-Response Relationship, Drug , Drug Evaluation, Preclinical , Drugs, Chinese Herbal , Pharmacology , Glucosides , Pharmacology , Humans , Monoterpenes , Pharmacology , Phenanthrenes , Pharmacology , Saponins , Pharmacology
16.
Article in Chinese | WPRIM | ID: wpr-244532

ABSTRACT

To explore the characteristics and influenced factors associated with the onset of vertigo disease, analysis of 3 719 cases of hospitalized patients with vertigo disease from the real world. Analysis the date of patients diagnosed with vertigo disease from the hospital information system of 19 grade-III class-A hospital from 2004 to 2011, include general information, the doctor's advice, other diseases combined, diagnostic information and the relationship with the onset of 24 solar terms, and the treatment drugs. The median age of hospitalized patients with vertigo disease was 59, the number of women (65.91%) was more than men (34.09%), manual workers (85.32%) were the majority career, most patients (81.63%) condition were general by the time they were hospital admission, patients more like admitted to neurologist (70.34%) when they first time to outpatient serves, hospitalization days were in 8-14 days (46.65%), 46.04% of the patients in the hospital total cost is in 5 000 RMB to 10 000 RMB, 73.86% of patients paid by National Health Medical Insurance. Hypertension (20.79%) was the most common underlying health problems, The most common syndromes was deficiency of liver-Yin and kidney-Yin(44. 21%) , followed by hyperactivity of liver-yang, disease of phlegm turbidity in mongolia and deficiency of Qi and blood. There were more deficiency syndrome and less excess syndrome. The highest rate of hospital admission solar terms in 2009 was the insects awaken throttle (5.21%), In 2010, the highest rate solar terms of hospital admission was the rain throttle (6.14%). The most frequently used traditional Chinese medicine was gastrodine injection (20.55%), the most frequently used western medicine for betahistine (10.19%), gastrodine injection was the most traditional Chinese medicine that combination with other western medicine. Hypertension was the most underlying health problems in the patients with vertigo disease in the real world, although the mental factors should also be attention. Liver was the most closely internal organs with vertigo, and solar terms in spring was the highest-frequency time. Gastrodine injection was the most commonly used traditional Chinese medicin in clinical to treat vertigo diserse, the therapeutic regimen combining with traditional Chinese and western medicine has more advantages. We should pay more attention to the guidance of Chinese medicine "syncretism between heaven and man", to keep up with the rhythm of change, adapt to the changes in the human body growth and decline of the Yin and Yang, by adopting the method of syndrome differentiation in traditional Chinese medicine to prevention and treatment vertigo disease.


Subject(s)
Adolescent , Adult , Aged , Benzyl Alcohols , Therapeutic Uses , Betahistine , Therapeutic Uses , Diagnosis, Differential , Female , Glucosides , Therapeutic Uses , Humans , Male , Medicine, Chinese Traditional , Methods , Middle Aged , Vertigo , Diagnosis , Drug Therapy , Epidemiology , Young Adult
17.
Article in Chinese | WPRIM | ID: wpr-318621

ABSTRACT

<p><b>OBJECTIVE</b>To study in situ intestinal absorption kinetics of baicalin contained in Tiangou Jiangya capsules, and the effect of different intestinal segments, pH value, drug concentration and P-gp inhibitor on the absorption.</p><p><b>METHOD</b>The in situ intestinal perfusion test was adopted, and HPLC method was used to determine the content of baicalin in samples at different time points. Ultra-violet (UV) spectrophotometry was used to determine the content of phenol red in samples at different time points.</p><p><b>RESULT</b>When pH value was at 5. 0, 6. 5, 7. 4, the absorption of baicalin was not impacted. P-gp inhibitor verapamil could enhance the absorption of baicalin. When the quality concentration of the test solution ranged between 5-20 g L -1 , the linearity of the absorption amount of baicalin increased. The absorption kinetic equation of baicalin was Y = -0. 073 7X +0. 118 7 (r = 0. 994 8) , K. 0. 073 7 h -1 , t1/2 9. 40 h.</p><p><b>CONCLUSION</b>Baicalin is mainly absorbed in colon. The absorption of baicalin shows the first-order kinetics process, with the absorption mechanism of passive diffusion. Baicalin is a substrate for P-gp.</p>


Subject(s)
ATP Binding Cassette Transporter, Subfamily B, Member 1 , Animals , Benzyl Alcohols , Chemistry , Reference Standards , Female , Flavonoids , Chemistry , Metabolism , Reference Standards , Furans , Chemistry , Reference Standards , Glucosides , Chemistry , Reference Standards , Hydrogen-Ion Concentration , Intestinal Absorption , Kinetics , Lignans , Chemistry , Reference Standards , Male , Quality Control , Rats , Rats, Wistar , Verapamil , Pharmacology
18.
Article in Chinese | WPRIM | ID: wpr-238590

ABSTRACT

To determine the concentration of gastrodigenin in tissue homogenates with high performance liquid chromatography (HPLC) , in order to study the changes of the distribution of gastrodigenin before and after combined application in rat tissues, including heart, liver, spleen, lung, kidney and brain tissues. The study showed that gastrodigenin could be found in kidney, liver, heart, lungs, spleen and brain tissues. After the combined application of Gastrodiae Rhizoma and Ligustici Wallichii Rhizoma, the content of gastrodigenin decreased in kidney and liver to varying degrees, while increasing in lung and brain. This indicated that Ligustici Wallichii Rhizoma had certain impact on the in vivo distribution of gastrodigenin, an active ingredient in Gastrodiae Rhizoma, because it could improve gastrodigenin's distribution in lung and brain tissues. The study provides scientific basis for the combined application of Gastrodiae Rhizoma and Ligustici Wallichii Rhizoma in treating brain diseases.


Subject(s)
Animals , Benzyl Alcohols , Metabolism , Pharmacokinetics , Brain , Metabolism , Chromatography, High Pressure Liquid , Female , Gastrodia , Chemistry , Kidney , Metabolism , Ligusticum , Chemistry , Liver , Metabolism , Lung , Metabolism , Male , Rats , Spleen , Metabolism
19.
Article in Chinese | WPRIM | ID: wpr-338688

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the effect of gastrodin in relaxing isolated thoracic aorta rings in rats and discuss its possible mechanism.</p><p><b>METHOD</b>Isotonic tension of isolated thoracic aortic rings in rats with norepineprine (NE) and KCl was recorded to observe the vasodilatory effect of gastrodin and the influence of various drugs on it.</p><p><b>RESULT</b>Gastrodin had the effect in relaxing thoracic aortas with or without endothelium, and there was no significant difference. NG-nitro-L-argininemethylester (L-NAME, 1 x 10(-4) mol x L(-1)), methylene blue (MB, 1 x 10(-5) mol x L(-1)), indomethacin (INDO, 1 x 10(-5) mol x L(-1)) had no effect on the vasodilation action of gastrodin on thoracic aortas precontracted by NE. 4-aminopyrimide (4-AP, 1 x 10(-4) mol x L(-1)), tetrathylamonium (TEA, 1 x 10(-3) mol x L(-1)), BaCl2 (1 x 10(-4) mol x L(-1)) and glibenclamide (Gli, 1 x 10(-5) mol x L(-1)) could inhibit gastrodin's effect in relaxing thoracic aorta rings. In the absence of Ca2+, pre-incubated gastrodin showed a notable inhibitory effect in relaxing NE contraction.</p><p><b>CONCLUSION</b>Gastrodin shows a dose-dependent and endothelium-independent effect in relaxing rat isolated thoracic aorta rings. The mechanism is related to K+ channel, inhibition of release of Ca+ stored in endoplasmic reticulum of vascular smooth muscle cells and inflow of external calcium Ca2+.</p>


Subject(s)
Animals , Aorta, Thoracic , Physiology , Benzyl Alcohols , Pharmacology , Calcium , Metabolism , Endothelium, Vascular , Physiology , Glucosides , Pharmacology , In Vitro Techniques , Male , Norepinephrine , Pharmacology , Rats , Rats, Sprague-Dawley , Vasodilation
20.
Article in Chinese | WPRIM | ID: wpr-288690

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the intestinal absorption characteristics of gastrodigenin.</p><p><b>METHOD</b>In vitro everted gut sac model and in situ rat single-pass intestinal perfusion model were used to evaluate the absorption characteristics of gastrodigenin in the different intestinal segments. The concentrations of gastrodigenin in the samples were determined by Ultra Performance Liquid Chromatography (UPLC) method, and the relevant absorption parameters were calculated.</p><p><b>RESULT</b>In the everted gut sac tests, no significant difference of absorption among the four segments was observed. A positive correlation was found between drug concentration and the accumulated absorption amount (Q). At the concentration of 400 mg x L(-1), the Q of gastrodigenin in the duodenum, jejunum, ileum and colon were 224.33, 225.81, 233.18 and 189.25 microg, respectively. The in situ rat single-pass intestinal perfusion tests showed that there was also no significant difference of absorption among the four segments. The absorption rates (A) of gastrodigenin in the duodenum, jejunum, ileum and colon were 45.8%, 48.39%, 47.00%, 54.35%, respectively.</p><p><b>CONCLUSION</b>Gastrodigenin can be well absorbed via passive diffusion in the intestine. The absorption rates of gastrodigenin in the different intestinal segments show no regioselectivity.</p>


Subject(s)
Animals , Benzyl Alcohols , Pharmacokinetics , Chromatography, Liquid , Methods , Intestinal Absorption , Intestines , Metabolism , Male , Medicine, Chinese Traditional , Models, Biological , Perfusion , Methods , Rats , Rats, Sprague-Dawley
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