Background Hypertension,ischemia and hypoxia induce the increase of glutamate level in eye tissue and furthermore produce excitatory damage and apoptosis of retinal ganglion cells(RGCs).At present,the study on the protection of traditional Chinese medicine on glutamate-induced retinal excitatory damage is lack.objective Present study was to explore the protective effects of Huoxue huayu decoction,a Chinese herbal recipe,on RGCs in acute ocular hypertension model. Methods Fony-five healthy clean Wistar rats were divided into three groups randomly.The acute ocular hypertension models were established in 40 Wistar rats by injecting the normal saline solution into the anterior chamber to elevate the intraocular pressure for 60 minutes.Huoxue huayu decoction of 4 ml was administered intragastrically once per day in 20 model rats.Other matched 5 normal Wistar rats served as normal control group.The rats were sacrificed on 1,3,7 and 14 days after modeling and the retinas were isolated for the histopathologieal and uhrastructure examination.Expression of glutamate transporter in the retina of acute ocular hypertension and normal rat retina were detected using quantitative real-time polymerase chain reaction.The utilization of animals followed the Association for Research in vision and Ophthalmology. Results After acute ocular hypertension.the retina thickness attenuated and the numbers of RGCs decreased under the light microscope in 1,3,7 and 14 days after modeling in comparison with normal control rats.The degradation of the organelle and edema as well as changes of cell nuclei were seen in model rats under the transmission electron microscopy.The expression of glutamate transporter mRNA in model group and glutamate transporter group was rapidly elevated in the first day (P<0.05),descended at the third days(P<0.01)and returned to the normal level 7 days later(P>0.05).Conclusion Huoxue huayu decoction can protect the retina against RGCs damage in the acute ocular hypertension by elevating the expression of glutamate transporters in retina.

Objective To study the protection and mechanism of co-administration of vitamin E with coenzyme Q10(CoQ10) to valproate-associated hepatotoxicity in infantal rats.Methods The rat models were established by oral administration of valproic acid(VPA) in ablactation(21 days) Wistar rats,at doses of 500 mg/(kg?d) during 30 days,other groups received the same amount of VPA with phemobarbitone(PB) and co-administration with vitamin E and CoQ10.The changes of liver cell morphology and the blood coagulation test,as well as the contents of succinic dehydrogenase(SDH),cytochrome oxidase(CCO),cytochrome,the levels of glutothione(GSH) and malondial dehyde(MDA) in rat liver mitochondria were detected by chromatometry,HPLC,Oil-Red-O staining and electron microscope,respectively.Results 1.Average content of cytochrome aa3 in liver mitochondria of infantal rats were reduced by 58.80% and(61.80%) because of administration of VPA and VPA added with PB.The protection against the loss of cytochrome aa3 by coadministration of VitE and CoQ10 was obvious.As for activities of SDH and CCO,which affected by VPA and VPA added with PB in rats,were significantly lowered compared with control group(P

The study aims to evaluate the bioequivalence of valsartan hydrochlorothiazide tablets, and to investigate the potential cause of bioinequivalence. This was a single-center study with an open, randomized double-way crossover design. Test and reference preparations containing 160 mg of valsartan and 25 mg of hydrochlorothiazide were given to 36 healthy male volunteers. Plasma concentrations of valsartan and hydrochlorothiazide were determined simultaneously by LC-MS/MS. The pharmacokinetic parameters and relative bioavailability were calculated, while the bioequivalence between test and reference preparations were evaluated. The dissolution profiles of test and reference preparations in four different mediums were determined via dissolution test and HPLC. The similarity was investigated according to the similarity factors (f2). The F(o-t) and F(0-infinity) were (139.4 +/- 65.2)% and (137.5 +/- 61.2)% for valsartan of test preparations. It led to get the conclusion that test and reference preparations were not bioequivalent for valsartan. A significant difference was observed between test and reference tablets in the valsartan dissolution test of pH 1.2 hydrochloric acid solution. The key factor of the bioinequivalence might be that dissolution of valsartan in acid medium has marked difference between two preparations.
Administration, Oral ; Adolescent ; Adult ; Angiotensin II Type 1 Receptor Blockers ; administration & dosage ; adverse effects ; blood ; pharmacokinetics ; Antihypertensive Agents ; administration & dosage ; adverse effects ; blood ; pharmacokinetics ; Area Under Curve ; Chromatography, Liquid ; Cross-Over Studies ; Drug Liberation ; Humans ; Hydrochlorothiazide ; administration & dosage ; adverse effects ; blood ; pharmacokinetics ; Male ; Tablets ; Tandem Mass Spectrometry ; Therapeutic Equivalency ; Valsartan ; administration & dosage ; adverse effects ; blood ; pharmacokinetics ; Young Adult

A chiral LC-MS/MS method for the simultaneous analysis of desvenlafaxine (DVS) enantiomers in human plasma was developed and applied to a pharmacokinetic study on 12 Chinese healthy volunteers. d6-Desvenlafaxine was used as internal standard (IS). Chromatographic separation was performed on the Astec Chirobiotic V chiral column (150 mm x 4.6 mm, 5 μm). The assay was linear over the concentration range of 0.500-150 ng x mL(-1) for both enantiomers (r2 > 0.99). The method was successfully applied to a stereoselective pharmacokinetic study of 100 mg desvenlafaxine sustained release tablets on 12 Chinese healthy volunteers under fasting conditions. The results showed that the pharmacokinetic parameters were similar to both enantiomers in Chinese healthy volunteers. The AUC(0-t), and C(max) of the two enantiomers were about 1.5 times higher than those of blacks and whites reported in the literature.
Administration, Oral ; Area Under Curve ; Asian Continental Ancestry Group ; Chromatography, Liquid ; Cyclohexanols ; blood ; pharmacokinetics ; Delayed-Action Preparations ; Desvenlafaxine Succinate ; Dose-Response Relationship, Drug ; Healthy Volunteers ; Humans ; Male ; Plasma ; chemistry ; Stereoisomerism ; Tablets ; Tandem Mass Spectrometry

To study the metabolite excretion of theophylline, a rapid and specific method by liquid chromatography with heated electrospray ionization tandem mass spectrometry (LC-HESI/MS/MS) method for simultaneous determination of theophylline, 1, 3-dimethyluric acid (1,3-DMU), 3-methylxanthine (3-MX) and 1-methyluric acid (1-MU) in human urine was developed using theophylline-d6 and 5-fluorouracil as internal standards. Selected reaction monitoring (SRM) with heated electrospray ionization (HESI) was used in the negative mode for mass spectrometric detection. After diluted with methanol and centrifuged, the analytes and ISs were separated on a XDB-Phenyl (150 mm x 4.6 mm, 5 microm) column with a mixture of water-methanol-formic acid (30 : 70 : 0.15) as mobile phase at a flow rate of 0.6 mL x min(-1). The linear calibration curves for theophylline, 1, 3-DMU, 3-MX and 1-MU were obtained in the concentration range of 1.0-250 microg x mL(-1), separately. The method herein described is effective and convenient, and can be used for determination of theophylline and its three metabolites. The results showed that urinary excretion ratio of theophylline, 1,3-DMU, 3-MX and 1-MU is approximately 1 : 3 : 1 : 2 in Chinese subjects, which is similar to the reported excretion pattern in Caucasian.
Administration, Oral ; Asian Continental Ancestry Group ; Calibration ; Chromatography, Liquid ; Delayed-Action Preparations ; metabolism ; Healthy Volunteers ; Humans ; Spectrometry, Mass, Electrospray Ionization ; Tablets ; Tandem Mass Spectrometry ; Theophylline ; metabolism ; urine ; Uric Acid ; analogs & derivatives ; urine ; Xanthines ; urine

AIM:To investigate whether Smad pathway participates the process of extracellular signal regulated kinase (ERK) induced the proliferation of vascular smooth muscle cells (VSMCs). METHODS: Human umbilical artery smooth muscle cells (hUASMCs) were divided into four groups: control group, PDGF (platelet derived growth factor) group, ERK blocking agent group and PDGF+ERK blocking agent group. MTT assay was used to detect the proliferation of hUASMCs (A value). Immunohistochemical technique was used to detect the expression of PCNA, phosphorylated ERK (p-ERK) and phosphorylated Smad2/3 (p-Smad2/3) protein in hUASMCs. The expression of Smad2/3 mRNA in hUASMCs was detected by RT-PCR. RESULTS: The proliferation of hUASMCs and the expression of PCNA, p-ERK and p-Smad2/3 proteins in hUASMCs in PDGF group were increased obviously than those in other groups (P

Objective To study the inhibition effects of antibacterial proteins from Musca domestica larvae on JEC and A375 tumour cells. Methods Antibacterial proteins with concentrations of 0.02%,0.1%,0.5%,2.5% and 12.5% were supplied in the culture of JEC and A375 tumour cells in vitro.The cell cycles and apoptosis of JEC and A375 tumour cells were detected by flow cytometry,and the apoptosis index(AI) was measured.The morphology of apoptotic cells was observed with HE stainings and AO staining.The culture without antibacterial proteins was served as control. ResultsThe ratio of apoptosis index/proliferation index(AI/PI) of JEC cells increased with the concentration of antibacterial proteins.The PI and apoptosis rate of 2.5% antibacterial proteins group and 12.5% antibacterial proteins group significantly increased,and G0/G1 significantly decreased.For A375 cells,there were significant differences in G2/M, S,G0/G1,G2/M,AI/PI and PI between 12.5% antibacterial proteins group and control group(P

AIM: To compare the accuracy of intraocular lens(IOL)power calculations by using five formulas(Haigis, SRK-T, Hoffer Q, Holladay-1, SRK-Ⅱ)in eyes with long axial lengths in order to improve the accuracy of predicating IOL powers.METHODS: Fifty-one eyes of 51 cases of age-related cataract and with mild long axial(24.5mm27mm) were collected who`s optical biometry were performed by the Zeiss IOL Master500 before operation.They underwent regular phacoemulsification and posterior chamber IOL implantation.The actual postoperative refraction was measured with the methods of phoropter and subjective optometry 3mo after surgery.Then we compared the differences of the predicted and actual postoperative refraction of the five formulas in each group.RESULTS: In the mild axial lengths cases, the differences between SRK Ⅱ formula and the other four formulas were statistically significant (P<0.05), and the difference between Hoffer Q and SRK-T formula was statistically significant (P<0.05);there was no difference among the other formulas (P>0.05).In the moderate and severe long axial lengths cases, the differences between SRK Ⅱ formula and the other four formulas were statistically significant (P<0.05), and the difference between Hoffer Q and SRK-T formula, Hoffer Q and Haigis formula were statistically significant (P<0.05);there was no difference among the other formulas (P>0.05).The differences of all the five formulas between the two groups were statistically significant (P<0.05).CONCLUSION: In the mild axial lengths cases, Haigis, SRK-T, Hoffer Q, Holladay-1 performed well.In the moderate and severe long axial lengths cases, Haigis, SRK-T and Holladay-1 performed better than other formulas.The accuracy of all the five formulas decreases as the axial length getting longer.

Objective To investigate the characteristic and clinical significance of airway inflammation in children with acute asth-ma. Methods Underwent sputum induction and sputum induction in children (n=34) with acute asthma was repented in recovered children ( n = 24).Induced sputum were also taken from 15 healthy children as controls.Total and differential cell counts were per-formed. Interleukin(IL)-8、IL-6 were measured,The relationship between inflammatory cells and IL-8、 IL-6、peak expiratory (PEF) were analyzed.Results The inflammatory cell infiltrate was mixed including eosmophilic granulocytes, neutrophils, and macrophages. They decreased significantly, but eosinophilic granulocyte remained a higher percentage compared with healthy subjects. There was low-er percentage of lymphocytes at acute exacerhation.Eosinophilic granulocytes were correlated with the degree of airflow obstruction. Levels of IL-8、IL-6 were elevated during the acute exacerbation and decreased at resolution.IL-8 was correlated significantly with neutrophils at acute exacerhation and resolution.IL-6 was correlated signifficantly with eosinophilic granulocytes at acute exacerbation. Conclusions Airway inflammation is chataeterized by infiltration of eosinophils, neutrophils and macrophages.IL-8、IL-6 possibly is the important cytokines of airway inflammation in children with acute asthma. Increased eosinophils in induced sputum correlates with asthma severity. Therapy to the cytokines may have potential values.J Appl Clin pediatr,2004,19(12): 1023-1025