Objective To investigate the effects of ciyelosporine-A(CsA).a calcinenrin(CAN)inhibitor,on electrophysiological propertiesof atria in canine tachycardia-induced model of AF.Methods Eighteen healthy adult mongrel canines weighing 17.0 to 23.2 kg(rangedfrom 2 to 4 years old)were randomized to 3 groups,Sham group(no pacemaker was implanted),atrial tachypacing group(ATP group)each group at baseline and after 8 weeks' tachypacing.Measurements included atrial effective refractory period(AERP),conductionvelocity(CV),wave length(WE),atrial fibrillation load and rate-adaptability. Results After 8 weeks' atrial tachypacing,ATP andCsA groups showed significant longer duration of the P wave,shorter AERP,decreased adaptation of AERE slower CV,shorter Wland longer AF duration compared to the shamg roup (all P＜0.05).AERP of the CsA group was longer than that of ATP group (P＜0.05),but there were no differences in rate-adaptability,CV,incidence of induced AF and AF duration between CsA group and ATP group.Conclusions Our results suggest that calcineurin pathway intervention by CsA have a positive effect on tachycardia-inducedelectrical remodeling of atria,but can not prevent or reverse AF.

Wuzhuyu Tang is a classical formula for treating migraine, but its' pharmacological ingredients is unclear yet. Present study employed the everted intestinal sac model to collect the absorption samples of 10 kinds of Wuzhuyu decoction, and then analyzed the contents of 9 ingredients in Wuzhuyu Tang and absorption samples quantitatively or semi-quantitatively by HPLC-DAD method. Reserpine was used to establish the mice model of migraine, and then the contents and activities of 5-hydroxytryptamine, noradrenaline, dopamine, nitric oxide and nitricoxide synthase in brain tissues and serums were determined respectively after oral administration of Wuzhuyu Tang. Using the partial least squares regression method to correlate the total absorption quantity of 9 ingredients and pharmacodynamics. The result shows that limocitrin-3-O-beta-D-glucoside, ginsenoside Rg1 and Rb1, rutaevine, limonin, evodiamine and rutaecarpine are the main ingredients influenced the effects in absorption samples in everted intestinal sacs, especially ginsenoside Rg1, rutaevine, evodiamine and rutaecarpine among them have obvious improving effects to most pharmacodynamics index, might be the pharmacological ingredients influenced the therapeutical effects of Wuzhuyu Tang treating migraine.
Animals ; Drugs, Chinese Herbal ; pharmacology ; Female ; Intestinal Absorption ; drug effects ; Intestines ; drug effects ; Male ; Mice ; Mice, Inbred ICR ; Migraine Disorders ; drug therapy ; Rats ; Rats, Wistar

OBJECTIVETo investigate the impact of cyclosporine A (CsA) on atrial expression change of L-type calcium channel alpha1c subunit in a canine model of atrial fibrillation (AF).

METHODSAF was induced by rapid atrial pacing (400 beats/min) for 8 weeks in adult male dogs and placebo (n = 6) or CsA (5 mg x kg(-1) x d(-1), n = 6) were orally administered to these animals. Sham operated animals served as normal controls (n = 6). The atrial electrophysiological parameters including P wave duration, atrial effective refractory period (AERP) were recorded and analyzed at baseline and 8 weeks later. Animals were scarified at 8 weeks post final electrophysiological examinations and atrial expressions of L-type calcium channel alpha1c subunit were determined by Western blot.

RESULTSCompared to sham group, the P wave duration was significantly prolonged while AERP was significantly decreased in AF and CsA groups (all P < 0.05). AERP was significantly longer in CsA group than that in AF group (P < 0.05). L-type calcium channel alpha1c subunit expression was significantly downregulated in AF group compared to sham group (P < 0.05) and CsA significantly attenuated this downregulation (P < 0.01 vs. AF group).

CONCLUSIONCsA could attenuate the downregulation of the L-type calcium channel alpha1c subunit expression and improve the atrial electrophysiological remodeling in this canine model of AF.

Animals ; Atrial Fibrillation ; drug therapy ; metabolism ; Calcium Channels, L-Type ; metabolism ; Cyclosporine ; pharmacology ; therapeutic use ; Dogs ; Heart Atria ; metabolism ; physiopathology ; Male

To study the chemical constituents of the traditional Chinese herb Baeckea Frutescens L., a new flavonol glycoside, named 6, 8-dimethylkaempferol-3-O-alpha-L-rhamnoside (1), together with seven known compounds: quercetin (2), quercetin-3-O-alpha-L-rhamnoside (3), myricetin (4), myricetin-3-O-alpha-L-rhamnoside (5), gallic acid (6), ursolic acid (7) and 1,3-dihydroxy-2-(2'-methoxylpropionyl)-5-methoxy-6-methylbenzene (8) were isolated by using silica gel column chromatography, polyamide column chromatography and recrytallization. Their structures were identified on the basis of physicochemical properties and spectroscopic analysis. Among them, compounds 2-7 were isolated from this plant for the first time and compound 8 was first isolated from plant.
Flavonoids ; chemistry ; isolation & purification ; Flavonols ; chemistry ; isolation & purification ; Glycosides ; chemistry ; isolation & purification ; Kaempferols ; chemistry ; isolation & purification ; Molecular Structure ; Myrtaceae ; chemistry ; Plants, Medicinal ; chemistry ; Quercetin ; chemistry ; isolation & purification ; Toluene ; analogs & derivatives ; chemistry ; isolation & purification ; Triterpenes ; chemistry ; isolation & purification

Objective: To observe the effects of herb-partitioned moxibustion and ginger-partitioned moxibustion on the growth of colon tumors in rats with colitis-associated colon cancer (CACC), and explore the mechanism of moxibustion intervening CACC through the purinergic receptor P2X ligand-gated ion channel 7 (P2X7R)/signal transducer and activator of transcription 3 (STAT3)/vascular endothelial growth factor (VEGF) pathway. Methods: A total of 26 male Sprague-Dawley rats were selected. According to the random number table method, 6 rats were selected as the normal group. The remaining 20 rats were injected intraperitoneally with azoxymethane (AOM) combined with oral dextran sodium sulfate (DSS) to prepare the CACC model. After the model was successfully established, 2 rats were randomly selected for model identification. The remaining 18 rats which were successfully modeled were randomly divided into a model group, a herb-partitioned moxibustion group and a ginger-partitioned moxibustion group, with 6 rats in each group. Moxibustion intervention was performed in the herb-partitioned moxibustion group and the ginger-partitioned moxibustion group at Qihai (CV 6) and bilateral Tianshu (ST 25). Moxibustion was performed twice at each point each time, once a day, at a 1-day interval after 6 consecutive interventions, for a total of 30 interventions. After intervention, the colon tumor load, pathological change and histopathological score were observed. Immunohistochemistry was used to detect the expressions of VEGF, P2X7R, phospho-STAT3 (p-STAT3), and nuclear factor-kappa B p65 (NF-κB p65) proteins in rat colon tissue. Western blot was used to detect the levels of p-STAT3 and NF-κB p65 proteins in rat colon tissue. Results: Compared with the normal group, the colon tumor load and histopathological score in the model group were significantly increased (both P<0.001), and different grades of dysplasia were observed in colon tissue from the model group, reaching the degree of adenocarcinoma; the expression level of P2X7R protein in colon tissue was significantly decreased (P<0.001), and the expression levels of p-STAT3, NF-κB p65 and VEGF proteins were significantly increased (all P<0.001) in the model group. Compared with the model group, the colon tumor load, colon histopathological score and the levels of p-STAT3, NF-κB p65 and VEGF proteins in colon tissue were significantly decreased (all P<0.05) in the herb-partitioned moxibustion group and the ginger-partitioned moxibustion group while the expression levels of P2X7R protein in colon tissue were significantly increased (both P<0.05). Conclusion: Both herb-partitioned moxibustion and ginger-partitioned moxibustion can reduce the colon tumor load in CACC rats and delay the progression of colon adenomas. The mechanism may be mediated by the P2X7R/STAT3 pathway to inhibit STAT3 phosphorylation, thereby reducing VEGF protein expression.

OBJECTIVETo compare the behavioral effects of psychoactive drugs between two strains of mice.

METHODSThe Kunming (KM) and ICR mice were injected intraperitoneally with caffeine (3, 10, 30, 100 mg/kg), ephedrine (3, 10, 30, 100 mg/kg), diazepam (1, 3,1 0 mg/kg) and chloral hydrate (10, 30, 100 mg/kg), respectively. Ten min after injection, the locomotor activity in the open field was recorded for 2 h. The total distance, the distance ratio to total distance and the time in central region were analyzed for each drugs. Thirty min after injection, the latent time in the passive avoidance test was measured in a shuttle box.

RESULTSCaffeine and diazepam prolonged the latent time, and ephedrine and chloral hydrate decreased the latent time, but there were no differences between the two strains. The two strains of mice exhibited significant differences in the total distance after injection of ephedrine 10 mg/kg, diazepam 3 mg/kg and chloral hydrate 100 mg/kg. Compared to KM mice, ICR mice exhibited an increase in the distance ratio and the time in central region after injection of ephedrine 10-100 mg/kg, but a decrease after diazepam 3-10 mg/kg.

CONCLUSIONKM and ICR mice show no differences in latent time, but significant differences in the total distance, the distance ratio and the time in central region in the locomotor activity. Therefore, selection of mouse strains is important in the study of psychoactive drugs.

Animals ; Caffeine ; pharmacology ; Central Nervous System Agents ; pharmacology ; Chloral Hydrate ; pharmacology ; Diazepam ; pharmacology ; Dose-Response Relationship, Drug ; Ephedrine ; pharmacology ; Mice ; Mice, Inbred ICR ; Motor Activity ; drug effects

Aromatic traditional Chinese medicines have a long history in China, with wide varieties. Volatile oils are active ingredients extracted from aromatic herbal medicines, which usually contain tens or hundreds of ingredients, with many biological activities. Therefore, volatile oils are often used in combined prescriptions and made into various efficient preparations for oral administration or external use. Based on the sources from the database of Newly Edited National Chinese Traditional Patent Medicines (the second edition), the author selected 266 Chinese patent medicines containing volatile oils in this paper, and then established an information sheet covering such items as name, dosage, dosage form, specification and usage, and main functions. Subsequently, on the basis of the multidisciplinary knowledge of pharmaceutics, traditional Chinese pharmacology and basic theory of traditional Chinese medicine, efforts were also made in the statistics of the dosage form and usage, variety of volatile oils and main functions, as well as the status analysis on volatile oils in terms of the dosage form development, prescription development, drug instruction and quality control, in order to lay a foundation for the further exploration of the market development situations of volatile oils and the future development orientation.
Databases, Pharmaceutical ; statistics & numerical data ; Drug Therapy ; statistics & numerical data ; Humans ; Medicine, Chinese Traditional ; Nonprescription Drugs ; Oils, Volatile ; classification ; therapeutic use ; Outcome Assessment (Health Care) ; statistics & numerical data ; Phytotherapy ; statistics & numerical data ; Plant Oils ; classification ; therapeutic use

To investigate theological properties of common hydrophilic gel excipients such as Carbopol based on viscosity, the viscosity was determined by rotation method and falling-ball method. Linear regression was made between ln(eta) and concentration, the slope of which was used to explore the relation between viscosity and concentration of different excipients. The viscosity flow active energy (E(eta)) was calculated according to Arrhenius equation and was used to investigate the relation between viscosity and temperature of different excipients. The results showed that viscosities measured by two methods were consistent. Concentration of guargum (GG) and hydroxypropylmethyl cellulose (HPMC) solution had a great influence on the viscosity, k > 5; while concentration of polyvinylpyrrolidone-K30 (PVP-K30) and polyethylene glycol 6000 (PEG6000) exerted a less effect on viscosity, k < 0.2; viscosity flow active energy of different excipients were close, which ranged from 30 to 40 kJ x mol(-1). Therefore, theological properties study could provide the basis for application of excipients and establish a foundation for the research of relation between excipients structure, property and function.
Excipients ; chemistry ; Gels ; chemistry ; Polyethylene Glycols ; chemistry ; Polyvinyls ; chemistry ; Povidone ; chemistry ; Rheology ; Temperature ; Viscosity

OBJECTIVETo investigate the prevalence of mental disorder through the 12-item general health questionnaire (GHQ-12) survey and its related factors in community settings in Zhejiang Province.

METHODSA muti-level model was analyzed using data of 14,632 respondents nested in counties (cities), townships (urban districts), villages (urban neighborhoods) from the epidemiological survey of mental illnesses above 15 years old.

RESULTSThe mean score measured by GHQ-12 was (1.54 +/- 2.15), which was lower than that of samples from four cities of Guangzhou, Chongqing, Taiyuan and Hangzhou (U = 11.08, P < 0.01). The mental disorder clustered within county (city) level, which represented 4.3% (chi(2) = 3.94, P < 0.05) of the total variance including four levels. After controlling for the county level, the mental disorder was associated with age, marital status, residency patterns, education, occupation and household incoming. In particular, it was reported that higher household incoming was significantly associated with better mental disorder among population in community settings.

CONCLUSIONThe prevalence of mental disorder clustered at the county (city) level is relatively lower with vulnerable groups including divorced, widowed, unemployed, retired, lower-income ones in community settings in Zhejiang Province.

Adult ; China ; epidemiology ; Cross-Sectional Studies ; Female ; Humans ; Male ; Mental Disorders ; epidemiology ; Middle Aged ; Population Surveillance ; Prevalence ; Surveys and Questionnaires

In order to study function of NAC transcription in development, hormone regulation and the stress response of Salvia miltiorrhiza, the NAC transcription was cloned and analyzed. By retrieving cDNA database of S. miltiorrhiza hairy root one NAC unigene was found, then a full length of cDNA was cloned by designing specific primers and PCR amplifying. Using ORF finder it was found that the cDNA containing a NAC-AB conserved domain in N-terminal, so the cDNA was a NAC transcription factor, named as SmNAC1 (kF006346). Bioinformatics analysis showed that SmNAC1 had an open reading frame (ORF) of 591 bp encoding 196 amino acids. The calculated protein had isoelectric point (pI) of 4.36 with molecular weight about 21.66 kDa. The transcription level of SmNAC1 after dealing with yeast extract (YE) and silver ion (Ag+) in S. miltiorrhiza hairy root was markedly stimulated up regulating. It was 1.4 fold compared with the control after induction 2 h, and maintained 2.0 fold on 4-12 h after induction. SmNAC1 may participate in regulation of stress response of YE + Ag+.
Cloning, Molecular ; Computational Biology ; Phylogeny ; Plant Proteins ; genetics ; physiology ; Plant Roots ; chemistry ; Salvia miltiorrhiza ; chemistry ; genetics ; Trans-Activators ; genetics ; physiology