OBJECTIVE:To establish a method for the dissolution determination of Dronedarone hydrochloride tablet,and eval-uate the quality consistency of its generic and original preparations. METHODS:UV spectrometry was performed on the column of 288 nm,dissolution media of Phosphate buffer solution (pH4.5),0.1 mol/L Hydrochloric acid solution [adding into 0.5% sodium dodecyl sulfate(SDS)],Phosphate buffer solution [pH6.8,adding into 0.5%SDS] and water,volume of dissolution medium was 1 000 ml,rotation speed was 75 r/min,the dissolution of generic and original preparations of Dronedarone hydrochloride tablet was detected,and the similarity of dissolution curve was evaluated by calculating the similarity factor (f2). RESULTS:The linear range of dronedarone hydrochloride was 2.147-25.764 μg/ml;RSDs of precision,stability and reproducibility tests were lower than 2.0%;recoveries 4 dissolution media were 99.53%-101.05%(RSD=0.48%,n=9),98.95%-100.05%(RSD=0.39%,n=9), 99.54%-100.20%(RSD=0.24%,n=9)and 98.54%-100.06%(RSD=0.44%,n=9). In the 4 dissolution media,f2 of the dissolu-tion curve of 3 batches of generic and original preparations of Dronedarone hydrochloride tablet was 56,60,63,68,68,52,59, 67,65,68,76,62,respectively. CONCLUSIONS:The method is suitable for the dissolution determination of Dronedarone hydro-chloride tablet;meanwhile,the in vitro dissolution curves of generic and original preparations of Dronedarone hydrochloride tablet show similarity,so the quality consistency is good.

OBJECTIVETo explore the effect of Shoutai Pill (STP) containing serum on bioactivity behaviors of trophoblast cells in spontaneous abortion (SA) patients such as cell proliferation, invasion, migration and secretion.

METHODSTrophoblast cells in artificial abortion in normal pregnancy and SA patients were isolated and cultured in vitro, which were then treated with STP containing serum at various concentrations (5%, 10%, 20%, respectively). Blank serum was taken as the normal control group and dydrogesterone containing serum as the dydrogesterone control group. The proliferation, cycle distribution, invasion and migration capacity, and beta human chorionic gonadotropin (p-HCG) level were detected by methyl thiazolyl tetrazolium (MTT) colorimetry, flow cytometry (FCM), Transwell experiments, and ELISA, respectively.

RESULTSCompared with the normal control group, the activity of cell proliferation obviously decreased, ratios of apoptotic cells (SubGO/G1) and G2/M phase were obviously elevated, S phase cell ratio was obviously reduced (all P < 0.05). Transwell experiments indicated invasion and migration capacity obviously decreased, secreted beta-HCG level were obviously reduced after 72-h intervention (P < 0.05). Compared with the SA group, the activity of cell proliferation obviously increased, ratios of apoptotic cells and G2/M phase were obviously reduced, S phase cell ratio was obviously elevated, invasion and migration capacity were obviously enhanced, secreted beta-HCG level were obviously elevated after 72-h intervention in the dydrogesterone control group and each STP containing serum group (all P < 0.05). The activity of trophoblastic cell proliferation, S phase cell ratio, invasion and migration capacity, and secreted beta-HCG level were strengthened along with increased STP containing serum. Besides, the effects of 20% STP containing serum group were significantly superior to those of the dydrogesterone control group (P < 0.05).

CONCLUSIONSTP containing serum could dose-dependently enhance the proliferative activity of trophoblastic cells, invasion and migration capacity, secretion of beta-HCG, and reduce the apoptosis of trophoblast cells, which might be one of mechanisms for STP preventing and treating SA.

Abortion, Spontaneous ; Apoptosis ; Cell Cycle ; Cell Proliferation ; Cells, Cultured ; Drugs, Chinese Herbal ; pharmacology ; Dydrogesterone ; pharmacology ; Female ; Humans ; Pregnancy ; Trophoblasts ; drug effects

OBJECTIVETo explore the molecular mechanism of Wenxin Capsule (WXC, an effective Chinese composite drug) in preventing and treating myocardial ischemia of coronary heart disease.

METHODSRat model of myocardial ischemia was established by subcutaneous multi-point injecting isoproterenol. Effect of WXC on cell apoptosis was observed by transmission electron microscopy and TUNEL method, and its effect on apoptotic related gene Bcl-2 and Fas gene protein expression was observed by immunohistochemical method.

RESULTSIsoproterenol induced myocardial ischemic injury could cause evident cardial cell apoptosis, obvious enhance Fas gene protein expression and mild enhance Bcl-2 gene protein expression. WXC could significantly down-regulate Fas, up-regulate Bcl-2 gene protein expression, significantly inhibit and block the myocardial cell apoptosis.

CONCLUSIONSTo inhibit and block the event of cell apoptosis through regulating Bcl-2 and Fas gene protein expression in ischemic myocardium might be one of the mechanisms of WXT in preventing and treating myocardial ischemic injury of coronary heart disease.

Animals ; Apoptosis ; drug effects ; Drug Combinations ; Drugs, Chinese Herbal ; pharmacology ; Isoproterenol ; Male ; Myocardial Ischemia ; chemically induced ; metabolism ; pathology ; Myocytes, Cardiac ; pathology ; Proto-Oncogene Proteins c-bcl-2 ; biosynthesis ; genetics ; Rats ; Rats, Wistar ; fas Receptor ; biosynthesis ; genetics

purpose To investigate the protective effect and character of dl-praeruptorin A(Pd-Ia)on focal cerebral ischemia in mice.Methods Transient focal cerebral ischemia in mice WaS induced by middle cerebral artery occlusion for 1.5 h.Pd-Ia was administered intraperitoneally either with multiple doses(1,5 and 10ms/ks)at 0.5 h before ischemia or single dose(5 ms/kg)at 0.5 h and 1 h before ischemic,the same time of ischemia,the same time of reperfusion,or 0.5 h and 1 h after reperfusion respectively.Neurological deficit score,infarct volume,brain edema,the activities of SOD and the contents of MDA were determined.Results Pretreatment with multiple doses(5 and 10 ms/ks)of Pd-Ia at 0.5 h before ischemia or single dose(5 mg/kg)of Pd-Ia at 0.5 h before ischemia,at the same time of ischemic,at the same time of reperfusion and 0.5 h after reperfusion significantly attenuated neurological deficit score,decreased infarct volume and alleviated brain edema,and the treatment at the time of reperfusion had the most marked effect.Pd-Ia(5 or 10 ms/ks)can significantly enhance the activities of SOD and lower the contents MDA.Conclusion dl-praeruptorin A has a neuroprotective effect on the injury in the acute phase of transient focal cerebral ischemia in mice,with optimal doses of 5 ms/ks and the optimal therapeutic time point of the same time of reperfusion.

Using the concepts and methods of epigenetics and metabolomics, to investigate the overall action molecular mechanism of Chrysanthemi indici C (CIC), the anti-hepatitis B virus (HBV) active extracts from Flos chrysanthemi indici. The inhibitory effects of CIC on proliferation and hepatitis B surface antigen (HBsAg), hepatitis B envelope antigen (HBeAg) and HBV-DNA of HepG2.2.15 cells were detected by CCK-8 and antigen kit. The DNA methyltransferases (DNMTs)/ten-eleven-translocation-2 (TET2) equilibrium was detected by ELISA. Illumina 850K methylation chip, pyrosequencing and qPCR were used to determine the action pathway and target of CIC by GO and KEGG analysis. Cell metabolites were extracted with 80% methanol, and the changes of differential metabolites, differential metabolic pathways and cell microenvironment were detected by LC-MS and other metabolomics methods. The results showed that CIC could inhibit the proliferation, HBsAg, HBeAg and HBV-DNA of HepG2.2.15 cells obviously, down-regulate DNA methyltransferase 1 (DNMT1), DNA methyltransferase 3a (DNMT3a) and DNA methyltransferase 3b (DNMT3b), up-regulate TET2, and restore the balance of DNMTs/TET2. The action targets of CIC were phospholipase C gamma 2 (PLCG2), phosphoinositide-3-kinase regulatory subunit 3 (PIK3R3), 1-acylglycerol-3-phosphate O-acyltransferase 2 (AGPAT2), 5-hydroxytryptamine receptor 2B (HTR2B), nerve growth factor (NGF), mainly involved in lipid metabolism, inflammation mediated regulation of transient receptor potential (TRP), phospholipase D signaling and advanced glycation end product-receptor for AGE (AGE-RAGE) signaling in diabetic complications pathways. CIC could significantly affect fatty acid metabolism and had great influence on phenolic acid, alkaloid and lipid metabolites in cell microenvironment. These results suggest that the action mechanism of CIC may be the synergistic action of multiple pathways and multiple targets, including related inflammatory pathways, immune pathways and lipid metabolism, through regulating epigenetic expression balance and restoring the balance of cell microenvironment.

Objective To explore the relationship between methionine synthase reductase (MTRR) gene polymorphism and cerebral infarction in young and middle-aged patients. Methods The genotype of MTRR A66G was analyzed by polymerase chain reaction-restrictive fragment length polymorphism (PCR-RFLP) and the plasma homocysteine (Hcy) level was measured by high performance liquid chromatography in 105 young and middle-aged patients with cerebral infarction and 116 age-matched healthy controls. Results The genotype distribution and allele frequencies of MTRR A 66G gene between the 2 groups had no statistical significance (P＞0.05).Stratified analysis,performed according to whether cerebral infarction was complicated with hypertension,diabetes or coronary heart disease,indicated that the frequencies ofGG genotype and G allele in cerebral infarction patients without complications were obviously higher than those in controls (36.4％ vs.23.3％,62.1％ vs.52.2％),but no statistical significance was noted between them (P＞0.05).No statistical difference was observed between cerebral infarction patients with complications and controls (P＞0.05). The mean plasma Hcy level in patients and controls with GG genotype was significantly higher than that in patients and controls with AA genotype (P＜0.05). Conclusion No association between MTRR A 66G polymorphism and cerebral infarction is noted in young and middle-aged patients, while GG mutant homozygous ofMTRR A66G gene can significantly raise the plasma Hcy level.

Objective To investigate the relationship between serum thyrotrophin(TSH)and dyslipidemia in subclinical hypothyroid and euthyroid subjects. Methods An epidemiological study on diabetes and thyroid diseases was performed in Dadong community, Shenyang city, in 2007. 110 subjects with subclinical hypothyroidism(SCH)and 1 240 euthyroid subjects were enrolled in the study. Neither history of thyroid diseases nor administration of thyroid-related and lipid-regulating medicines were reported in these subjects. The levels of serum thyroid hormones, lipids, fasting plasma glucose(FPG), and insulin were determined. Results (1)Patients with SCH had significantly lower HDL-C levels than those who were euthyroid.(2)According to the guideline of treatment of adult dyslipidemia in China, the lipid profiles were each categorized. Mean TSH levels were higher in subjects in the dyslipidemia subclass than subjects in the normal subclass. The differences were significant in high LDL-C subclass in overweight individuals. In euthyroid overweight women, mean TSH levels were significantly higher in high LDL-C subclass. In the euthyroid population, TSH was positively associated with total cholesterol in overweight population. The association was not modified by the homestasis model assessment for insulin resistance(HOMA-IR)values.(3)TSH was associated positively with serum triglycerides and negatively with serum HDL-C in women. TSH was positively associated with total cholesterol in overweight population and positively associated with total cholesterol and LDL-C in overweight women after adjustment for age, sex, and body mass index. Conclusion Raised serum TSH seems to be a risk factor of dyslipidemia in subclinical hypothyroid and euthyroid subjects, which is independent of insulin sensitivity.

BACKGROUNDTo explore the feasibility of extended resection in selective patients with centrally located lung cancer.

METHODSFrom January, 1987 to December, 2001, lobectomy or pneumonectomy combined with extended resection of trachea, bronchus, heart or great vessels were carried out in 134 patients with centrally located lung cancer. The operations included bronchoplastic procedures in 80 cases, extended resection and reconstruction of left atrium and/or great vessels in 54 cases (32 cases with contemporary bronchoplasty).

RESULTSOperative death occurred in one case. Postoperative complications happened in 16 cases (11.9%). One hundred and seventeen cases (94.4%) were followed up. The 1-, 3-, 5-year survival rate was 84.7% (61/72), 56.7% (34/60) and 45.7% (21/46) respectively, while of those combined with tracheo bronchoplasty and/or cardiovascular reconstruction, the 1-, 3-, 5-year survival rate was 69.2% (36/52), 46.8% (22/47) and 22.2% (8/36) respectively. (P < 0.05), while expression of KAI1 mRNA did not relate to mutant P53 protein expression (P > 0.05).

CONCLUSIONSExtended resection combined with tracheo-bronchoplasty and/or cardiovascular reconstruction is feasible for selected patients with centrally located lung cancer and could improve the survival and life quality of patients.

Adolescent ; Adult ; China ; epidemiology ; Disease Outbreaks ; Female ; Humans ; Incidence ; Legionnaires' Disease ; classification ; epidemiology ; transmission ; Male

OBJECTIVETo investigate the relationship between sympathetic remodeling and electrical remodeling at the infarcted border zone (IBZ) of rabbit with chronic myocardial infarction (MI).

METHODSThirty rabbits were randomly assigned into two groups: MI group (n = 20): ligation of the anterior descending coronary; sham operation (SO) group (n = 10): without contrary ligation. Eight weeks after surgery, transmural dispersion of repolarization (TDR) at baseline, during sympathetic nerve stimulation, TDR change (DeltaTDR) during sympathetic nerve stimulation and ventricular fibrillation threshold (VFT) were measured at the IBZ in MI group and corresponding zone in SO group. The distribution and densities of growth associated protein 43 (GAP43) and tyrosine hydroxylase (TH) positive nerves in ventricle were also detected with immunohistochemical techniques.

RESULTSEighteen rabbits in the MI group and 10 in the SO group survived to the end of the study. The densities of GAP43 and TH at the IBZ in the MI group were significantly higher than that at the corresponding zone in the SO group (both P < 0.05). The densities of GAP43 and TH in MI rabbits positively correlated with TDR at baseline, TDR or DeltaTDR during sympathetic nerve stimulation (all P < 0.01) and both showed a weak negative correlation with VFT (r =-0.44, P = 0.07; r = -0.41, P = 0.09, respectively).

CONCLUSIONSympathetic remodeling is correlated with electrical remodeling at the IBZ in rabbits with chronic MI.

Action Potentials ; Animals ; Humans ; Male ; Myocardial Infarction ; pathology ; physiopathology ; Rabbits ; Random Allocation ; Sympathetic Nervous System ; physiopathology