The aim of the present study was to investigate the effects of quercetin on colon contractility and voltage-dependent Ca(2+) channels in the single smooth muscle cell isolated from the proximal colon of guinea-pig and to clarify whether its effect on L-type Ca(2+) current (I(Ca,L)) would be related to its myorelaxing properties. Colon smooth muscle strips were used to take contractile tension recordings. Smooth muscle cells were freshly isolated from the proximal colon of guinea-pig by means of papain treatment. I(Ba,L) (barium instead of calcium as current carrier) was measured by using whole-cell patch-clamp techniques. The results showed that quercetin relaxed colon muscle strips in a concentration-dependent manner and antagonized the contractile effect of acetylcholine and neostigmine. Preincubation with indomethcin [cyclooxygenase (COX) inhibitor] and methylene blue [guanylate cyclase (GC) inhibitor] significantly attenuated the relaxing effect of quercetin, respectively. Quercetin increased I(Ba,L) in a concentration- [EC(50)= (7.59+/-0.38) mumol/L] and voltage-dependent pattern, and shifted the maximum of the current-voltage curve by 10 mV in the depolarizing direction without modifying the threshold potential for Ca(2+) influx. Quercetin shifted the steady-state inactivation curve toward more positive potentials by approximately 3.75 mV without affecting the slope of activation and inactivation curve. H-89 (PKA inhibitor) abolished quercetin-induced I(Ba,L) increase, while cAMP enhanced the quercetin-induced I(Ba,L) increase. The patch-clamp results proved that quercetin increased I(Ba,L) via PKA pathway. It is therefore suggested that the relaxing effect of quercetin attributes to the interaction of GC and COX stimulation, as well as the antagonism effect on acetylcholine, which hierarchically prevails over the increase in the Ca(2+) influx to be expected from I(Ca,L) stimulation.
Animals ; Calcium Channels, L-Type ; metabolism ; Cells, Cultured ; Colon ; drug effects ; Guinea Pigs ; Muscle Contraction ; Myocytes, Smooth Muscle ; drug effects ; Patch-Clamp Techniques ; Quercetin ; pharmacology

Diastole ; physiology ; Exercise ; physiology ; Fractional Flow Reserve, Myocardial ; Heart Rate ; Humans ; Systole ; physiology ; Young Adult

The borneol was included with β-CD and prepared Fufang Danshen intestinal adhesion pellets. GC method for determination of borneol in Fufang Danshen intestinal adhesion pellets was established to study its in vitro dissolution and make a comparison with the Fufang Danshen tablet, in this way, the rationality of dosage form was evaluated. The first method of dissolution determination was used for determining the in vitro dissolution of borneol in Fufang Danshen intestinal adhesion pellets in artificial intestinal juice, and Fufang Danshen tablet in artificial gastric juice and intestinal juice, respectively. Result shows: the concentration of borneol in Fufang Danshen intestinal adhesion pellets and Fufang Danshen tablet was 0.79% and 0.80%, respectively. Its in vitro dissolution was nearly 70% within 12 h in Fufang Danshen intestinal adhesion pellets, and in Fufang Danshen tablet, the dissolution was about 60% within 20 min and more than 90% within 40 min, and in artificial gastric juice, was less than 20% within 40 min but more than 80% till 150 min. Research suggests that in comparison with Fufang Danshen tablet, in vitro dissolution of borneol in the Fufang Danshen intestinal adhesion pellets showed an obvious sustained release behavior. The borneol in Fufang Danshen intestinal adhesion pellets was included with β-CD and prepared enteric preparations. To some extent, the stimulation on stomach and intestinal mucosa can be reduced and safety can be improved.
Bornanes ; adverse effects ; chemistry ; pharmacology ; Chemistry, Pharmaceutical ; methods ; Dosage Forms ; Drugs, Chinese Herbal ; adverse effects ; chemistry ; pharmacology ; Humans ; Intestinal Mucosa ; drug effects ; metabolism ; Models, Biological ; Solubility

AIMTo assess the possible role of genetic polymorphisms in DNA repair gene XRCC1 (X-ray repair cross-complementing group 1) during spermatogenesis by investigating the associations of one promoter polymorphism (T-77C) and two exonic polymorphisms (Arg194Trp and Arg399Gln) in XRCC1 gene with risk of idiopathic azoospermia in a Chinese population.

METHODSThe genotype and allele frequencies of three observed polymorphisms were examined by polymerase chain reaction-restriction fragment length polymorphism based on a Chinese population consisting of 171 idiopathic azoospermia subjects and 247 normal-spermatogenesis controls.

RESULTSIn our study, all the observed genotype frequencies were in agreement with Hardy-Weinberg equilibrium. The 399A (GA+AA) allele frequency for idiopathic azoospermia subjects and controls was 0.216 and 0.269, respectively. Compared with GG genotype, the AA genotype of Arg399Gln showed a significant association with a decreased risk of idiopathic azoospermia (odds ratio = 0.315; 95% confidence interval = 0.12-0.86). However, no significant differences were found between the cases and controls for T-77C and Arg194Trp polymorphisms. The major haplotypes of XRCC1 gene were TCG, TTG and TCA, whereas no haplotypes appeared to be significantly associated with idiopathic azoospermia based on the cutoff of P < 0.05.

CONCLUSIONIn a selected Chinese population, AA genotype of Arg399Gln appears to contribute to a decreased risk of idiopathic azoospermia, while we have not any evidence of involvement of XRCC1 T-77C and Arg194Trp polymorphisms in idiopathic azoospermia.

Adult ; Asian Continental Ancestry Group ; ethnology ; genetics ; Azoospermia ; ethnology ; genetics ; Case-Control Studies ; China ; DNA-Binding Proteins ; genetics ; Gene Frequency ; Genetic Predisposition to Disease ; Genotype ; Humans ; Infertility, Male ; genetics ; Male ; Polymorphism, Restriction Fragment Length ; genetics ; Risk Factors ; Spermatogenesis ; genetics ; X-ray Repair Cross Complementing Protein 1

Recently, compound Ejiao slurry (FFEJJ) had been applied to treat cancer patients in clinic, with obvious curative effect. In this study, data and literatures were collected from the TCM chemical component database to establish the chemical component database of FFEJJ. Afterwards, MetaDrug software was used to predict the targets of FFEJJ and obtain the compound-target network. Next, the compound-target network was compared and analyzed to obtain the "compound-target-tumor target" heterogeneous network. Besides, further analysis was made on gene functions and metabolic pathway. The results indicated that FFEJJ could directly resist tumors by regulating cancer cell differentiation, growth, proliferation and apoptosis, and show an adjuvant therapeutic effect by enriching the blood and increasing the immunity.
Adjuvants, Pharmaceutic ; therapeutic use ; Antineoplastic Agents ; therapeutic use ; Drugs, Chinese Herbal ; therapeutic use ; Gene Regulatory Networks ; drug effects ; Humans ; Molecular Targeted Therapy ; Neoplasms ; drug therapy ; genetics ; metabolism

OBJECTIVETo establish a model for predicting the density of Aedes albopictus based on the climate factors.

METHODSThe data of Aedes albopictus density and climate changes from 1995 to 2001 in Guangzhou were collected and analyzed. The predicting model for Aedes albopictus density was established using the Artificial Neural Network Toolbox of Matlab 7.0 software package. The climate factors used to establish the model included the average monthly pressure, evaporation capacity, relative humidity, sunshine hour, temperature, wind speed, and precipitation, and the established model was tested and verified.

RESULTSThe BP network model was established according to data of mosquito density and climate factors. After training the neural network for 25 times, the error of performance decreased from 0.305 539 to 2.937 51x10(-14). Verification of the model with the data of mosquito density showed a concordance rate of prediction of 80%.

CONCLUSIONThe neural network model based on the climate factors is effective for predicting Aedes albopictus density.

Aedes ; physiology ; Animals ; Climate ; Neural Networks (Computer) ; Seasons ; Software

OBJECTIVETo explore the relationship between polymorphisms of natural resistance-associated macrophage protein 1 (NRAMP1) gene and genetic susceptibility of pulmonary tuberculosis (PTB) in workers exposed to silica dusts.

METHODSA 1:2 case control study of 61 male workers with PTB (50 silicosis patients and 11 unsilicosis workers) as the case group and 122 male PTB-free workers (100 silicosis patients and 22 unsilicosis workers) as the control group was conducted with the frequency matched for age of +/- 5 years, the job, the silica exposure, and the condition of cigarette smoking and alcohol drinking. The polymerase chain reaction-restrained fragment length polymorphism technique (PCR-RFLP) was used to detect the single nucleotide polymorphisms (SNPs) of NRAMP1 INT4 and D543N.

RESULTSThere was a 2.73 times (95% CI: 1.32 approximately 5.64) increased risk of silicosis for individuals with C allele of NRAMP1 INT4 compared with individuals carrying homozygote (G/G), while SNPs of NRAMP1 D543N was not associated with PTB (P > 0.05).

CONCLUSIONThe G > C mutation of intron 4 of NRAMP1 gene might be a susceptible factor of silica for the workers exposed to PTB.

Aged ; Alleles ; Case-Control Studies ; Cation Transport Proteins ; genetics ; Genetic Predisposition to Disease ; Humans ; Middle Aged ; Polymerase Chain Reaction ; Polymorphism, Restriction Fragment Length ; Silicosis ; complications ; Tuberculosis, Pulmonary ; complications ; genetics

OBJECTIVETo study the effects of carbon disulfide (CS(2)) on the health of workers, and to provide the basis for the further preventive measures.

METHODSThe occupational health examination of 881 workers exposed to CS(2) in a chemical fiber factory was carried out according to the national technical standard of occupational health surveillance. The time weighted average concentrations (TWA) of CS(2) in the workshops of short silk and long silk exceeded the national standard, The workers in these two workshops served as the high exposure group. The workers of the other workshops were classified as low exposure group, in which TWA met the national standard. All exposed workers were also divided into long-term exposure group and short-term exposure group on the basis of average exposure years (16 years). The statistical analysis was used by t test, χ(2), and fisher exact test.

RESULTSThe symptom rates of numbness, fatigue, dizziness, insomnia and headache were 12.5%, 8.5%, 8.2%, 7.5%, and 7.2% respectively. The abnormal rates of superficial sensation, three fibrillation, achilles tendon reflex, patellar reflex, EMG, hypertension, triglycerides, low-density lipoprotein, and apolipoprotein B were 33.0%, 26.1%, 20.8%, 18.6%, 10.8%, 33.4%, 24.5%, 17.0% and 9.3% respectively. Among the high exposure group, the abnormal detectable rates of dizziness, headache, fatigue, insomnia, numbness, achilles tendon reflex, superficial and deep sensation, EMG, hypertension, ECG, total cholesterol, triglyceride and low density lipoprotein in long-term exposure group were significantly higher than those in short-term exposure group (P < 0.05 or P < 0.01). However, among the low exposure group, the abnormal rates of the insomnia achilles tendon reflex and superficial sensation in long term exposure group were significantly higher than those of short term exposure group (P < 0.05 or P < 0.01). The detected rates of hypertension, triglycerides, low-density lipoprotein, creatinine and uric acid were in males significantly greater than those in females (P < 0.05 or P < 0.01).

CONCLUSIONLong-term exposure to high concentrations of CS(2) could lead to the damage of nervous system, elevate blood pressure and promote the development and progression of hyperlipemia and atherosclerosis. Furthermore, CS(2) had greater effects on blood pressure and lipid in males than in females.

Adult ; Carbon Disulfide ; adverse effects ; Cardiovascular System ; Chemical Industry ; Female ; Health Status ; Humans ; Male ; Middle Aged ; Multiphasic Screening ; Nervous System Diseases ; epidemiology ; Occupational Exposure ; Young Adult

In order to study the possibility of xenotransfusion from porcine red blood cell (pRBC) to primate, the antigens on pRBC surface were modified to make it more compatible to primate sera. Porcine RBCs were subjected to both enzymatic removal of membrane alpha-Gal antigens with recombinant alpha-galactosidase (AGL) and covalent attachment of succinimid propionate-linked methoxypolyethyleneglycol (mPEG-SPA) to camouflage non-alphaGal antigens. The effects of double modifications were determinated by hemagglutination and clinical cross-match testing with rhesus sera. In vivo clearance rates and safety of modified pRBCs were measured after it was transfused into Rhesus monkey with or without immunosuppressant treatment. The validity of pRBC was detected in exsanguine Rhesus monkey model. The results showed that AGL could effectively remove alpha-Gal xenoantigens on pRBC membrane and reduce hemagglutination. The combination of mPEG modification with AGL treatment could significantly increased compatibility between pRBCs and Rhesus monkey sera. Modified pRBCs were detectable in Rhesus monkey blood at 12 hours after transfusion, and their survival time was 40 hours in the immunosuppressant-treated Rhesus monkey. In vivo survival rates of pRBCs were 38% in exsanguine Rhesus monkey at 8 hours after transfusion, and during that time, the hemoglobin and hematocrit of Rhesus monkey were maintained at the same level as before it lost blood. It is concluded that the modified pRBC can be safely transfused into Rhesus monkey and relieve the anemic symptom exsanguine Rhesus monkey. It suggested that pRBC can be hopefully used as a blood substitute for primate and human in the future.
Animals ; Erythrocyte Transfusion ; methods ; Erythrocytes ; drug effects ; immunology ; Hemagglutination Tests ; Macaca mulatta ; immunology ; Polyethylene Glycols ; pharmacology ; Swine ; blood ; Transplantation, Heterologous ; methods ; alpha-Galactosidase ; pharmacology

OBJECTIVETo study the chemical constituents in the Galeobdolon chinense.

METHODThe chemical constituents were separated by means of chromatogrophy, and their structures were identified by spectra of FAB-MS, IR, UV, 1H-NMR, 13C-NMR, DEPT, HMQC and HMBC.

RESULTTwo compounds were obtained and identified as galeobdoside (I) whose structure was apigenin-7-O-beta-D-(6'-p-hydoxy-cinnamoyloxy)-mannoside and verbascoside (II).

CONCLUSIONCompound I was a new compound and compound II was obtained from this plant for the first time.

Flavonoids ; chemistry ; isolation & purification ; Glucosides ; chemistry ; isolation & purification ; Lamiaceae ; chemistry ; Mannosides ; chemistry ; isolation & purification ; Molecular Conformation ; Molecular Structure ; Phenols ; chemistry ; isolation & purification ; Plants, Medicinal ; chemistry