Objective To develop an in vitro method to determine the effects of drugs on tyrosinase(TYR)activity and screen the inhibitory effects on TYR of14extracted components of Chinese medicinal herbs.Methods The activity of TYR was detected by revised Matsuda's method.Effects of14extracted com-ponents on tyrosinase system were observed in vitro.Results Ten of the14components showed dose-depen-dent down-regulation of tyrosinase activity and melanogenesis.The inhibitory activities of eugenol,curcumin and gallic acid were significantly higher than those of arbutin(P

Aim To observe the effect of Guishao-tongluo ( GSTL ) on the angiogenesis of vasa vasorum and oxidative stress in the early stage of atherosclero-sis. Methods The rabbits ( n =84 ) were randomly divided into 7 groups (n=12):control group,high-fat group, adventitial injury group, GSTL high(GH)and medium ( GM ) dose group, atorvastain group ( ATO ) , and Tongxinluo group ( TXL ) . The normal group was fed with common foodstuffs, and high-fat foodstuffs for the high-fat group to establish an early model of hyper-lipidemia, and all the other groups were fed with high-fat diet combined with carotid artery cannula to build early atherosclerosis carotid artery injury rabbit mod-els. The GSTL high and medium dose was given Guishaotongluo ultrafine powder 4. 16,2. 08 g·kg-1 · d-1 respectively. The atorvastain group and Tongxinluo group were given suspension of atorvastain solution 2. 5 mg·kg-1 ·d-1 , Tongxinluo supermicro powder 0. 6 g ·kg-1 ·d-1 . All groups were treated with gastric per-fusion for 4 weeks. Biochemical method was applied to detect blood lipid change. HE staining was used to ob-serve the pathological morphology of intima-media. Aactivity of serum superoxide dismutase( SOD) ,malon-dialdehyde ( MDA ) content and the total antioxidant capacity ( T-AOC ) in artery serum were detected. NADPH subunits p22phox mRNA, gp91phox mRNA in carotid arteries were located and semi-quantitated by fluorescence in situ hybridization. The expression of VEGF, VEGFR-2 in the carotid artery adventitia was detected by Western blot. Results Compared with normal group,the contents of TC,TG and LDL-C were significantly increased, and VEGF, VEGFR-2 protein levels were remarkly increased in high-fat and adventi-tial injury group. The carotid artery injuries,the degree of angiogenesis of vasa vasorum and NADPH subunits p22phox, gp91phox mRNA in adventitia tissue of the GH,GM, ATO and TXL group were milder in varying degrees compared with those of the vasa injury group. Also the activity of SOD,T-AOC increased,while MDA content,VEGF,VEGFR-2 protein levels were remarkly decreased ( P < 0. 5 or P < 0. 01 ) . Conclusions GSTL can inbibit adventitial neovascularization in the early stage of atherosclerosis, and its mechanism might be related to the increase of total antioxidant capacity of the vascular system and adventitia tissue.

Objective To explore the impact of intermittent androgen deprivation therapy on prostate volume and lower urinary tract symptoms (LUTS) in patients with prostate cancer combined with prostatic hyperplasia (BPH),and to evaluate the clinical effect of intermittent androgen deprivation therapy as compared with conventional drug in patients with BPH.Methods Patients with prostate cancer (n=57) and BPH (n=83) were respectively treated with intermittent androgen deprivation therapy and finasteride combined with alpha-receptor antagonist.Prostate volume,international prostate symptom score (IPSS),quality of life index (QOL) and maximum urinary flow rate (Qmax) in patients were observed before and 1,3,6 and 12 months after treatment.Results The improvements in prostate volume,IPSS,QOL and Qmax were higher in prostate cancer patients treated with intermittent androgen deprivation therapy than in BPH patients treated with finasteride combined with alpha-receptor antagonist (P ＜ 0.05).Conclusions Intermittent androgen deprivation therapy can significantly reduce prostate volume and improve LUTS in patients with prostate cancer,and has a better clinical effect than finasteride combined with alpha-receptor antagonist treatment.

Objective To investigate the relationship between chronic prostatitis (CP) and male infertility. Methods 120 cases of male infertility patients with chronic prostatitis and 120 cases of male infertility patients with-out chronic prostatitis were analyzed. Results The differences of sperm quality、sperm movement function, partial bio-chemical indicator in semen and sperm aggregation in the two groups are significant (P<0.05). Conclusion CP plays an important negative role in male infertility.

[ ABSTRACT] AIM:To investigate the transient outward potassium channel protein expression in paraventricular nucleus (PVN) and its contribution to renal sympathetic nerve activity (RSNA) in rats with chronic heart failure (CHF). METHODS:A rat model of CHF was prepared by acute myocardial infarction that was induced by ligation of the left ante -rior descending coronary artery .Four weeks after heart failure , echocardiogram was applied to identify the CHF model and plasma norepinephrine (NE), serum NH2-terminal pro-brain natriuretic peptide (NT-proBNP) were detected by ELISA. The expression of ransient outward potassium channel proteins Kv 4.2 and Kv4.3 at mRNA and protein levels was deter-mined by real-time PCR and Western blot .The mean arterial pressure ( MAP) , heart rate ( HR) and RSNA were measured in anesthetized rats with PVN microinjection of potassium channel blockers 4-AP.RESULTS:In CHF group , the rat car-diac function and Kv4.2 and Kv4.3 expression in PVN were obviously lower while plasma NE and serum NT-proBNP were obviously higher than those in sham group .Microinjection of 4-AP into PVN induced an increase in MAP , HR and RSNA in both sham and CHF rats , while the CHF rats exhibited smaller responses to 4-AP than sham-operated rats .CONCLU-SION:Downregulation of Kv4.2 and Kv4.3 expression in the PVN may be a potential mechanism for sympathoexciation in the rats with chronic heart failure .

Objective: To observe the effect of Tongxinluo (TXL) on homocysteine-induced rat’s cardiac micro vascular endothelial cell (RCMECs) injury and to study the oxidative stress mechanism. Methods: Primary RCMECs were cultured with tissue explants process, cell morphology was observed by inverted microscope and the cell was identiifed by CD31 immunolfuorescence method. RCMEC injury model was established by Homocysteine (Hcy) induction and the cells were divided into 5 groups: Control group, with normal cells, Hcy group, the cells were treated by Hcy at 10 mmol/L, Low-dose TXL group, Hcy treated cells were cultured with TXL at 100 mg/L, Middle-dose TXL (200 mg/L) group and high-dose TXL (400 mg/L) group. Cell survival rates were detected, supernatant levels of superoxide dismutase (SOD) activity and malondialdehyde (MDA) content were examined, intracellular protein expressions of reactive oxygen species (ROS) and endothelial nitric oxide synthase (eNOS) were detected and mRNA expression of endothelin-1 (ET-1) was measured in different groups respectively. Results: Compared with Control group, Hcy group showed decreased cell survival rate (74.61 ± 2.88)% vs (100.00 ± 2.07)%, increased supernatant level of MDA (4.10 ± 0.18) nmol/ml vs (1.92 ± 0.10) nmol/ml, reduced SOD activity (7.55 ± 0.71) U/ml vs (20.77 ± 0.68) U/ml, elevated ROS level(38.17 ± 10.28) % vs (19.83 ± 2.97) %, up-regulated mRNA expression of ET-1 and down-regulated protein expression of eNOS. Compared with Hcy group, the above indexes were improved in each TXL group at different levels. Conclusion: TXL could decrease Hcy induced RCMECs injury, such protection was conducted by reducing the oxidative stress mechanism in cells.

This paper is to report the polymorphism of raw materials of clopidogrel bisulfate at home and abroad. By the analysis of Fourier transform infrared spectroscopy (FTIR) and powder X-ray diffraction (p-XRD), samples are roughly classified into two groups, except one patent material. And the differential scanning calorimeter (DSC) examination showed more detailed information for these materials. The results of the study could provide comprehensive basis for the quality evaluation of clopidogrel bisulfate.
Calorimetry, Differential Scanning ; Crystallization ; Evaluation Studies as Topic ; Platelet Aggregation Inhibitors ; chemistry ; Spectroscopy, Fourier Transform Infrared ; Ticlopidine ; analogs & derivatives ; chemistry ; X-Ray Diffraction

OBJECTIVE: To analyze the clinical and genetic characteristics of a boy featuring unexplained developmental delay, malnutrition and distinct facial appearance. METHODS: Physical examination was carried out for the child. Peripheral blood samples were collected from the child and his parents for the extraction of genomic DNA and trio-whole exome sequencing. Candidate variants were verified by Sanger sequencing. RESULTS: The patient had facial dysmorphism including nasal alae aplasia, scalp defect and teeth deformities, in addition with recurrent diarrhea due to pancreatic exocrine insufficiency. DNA sequencing revealed that he has harbored compound heterozygous variants of the UBR1 gene, namely c.3167C>G (p.S1056X) and c.1911+14C>G, which were inherited from his father and mother, respectively. Database search has suggested the c.3167C>G to be a novel nonsense variant and c.1911+14C>G a known splicing variant. Based on the guidelines of the American College of Medical Genetics and Genomics, the two variants were predicted to be pathogenic and likely pathogenic, respectively. CONCLUSION The child was diagnosed with Johanson-Blizzard syndrome due to the compound heterozygous variants of the UBR1 gene. Above finding has enriched the mutational spectrum of the UBR1 gene and provided a basis for genetic counseling for this family.
Child ; Humans ; Male ; Ectodermal Dysplasia/genetics* ; Pancreatic Diseases/genetics* ; Ubiquitin-Protein Ligases/genetics*

Objective To analyze the composition and influencing factors of hospitalization expenses for diabetic patients，and to provide reference for effective control of medical expenses. Methods The hospitalization cost data of diabetes patients in rural areas of Wugang from 2013 to 2017 were collected. Structural change analysis，non-parametric test and BP (Back Propagation)neural network model were used to analyze the hospitalization expenses and influencing factors. Results The top three components of hospitalization expenses were drug cost (50.02%), examination cost (15.35%) and laboratory cost (12.06%). The contribution rates of structural change of hospitalization expenses were the examination fee (41.00%), drug fee (34.92%) and treatment fee (13.41%), respectively. Factors affecting the total hospitalization cost of diabetic patients included length of stay, operation or not, hospital level, age, discharge year, complication or not and gender (P<0.05), among which length of stay had the greatest impact (sensitivity value was 0.669). Conclusion The hospitalization expenses of patients with diabetes is affected by a variety of factors. It is suggested to optimize the composition of hospitalization expenses by improving the price mechanism of medical services, and to control and reasonably reduce hospitalization expenses by implementing standardized management of clinical pathways, implementing two-way referral and strengthening tertiary prevention.