A double targets of high throughput screening model for xanthine oxidase inhibitors and superoxide anion scavengers was established. In the reaction system of xanthine oxidase, WST-1 works as the probe for the ultra oxygen anion generation, and product uric acid works as xanthine oxidase activity indicator. By using SpectraMax M5 continuous spectrum enzyme sign reflectoscope reflector, the changes of these indicators' concentration were observed and the influence factors of this reaction system to establish the high throughput screening model were studied. And the model is confirmed by positive drugs. In the reaction system, the final volume of reaction system is 50 μL and the concentrations of xanthine oxidase is 4 mU x mL(-1), xanthine 250 μmol x L(-1) and WST-1 100 μmol x L(-1), separately. The Z'-factor of model for xanthine oxidase inhibitors is 0.537 4, S/N is 47.519 9; the Z'-factor of model for superoxide anion scavengers is 0.507 4, S/N is 5.388 9. This model for xanthine oxidase inhibitors and superoxide anion scavengers has more common characteristics of the good stability, the fewer reagent types and quantity, the good repeatability, and so on. And it can be widely applied in high-throughput screening research.
Enzyme Inhibitors ; pharmacology ; Free Radical Scavengers ; pharmacology ; High-Throughput Screening Assays ; Superoxides ; Uric Acid ; Xanthine ; Xanthine Oxidase ; antagonists & inhibitors

To enhance the quality and efficiency of ozagrel by investigating the differences between the ozagrel polymorphs in bioavailability. Solid ozagrel in different polymorph forms were orally administered to SD rats. An HPLC method was established to determinate plasma level of ozagrel. The bioavailabilities of two polymorph forms were calculated and compared. The pharmacokinetic parameters of ozagrel, were as follows: Cmax was 32.72 ± 17.04 and 34.01 ± 19.13 mg · L(-1), respectively; AUC0-t was 61.14 ± 14.76 and 85.56 ± 18.08 mg · L(-1) · h, respectively; t½ was 1.53 ± 0.51 and 4.73 ± 3.00 h, respectively. There was no significant difference in pharmacokinetic parameters between form I and II polymorphs of ozagrel while the t½ of form II is longer, which indicates that the use of form II polymorph as pharmaceutical product may prolong the effective action time in clinics. This would help the polymorph quality control in drug production.
Animals ; Biological Availability ; Chromatography, High Pressure Liquid ; Methacrylates ; chemistry ; pharmacokinetics ; Rats ; Rats, Sprague-Dawley

No abstract available.
Gastrins*

OBJECTIVETo record the electrical activities of Antirior cingulate cortex (ACC) neurons by in vivo multi-channel recording methods using the model of complete freund's adjuvant (CFA) induced conditioned place avoidance (C-CPA), which has been set up in our previous studies.

METHODSThe electrode was self-made and the CPA responses were recorded by in vivo multi-channel recording method.

RESULTS(1) The electrical activities of ACC neurons could be successfully recorded by the self-made electrode. (2) Before or after the injection of CFA, rats were respectively conditioned to the different place. The firing rates of ACC neurons in the CFA-paired place vs that in the non-CFA-paired place was (0.853 ± 1.377) imp/s vs (0.221 ± 0.971) imp/s (P < 0.05, n = 26). (3) The CPA responses in the CFA-paired place vs that in the non-CFA-paired place were (303.55 ± 61.77)s vs (140.32 ± 33.52)s(P < 0.05, n = 6).

CONCLUSIONThe firing rates of rACC (rostral Anterior Cingulate Cortex) neurons were involved in the occurrence of the affective pain.

Animals ; Electrodes ; Freund's Adjuvant ; Gyrus Cinguli ; cytology ; Neurons ; cytology ; Pain ; diagnosis ; Pain Measurement ; methods ; Rats ; Rats, Sprague-Dawley

No abstract available.
Angiotensin II* ; Angiotensins* ; Hydrocortisone* ; Insulin*

Japan moxibustion methods originate from China and form moxibustion methods with Japanese characteristics and diathermal moxibustion as main, in combination with Japanese practice in development course. In the present paper, diathermal moxibustion and folk traditional moxibustion methods in Japan are introduced and moxibustion methods between China and Japan are preliminarily compared.
Humans ; Japan ; Medicine, East Asian Traditional ; Moxibustion ; methods

Objective In order to analyze the variation of HA genes of influenza viruses (H1N1) by being compared with the vaccine strain A/California/07/2009(H1N1) recommended by WHO ,influenza viruses (H1N1) isolated from 2009 to 2014 were selected to do this study .Methods According to the different isolating time and place ,47 strains of H1N1 collected from 2011 to 2014 were selected .Then the 47 strains′ nucleotide sequence of HA genes which were sequenced in the study and other 25 se‐quences of HA genes which were sequenced in 2009 were collected .Nucleotide and amino acid sequences were analyzed by using molecular biology software ,and the phylogenetic trees were drawn .Results A total of 72 strains isolated from 2009 to 2014 were closely related to the vaccine strain A/California/07/2009(H1N1) ,the nucleotide variance and amino acid variance between the 72 strains were 0-2 .7% and 0-3 .1% respectively .Compared with the vaccine strain A/California/07/2009(H1N1) ,the nucleotide variance and amino acid sequence variance were 0 .4% -2 .4% and 0 .9% -3 .1% respectively .The amino acids sequence indicated that ,although the variance was increased by years ,the H1N1 viruses were still showed characteristics of low pathogenic influenza viruses .It was also found that there were 9 strains lost their potential glycosylation site at HA protein site 481 in 2009 ,while in 2013 there were 6 strains got new potential glycosylation sites at HA protein site 162 .Conclusion The vaccines (H1N1) recom‐mended by WHO was still protective to people in Chongqing .But as time goes by ,antigen drift may occur in some new antigenic drift strains and the routine monitoring of influenza viruses should be continued .

OBJECTIVE To investigate the bacterial distribution and drug resistance in patients in intensive care unit(ICU) and provide theoretical bases for rational usage of antibiotics.METHODS The distribution and drug resistance of 372 strains isolated from patients in ICU collected from Jul 2007 to Jun 2008 were investigated and studied retrospectively.RESULTS Among them,the Gram-negative bacilli covered 59.14 %,the Gram-positive cocci 28.49%,and the fungi covered 12.37%.Pseudomonas aeruginosa,Klebsiella,Stenotrophomonas maltophilia and Ancinetobacter were the main Gram-negative bacilli.Staphylococcus aureus,coagulation-negative Staphylococcus and Enterococcus were the main Gram-positive cocci.The resistance rate of P.aeruginosa,S.maltophilia and Acinetobacter to imipenem was over 10%,and the S.maltophilia was 96.7%,the resistance rate of three main Gram-positive cocci to vancomycin and teicoplanin was zero,and the isolated bacteria showed serious multidrug-resistance.CONCLUSIONS Periodic monitoring should be done to learn the drug resistance and bacterial distribution in ICU in order to rationally use antibiotics to avoid the generation of new drug resistant strains and control the infection of patients in ICU.

OBJECTIVE To investigate the change of antibiotics resistance of the Pseudomonas aeruginosa isolated from patients′s sputum in our hospital from Jan 2006 to Dec 2008,and offer basis for prevention of clinical infection and the reasonable use of drugs.METHODS The culture,identification and sensitivity to antibiotics of P.aeruginosa from the clinical sputum specimens were analyzed using USA VITEK-32 system.RESULTS Totally 196 strains of P.aeruginosa were isolated and characterized during the three years.The rates of resistance to cefoperazone/sulbactam were 18.37%,piperacillin/tazobactam 16.84%,netilmicin 17.35%,trimethoprim/sulfamesoxazole 100.00%,ampicillin 99.49%,cefazolin 99.49%,cefotetan 88.78%,and to ceftriaxone were 79.08%.The resistance rate to cephalosporins showed rising tendency.But the resistance rate to ?-lactam antibiotics showed deereasing tendency.CONCLUSIONS P.aeruginosa has single and multi-resistance to antibiotics seriously,but sensitive to ?-lactam antibiotics and aminoglycosides.Using antibiotics reasonably based on bacteria identification and sensitivity test is the best way to reduce the resistance of the pathogens.

OBJECTIVE: To analyze the correlation of the tympanic injection of triamcinolone acetonide, middle ear pressure (MEP) and radioactive secretory otitis media (RSOM) with nasopharyngeal carcinoma (NPC) after radiotherapy. METHOD: Fifty-two patients suffering NPC without otitis media before radiotherapy were randomly divided into three groups. 17 cases with 34 ears were distributed into treatment group I, and radiotherapy 1 hour before the start of each side of the tympanic cavity injection of triamcinolone acetonide injection, 1-7 weeks 1 times a week. Treatment group I had 17 cases with 34 ears,and radiotherapy 1 hour before the start of each side of the tympanic cavity injection of triamcinolone acetonide injection, 1-12 weeks 1 times a week. And control group consisted of 18 cases with 36 ears who didn't accept such treatment. In all 104 ears, MEP was tested at the begin of radiotherapy and the end of 1st, 2nd, 3rd month after radiotherapy. RESULT: From the beginning of radiotherapy to the end of th 1st, 2nd, 3rd month after radiotherapy, the morbidity of RSOM gradually increased and MEP decreased in the treatment group I , II and the control group, in which treatment group II showed the lowest morbidity of RSOM and MEP was maximum (P < 0.01), and the treatment group I showed the lower morbidity of RSOM and MEP was greater (P < 0. 05), while the control group showed the highest morbidity of RSOM and MEP was minimum (P > 0.05). CONCLUSION Tympanic injection of triamcinolone acetonide could reduce radiation injury, and medication time was positively correlated with the MEP, and a negative correlation with RSOM morbidity, and the longer treatment, the more significant the effect is. The difference is most obvious at the end of 3rd month after radiotherapy. It may be due to the more active repairation after radiation damage in middle ears, but long-term efficacy must continue to observe.
Anti-Inflammatory Agents ; administration & dosage ; Carcinoma ; Ear, Middle ; Humans ; Injections ; Nasopharyngeal Carcinoma ; Nasopharyngeal Neoplasms ; radiotherapy ; Otitis Media with Effusion ; drug therapy ; Radiation Injuries ; Triamcinolone Acetonide ; administration & dosage