No abstract available.
Pyrazoles ; Sulfonamides ; Celecoxib

No abstract available.
Primary Myelofibrosis ; Pyrazoles ; Transplants

Humans ; Pulmonary Embolism ; Pyrazoles ; Pyridones ; Venous Thrombosis

A field trial on the control effect of fipronil poison bait against German cockroaches (Blatella germanica) was carried out at different restaurant types in Sinchon, Seoul, Republic of Korea. Monitoring was performed applying food baited traps for 2 days per week. Reduction rates of German cockroaches by applying fipronil baits were 90.9% at Korean restaurants, 96.4% at Chinese restaurants, and 89.4% in beer hall kitchens after 4 weeks of the treatment. Overall average of the reduction rate was 93.9%. As the natural reduction rate at untreated restaurants was 11.5% after 4 weeks, a correction of the average reduction rate by applying the Abbot formula was 93.1%.
*Pyrazoles ; *Insecticides ; Insect Control/*methods ; *Cockroaches ; Animals

OBJECTIVETo evaluate the efficacy and safety of ruxolitinib in treatment of myeloproliferative neoplasm.

METHODSRandom clinical trials (~September 30, 2017) were identified from PubMed, Embase, Cochrane Library, Clinical Trials, CBM and Chinese Journal Full-text Database. The quality of RCT was assessed by Cochrane risk bias. Meta analysis was performed with Revman 5.3.

RESULTSRuxolitinib was efficacious in relieving splenomegaly (RR 49.12, 95% CI [15.81-152.59], P<0.001). The incidence of anemia significantly increased after ruxolitinib treatment (RR 1.71, 95% CI [1.05-2.77], P=0.16), while the thrombocytopenia (RR 1.04, 95% CI [0.50-2.16], P=0.92) and neutropenia (RR 2.46, 95% CI [0.91-6.61], P=0.07) had no statistical difference as compared with that in control group. Ischemia events had no significant difference as compared with control (RR 0.57, 95% CI [0.33-1.00], P=0.05). Infection events had no significant difference as compared with the control group (RR 1.18, 95% CI [0.79-1.78], P=0.24).

CONCLUSIONRuxolitinib is an efficacious therapeutic strategy on MPD with controlling splenomegaly. However,anemia events and bleeding events may threat its clinical safety, so more high quality RCT are needed.

Humans ; Myeloproliferative Disorders ; Neoplasms ; Pyrazoles ; Thrombocytopenia

Animals ; Diazepam ; pharmacology ; Drug Antagonism ; Electroencephalography ; Female ; Male ; Pyrazoles ; poisoning ; toxicity ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo establish a high-performance liquid chromatography (HPLC)-based method for determining celecoxib concentration in the tongue tissue of hamsters.

METHODSCelecoxib mixed with the matrix (final concentration of 6%) was smeared on the surface of the tongue mucosa of hamsters, and the concentration and absorption rate of celecoxib in the tongue tissue were determined by HPLC at 5, 10, 15, 30, 60, 90, 120 min after the application.

RESULTSIn this system, the retention time of celecoxib was 4.4 min. Celecoxib concentration showed a good linear range within 25-800 microg/L (R2=0.9991, n=6), with the detection limit for celecoxib of 10 g/L (S/N=3). The extraction recoveries and method recoveries for celecoxib were 83.75%-90.01% and 91.98%-99.07%, respectively. The inter-day RSDs were 2.15%, 3.16% and 3.67%, and intra-day RSDs were 3.40%, 4.56% and 4.42%, respectively. The concentration of celecoxib in hamster tongue tissue within the first 120 min ranged from 0.685-/+0.019 microg/g to 3.168-/+0.143 g/g, reaching the peak level at 15 min.

CONCLUSIONCelecoxib can be rapidly absorbed through the tongue mucosa to reach a high concentration in the tongue tissue, indicating the possibility of oral COX-2 inhibitors to prevent oral cancer and precancerous lesions.

Animals ; Celecoxib ; Chromatography, High Pressure Liquid ; methods ; Cricetinae ; Pyrazoles ; analysis ; pharmacokinetics ; Sulfonamides ; analysis ; pharmacokinetics ; Tongue ; metabolism

OBJECTIVETo study the apoptosis and mechanism of Fipronil on PC12 Cells.

METHODSThe effect of fipronil on the apoptosis and necrosis of PC12 cells of 3.13 x 10(-6), 1.25 x 10(-5) and 5.00 x 10(-5) mol/L three dose groups after 24 h treatment was detected by morphology and the apoptosis rate was detected by flow cytometer (FCM). The expression of Bcl-2 protein in PC12 cells of 3.13 x 10(-6), 1.25 x 10(-5) and 5.00 x 10(-5) mol/L three dose groups after 24 h treatment was measured by immunofluorescence.

RESULTSThe number of apoptotic cells of 3.13 x 10(-6) mol/L group was more than the control group examined by fluorescence microscope, and the number of dead cells of 5.00 x 10(-5) mol/L group was more than the control group. The apoptotic rates of PC12 cells was higher in the 3.13 x 10(-6) mol/L group than the control group measured by FCM, and the dead rates of PC12 cells was higher in the 5.00 x 10(-5) mol/L group than the control group (P < 0.05). Immunofluorescence cytochemistry experiment demonstrated that the level of Bcl-2 expression was significantly lower in the 3.13 x 10(-6) mol/L group than the control group.

CONCLUSIONAt low dosage, fipronil increases the apoptotic rates of PC12 cells possibly by decreasing the expression of Bcl-2 protein while at high dosage, fipronil only increases the amount of necrotic cells.

Animals ; Apoptosis ; drug effects ; PC12 Cells ; Proto-Oncogene Proteins c-bcl-2 ; metabolism ; Pyrazoles ; toxicity ; Rats

Humans ; Leukemia, Myelogenous, Chronic, BCR-ABL Positive ; Neoplastic Stem Cells ; Pyrazoles ; Pyrimidines

OBJECTIVETo observe whether Celecoxib could inhibit the growth, regulate the expression of COX-2 and induce apoptosis of Tca8113 cells.

METHODSTca8113 cells were incubated with different concentrations of Celecoxib for 24, 48 and 72 h, and MTT was used to calculate growth inhibition rate. The expression of COX-2 protein and mRNA in Tca8113 cells was detected with SP immunohistochemistry staining and fluorescent quantitative real-time RT-PCR. Morphology of apoptosis cells was observed by fluorescence microscopy, and Annexin V-FITC/PI double labeling method was employed to detect early stage cell apoptosis.

RESULTSCOX-2 protein was strongly expressed in Tca8113 cells and was suppressed by Celecoxib. The growth and proliferation of Tca8113 cells treated with Celecoxib were inhibited in a dose-dependent manner. Celecoxib treatment resulted in significant increase in apoptosis and early apoptotic rate. Fluorescent quantitative real-time RT-PCR results showed no significant effet on regulating expression of COX-2 mRNA.

CONCLUSIONCelecoxib shows a significant effect on inhibiting expression of COX-2 in Tca8113 cells, this is probably related to growth inhibition and inducing apoptosis of Tca8113 cells.

Apoptosis ; Celecoxib ; Cell Line ; Cell Line, Tumor ; Cell Proliferation ; Cyclooxygenase 2 ; Humans ; Pyrazoles ; Sulfonamides