Currently, the resistance of first-line anti-tuberculosis drugs has made the prevention and treatment of tuberculosis increasingly difficult, posing a serious threat to global public health. Several studies have shown that efflux pumps are one of the important causes for bacteria to develop multi-drug resistance and extremely-drug resistance, and efflux pump inhibitors can inhibit the efflux of antibacterial drugs, thereby reducing bacterial drug resistance. Numerous natural products and synthetic compounds have been reported to possess efflux pump inhibitory activity, but they have not been applied in clinical settings because of their toxicity, pharmacokinetic properties, etc. Therefore, we summarized the efflux pump inhibitory activity, antimicrobial activity, and structure-activity relationships of reported efflux pump inhibitors against Mycobacterium tuberculosis in recent years, providing references for the development of new efflux pump inhibitors with better activity and lower toxicity.

Objective To compare the dijference of prostate cancer detection rate (PCDR) between 12 + 1-core biopsy and 6-core biopsy of the prostate system guided by transrectal ultrasonography (TRUS).Methods The clinical data of 2 707 patients with prostate biopsy from July 1999 to June 2012 were retrospectively analyzed.These patients were 54 to 92 years old,mean age was 69 years old.The range of PSA was 0.02-158.56 ng/ml,with an average of 16.97 ng/mt.People in the range of PSA 0-4.00,4.01-10.00,10.01-20.00,20.01-30.00,and ＞ 30.00 were 161,826,827,312,581,respectively.The volume of the prostate ranged from 14.1 to 82.6 cm3,mean 47.9 cm3.The 1 603 cases before the July 2009 were performed 6-core biopsy guided by the finger,followed by 1104 TRUS-guided 12 + 1-core biopsy.In addition,after March 2012,60 patients accepeted the MRI examination before prostate biopsy.The strategy of prostate biopsy was medial 6-core,lateral 6-core,the 13th core was positioned at abnormal signal area of TRUS and MRI.Explore the difference of PCDR medial 6-core,lateral 6-core,systematic 12-and 12 + 1-core,and the difference of 13th core and the other 12 cores,with the cut off value of PSA quartile of 30 ng/ml and PV quartile of 46 cm3.Results Comparison of clinical characteristics of prostate biopsy between positive group and negative group was performed,and the result suggested that The positive outcome of prostate cancer biopsy was related with element such as high PSA,old age [(71.7 ±7.1)vs.(68.3 ± 8.1),P =0.008],large fPSA [(8.5 ± 36.4) vs.(2.3 ± 3.4),P ＜ 0.001],small prostate volume [(41.3 ±22.9) vs.(52.3 ±29.3),P ＜0.001],small value of f/t[(0.12 ± 0.07) vs.(0.17 ±0.10,P ＜0.001)],high density of PSA [(2.04 ± 9.36) vs.(0.32 ± 0.42),P ＜ 0.001],digital rectal examination [72.0％ (522/725) vs.23.1％ (457/1 982),P ＜ 0.001],irregular echo level [41.1％ (695/1 693) vs.28.0％ (284/1 014),P ＜ 0.001],hypoechoic [64.3％ (695/1 081) vs.17.5％ (284/1 626),P ＜ 0.001],microcalcifcation[56.8％ (586/1 032) vs.23.5％ (393/ 675),P ＜ 0.001].PCDR of 12 + 1-core biopsy was significantly higher than lateral 6-core biopsy[41.5％ (458/1 104)vs.37.0％ (408/1 104),P =0.033].However,PCDR of 12-core biopsy had no statistical differences with 6-core biopsy[40.7％ (449/1 104) vs.37.0％ (408/1 104),P =0.081].PCDR of TRUS-guided biopsy was higher than that of finger-guided biopsy in patients with PSA≤30 ng/ml and PV ＞46 cm3 [30.0％ (254/846)vs.22.2％ (284/1 280),P ＜0.001;31.7％ (124/391)vs.18.1％ (131/723),P ＜0.001].PCDR of the 13th core positioned at abnormal signal area of TRUS and MRI was higher than the average PCDR of other 12 cores [70.9％ (107/151) vs.56.6％ (3 109/5 496),P ＜ 0.001].Conclusion PCDR of TRUS-guided biopsy was higher than that of finger-guided biopsy in patients with PSA≤30 ng/ml and PV ＞46 cm3.PCDR of 12 + 1-core biopsy was significantly higher than that of lateral 6-core biopsy.However,PCDR of 12-core biopsy had no statistical differences with that of 6-core biopsy.PCDR of the 13th core positioned at abnormal signal area of TRUS was higher than the average PCDR of other 12 cores.

China ; epidemiology ; Drug Resistance, Bacterial ; Electrophoresis, Gel, Pulsed-Field ; Humans ; Listeria monocytogenes ; physiology ; Listeriosis ; epidemiology ; Serotyping

Objective To study the imaging of inner ear malformations in children with congenital sensorineural hearing loss(SNHL).Methods CT and MRI examinations were performed on children with SNHL diagnosed by audiological test.One hundred and eighty-eight patients with complete imaging information were obtained.The imaging of inner ear malformations was analyzed according to Sennaroglu's classification. Results Thirty-five patients(54 ears) were found with inner ear malformations by CT and MRI,3 of whom(5 ears) were accompanied by outer and middle ear malformations.Among the 35 patients,2(4 ears) were found to be common cavity deformity,1(1 ear) cochlear hypoplasia,13(26 ears) incomplete partition II(Mondini deformity),4(7 ears) vestibule dilation,13(19 ears) semicircular canal deformity and 19(34 ears) large vestibular aqueduct.Internal auditory canal was found narrow in 7 patients(10 ears) and wide in 1(2 ears) with classic Mondini deformity. Conclusion CT and MRI examinations are of great importance to the diagnosis and treatment of inner ear malformations in children with congenital SNHL,especially for the candidates of cochlear implantation.

Objective To investigate the effects of Shenfu injection ( SF,a Chinese herbal medicine preparation made of Codonopsis pilosula and Aconitum carmichaeli) on the cell apoptosis of focal cerebral ischemic-reperfusion injured rats and the expression of heme oxygenase-1 (HO-1). Methods Forty-two male Sprague-Dawley rats used for producing unilateral brain ischemia reperfusion model were randomly divided into three groups:sham operation group ( Sham group),ischemia reperfusion group ( IR group),and SF Injection group (SF group).The model of focal cerebral ischemia-reperfusion injury was induced by transient occlusion of middle cerebral artery (ischemia for 2 h,and reperfusion for 3,6 h respectively).In SF group,SF ( 10 mg/kg) was intraperitoneally injected duri(n)g reperfusion.Cell apoptosis rate in brain tissue was detected by the technique of Annexin-V-PI double staining and was counted in flow cytometer.Expression of HO-1 in brain was measured by RT-PCR,while the pathological and ultra structure changes of cerebral tissue were also observed.Results Cell apoptosis rate of brain tissue were significantly higher in IR group than that in Sham group (P ＜0.01 ),while SF group had less significant changes in cell apoptosis rate, HO-1 level of brain tissue than IR group (P ＜ O.01 ).The ultra structure change of brain tissue was less in SF group than that in IR group.Conclusions During early stage of brain IR injury,SF inhibits cellular apoptosis and in turn protects the brain from injury which is attributed to the increase in HO-1 expression induced by SF.

Objective To investigate the differences in clinical, laboratory and therapeutic aspects of primary Sjogren's syndrome (pSS) between young/middle-age group and old group.Methods The 84 pSS patients were divided into the young and middle-age group (n=54) and the old group (n = 30). The differences in clinical features, laboratory indices and drug therapy were retrospectively analyzed. The chi-square test was used for statistical analysis. Results The positive incidences of xerostomia, dry eye symptom and rampant teeth were 80.0%, 76.7% and 43.3%respectively in the old group. And they were all significantly higher than in young and middle-aged group (57.4%, 51.9% and 20.4%, all P＜0. 05). The positive rates of rheumatoid factor (RF)elevation, antiRo/SSA and antiLa/SSB antibodies were 13. 0%, 36.7% and 16.7% in the old group,and significantly lower than in young and middle-age group (44.4%, 59.3% and 42.6%, all P＜0.05). The incidences of leukopenia and thyroid gland involvement were much lower in the aged group (13.3% and 10.0%) than in the young and middle-age group (48. 1% and 37.0%, P＜0. 05). The percentage of patients receiving hydroxychloroquine as the main medicine was much lower in the aged group than in the young and middle-age group (16.7% vs. 40. 7%, P＜0. 05), while percentage of treatment with exclusive glucosides of Paeony Capsules was much higher (33.3% vs. 14.8%, P＜0.05). There were no statistical differences between two groups in ophthalmological examination,immunoglobulin level and sialography. Conclusions Those pSS patients with late onset exhibit more abnormalities in clinical parameters, but fewer in immunological parameters, which may be helpful in estimating prognosis and pathogenetic factors in pSS.

Humans ; Inhibitor of Apoptosis Proteins ; Microtubule-Associated Proteins ; genetics ; metabolism ; Protein Isoforms ; genetics ; metabolism ; Stomach Neoplasms ; genetics ; metabolism ; Tumor Cells, Cultured

OBJECTIVETo introduce the clinical application of venous nutrition flap pedicled by medial plantar artery of the hallux on the medical aspect of the foot.

METHODSBased on the anastomoses between the medial plantar artery of the hallux and the nutritional vein, the flap was designed with the perforator of medial plantar artery adjacent to the first metatarsal bone as the rotation point. The flap axis was along the vein at the medial aspect of the foot between rotation point and medial malleolus.

RESULTS5 cases were treated with primary healing and complete survival flaps. The patients were followed up for 1-12 months with good match of texture and color.

CONCLUSIONSThe venous nutrition flap pedicled by medial plantar artery of the hallux on the medical aspect of the foot can be transpositioned to repair the defect at forefoot.

Arteries ; Forefoot, Human ; Hallux ; blood supply ; Humans ; Metatarsal Bones ; Surgical Flaps ; blood supply ; Veins ; Wound Healing

To investigate the metabolic rate and metabolites of 9-dehydro-17-dehydro-andrographolide, which is the main active ingredient in Xiyanping injection, by using the in vitro rat liver microsome incubation system. 9-dehydro-17-dehydro-andrographolide was incubated together with liver microsome mixed with NADPH. Its metabolic rate was studied by determining its residual concentrations with the UHPLC-MS/MS method; Its metabolites were identified by the UPLC-TOF-MS(E) method. The results showed that 9-dehydro-17-dehydro-andrographolide was metabolized faster than rat liver microsomes mixed with coenzymes, with t½ and CL of (19.7 ± 0.5) min and (35.1 ± 0.8) mL x min(-1) x g(-1) (protein), respectively. Based on the high resolution mass spectrum data and information from literatures, altogether nine metabolites of 9-dehydro-17-dehydro-andrographolide were identified in the incubation system, particularly hydroxylated and dehydrogenized products. The results of identification would provide a basis for screening out more active andrographolide derivatives.
Animals ; Chromatography, High Pressure Liquid ; Diterpenes ; chemistry ; metabolism ; Drugs, Chinese Herbal ; chemistry ; metabolism ; Microsomes, Liver ; chemistry ; metabolism ; Molecular Structure ; Rats ; Tandem Mass Spectrometry

Adult ; Aged ; Angiopoietin-2 ; physiology ; Female ; Glioma ; blood ; physiopathology ; Humans ; Hypoxia ; blood ; metabolism ; Male ; Middle Aged ; Neovascularization, Pathologic ; physiopathology