To explore new agents of quinolone derivatives with high antibacterial activity, 7-(4-alkoxyimino-3-methyl-3-methylaminopiperidin-1-yl)quinolones were designed and synthesized, and their activity against gram-positive and gram-negative strains was tested in vitro. Sixteen target compounds were obtained. Their structures were established by 1H NMR, HRMS and X-ray crystallographic analysis. Compounds 14k and 14m-14o show good antibacterial activity against the tested five gram-positive strains and five gram-negative strains (MIC: 0.25-16 micromg x mL(-1)), of which the most active compound 14o is 8-fold more potent than levofloxacin against S. pneumoniae (MIC: 4 microg x mL(-1)), and comparable to levofloxacin against S. aureus, S. epidermidis, E. faecalis and E. coli (MIC: 0.25-1 microg x mL(-1)), but generally less potent than gemifloxacin.

FRTL cells were incubated in the culture medium containing 10 -6 -10-3 mol/L KI for 24, 48 and 72 h, and the levels of sodium iodide symporter (NIS) mRNA and protein were measured using RT-PCR and Western blot. The levels of NIS mRNA in FRTL cells incubated with different concentrations of iodide for 24 and 48 h showed no significant difference as compared with the control group, however, NIS protein was reduced gradually in FRTL cells incubated with different concentrations of iodide for 48 and 72 h as compared with that in control group. The higher the iodide concentration, the lower the levels of NIS protein. The results show that acute iodine excess does not affect the expression of NIS mRNA, but down-regulates NIS protein expression. Iodine excess may regulate the expression of NIS through post-transcription.

Objective: To explore the effect of iodine overdose on cathepsin B and D in thyroidcell line (FRTL). Method: The cells were treated with potassium iodide (0, 1, 5, 10, 50 and 100mmol/L). After treatment 6, 12, 24, 48 and 72 hours, the cells were collected. The activities of cathepsin B (CB) and cathepsin D (CD) were assayed by fluorospectrophotometry and Lowry, respectively. The mRNA levels of CB and CD were determined with real-time PCR. Results: After 12 and 24 hours, the activities of CB and CD, treated by 50mmol/L potassium iodide were decreased significanty. The mRNA levels of CB and CD of 50mmol/L potassium iodide group were decreased significanty after treatment 24 hours. Conclusion: The decreased activities of CB and CD were one of reasons of thyroid colloid retention resulted from iodine excess.

Objective: To detect the damage of excessive iodine on the activities and mRNA of cathepsin B and D and observe the effects of selenium intervention. Method: Thyroid follicular epithelial cell line FRTL was cultured in Kaighn’s modified Ham’s F-12 medium. ① The cells were divided into 8 groups for detection of activities of cathepsin B and D (CB and CD). The medium of NI group did not contain selenium or iodine, while EI group contained 50 mmol/L KI, and IS group contained 50mmol/L KI and different dosages of 0.1,0.2,0.5,1.0,2.0 and 5.0 ?mol/L selenium (sodium selenite). ②The mRNA levels of cathepsin B and D were detected by real-time PCR. The medium of NI group and EI group was same as above, but IS group only contained 0.1?mol/L selenium besides 50mmol/L KI. Results: The activities of CB decreased in EI group (50mmol/L KI treated 12 h), while CD decreased after 24 h and both activities were improved in IS groups with 0.1~0.5?mol/L selenium. The mRNA levels of CB and CD in EI group decreased, while in IS group were improved. Conclusion: Excessive iodine resulted in goiter through decreased levels of activities and mRNA of CB and CD. The intervention of selenium on goiter mayinduce its amelioration effect on decrease of CB and CD activities and the optimal dosage ranges from 0.1?mol/L to 0.5?mol/L.

Objective To observe the pathological characteristics of thyroiditis induced by iodine excess and thyroglobulin (Tg) immunization and to explore the mechanism of thyroiditis induced by iodine excess. Methods NOD mice were used for intaking 0.05% Nal water and(or) Tg immunization. Morphologic change in thyroid and apoptosis were observed. The levels of serum TT4, TSH, thyroglobulin antibody (TgAb) and thyroid peroxidase antibody (TPOAb) were measured. Responding to Tg, lymphocytic proliferation of lymph node and spleen, interleukin-4(IL-4)and γ-interferon(IFN-γ) levels in culture medium of splenocytes were detected. Real-time PCR Was used to detect mRNA expressions of IL-4, IFN-γ, chemokine ligand 10 (CXCL10) and intercellular adhesion molecular-1(ICAM-1) in thyroid. Results Distended thyroid follicles,colloid accumulation, intense lymphocytic infiltration and disorganization were seen in thyroid of iodine excess group, along with increased apoptosis of thyroid cells(34.66～ 2.78 vs 5.11±0.62 ,P<0.01). The levels of TT4 were lowered while TSH raised ,but no production of thyroid-specific autoantibodies was revealed. Lymph node and spleen cells showed positive respornse under stimulation of Tg. The level of IFN-γ[(1. 272±0.049 vs 1. 139±0. 025)ng/L,P<0. 01] was raised in culture medium of splenocytes but not IL-4. The expression of IFN-γ, CXCLI0 and ICAM-1 mRNA were increased in thyroid. But in Tg group, some lymphocytes were scattered in thyroid, autoantibodies emerged ,and the level of IL-4 was increased in cuhure medium of splenocytes[(18. 508±0. 113 vs 13. 368±0. 016)ng/L, P<0. 01]. ledine excess combined with Tg enhanced these inflammatory reaction. Conclusion Iodine excess induced thyroiditis in NOD mice. The process seems to be Th1 response dominant organ-specific autoimmune diseases. Iodine excess and Tg immunizatiou play a synergistic role in inducing experimental autoimmune thyroiditis.

Objective: To determine the protective effect of zero-balanced ultraifltration and modiifed ultraifltration on infants’ pulmonary function atfer cardiac surgery. Methods: Sixty infants with congenital heart diseases were randomly divided into 3 groups: a zero-balanced ultraifltration group (Z group), a modiifed ultraifltration group (M group) and a zero-balanced ultraifltrationwith modified ultrafiltration group (Z+M group). Oxygenation index (OI), difference of alveoli-arterial oxygen pressure (P(A-α)O2), static lung compliance (Cstat), and airway resistance (Raw) were measured before caridopulmonary bypass (CPB, T1), 20 minutes atfer the CPB (T2), 2 h atfer the operation (T3), 6 h atfer the operation (T4) and 12 h atfer the operation (T5). hTe time of mechanical ventilation was also monitored. Results:Atfer the CPB, OI and Cstat in all groups decreased signiifcantly, while Raw and P(A-α)O2 increased signiifcantly. At T3, T4 and T5, OI and Cstat in the Z+M group were signiifcantly higher than those in the Z group and the M group (P<0.05), Raw andP(A-α)O2 in the Z+M group were signiifcantly lower than those in the Z group and the M group (P<0.05). hTe ventilation time in the Z+M group was signiifcantly shorter than that in the Z group and the M group (P<0.05). Conclusion:Zero-balanced ultrafiltration and modified ultrafiltration can effectively promote the pulmonary function atfer cardiac surgery in infants.

BACKGROUND:Studies have shown that bone marrow mesenchymal stem cells have the ability to persistently generate hepatocytes and biliary cells, and thus in the repair process of liver injury, replenish the reduced number of hepatocytes due to damage and participate in damaged liver structure.
OBJECTIVE:To investigate the effect of bone marrow mesenchymal stem cells transplantation on acute liver failure and the expression of CD163 and interleukin-10 in rat serum and liver tissue.
METHODS:D-galactose and lipopolysaccharidewere used to make acute liver failure models in 60 Sprague-Dawley rats. Then, the rats were divided into control group and transplantation group. Bone marrow mesenchymal stem cells at passage 3 were injected through tail vein in the transplantation group, and normal saline was injected in the control group. After transplantation 24, 120, 168 hours, serum samples and liver tissues were col ected.
RESULTS AND CONCLUSION:After transplantation 120 and 168 hours, the serum alanine transaminase and aspartate aminotransferase activities of the transplantation were significantly lower than those of the control group (P<0.05). In the transplantation group the apoptotic index was stil lower compared with the control group, and the difference was significant (P<0.05). The levels of CD163 and interleukin-10 in the serum and liver tissue in the transplantation group were decreased significantly compared with the control group (P<0.05). The results suggested that there were highly significant correlations between CD163 and interleukin-10 (P<0.01). Bone marrow mesenchymal stem celltransplantation has a therapeutic effect on acute liver failure rats. CDl63 and interleukin-10 play a very important role in the pathogenesis of acute liver failure, which can be used as sensitive serum marker proteins for diagnosis and prognosis of acute liver failure.

Objective:The present study aimed to conduct a clinical analysis of nosocomial infections in hospitalized cancer pa-tients and propose effective precautionary measures. Methods:We retrospectively analyzed 56,430 cases of discharges from the Cancer Institute and Hospital of Tianjin Medical University between January and December 2012. Results:Among 825 cases, the rate of noso-comial infections was 1.46%;46.42%of the patients aged>60 years. The highest infection rate was observed in the Medical Depart-ment of Stomach Cancer. The highest composing rate was recorded in the Department of Hepatobiliary Cancer. The major pathogenic bacteria were Gram-negative bacilli;fungal infections were relatively rare. The most vulnerable body parts were the abdomen and diges-tive tract, which were mainly infected by pathogenic Escherichia coli. Conclusion:Healthcare workers should consider the importance of influencing factors and take precautionary measures to reduce the rate of nosocomial infections in cancer patients.

This study was aimed to compare the expression of BMP4 mRNA in the in-vivo tissue engineering bone constructed with Ca/P ceramics against the expression of BMP4 mRNA in the naturally healing bone. 20 porous Ca/P ceramics cylinders with Phi 5 mm x 8 mm were made and implanted into the dorsal muscles of 5 dogs. As control, one molar tooth was pulled out from each dog to create bone defect for the naturally healing bone at the same time. The specimens and the naturally healing bone were harvested at 1, 2, 4, 12 and 24 weeks post-implantation. After RNA extraction and reverse transcription, bone morphogenetic protein 4 (BMP4) and GAPDH mRNA were detected by real-time quantitative polymerase chain reaction (PCR) method. The results showed that the expression level of BMP4 mRNA of the in-vivo tissue engineering bone constructed with Ca/P ceramics was higher than that of the naturally healing bone in the period of experiment. However, the in-vivo tissue engineering bone had the same chronological order of BMP mRNA expression that the naturally healing bone did. As a bone substitute analogous to autologous bone, the in-vivo tissue engineering bone constructed with Ca/P ceramics has the potential for clinical application.
Animals ; Bone Morphogenetic Protein 4 ; genetics ; metabolism ; Bone Substitutes ; chemistry ; Calcium Phosphates ; chemistry ; Ceramics ; chemistry ; Dogs ; Humans ; Implants, Experimental ; RNA, Messenger ; genetics ; metabolism ; Tissue Engineering

Objective To explore the value of Chinese ink in identifying sentinel lymph nodes(SLN) during radical resection of cervical carcinoma.Methods After sterilized Chinese ink(1ml) was infused in normal tissue at four points,extensive cervical resection and cleaning operation of pelvic lymph nodes were performed.Lymph nodes staining black in drainage field of pelvic lymph system were investigated.Results Lymph nodes staining black were found in 15 cases.The identifying rate was 100%(15/15).Positive lymph nodes were found in 2 cases with lymph node metastasis.The accurate rate of pelvic lymph nodes metastasis was 100%.Conclusion The effect is reliable by using Chinese ink as tracer of SLNs in cervical carcinoma.