To find antibacterial candidate compounds, eighteen novel sulfonamide derivatives containing a fused-ring were designed and synthesized on the basis of previous studies, with structures confirmed by ¹H NMR, ¹³C NMR and MS. Antibacterial activities of the products were evaluated by the agar dilution method. The results show that these derivatives have different degrees of inhibitory activity on the tested bacteria, with the compounds IIi and IIr the most potent. The MIC of IIi for S. aureus, E. coli and MRSA was 8, 32 and 16 μg·mL^-1, respectively, and the MIC of the IIr was 8, 64 and 32 μg·mL^-1, respectively. The anti-MRSA activities of the two compounds is significant and is worthy of further structural optimization and study.

Objective To study the mechanism of mast cell increase in cellular leiomyoma of uterus.Methods Tissue sections from 30 cases of cellular leiomyoma of uterus,15 cases of leiomyosarcoma and 30 cases of ordinary leiomyoma were studied using immunohistochemical double labeling techniques.The expression of mast cell tryptase ahd Ki-67 as well as mast cell tryptase and chemotactic factors RANTES,Eotaxin,monocyte chemoattractant protein-1(MCP-1),transforming growth factor-? (TGF-?)were double immunostained.Results Ki-67 in mast cells was rarely expressed in each group. Expressions of regulate upon activation normal T cell expressed and secreted(RANTES),Eotaxin and TGF-? in cellular leiomyoma were 78%,89%,91%,respectively.They were all higher than those in ordinary leiomyoma and leiomyosarcoma(P

The traditional Chinese medicine of Radix Hedysari plays an important role in invigorating gas for as-cending, benefiting blood for promoting production of fluid, and promoting circulation for removing obstruction in collaterals, which is consistent with the principle of treatment for osteoporosis. This study is designed to investigate the bioactive components on increasing peak bone mass (PBM) by exploring the spectrum-effect relationship between chromatography fingerprints and effect. Multiple indicators are selected to evaluate the pharmacological activity. In fingerprints, 21 common peaks are obtained, five of which are identified. Furthermore, gray relational analysis (GRA) is a quantitative method of gray system theory and is used to describe the correlation degree of common peaks and pharmacological activities with relational value. 21 components are then divided into three different regions, of which ononin and calycosin play an extremely significant role in increasing PBM. In addition, factor analysis and hierarchical cluster analysis (HCA) are used to screen the optimal producing area for Radix Hedysari. This provides a comprehensive and efficient method to improve the quality evaluation of Radix Hedysari, confirming the bioactive components for PBM-enhancement and further develop its medicinal value.

Objective To observe the effects of acupuncture treatment on the levels of HPA axis related hormones and acupoint compatibility in insomnia rats; To discuss the mechanism of action for acupuncture treatment. Methods Chlorophenylalanine suspension was under intraperitoneal injection to establish insomnia model rats. Sixty SD rats were randomly divided into blank group, model group, Baihui+Shenmen group, Baihui+Sanyinjiao group, Baihui+non-acupoint group, with 12 rats in each group. Each treatment group received acupuncture in relevant acupoints, 30 min each time, for 7 d. ELISA was used to measure the levels of CRH, ACTH and CORT. Results Compared with the model group, the levels of CRH, ACTH and CORT of the acupuncture groups decreased to some extent. In the three acupuncture groups, the efficacy of Baihui+Shenmen group was better than that of Baihui+Sanyinjiao group and Baihui+non-non-acupoint group. Conclusion Acupuncture treatment may calm and soothe the nerves to release the insomnia through regulating HPA axis related hormones. Acupuncture acupoints at different meridians may be one of the factors that cause the difference of acupoints compatibility effect.

OBJECTIVESTo construct a recombinant adeno-associated virus vector pSNAV expressing CTLA-4Ig and to demonstrate its expression in transplanted liver allografts and to see if a long term inhibitive effect of CTLA-4Ig could be obtained though its use.

METHODSAfter AAVCTLA-4Ig and PUC18 were cut with BamHI, CTLA-4Ig cDNA was inserted into the plasmid PUC18 by T4DNA ligase and PUC18-CTLA-4Ig was constructed. The obtained PUC18-CTLA-4Ig and pSNAV cut with Kpn I and EcoR I, CTLA-4Ig cDNA was inserted into plasmid pSNAV to construct the recombinant vector pSNAV-CTLA-4Ig, which was transfected into BHK-21 packaging cells by lipofectine-mediated transfection. Then the BHK-21 cell line was infected with HSV1-rc to produce a large amount of pSNAV- CTLA-4Ig. The specificity of the expressed product was identified by digestion with BamHI, PCR and sequence determination. The titer of the virus was detected. The product was infused into rats liver allografts via portal vein and its expression in the transplanted livers was detected immunohistochemically.

RESULTSRecombinant adeno-associated virus vector pSNAV-CTLA-4Ig was generated and purified into 8.5 x 10(11)/ml. Agarose gel analysis of PCR products verified the presence of CTLA-4Ig. Digestion with BamHI and sequence determination confirmed that pSNAV-CTLA-4Ig was constructed. Expression of CTLA-4Ig in the transplanted livers was detected successfully.

CONCLUSIONPrepared pSNAV-CTLA-4Ig was constructed correctly and can express CTLA-4Ig effectively. Besides this, it can express CTLA-4Ig in rat liver allografts. It may be used in the study of transplant tolerance.

Abatacept ; Animals ; Dependovirus ; genetics ; metabolism ; Genetic Vectors ; Immunoconjugates ; genetics ; metabolism ; Liver Transplantation ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Rats, Wistar ; Transplantation, Homologous

OBJECTIVETo study the construction of the PCI-neo mammalian expression vector system containing murine 4-1BBL gene and its stable and effective expression in rat hepatocellular carcinoma cell line CBRH7919.

METHODSThe murine full-length 4-1BBL cDNA was obtained and subcloned into the PCI-neo mammalian expression vector. The recombinant named as PCI-neo-4-1BBL was identificated by restriction enzyme digestion and sequencing. Subsequently, PCI-neo-4-1BBL was transfected into CBRH7919 with lipofectamine reagent, then G418-resistance clone was acquired and named as PCI-neo-4-1BBL-CBRH7919+. The stable expression of 4-1BBL mRNA in PCI-neo-4-1BBL-CBRH7919+ was detected by RT-PCR.

RESULTSThe fragment of 980 bp (4-1BBL) and 5.4 kb (PCI-neo) was shown after PCI-neo-4-1BBL had been digested by EcoR I and Not I and agarose gel electrophoresis. The DNA sequencing of 4-1BBL, proved to be identical to the data of 4-1BBL in Genebank, showed stable and effective expression in PCI-neo-4-1BBL-CBRH7919+.

CONCLUSIONThe PCI-neo mammalian expression vector system containing murine 4-1BBL has been constructed successfully, which shows stable and effective expression in CBRH7919.

4-1BB Ligand ; Animals ; Cell Line, Tumor ; Cloning, Molecular ; DNA, Complementary ; genetics ; Genetic Vectors ; Liver Neoplasms, Experimental ; metabolism ; pathology ; RNA, Messenger ; biosynthesis ; genetics ; Rats ; Rats, Wistar ; Recombination, Genetic ; Transfection ; Tumor Necrosis Factor-alpha ; biosynthesis ; genetics

BACKGROUNDCorticosteroid treatment of acute lung injury (ALI) and acute respiratory distress syndrome (ARDS) has been one of the most controversial clinical issues in critical care. Although the administration of high-dose corticosteroids does not benefit patients with early septic shock and ARDS, recent clinical trials have indicated that treatment with relatively low-dose corticosteroids (2 to 3 mg/kg/day of methylprednisolone or equivalent) may improve outcome when used for late ARDS or persistent septic shock. The underlying mechanism was not fully clarified. Whether the administration of corticosteroids can arrest neutrophil-driven organ injury once started remains to be elucidated.

OBJECTIVETo observe the effects of hydrocortisone (HC, 6 mg/kg) on oxygen free radicals (OFR) released by PMN and pulmonary pathological changes in rat ALI model induced by lipopolysaccharide (LPS), to investigate the possible mechanism through which corticosteroids exert protective effect on ALI.

METHODSA rat model of ALI was induced by peritoneal injection of 2 x 10(12) Escherichia coli/kg. Fifty-six rats were randomly divided into three groups: normal control group, LPS group and HC group (6 mg/kg). Samples were collected 2 h, 4 h and 6 h after giving LPS to LPS and HC group (6 h after giving normal saline in normal control group) to measure the level of OFR released by PMN using chemiluminescence method based on lumino, and to compae of pulmonary pathological changes among the three groups.

RESULTSPathological examination with light microscope in LPS group showed thickened pulmonary interstitia, inflammatory cell infiltration, edema and hemorrhage, which were in accordance with the features of ALI. There were significant differences in the release of OFR by PMN among the three groups (P < 0.01). The level of OFR released by PMN in LPS group was significantly higher than that of the control group, and continued to increase during the observation period (2 - 6 h after LPS). The release of OFR by PMN in HC group was significantly suppressed as compared with LPS group, which was peaked at 4 h after LPS injection (to 98.2%); there were also significant differences in the grades of ALI pathologic changes among the three groups (P < 0.01). The grades of ALI pathologic changes in LPS group were significantly increased when compared with the normal control group (P < 0.05) while significantly decreased in HC group as compared with LPS group (P < 0.05).

CONCLUSIONIt was demonstrated in the LPS induced ALI model that OFR might play an important role in onset of ALI. Intervening with HC (6 mg/kg) treatment could ameliorate the lung injury and exert significant and sustained suppression on the release of OFR by PMN, showing that HC has a protective effect on LPS induced ALI and its theraputic effect occurs possibly through suppression on the release of OFR by PMN.

Acute Lung Injury ; etiology ; immunology ; Animals ; Disease Models, Animal ; Free Radicals ; metabolism ; Glucocorticoids ; pharmacology ; Hydrocortisone ; pharmacology ; Lipopolysaccharides ; adverse effects ; Lung ; immunology ; pathology ; Mice ; Neutrophils ; drug effects ; metabolism

Biopsy ; methods ; Esophageal Neoplasms ; pathology ; surgery ; Esophagoscopy ; Esophagus ; pathology ; Humans ; Mucous Membrane ; pathology ; Precancerous Conditions ; pathology ; surgery

BACKGROUNDCerebral venous thrombosis (CVT) may lead to serious neurological disorders; however, little is known about the risk factors for recurrent CVT. Our aim was to determine the association between elevated fibrinogen and decreased high-density lipoprotein cholesterol (HDL-C) levels with recurrent CVT.

METHODSThis retrospective cohort study included participants if they had a first episode of objectively defined CVT and were admitted to Xuan Wu Hospital, Capital Medical University from August 2005 to September 2009. Demographic and clinical variables were collected, as well as laboratory parameters, including plasma fibrinogen and HDL-C. Patients with CVT were followed for recurrent symptomatic CVT. Follow-up was through the end of September 2010. Potential predictors of recurrence were analyzed using Cox survival analysis.

RESULTSAt the end of the follow-up, 95 patients were eligible for the study. Twelve of 95 patients (12.6%) had recurred CVT. The median time of recurrence was 7 months (range: 1-39 months). Eight of these 12 (66.7%) experienced recurrence within the first 12 months after their initial CVT. The recurrence rate of CVT was 2.76 per 100 patient-years. Multivariate Cox regression analysis demonstrated that the coexistence of high fibrinogen (>4.00 g/L) and low HDL-C (<1.08 mmol/L) levels at baseline was the only independent predictor for recurrent CVT (hazard ratio: 4.69; 95% confidence interval: 1.10-20.11; P < 0.05). Of the twelve patients with recurrent CVT in our study, 7 (58.3%) had high fibrinogen plus low HDL-C levels. All 7 of these patients took warfarin for 3-12 months, and 6 of 7 had recurrent CVT after the discontinuation of anticoagulant treatment.

CONCLUSIONSConcomitant high fibrinogen and low HDL-C levels may be associated with recurrence of CVT. The effect of potential risk factors related to atherothrombosis on recurrent CVT should be closely monitored.

Adolescent ; Adult ; Aged ; Cholesterol, HDL ; metabolism ; Cohort Studies ; Female ; Fibrinogen ; metabolism ; Humans ; Intracranial Thrombosis ; metabolism ; pathology ; Male ; Middle Aged ; Recurrence ; Retrospective Studies ; Young Adult

OBJECTIVETo seek a kind of safe and effective method to treat scar contracture abnormality on the neck of the children.

METHODSWe take the trunk line of transverse cervical artery as the vessel pedicle, and shift huge trapezius muscle flap expanded to the neck in order to treat scar contracture abnormality on the neck of the children.

RESULTSClinically, we applied this method to treat ten children who suffered from contracture abnormality on the neck, and not only provide enough skin soft tissue (the length may be beyond the midline) to treat the abnormality, but also make the flap alive, obtain the satisfying postoperative effect.

CONCLUSIONSBased on the warranty of the flap blood supply, this flap is very suitable to treat scar contracture abnormality on the neck of the children.

Child ; Child, Preschool ; Cicatrix ; surgery ; Contracture ; surgery ; Humans ; Infant ; Male ; Neck Muscles ; transplantation ; Reconstructive Surgical Procedures ; methods ; Skin Transplantation ; Surgical Flaps