OBJECTIVETo explore the effects of arecoline on hepatic insulin resistance in type 2 diabetes rats and to elucidate its possible mechanism.

METHODSForty five Wistar rats were fed with high fructose diet for 12 weeks to induce type 2 diabetic rat model. rats were randomly divided into 5 groups (n = 8): control group, model group and model group were treated with different dose (0, 0.5, 1, 5 mg/kg) of arecoline. After 4 weeks, the fasting blood glucose, blood lipid and insulin level measured , mRNA expression of liver constitutive androstane receptor (CAR), pregnane X receptor (PXR), glucose-6-phosphatase (G6Pase), phosphoenolpyruvate carboxykinase (PEPCK), interleukin-6 (IL-6) and tumor necrosis factor-alpha (TNF-alpha) were detected by reverse transcription polymerase chain reaction (RT-PCR), the protein expression of p-AKT and glucose transporter4 (GLUT4) were detected by Western blot.

RESULTS1.5 mg/kg arecoline could significantly decrease the level of fasting blood glucose, blood lipid, blood insulin level and liver G6Pase, PEPCK, IL-6, TNF-alpha mRNA level in type 2 diabetes rats. 1.5 mg/kg arecoline also could significantly increase CAR, PXR mRNA level and p-AKT and GLUT4 protein expression.

CONCLUSIONArecoline improved hepatic insulin resistance in type 2 diabetes rats by increasing the mRNA levels of CAR and PXR leading to the creased glucose metabolism and inflammation related genes expression.

Animals ; Arecoline ; pharmacology ; Diabetes Mellitus, Experimental ; metabolism ; Diabetes Mellitus, Type 2 ; metabolism ; Glucose Transporter Type 4 ; metabolism ; Glucose-6-Phosphatase ; metabolism ; Insulin Resistance ; Interleukin-6 ; metabolism ; Intracellular Signaling Peptides and Proteins ; metabolism ; Liver ; drug effects ; metabolism ; Male ; Phosphoenolpyruvate Carboxykinase (GTP) ; metabolism ; Proto-Oncogene Proteins c-akt ; metabolism ; Rats ; Rats, Wistar ; Receptors, Cytoplasmic and Nuclear ; metabolism ; Receptors, Steroid ; metabolism ; Tumor Necrosis Factor-alpha ; metabolism

The methods of 1H Nuclear Magnetic Resonance (NMR) and mass spectroscopy were used in detecting the metabolites of brodimoprim (BDP) in rat plasma. The endogenic compounds in the plasma were removed with solid phase extraction (SPE) column firstly, then the mixture of metabolites was identified with 1H NMR and mass spectroscopy (MS). Two metabolites of BDP in the plasma at 20h were detected, they were demethyl-brodimorpim glucuronide and brodimoprim sulfurate. The study proved that the method of SPE coupled with NMR and MS can be applied to the analysis of metbolites in plasma quickly and conveniently.

OBJECTIVE: To determine the content of zinc in Mongolia patent drug Zhuangxiyin Powder. METHODS: Differential pulse stripping voltammetry was employed for measurement of zinc. RESULTS: The zinc content in three samples of the drug was (493+/-11.95)microg/g, (526+/-13.74)microg/g and (554+/-9.84) microg/g respectively, and the relative standard deviation (RSD) was 2.42%, 2.61% and 1.78% respectively. CONCLUSION: The content of zinc in Zhuangxiyin Powder of daily dosage is higher than the needed daily intake of healthy people.

In order to clarify the metabolism pathways of scandoside methyl ester, the analysis of metabolites profiling in four kinds of liver microsomes was performed by using an ultra-performance liquid chromatography/ electrospray-tandem mass spectrometry (UPLC-ESI-MS). The data obtained from the 0 h-incubation and the 2 h-incubation were compared and analyzed. After incubation, 5 metabolites of scandoside methyl ester were found in rat, Beagles, rhesus monkey and human liver microsome. The results showed that scandoside methyl ester's major metabolic pathway in the liver microsomes is hydrolysis, oxidation and reduction reactions, and there are certain kinds differences between species. The study provides a research base for further research about iridoid compounds in vivo metabolic pathways.

Aim To explore the differences in hyper-trophic marker genes such as atrial natriuretic peptide ( ANP) , brain natriuretic peptide ( BNP) and β-myo-sin heavy chain (β-MHC) genes in different models of cardiac hypertrophy. Methods Respectively using re-nal abdominal aortic coarctation ( AAC) , arteriovenous fistula ( AVF) and isoproterenol ( ISO) methods to es-tablish C57BL/6 mouse model of cardiac hypertrophy. After modeling, each mouse ’ s body weight ( BW ) , heart weight ( HW) and left ventricular weight ( LVW) were weighed, and the heart weight ( HW/BW) and left ventricular index ( LVW/BW ) were calculated;myocardium by HE staining, pathological morphologi-cal changes were observed; myocardium by immuno-histochemistry, ANP, BNP and β-MHC protein ex-pression was observed;myocardium by Real-time PCR detection, ANP, BNP and β-MHC mRNA expression was observed. Results Compared with control group, HW/BW and LVW/BW were increased in three mod-els. Through the light microscope, each mouse model showed varying degrees of cardiac hypertrophy. ANP, BNP and β-MHC were increased in the protein and mRNA expression. Compared with AAC group, AVF and ISO groups’ myocardial tissue ANP, BNP and β-MHC expression were decreased in the protein and mRNA expression. Conclusions Three cardiac hy-pertrophy models are successful. Cardiac tissue ANP, BNP and β-MHC expression in AAC model exceeds AVF and ISO model.

OBJECTIVE: Dynamic observation of Epstein-Barr virus (EBV) DNA load before and after the treatment in patients with Nasopharyngeal carcinoma (NPC), predicting the incidence of distant metastasis and offering more personalised choice of therapies. METHOD: Fifty-four cases of patients with NPC were taken by fluorescence quantitative PCR assay of EBV DNA load before and after the treatment, all patients were followed up according to plan and carried out the progression-free survival (PFS) and overall survival (OS). RESULT: EBV DNA load in plasma of patients with NPC can partly reflect the clinical characteristics of patients; EBV DNA load in some patients with distant metastasis was higher than those patients with continuous remission when they were not started treatment (P < 0.05); For those patients whose EBV DNA copies were lower than 20,000 copies/mI before the treatment, the progression-free survival and overall survival rates were higher than those high expression patients, and the difference were statistically significant (PF < 0.01 and P < 0.05). CONCLUSION The EBV DNA load in the plasma of NPC patients can partly predict the occurrence of distant metastases before treatment.
Adolescent ; Adult ; Aged ; Carcinoma ; DNA, Viral ; blood ; Female ; Herpesvirus 4, Human ; genetics ; Humans ; Male ; Middle Aged ; Nasopharyngeal Carcinoma ; Nasopharyngeal Neoplasms ; therapy ; virology ; Neoplasm Metastasis ; Viral Load ; Young Adult

In order to clarify the metabolism pathways of scandoside methyl ester, the analysis of metabolites profiling in four kinds of liver microsomes was performed by using an ultra-performance liquid chromatography/ electrospray-tandem mass spectrometry (UPLC-ESI-MS). The data obtained from the 0 h-incubation and the 2 h-incubation were compared and analyzed. After incubation, 5 metabolites of scandoside methyl ester were found in rat, Beagles, rhesus monkey and human liver microsome. The results showed that scandoside methyl ester's major metabolic pathway in the liver microsomes is hydrolysis, oxidation and reduction reactions, and there are certain kinds differences between species. The study provides a research base for further research about iridoid compounds in vivo metabolic pathways.
Animals ; Chromatography, High Pressure Liquid ; Dogs ; Esters ; metabolism ; Humans ; Iridoids ; metabolism ; Macaca mulatta ; Microsomes, Liver ; metabolism ; Rats ; Spectrometry, Mass, Electrospray Ionization

OBJECTIVETo explore the clinical effects of total vertebral column resection combined with anterior mesh cage support in treating severe congenital kyphoscoliosis.

METHODSFrom April 2008 to April 2012,21 patients with severe congenital kyphoscoliosis were treated with total vertebral column resection and internal fixation through posterior approach combined with anterior mesh cage support. There were 8 males and 13 females with an average age of 19.4 years old (ranged from 10 to 35). And 6 cases were thoracic segments deformity,13 cases were thoracolumbar segments and 2 cases were lumbar segments, of them, 2 cases were accompanied with Chairs deformity, 6 cases with diastematomyelia, 4 cases with syringomyelia,and 1 case with neurofibromatosis. According to the Frankel grade system, 3 cases were grade C, 5 cases grade D and 13 cases grade E. Blood loss, operative time, and perioperative complications were recorded. Coronal and sagittal Cobb angle, apical vertebral offset distance, sagittal offset, the relative height of shoulders, razor back deformities were measured and analyzed before and after operation.

RESULTSThe average operative time was 5.2 h (3.5 to 6.5 h) and blood loss was 2,500 ml (1,400 to 4,900 ml). The 2nd day after operation, apical vertebral offset distance, sagittal offset, the relative height of shoulders, razor back deformities had obviously improved than preoperative (P < 0.05). There was no significant difference in above items between postoperative on the 2nd day and final follow-up (P > 0.05). The corrective rate of kyphosis and scoliosis were (60.97 +/- 6.30)% and (62.24 +/- 5.82)%, respectively. On the first day after surgery,2 cases of Frankel grade E aggravated to grade D, and obtained recovery at 2 week after conservative treatment. And 1 case palinesthesia later,grade D aggravated to grade C and obtained recovery after revision surgery in time. One case complicated with permanent blindness of left eye, 1 case occurred injury of pleura and 2 cases had cerebrospinal fluid leak during operation. All patients were followed up from 9 to 31 months with an av- erage of 18.6 months. At final follow-up,all patients obtained bone union, Frankel grade D in 4 cases and grade E in 17 cases, no correction loss and internal fixation loosening was found.

CONCLUSIONTotal vertebral column resection combined with anterior mesh cage support can effectively correct kyphosis and scoliosis in severe congenital kyphoscoliosis and can avoid injury of spine cord by spinal crispation, but intraoperative position and neurologic complications should still be considered.

Adolescent ; Adult ; Child ; Female ; Humans ; Kyphosis ; complications ; congenital ; diagnostic imaging ; surgery ; Male ; Retrospective Studies ; Scoliosis ; complications ; congenital ; diagnostic imaging ; surgery ; Spine ; surgery ; Tomography, X-Ray Computed ; Young Adult

Melittin exhibits high antibacterial potency against drug-resistant bacteria. However, the clinical utility of melittin is limited by its serious hemolytic activity. Thus, the need for developing novel melittin analogues with high antimicrobial activity and low hemolytic activity has grown. We designed, synthesized, and evaluated 20 novel melittin analogues with varying hydrophobic, polar or positively charged amino acids. The results showed that 8 compounds had antimicrobial activity (MIC: 1-4 μg·mL^-1) against gram-positive pathogens equal to or better than that of melittin, and 16 compounds had low hemolytic activity (HC₅₀ ≥ 11.9 μg·mL^-1). Compounds 13 (MIC: 2-4 μg·mL^-1) and 15 (MIC: 1-2 μg·mL^-1) showed equal or better antimicrobial activity against both susceptible and resistant strains of Staphylococcus aureus and Enterococcus faecium compared to melittin (MIC: 4 μg·mL^-1). Compound 13 (HC₅₀: 24.0 ± 4.3 μg·mL^-1) displayed noticeably decreased hemolytic activity compared to melittin (HC₅₀: 5.3 ± 0.4 μg·mL^-1). This work established a base for further study on the structure-activity relationships and structure-toxicity relationships of melittin.

BACKGROUNDHypertrophic scar is one of the most common complications and often causes the disfigurement or deformity in burn or trauma patients. Therapeutic methods on hypertrophic scar treatment have limitations due to the poor understanding of mechanisms of hypertrophic scar formation. To throw light on the molecular mechanism of hypertrophic scar formation will definitely improve the outcome of the treatment. This study aimed to illustrate the negative role of eukaryotic initiation factor 6 (eIF6) in the process of human hypertrophic scar formation, and provide a possible indicator of hypertrophic scar treatment and a potential target molecule for hypertrophic scar.

METHODSIn the present study, we investigated the protein expression of eIF6 in the human hypertrophic scar of different periods by immunohistochemistry and Western blot analysis.

RESULTSIn the hypertrophic scar tissue, eIF6 expression was significantly decreased and absent in the basal layer of epidermis in the early period, and increased slowly and began to appear in the basal layer of epidermis by the scar formation time.

CONCLUSIONSThis study confirmed that eIF6 expression was significantly related to the development of hypertrophic scar, and the eIF6 may be a target molecule for hypertrophic scar control or could be an indicator of the outcomes for other treatment modalities.

Adult ; Blotting, Western ; Cicatrix, Hypertrophic ; metabolism ; Female ; Gene Expression Regulation ; genetics ; Humans ; Immunohistochemistry ; Male ; Middle Aged ; Peptide Initiation Factors ; metabolism ; Pregnancy ; Retrospective Studies ; Young Adult