Aim To observe the effect of new com-pound L11 on the affinity and function of sigma-1 re-ceptor,as well as the mouse acute toxicity and analge-sic effect, so as to provide the experimental basis for its pharmacodynamics and preliminary toxicity evalua-tion. Methods Using binding and function test of sig-ma-1 receptor in vitro, the acute toxicity and formalin model test of mice,as well as the rat chronic constric-tion injury(CCI) model test in vivo,the effects of L11 on the inhibitory rate and function of sigma-1 receptor, LD50,lifting/licking time of mice and mechanical pain threshold of rats were respectively measured to evaluate the analgesic effect and mechanism of L11. Results The inhibitory rate and Kiof L11 on the sigma-1 recep-tor were 103.07% and 4.81 nmol·L-1,respectively. The Kivalue was 8.10 nmol·L-1while adding pheny-toin (sigma-1 receptor allosteric modulator). The in-tragastric administration of L11 in mice was 1 680.03 mg·kg-1LD50,and the 95% confidence interval was (1 559.35 ~1 819.40) mg·kg-1. Compared with model group, the II phase lifting/licking time of mice was significantly reduced and the mechanical pain threshold of rat obviously increased by L11. Conclu-sions The new compound L11 has high affinity to sig-ma-1 receptor, which belongs to the antagonist of sig-ma-1 receptor;L11 is less toxic to intragastric adminis-tration and has obvious analgesic effect on the formalin model of mice and CCI model of rats, which may be relative with the sigma-1 receptor antagonism.

Objective To observe the effect of ginsenoside Rb1,the most abundant ginsenoside in ginseng root,on differentiation and lipolysis of 3T3-L1 cells and to explore its anti-diabetic mechanism.Methods 3T3-L1 preadipoeytes were induced under standard differentiation process in the presence of 0.1,1,10,100?mol/L ginsenoside Rb_1 for 6 days.Oil red O staining,measurement of triglyceride contents and glucose uptake assay were performed.The expressions of mRNA and protein of PPAR?2,C/EBP?,ap2,glucose transporter (Glut) 1,and Glut4 were analysed with quantitative real time-PCR and Western blot.The binding affinity of Rb_1 to PPAR?-LBD was evaluated by Surface Plasmon Resonance (SPR).Lipolysis of adipocytes was examined by the measurement of glycerol released from adipoeytes treated with Rb_1 for 1 h.Results Ginsenoside Rb_1 facilitated differentiation of 3T3-L1 preadipoeytes in a dose-depondent manner.10?mol/L ginsenoside Rb_1 increased lipid accumulation by about 56%.Treatment of differentiating adipocytes with 10?mol/L ginsenoside Rb_1 increased the expressions of PPAR?2 and C/EBP?mRNA and protein,as well as mRNA expression of ap2,one of their target genes.After treatment of differentiating adipoeytes with Rb_1,basal and insulin-mediated glucose transport augmented significantly accompanied by up-regulations of mRNA and protein level of Glut4,but not of Glutl.SPR showed Rb_1 could bind to PPAR?which suggested Rb_1 was a ligand of PPAR?.Ginsenoside Rb_1 inhibited basal lipolysis in adipoeytos in a dose-dependent manner.However,it did not affect isoproterenol-stimulated lipolysis.Conclusion As a PPAR?ligand,ginsenoside Rb_1 promotes adipogenesis,inhibitas basal lipolysis and inereasos basal and insulin-mediated glucose transport in cultured adipoeytes.Therefore,anti-diabetic and insulin-sensitizing activity of ginsenosides is,at least in part,involved in the enhancing effect on PPAR?2 and C/EBP?expressions,hence promoting adipogenesis and glucose uptake,and inhibiting lipolysis in adipocytes.

OBJECTIVETo investigate the severity related influencing factor and treatment strategy of severe acute pancreatitis with early organ dysfunction.

METHODSFrom July 2007 to December 2008, 167 patients with severe acute pancreatitis were treated in the Surgical Department of Ruijin Hospital. The relationships between the happening of early organ dysfunction and outcome of the patients were observed, with operative or nonoperative treatment strategy.

RESULTSAmong 167 patients, 68 patients have early organ dysfunction, in which 39 with single organ dysfunction and 29 with multiple organ dysfunction. The early organ dysfunction were involved in 47.1% in cardiovascular system, 35.3% in lung and 29.4% in kidney. Aging (P < 0.05) and higher APACHE II score (P < 0.05) predicted a poor prognosis, which were benefit from early operation.

CONCLUSIONSThe mortality of the patients with SAP is related to age, and the degree of organ dysfunction as well. In the first phase of the disease, the selection of operation depends on the trends and the degree of early organ dysfunction before infected necrosis happens, with the aid of SOFA score as a scale.

Acute Disease ; Aging ; Humans ; Multiple Organ Failure ; Pancreatitis ; diagnosis ; Prognosis

OBJECTIVETo investigate the relationship between the clinical character and therapeutic strategy and prognosis in severe acute pancreatitis.

METHODSFrom January 2001 to December 2005, 783 patients with SAP were treated. Therapeutic strategy was selected based on the preliminary scheme for diagnosis and treatment of severe acute pancreatitis by pancreatic surgery society of CMA. All the patients were divided into biliary group and non-biliary group, while 375 patients in biliary group, with 182 patients treated operatively and 193 patients treated nonoperatively; and 408 patients in non-biliary group, with 147 patients treated operatively and 261 patients treated nonoperatively.

RESULTSThere were 698 survivals, the overall survival rate was 89.1%. 357 survivals in the biliary SAP group, the survival rate was 95.0%, in which 171 survivals from operation treated cases, with the survival rate of 94.0%, and 186 survivals from non-operation treated cases, with the survival rate of 96.4%; 341 survivals in the non-biliary SAP group, the survival rate was 84.0%, in which 110 survivals from operation treated cases, with the survival rate of 74.8%, and 231 survivals from non-operation treated cases, with the survival rate of 88.5%. 48.3% patients of the survival group had organ dysfunction, and 18.3% patients had multiple organ dysfunctions, while 100% patients of the death group had organ dysfunction, and 97.6% patients had multiple organ dysfunction. Respiratory dysfunction was found to be the most common cause totally followed by nerve system dysfunction and shock, with the rates of 26.3%, 11.7% and 10.3%, respectively. Respiratory dysfunction, renal dysfunction and cardiac dysfunction are most commonly in death group, with the rate of 94.1%, 60.0% and 60.0%, respectively. The rate of fungi infection in the survival group and death group were 8.9% and 37.6%. The rates of alimentary tract fistula in the survival and death group were 0.9% and 14.1%, respectively.

CONCLUSIONSThe therapy aiming at the cause for biliary SAP and the operation aiming at infected pancreatic necrosis is helpful to improve curative rate; MODS is the main cause of death in severe acute pancreatitis. Respiratory dysfunction, renal dysfunction and cardiac dysfunction are high risk factors.

Female ; Humans ; Male ; Middle Aged ; Pancreatitis, Acute Necrotizing ; diagnosis ; mortality ; therapy ; Prognosis ; Retrospective Studies ; Survival Rate

OBJECTIVETo evaluate the health-related quality of life and postdischarge long-term outcome after severe acute pancreatitis.

METHODSThe hospital records of patients with SAP discharged healthy from January 2003 to December 2003 were reviewed. The Rand 36-item Health Survey with accessory question was mailed to each patient. The means and deviations for each of eight scales scores of SF-36 were calculated, the study population scores were compared with general Chinese population; Univariate analysis was applied to determining the effects of variables such as age, sex, causes of disease, mode of treatment, frequency of surgery, financial burden, length of stay, chronic complications. Accessory questions were analyzed separately.

RESULTSThe means and deviations for each of eight scales (PF, RP, RE, BP, VT, MH, SF, GH) scores of SF-36 in SAP patients were 83 +/- 15, 62 +/- 42, 69 +/- 36, 80 +/- 15, 69 +/- 19, 72 +/- 15, 75 +/- 18, 65 +/- 18, compared with general people. Except RP and SF, the others were similar. In the ANOVA of Physical Component Summary, the three variables mode of treatment, financial burden and length of stay were included (P < 0.05), while in that of Mental Component Summary, the two variables of gender and financial burden were included (P < 0.05).

CONCLUSIONSThe health-related quality of life in SAP patients is similar to that of general people. Greater attention should be given to mode of treatment, length of stay and financial burden to improve quality of life.

APACHE ; Adolescent ; Adult ; Aged ; Analysis of Variance ; Female ; Follow-Up Studies ; Humans ; Male ; Middle Aged ; Pancreatitis, Acute Necrotizing ; psychology ; therapy ; Quality of Life ; Retrospective Studies ; Surveys and Questionnaires ; Survivors ; Treatment Outcome

The molecularly imprinted polymers membranes(MIPMs)were prepared for selective adsorption of lamotrigine(LTG)in plasma by surface molecular imprinting technology with polyvinylidenefluoride(PVDF)membranes as supporter,lamotrigine as template molecule,methyl methacrylate as functional monomer,ethylene glycol dimethacrylate as cross-linking agent,azodiisobutyronitrile as initiator and acetonitrile-dimethylformamide(1∶1.5,V/V)as pore-forming agent.The prepared MIPMs were characterized by scanning electron microscope,Fourier transform infrared spectroscopy,Brunaner-emmet-teller measurements,X-ray photoelectron spectroscopy,and thermogravimetric analysis.The adsorption properties of the materials were investigated by kinetic adsorption,isothermal adsorption,selective adsorption,adsorption-desorption and reusability experiments.The results showed that the imprinted layer of LTG was successfully coated on the surface of PVDF,and the materials had uniform particle size.The adsorption capacity and imprinting factor of the MIPMs towards LTG were 3.77 mg/g and 8.97,respectively.The nanomaterials showed fast mass transfer rate(30 min)and good reusability(the adsorption efficiency was 86.66%after 6 cycles),and could be used for the adsorption of LTG in plasma with low matrix interference,recoveries of 86.54%-90.48%and RSD of 1.51%-3.15%(n=5).The proposed LTG MIPMs were demonstrated to be simple and environment friendly,and had high selectivity in rapid separation and extraction of LTG in plasma.

OBJECTIVETo evaluate the feasibility of autologous peripheral CD(34)(+) cell transplantation for the treatment of severe autoimmune disease.

METHODSTen patients received mobilized and purified CD(34)(+) cells transplantation. The mobilization regimen was CTX plus rhG-CSF and the CD(34)(+) cells were selected by CliniMACS. (1.98 +/- 0.95) x 10(8) CD(34)(+) cells were obtained. The purity of CD(34)(+) cells was (91.4 +/- 10.6)% and the recovering rate was (60.5 +/- 19.8)%. The conditioning regimens were CTX (200 mg/kg) plus ATG (90 mg/kg) or CTX (150 mg/kg) plus TBI (4 - 6 Gy). (2.14 +/- 1.05) x 10(6)/kg CD(34)(+) cells were infused. The time of ANC >or= 0.5 x 10(9)/L was 8.6 +/- 2.5 days, and platelet >or= 20 x 10(9)/L was 9.0 +/- 5.2 days. After the hematopoietic recovery, the levels of CD(3)(+) T cell, CD(19)(+) B cells and CD(16)(+)CD(56)(+) NK cells were all below that of pre-transplantation. The main transplant-related complication was CMV infection. The transplant-related mortality was 2/10. All patients who survived showed improvement of the disease with DAI score decreasing from 17 to 4 in systemic lupus erythematosus patients, DAS 28 score from 6.4 to 1.8 in rheumatoid arthritis patients.

CONCLUSIONThe result suggests that autologous peripheral CD(34)(+) cell transplantation is an alternative choice for the treatment of severe autoimmune disease. The short-term outcome is satisfying.

Adolescent ; Adult ; Antigens, CD34 ; analysis ; Autoimmune Diseases ; immunology ; therapy ; Female ; Hematopoiesis ; Hematopoietic Stem Cell Mobilization ; Humans ; Immune Tolerance ; Male ; Middle Aged ; Peripheral Blood Stem Cell Transplantation ; adverse effects ; mortality ; Transplantation, Autologous

Metabolomics based on liquid chromatography coupled with mass spectrometry (LC-MS) was used to study the initiation and development of diabetes in rats, and the ability of Ginkgo biloba extract (GBE) to ameliorate this pathology. Diabetes mellitus (DM) was induced by intra-peritoneal injection of streptozotocin. The rats were randomly divided into a normal control group treated with drug-free solution (NC), a normal control group treated with GBE (N-GBE), a DM group treated with drug-free solution (DM), and a DM group treated with GBE (D-GBE); rats were maintained on this protocol for 9 weeks. Rat plasma was collected from the sixth week to the ninth week and then analyzed with LC-MS. Animal experimentation was approved by the Committee on the Ethics of Animal Experiments of Xuzhou Medical University. Twelve plasma metabolites with continuous differentiation were monitored to indicate dysfunction of metabolic pathways including fatty acid metabolism, phospholipid metabolism, amino acid metabolism, tricarboxylic acid cycle activity, bile acid metabolism, and purine metabolism to confirm the occurrence and development of DM. Treatment with GBE partially reversed the changes seen in five metabolites in DM rats, indicating that GBE could prevent the occurrence and development of DM by acting on fatty acid metabolism, phospholipid metabolism, amino acid metabolism, and the tricarboxylic acid cycle.

Ultra-high performance liquid chromatography coupled with quadrupole/time-of-flight tandem mass spectrometry (UPLC-Q/TOF-MS/MS) has been used to detect the metabolites of schaftoside in plasma, bile, urine and feces of mice after oral administration. The study was approved by the Experimental Animal Ethics Committee from Xuzhou Medical University (No. XZMULL201612024). Compounds were identified by analyzing their high-resolution mass spectrometry data, mass spectra, and comparison with reference substances and the literatures. The parent compound and 29 metabolites were detected in the plasma, bile, urine and feces samples of mice. The main metabolic pathways of schaftoside in mice include deglycosylation/glycosylation, hydroxylation/dehydroxylation, hydrogenation, methylation, acetylation, sulfation, and glucuronidation. This study provides references for the material basis of schaftoside in vivo.

The research on distribution and quality suitability division of Desmodium styracifolium were formulated by Maxent and ArcGIS model based on the content of schaftoside and polysaccharide of D. styracifolium and its field research in the south and southwest areas of China (Guangdong, Guangxi, Hainan and Yunnan), and the most suitable habitats of distribution suitability and quality suitability were screened. The distribution suitability results indicated that average air temperature in April,mean temperature of coldest quarter, soil type, coldness index were found as the four dominant factors contributing to the plant distribution. The quality suitability results indicated that: ①Polysaccharide content and precipitation in April show significant positive correlation;Schaftoside content and mean temperature of April, mean temperature of coldest quarter show significant negative correlation. Schaftoside content shows significant negative correlation with the precipitation in October and November and the sunshine duration in April and May, while there is a significant positive correlation between schaftoside content and precipitation in April and temperature seasonality standard deviation, and a highly significant positive correlation was found between schaftoside content and precipitation in February and March. ②The quality zoning map was drawn depend on general content of polysaccharide and schaftoside as the index of quality. And this research provides scientific location basis for the production regionalization, cultivation bases selection and directive breeding of D. styracifolium.