ObjectiveTo summarize the pathological features, methods of diagnosis and treatment of Mirizzi Syndrome to improve the outcomes of diagnosis and treatment.Methods Pre-operative and intraoperative data from 37 patients with Mirizzi Syndrome were retrospectively analyzed.ResultsFifteen of the 37 patients were diagnosed with Mirizze Syndrome definitely before operation, among whom 10 were given cholecystectomy.Another 11 patients were treated with cholecystectomy + common bile duct exploration + T tube drainage,9 with cholecystectomy + bile duct exploration and repair + T tube drainage.3 with hepatic ductjejunum Roux-en-Y anastomosis; 4 with cholecystectomy under laparoscope among whom 1 patients received routine abdominal surgical after failure of microscopical cholecystectomy for severe adhesion.One patients experienced complication of biliary fistula.All the patients were cured and left hospital.Conclusion Type-B ultrasound, magnetic resonance cholangiopancreatography, endoscopic retrograde cholangiopancreatography are major measures which can be comprehensively used for the diagnosis of Mirizzi Syndrome.Mirizzi Syndrome is heterogenous in the pathological features on which the surgical procedures should be based on.

Purpose To investigate the anti-inflammatory effect of Radix Rehmanniae Praeparata(RRP)on the footpad inflammation induced by complete Freund's adjuvant(CFA)in rats.Methods CFA 100 μL were injected subcutaneously to the Wistar rats at the pad of right hindfoots.19 days later,the rats were daily siven RRP water extract(0.625,1.250,2.500 g/kg·bw)or dexamethasone(0.5mg/ks·bw)intragastrically.The changes of body weight and foot volume were measured.The indexes of organ and blood were determined at the 29th day,the foot pad was removed,and routine paraffin section was performed.Results The model rats kept foot swelling and lymphocyte infiltrating,and the platelet number decreased.The other indexes were statistically insignificant when compared to the controls.RRP did not display any anti-inflammatory effect on the swollon foots,but thoracic gland and spleen indexes were rescued,and platelet number and creatinine content were increased by RRP administration in a dose-dependent manner.The anti-inflammation of dexamethasone was conspicuous,but the side effects were also significant.Conclusion RRP may be plays an adjunctive action in herbal recipes to treat rheumatoid arthritis.

A chiral high-performance liquid chromatography method was developed for the simultaneous determination of ibuprofen enantiomers in dog plasma. It was used to study the pharmacokinetics in the Beagle dog after intravenous administration of racemic-ibuprofen, S-ibuprofen and R-ibuprofen. Ketoprofen was chosen as the internal standard. After a simple precipitation using methanol as the precipitating solvent, both analytes and IS were separated on a Kromasil 100-5CHI-TBB chiral column (250 mm x4.6 mm, 5 μm) with isocratic elution using acetonitrile - 20 mmol x L(-1) phosphate buffer (pH 3.0, containing 5% methanol) (6 : 4) as the mobile phase. The detection wavelength was 220 nm. Liner calibration curves for both of the ibuprofen enantiomers were over the concentration range from 0.5 to 50 μg x mL(-1) with a lower limit of quantification of 0.5 μg x mL(-1), the accuracies were all in standard ranges. The intra- and inter- assay precisions were all below 7%. The recovery rate was 93.1% to 100.4%. The experiments proved that the method was simple, rapid and sensitive. It can be used in the quantitative determination of ibuprofen enantiomers in dog plasma. The method was used to determine the concentration of ibuprofen enantiomers in Beagle dog plasma after a single intravenous administration of racemic-ibuprofen, S-ibuprofen and R-ibuprofen (9 mg x kg(-1)) and the pharmacokinetics parameters were calculated based on the concentration-time curves. The C(max) of S-ibuprofen in Beagle dog plasma after a single intravenous administration of racemic-ibuprofen, S-ibuprofen and R-ibuprofen were 30.8 ± 4.7, 46.1 ± 5.9 and 20.0 ± 2.6 μg x mL(-1), respectively. In terms of the exposure of active ingredient, it revealed a significant difference between the administration of S-ibuprofen and the other two groups. The systematical R- to S- chiral inversion was discussed. Comparing the pharmacokinetic parameters at different doses, chiral inversion were 70.1% ± 36.6% and 76.4% ± 36.2%, respectively, after intravenous administration of racemic- and R-ibuprofen. This study provides a theoretical basis for the safety of ibuprofen formula of injection drug.

OBJECTIVE:To establish a method of determining the plasma concentration of capecitabine/polyethylene glycol 1000/montmorillonite (CAP/PEG1000/MMT) in rats’plasma for the study on pharmacokinetics of CAP compound in rats in vivo. METHODS:HPLC was adopted. The determination was performed on Kromasil C18 with mobile phase consisted of 0.1% glacial acetic acid-acetonitrile(73∶27),at the flow rate of 1.0 ml/min. The detection wavelength was 250 nm and column temperature was 40 ℃. The sample size was 10 μl. 18 Wistar rats were randomly divided into CAP group,CAP/MMT group(MMT as carrier)and CAP/PEG1000/MMT group(PEG1000/MMT as carrier)and ig given corresponding drugs,that equal to 200 mg/kg of CAP. Blood sample was respectively taken 15,30,60,90,120,180,240,300 and 360 min after the administration of drugs,and plasma was isolated and added with internal standard ferulic acid. The concentration of the drug in the plasma was determined by HPLC fol-lowing protein precipitation with methanol,based on which the pharmacokinetic parameters were calculated by 3p97 software. RE-SULTS:The linear range of CAP was 0.054 9-4.390 0 μg/ml (r=0.998 2) with the method recovery of 98.2%-102.1%(RSD=1.50%-3.29%, n=5) and absolute recovery of 76.2%-78.9%(RSD=2.29%-2.99%, n=5). In the above-mentioned three groups,t1/2 were(1.11±0.32),(1.57±0.32)and(1.62±0.10)h;cmax were(2.91±0.36),(0.91±0.23)and(0.91±0.14)μg/ml;AUC0-6 h were (8.70 ± 1.79),(3.76 ± 0.27) and (3.73 ± 0.25)μg·h/ml;and tmax were (0.97 ± 0.20),(1.55 ± 0.47) and (1.50 ± 0.07) h,respectively. There was no significant difference in the pharmacokinetic parameters between the CAP/MMT group and CAP/PEG1000/MMT group(P>0.05). CONCLUSIONS:The method is reliable and simple,and can be used for pharmacokinetic study of CAP/PEG1000/MMT in rats. MMT and PEG1000/MMT compound can prolong CAP acting time in the body.

OBJECTIVE:To study the in vitro antioxidant activity of chitosan(CTS)degradation derivatives and its preventive effects on drug-induced liver injury fibosis. METHODS:Acid hydrolysis method was used to prepare the CTS degradation deriva-tives CTS-3,CTS-6,CTS-8,CTS-10 for different hydrolysis time(3,6,8,10 h). The viscosity-average relative molecular mass and deacetylation degree of CTS and its degradation derivatives were determined,and its antioxidant activity was evaluated by de-tecting its in vitro scavenging ability on 1,1-diphenyl-2-trinitrophenylhydrazine (DPPH) and superoxide anion (O2-) radicals. Us-ing CTS-10 for in vivo liver injury fibosis prevention test,mice were randomly divided into normal control group(water),model group(water),CTS-10 high-dose,medium-dose,low-dose groups(100,50,25 mg/mL),8 in each group. Mice were intragastri-cally administrated 0.2 mL,then withdrawal after continuous 24 d. Then levofloxacin hydrochloride was intragastrically given for 7 d to establish drug-induced liver injury model(except for normal control group). Western blot method was used to detect the expres-sions of tumor necrosis factor α(TNF-α),transforming growth factor β1(TGF-β1)and Decorin protein in liver tissue of mice. RE-SULTS:The viscosity-average relative molecular mass of CTS,CTS-3,CTS-6,CTS-8,CTS-10 were 21.70×104,6.70×104,6.30× 104,5.01×104,4.87×104;and deacetylation degree were 83.44％,74.62％,67.28％,64.83％,54.23％,respectively. All of them had certain scavenging ability on DPPH and O2-,in which,CTS-10 was the strongest(25.47％ and 56.31％). Compared with nor-mal control group,expressions of TNF-α,TGF-β1 and Decorin protein in liver tissue in model group were enhanced (P<0.05). Compared with model group,expressions of TNF-α,TGF-β1 and Decorin protein in liver tissue in CTS-10 medium-dose and high-dose groups were weakened(P<0.01). CONCLUSIONS:The viscosity-average relative molecular mass and deacetylation de-gree of CTS-10 in CTS degradation derivatives are lower with stronger antioxidant activity,and show certain preventive effects on drug-induced liver injury fibosis in mice.

Peptide cyclization, a pivotal approach to modifying linear precursors of proteins and pepticles, has been used to enhance their biological activities and serum stabilities. Recently, sortase A (SrtA) from Staphyloccus aureus becomes a promising new technology for efficiently incorporating site specific modifications into proteins, conjugating the cell surface and cyclizing the linear peptides. In this study, we constructed two recombinant expression systems, one with chitin binding domain and the other with six-histidine tag and chitin binding domain on the N-terminal of SrtA, separately. The results of enzymatic kinetics indicate that the two recombinant tags do not impair the transpeptidase activity of SrtA compared with the standard reaction reported under the same reaction condition. The two synthesized peptides with N-ternimal three glycines and C-terminal penta-amino acid motif, LPETG, were cyclized using immobilized and recycled SrtA. The SrtA-based cyclization promises to represent a simple method for easy and efficient enzymatic synthesis of large cyclic peptides.
Aminoacyltransferases ; metabolism ; Bacterial Proteins ; metabolism ; Cyclization ; Cysteine Endopeptidases ; metabolism ; Enzymes, Immobilized ; metabolism ; Kinetics ; Peptides ; metabolism ; Peptides, Cyclic ; biosynthesis ; Staphylococcus aureus ; enzymology

Objective To construct human SREBP-1c-promoter reporter gene vector and to detect its function.Methods Human blood genome DNA was extracted and pGL3-Basic-SREBP-1c-promoter reporter gene vector was constructed.Furthermore,the function of SREBP-1c-promoter was confirmed by dual-luciferase reporter assay.ResultspGL3-Basic-SREBP-1c-promoter reporter gene vector was successfully constructed and the promoter activity was obviously repressed by co-transfection FoxO1.Overexpression FoxO1 inhibited the SREBP-1c protein expression.Conclusion FoxO1 repressed the SREBP-1c protein expression through inhibition the SREBP-1c transcription.

ObjectiveTo observe the effect of resveratrol on the oxidative stress and antioxidant levels of different mitochondrial subpopulations in the skeletal muscle and insulin sensitivity of rats fed with high-fat diet.MethodsMale SD rats,aged 8 weeks,were divided into normal chow (NC) group,high-fat diet(HF) group,high-fat diet plus resveratrol ( HFR ) group.After intervention for 8 weeks,the impacts of resveratrol on oxidative stress levels and antioxidant enzymes activities in subsarcolemmal ( SS ) and intermyofibrillar ( IMF ) mitochondria from skeletal muscle as well as general and skeletal mascle insulin sensitivity were assessed.ResultsCompared with NC group, insulin sensitivity was significantly reduced while reactiveoxygenspecies (ROS)and malondialdehyde(MDA) levels in SS and IMF mitochondria increased in HF group ( all P＜0.01 ).In addition,antioxidant enzyme activities were significantly decreased in SS mitochondrial and increased in IMF mitochondrial ( both P ＜ 0.05 ).Compared with HF group,the insulin sensitivity in HFR group was significantly improved.Moreover,the activities of antioxidant enzymes in SS and IMF mitochondrial were increased,and the oxidative stress levels returned to normal ( P ＜ 0.05 ).ConclusionResveratrol notably improves the oxidative stress of different skeletal muscle mitochondrial subpopulations and insulin resistance in rats fed with high-fat diet.

A chiral high-performance liquid chromatography method was developed for the simultaneous determination of ibuprofen enantiomers in dog plasma. It was used to study the pharmacokinetics in the Beagle dog after intravenous administration of racemic-ibuprofen, S-ibuprofen and R-ibuprofen. Ketoprofen was chosen as the internal standard. After a simple precipitation using methanol as the precipitating solvent, both analytes and IS were separated on a Kromasil 100-5CHI-TBB chiral column (250 mm x4.6 mm, 5 μm) with isocratic elution using acetonitrile - 20 mmol x L(-1) phosphate buffer (pH 3.0, containing 5% methanol) (6 : 4) as the mobile phase. The detection wavelength was 220 nm. Liner calibration curves for both of the ibuprofen enantiomers were over the concentration range from 0.5 to 50 μg x mL(-1) with a lower limit of quantification of 0.5 μg x mL(-1), the accuracies were all in standard ranges. The intra- and inter- assay precisions were all below 7%. The recovery rate was 93.1% to 100.4%. The experiments proved that the method was simple, rapid and sensitive. It can be used in the quantitative determination of ibuprofen enantiomers in dog plasma. The method was used to determine the concentration of ibuprofen enantiomers in Beagle dog plasma after a single intravenous administration of racemic-ibuprofen, S-ibuprofen and R-ibuprofen (9 mg x kg(-1)) and the pharmacokinetics parameters were calculated based on the concentration-time curves. The C(max) of S-ibuprofen in Beagle dog plasma after a single intravenous administration of racemic-ibuprofen, S-ibuprofen and R-ibuprofen were 30.8 ± 4.7, 46.1 ± 5.9 and 20.0 ± 2.6 μg x mL(-1), respectively. In terms of the exposure of active ingredient, it revealed a significant difference between the administration of S-ibuprofen and the other two groups. The systematical R- to S- chiral inversion was discussed. Comparing the pharmacokinetic parameters at different doses, chiral inversion were 70.1% ± 36.6% and 76.4% ± 36.2%, respectively, after intravenous administration of racemic- and R-ibuprofen. This study provides a theoretical basis for the safety of ibuprofen formula of injection drug.
Animals ; Chromatography, High Pressure Liquid ; Dogs ; Ibuprofen ; blood ; pharmacokinetics ; Stereoisomerism

Objective:To survey the expression of MMP-1,MMP-2 of human periodontal ligament cells(HPDLCs)treated by tea polyphenols(TP)and lipopolysaccharide(LPS).Methods:HPDLCs were in vitro cultured in vitro and treated by TP(200 μg/ml) and /or LPS(100 μg/ml)for 24,48 and 72 h respectively,the secretion of MMP-1 and MMP-2 were examined by ELISA,MMP-1 and MMP-2 mRNA expression was examined by real-time PCR.Results:The secression and mRNA expression of MMP-1 and MMP-2 of HPDLCs increased by LPS treatment and significantly inhibited by TP at the different times.Conclusion:TP can inhibit the col-lagen degradation of HPDLCs mediated by LPS.