Cathepsin B from Helicoverpa armigera (HCB) belongs to the group of cysteine proteinases. HCB is proved being involved in the degradation of yolk proteins during embryonic development,which is an acidic preferring enzyme and is resistant to SDS. The expression of the proenzyme may offer a model for investigating the activation of the enzyme. The HCB gene was constructed into pPIC9K and expressed in Pichia pastoris KM71 strain . After induction by methanol, HCB was expressed and secreted into the medium. The molecular weight of the recombinant procathepsin B was determined as about 38 kDa. The expressed product was confirmed to be HCB by immunoblotting assay using specific rabbit anti-HCB polyclonal antibody. The activity of the product was assayed by in situ hydrolysis (gelatin-SDS-PAGE). These results showed that HCB with proteolytic activity was expressed in P. pastoris KM71. This proenzyme can be used for further research on the activation of the proenzyme or industrial production.

Objective To investigate the antidiabetic effect of Acanthopanax senticosus extracts based on metabonomics by UPLC-MS/MS and to explore its mechanisms. Methods The type 2 diabetes mellitus(T2DM)mouse model was established by inject-ing streptozocin(streptozotocin,STZ)in combination with alloxan. The effect of A. senticosus extracts on the fasting blood glucose of mice was observed. Multivariate statistical analysis was employed to analyze serum metabolites. The differential metabolites were iden-tified by online and self-built databases. MetPA Was employed to analyze the corresponding metabolic pathways. Results The T2DM model was established successfully. Compared with the model group,the fasting blood glucose of mice in the A. senticosus extracts groups decreased significantly. Compared with the normal control group,the level of phenylalanine,LysoPC(16:0,18:0),tyrosine, serine,urea andβ-hydroxybutyric acid inecreased,while the level of alanine,glutamine,leucine,valine and lactic acid decreased significantly in the model group. Pathway enrichment displayed that these metabolites were mainly involved in five metabolic pathways. The above-mentioned metabolites reversed to the normal level in varying degrees after administration of A. senticosus glycosides or poly-saccharoses extracts. Conclusion The extracts of A. senticosus display a significant hypoglycemic effect which might be achieved by regulation of amino acid,energy and lipid metabolism.

The validity of fasting plasma glucose(FPG)combined with HbA_1c in diagnosing diabetes was assessed in patients with coronary heart disease.The results showed that the paired determination of FPG and HbA_1c helped to identify potentially diabetic subjects in patients with coronary heart disease.

Objective To investigate the pathotypes,epidemiological characteristics and antimicrobial resistance of diarrheagenic Escherichia coli (DEC) in children with acute bacterial diarrhea in Shanghai.Methods A total of 2 071 outpatient children with probable acute bacterial diarrhea referred to the enteric clinic of Children's Hospital of Fudan University during June 2012 to June 2014 were enrolled in our study.The stool samples were processed for routine microbiologic and biochemistry tests to identify enteric bacteria,including enteropathogenic Escherichia coli (EPEC),enterotoxigenic Escherichia coli (ETEC),enteroinvasive Escherichia coli (EIEC) and enterohemorrhagic Escherichia coli (EHEC).Kirby-Bauer method was used to identify the antibiotic sensitivity.Difference of means between groups was compared by chi-square test.Results Of 2 071 enrolled children,DEC were identified in 145 (7.0 ％)cases.148 strains were isolated with three of mix infection strains.All DEC isolates in this study included 106 (71.6％) EPEC,24 (16.2％) ETEC,16(10.8％) EIEC and 2(1.4％) EHEC.The median ages of diarrheal children with DEC infections were 14 months (range:3 months to 13 years) and 62.8％ of them were ＜2 years.Among 125 DEC isolates tested for antimicrobial susceptibility,the rates of resistance to ampicillin,trimethoprim-sulfamethoxazole,cefotaxime,cefepime,gentamicin,ceftazidime,amoxicillinclavulanate,ciprofloxacin,and ofloxacin in a descending order were 55.2％,35.2％,28.0％,27.2％,23.2％,8.8％,5.6％,4.0％ and 4.0％,respectively.Resistance rates of EIEC to cefotaxime,cefepime and ceftazidime were 50.0％,43.8％ and 25.0％,respectively,which were higher than those of EPEC,ETEC and EHEC.Conclusion DEC is the important enteric bacteria that causes bacterial diarrhea in children in this study.

The molecular descriptors of impurities with known structure in cefdinir were calculated, selected and associated with the chromatographic retention behavior to establish a model. This quantitative structure retention relationships (QSRR) model for the related substances of cefdinir was established under specific chromatographic condition and verified by other impurities. 12 molecular descriptors were used to establish the QSRR model, F_AFRBWF, Blbn_J, SsCH3, SssCH2, SsNH2, SssNH, SssS, SHdCH2, EEM_AFc, EEM_AFpl, EEM_XFpl and Pi_MaxQ. The relativity between true values and predictions in QSRR of cefdinir is R2 = 0.9836 (n = 18), ΔRRT is no more than 0.154, as 10.17% in RRT. The results indicate that the QSRR model for the related substances of cefdinir can be used to evaluate the analysis methods for related substances and predict the chromatographic behavior of new impurities, which will provide a new way for the evaluation of the effectiveness for drug quality control.
Cephalosporins ; chemistry ; standards ; Chromatography ; Models, Chemical ; Quality Control ; Structure-Activity Relationship

To explore novel coumarin derivatives with more potent anti-proliferative activity, a series of novel compounds were designed and synthesized by linking Schiff base and N, N-bis (2-chloroethyl) amine pharmacophore of nitrogen mustards to the coumarin's framework. Their structures were confirmed by 1H NMR, MS and element analysis techniques. In vitro anti-proliferative activities were evaluated against HepG2, DU145 and MCF7 cell lines by the standard MTT assay. The results showed that some of the target compounds exhibited strong anti-proliferative activities against selected tumor cells, and compounds 7c, 7f, 7g, 7h and 7q were better than or equal to the activities of positive control, they deserved further development.
Antineoplastic Agents ; chemical synthesis ; pharmacology ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Coumarins ; chemical synthesis ; pharmacology ; Drug Design ; Drug Screening Assays, Antitumor ; Humans ; Nitrogen Mustard Compounds ; chemical synthesis ; pharmacology ; Schiff Bases ; Structure-Activity Relationship

Powder X-ray diffraction (PXRD) technology combined with cluster analysis method was used to classify 75 batches of crystalline ceftriaxone sodium into subtypes, the crystalline characteristics of each subtype were measured with scanning electron microscope (SEM). By comparing some parameters of these subtypes correlated to crystallization process of ceftriaxone sodium, such as salification rate, water content in different subtypes, as well as by studying different lattice stabilities, different compatibilities with rubber closures during accelerated stability tests, the key point to improve the quality of domestic ceftriaxone sodium was disclosed. The results of this paper indicated that the fine structure of the products could be controlled well by improving the salification and crystallization process. As a result, the subtype II of ceftriaxone sodium with high stability can be produced.
Ceftriaxone ; chemistry ; classification ; Crystallization ; Microscopy, Electron, Scanning ; Powders ; Water ; X-Ray Diffraction

Objective:To investigate the imaging features of breast solid papillary carcinoma(SPC) by ultrasonography.Methods:The ultrasonic images of 218 breast SPC patients confirmed by pathology in Fudan University Cancer Center from December 2012 to January 2020 were retrospectively reviewed. The manifestations were preliminarily classified into 6 types, and the ultrasonic imaging features were summarized.Results:There were 22 cases with negative ultrasound findings. The cases of solid mass, nodular with ductal dilatation, cystic-solid mass, intraductal abnormal echo, simple ductal dilation and non-ductal flaky hypoechoic area or structural disorders were 79(36.2%), 33(15.1%), 29(13.3%), 30(13.8%), 20(9.2%) and 5(2.3%), respectively, and the diagnostic rates of ultrasound were 70.9%, 24.2%, 75.9%, 20%, 0 and 0, respectively.Conclusions:The ultrasonic manifestations of breast SPC are diverse, while cystic-solid findings can be seen as a clue of breast SPC.

OBJECTIVETo explore the effect of recombinant human adenovirus p53 (rAd-p53) combined with cisplatin on the expression of human lung adenocarcinoma A549 cells.

METHODSHuman lung adenocarcinoma A549 cells were treated with rAd-p53 combined with cisplatin (combination group) or with cisplatin alone(cisplatin group). The expressions of the cell genes were compared between these two groups and the results were analyzed by SAM software.

RESULTA total of 43 differential genes were found, 15 of which were up-regulated and 28 were down-regulated.

CONCLUSIONFollowing introduction of rAd-p53, many genes regulating cell cycle, proliferation and apoptosis expresses up or down which significantly enhance chemosensitivity and killing efficiency of cisplatin on human lung adenocarcinoma A549 cells.

Adenocarcinoma ; metabolism ; pathology ; Adenoviruses, Human ; genetics ; Cell Line, Tumor ; Cisplatin ; pharmacology ; Gene Expression Profiling ; Genes, p53 ; genetics ; Humans ; Lung Neoplasms ; metabolism ; pathology ; Transfection

A qualitative analysis method to identify related substances of rifampicin by correlation of spectra in chromatography was established. Standard chromatographic and spectral data obtained by high-performance liquid chromatography with diode array detection (HPLC-DAD) were developed and used in identification of peaks in samples by calculating correlation coefficients (R). The comparison of spectra was expanded to three-dimensional space. Peaks in chromatography can be identified accurately and rapidly through chromatographic system change. The identification results were validated by LC-MS. The threshold of R was set to 0.99 in order to discriminate the impurities and the minimal amount for identification was 30 ng. Taking full advantage of chromatographic separate efficiency and spectral exclusiveness, the method is accurate and reproducible as a new and effective way to identify multi-components in drugs.
Chromatography, High Pressure Liquid ; methods ; Hydrogen-Ion Concentration ; Mass Spectrometry ; Rifampin ; analogs & derivatives ; analysis