Actins ; metabolism ; Adult ; Breast ; pathology ; Breast Neoplasms ; metabolism ; pathology ; surgery ; Female ; Humans ; Mammography ; Neoplasms, Muscle Tissue ; metabolism ; pathology ; surgery ; Vimentin ; metabolism

Cost-Benefit Analysis ; Early Detection of Cancer ; Humans ; Mass Screening ; methods ; Neoplasms ; diagnosis ; epidemiology ; therapy ; Program Evaluation

·AIM:To investigate the effect of β1-integrin overexpression on the adhesion and migration of rabbit corneal epithelial (RCE) cells.·METHODS:Eukaryotic expression vector encoding β1-integrin-GFP fusion DNA was transfected into RCE cells,and the β1-integrin-GFP fusion gene was examined by RT-PCR and Western blot.The adhesion to Matrigel and the migration of the transfected cells were determined by adhesion and mobility assays.The phosphorylation of focal adhesion kinase (FAK) was examined by Western blot.·RESULTS:The overexpression of β1-integrin-GFP fusion gene by RCE cells was successfully established.β1-integrin transfection significantly promoted the adhesion of RCE cells to Matrigel ( P < 0.05 ).β1-integrin overexpression also promoted the migration ability of RCE cells and induced FAK phosphorylation in them (P < 0.05).·CONCLUSION:These data suggest that overexpression of β1-integrin promotes the adhesion and migration of RCE cells and that the FAK pathway may play an important role in this process.

Pain is one of the common clinical symptom, previous studies have implicated sodium channels as a key constituent in pain signaling. Sodium channel blockers with efficient sodium channel blockade effect play an important role in analgesic treatment. However, most drugs used in clinic have many drawbacks and can not meet the demand of the clinical use. Therefore, for the development of new generation of sodium channel blockers, it is of great significance to find small molecule sodium channel blocking lead compounds with novel chemical scaffolds and new structures, sodium channel blocking activity and structure-activity relationship are discussed in detail, and current problems and trends in future research are also emphasized.
Analgesics ; chemistry ; pharmacology ; therapeutic use ; Animals ; Drug Design ; Humans ; Molecular Structure ; Neuralgia ; drug therapy ; Pain ; drug therapy ; Pain Measurement ; Sodium Channel Blockers ; chemistry ; pharmacology ; therapeutic use ; Sodium Channels ; drug effects ; Structure-Activity Relationship

AIMTo establish the differential scanning calorimetric (DSC) methodology for controlling the crystal-type B form of nateglinide.

METHODSAccurately weighed pure dried (P2O5 as desiccant for 4 h at 80 degrees C in vacuum) fine powder of crystal-type B and H of nateglinide were measured dQ/dT by DSC at heating rate of 10 degrees C. min-1 and temperature between 100 degrees C and 200 degrees C to calculate the enthalpy delta HB and delta HH. Accurately weight a series of uniform mixtures of crystal-type B and H of dried fine powder of nateglinide in different proportions. The enthalpy of the mixtures is measured by DSC as above to calculate the enthalpy (sigma delta H). Using B% as X, sigma delta H as Y, the regression equation was obtained. According to this equation, the unknown composition of mixed crystal was evaluated by the sigma delta H values. The method was used to control the limitation of crystal-type B of nateglinide by the sigma delta H value of mixture of known composition as reference.

RESULTSThe results measured from different laboratories showed that the repeatability was 0.61% and the recoveries were 86.2%-127% when the amounts of crystal-type B were between 0-15%.

CONCLUSIONThis method can be used to evaluate the crystal-type B composition of nateglinide.

Designing of natural product-like compounds using natural products as template structures is an important strategy for the discovery of new drugs. Gambogic acid (GA), which is a Garcinia natural product with a unique caged xanthone scaffold, inhibits potent antitumor activity both in vitro and in vivo. This review summarized the researches on the identification of the antitumor pharmacophore of GA, and the design, structural optimization and structure-activity relationship (SAR) of natural product-like caged xanthones based on it.
Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Biological Products ; chemical synthesis ; chemistry ; isolation & purification ; pharmacology ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Drug Screening Assays, Antitumor ; Garcinia ; chemistry ; Humans ; Molecular Structure ; Structure-Activity Relationship ; Xanthones ; chemical synthesis ; chemistry ; isolation & purification ; pharmacology

Adult ; CD56 Antigen ; metabolism ; Carcinoma, Papillary ; diagnosis ; metabolism ; pathology ; surgery ; Endoscopic Ultrasound-Guided Fine Needle Aspiration ; methods ; Female ; Humans ; Male ; Neprilysin ; metabolism ; Pancreatic Neoplasms ; diagnosis ; metabolism ; pathology ; surgery ; Receptors, Progesterone ; metabolism ; Vimentin ; metabolism ; Young Adult ; beta Catenin ; metabolism

AIMIn order to find a way to prognosticate the region-selectivity in the O-methylation reaction of erythromycin and its derivatives, conformation search model of Hyperchem Pro 6.0 used in personal computer was used to establish it.

METHODSThe results of O-methylation reaction of compound 1, 2 and 3 showed the difference between 6-OH and 11-OH. Using the conformational search model of hyperchem, 1,000 conformations of compound 4, 5 and 6 were found with the parameter of dihedral angle. The 14-membered lactone ring was defined as a "plane". The position of carbonyl of 1- or 9- and hydroxyl of 6- or 11- is different, either "up-plane" or "down-plane". A statistic analysis of low-energy conformation clusters was used to sort these clusters by the parameter of the dihedral angle. The data is in accord with the results of the experiments.

RESULTSConformation numbers, energy minimum, energy average and position of the active groups of compounds 4, 5 and 6, the simplified structures of compound 1, 2 and 3, were given in Table 1. by sorting the dihedral angle.

CONCLUSIONThe interaction of the hydroxyl and carbonyl were analysed and found that O-methylation reactions of erythromycin and its derivatives were impacted by the space factor. The clusters of energy minimum, maximum number and "outside" were discussed. The selectivity of the O-methylation reaction of erythromycin and its derivatives can be prognosticated by analysing the parameter of the dihedral angle.

· AIM: To investigate the effect of β1-integrin overexpression on the apoptosis of rabbit corneal epithelial cells and the related mechanism. · METHODS: The plasmid expressing β1-integrin-GFP fusion protein was constructed by polymerase chain reaction (PCR), and this plasmid (β1 group) or the empty vector (mock group) was transfected into rabbit corneal epithelial cells, respectively. The expression of β1-integrin-GFP fusion gene was confirmed by reverse transcription-polymerase chain reaction (RT-PCR) and Western blot. The adhesion of transfected cells to extracellular matrix (ECM) proteins was determined by adhesion assay. The apoptosis of rabbit corneal epithelial cells was assayed by Hoechst 33342 staining and DNA ladder. The phosphorylation of mitogen-activated protein (MAP) kinase was examined by Western blot. · RESULTS: Rabbit corneal epithelial cells overexpressing β1 -integrin-GFP fusion gene were successfully established. Compared with mock group, β1-integrin transfection significantly promoted the adhesive of rabbit corneal epithelial cells to ECM proteins such as laminin, fibronectin, collagen Ⅰ and collagen Ⅳ. Β1-integrin overexpression inhibited apoptosis and induced MAP kinase phosphorylation in rabbit corneal epithelial cells (P<0.05).· CONCLUSION: These data suggest that overexpression of β1-integrin confers resistance to apoptosis in rabbit corneal epithelial cells, and MAP kinase pathway may play an important role in this process.

Objective To observe the effects of Jianpi Huoxue Prescription on the subcutaneous transplantation of tumor cell apoptosis and angiogenesis; To discuss its possible mechanism of action. Methods SMMC-7721 hepatoma mice models were established. 60 tumor bearing male mice were randomly divided into blank group, model group, 5-Fu group, Jianpi Huoxue Prescription high-, medium- and low-dosage groups, with 10 rats in each group. Model group and Jianpi Huoxue Prescription high-, medium- and low-dosage groups were given medicine with relevant concentrations for gavage, once a day. 5-Fu group was given 5-Fu for intraperitoneal injection every other day. The weight, tumor weight and tumor inhibitory rate of each group were compared two weeks later. The protein expressions of VEGF and VEGFR-2 were detected by immunohistochemistry, microvessel density (MVD) were calculated, and the expressions of Survivin and Caspase-3 mRNA were detected by RT-qPCR. Results Compared with model group, protein expressions of VEGF and VEGFR-2, MVD, Caspase-3 and Survivin mRNA decreased in Jianpi Huoxue Prescription high-, medium- and low-dosage groups, and the most obvious differences were in 5-Fu group and Jianpi Huoxue Prescription high-dosage group (P<0.05). Conclusion Jianpi Huoxue Prescription can inhibit tumor growth by inhibiting angiogenesis and inducing apoptosis.