Wnt/β-catenin signaling pathway plays an important role in the proliferation, growth, invasion, and metastasis of human cancers. Moreover, β-catenin/T-cell factor 4 (TCF4) interaction regulates the transcription of the key oncogenes in Wnt/β-catenin signaling pathway. Therefore, β-catenin/TCF4 interaction would be a promising therapeutic target for the development of highly selective anticancer agents. At present, most ongoing small-molecule inhibitors targeting β-catenin/TCF4 interaction, including PKF222-815, iCRT3/5/14, LF3, and sanguinarine, have been developed in preclinical studies for human cancer therapeutics. In this review, we summarized the research advances of up-to date inhibitors targeting β-catenin/TCF4 interaction, including the molecular structure and cellular functions of β-catenin in canonical Wnt signaling pathway. This review holds a hopeful avenue for the development of novel and highly selective Wnt inhibitors targeting β-catenin/TCF4 interaction for future anticancer strategy.

Objective:To provide scentific evidence for determining the harvest period of Cortex Abizziae by studying the dynamic variation of the content of lignan glycoside I in Cortex Abizziae.Methods:Chromatography was performed on a Boston Green ODS C18 (250 mm×4.6 mm,5 μm) column,the mobile phase was acetonitrile-0.04% phosphate (18∶82),the flow rate was 1.0 ml·min-1,the detection wavelength was 204 nm,and the column temperature was at 25℃.Results:There were differences in the contents of lignan glycoside I in Cortex Abizziae at different harvest periods.The content of lignan glycoside I reached the highest level in January,decreased quickly from January to March,and gradually increased from April to December.Conclusion:The content of lignan glycoside I in Cortex Abizziae at different harvest periods is different,and the optimum harvest time of Cortex Abizziae is determined from November to January of the following year.

Objective To systematically evaluate the association between protein C and Legg -Calve -Perthes disease.Methods A literature research was performed through PubMed,Embase,Cochrane library,Web of Science,Chinese Biomedical Literature Database(CBM),China National Knowledge Infrastructure(CNKI)and Wan-fang Database from inception to February 201 6 on the association between protein C and Legg -Calve -Perthes disease.According to the Newcastle -Ottawa Scale(NOS)criteria,the quality of studies was evaluated and data were extracted.Meta -analysis was performed with Stata 1 1 .0 software.Results A total of 1 4 articles were included.Twelve articles on protein C and Legg -Calve -Perthes disease in the study group and the control group were compared.The results of Meta -analysis showed that there was no significant difference in protein C levels between the study group and the control group[odds radio(OR)=1 .41 ,95% confidence interval(CI)(0.87,2.28),P =0.1 47];five articles on protein C and the white race of Legg -Calve -Perthes disease between the study group and the control group were com-pared,The results of Meta -analysis showed that there was no significant difference in protein C levels between the whiteskin patients′group and the control group[OR =0.61 2,95%CI(1 .83,7.29),P =0.61 2];three articles on pro-tein C and the yellow race of Legg -Calve -Perthes disease between the study group and the control group were com-pared,and the results of Meta -analysis showed that there was no significant difference in protein C levels between the yellow skin patients group and the control group[OR =0.59,95%CI(0.05,6.72),P =0.080].Conclusion There is no significant correlation between protein C and Legg -Calve -Perthes disease.

AIM: To compare intraocular pressure (IOP) fluctuations measured at home and in the clinic over a 24-hour period.METHODS: A prospective investigational study.A total of 120 Chinese participants were selected from five communities in the Chengdu area.Patients underwent a clinical interview and IOP was measured both at home and in the clinic.IOP were measured at 8 a.m., 10 a.m., 12 a.m., 2 p.m., 4 p.m., 6 p.m., 8 p.m., 10 p.m., 2 a.m., 6 a.m.using the same pneumatonometer.Measurements were taken in the sitting position.RESULTS: The average 24-hour IOP measured in the clinic was slightly lower than that at home.The mean difference in 24-hour IOP measurements between home and clinic was 0.27 mmHg.The IOP fluctuation in the clinic was higher than at home (the mean difference was 0.01 mmHg).There was no statistically significant difference in the average 24-hour IOP measured at home vs in the clinic.The average IOP measured at 2 p.m.at home (16.04±5.95 mmHg) was significantly higher compared with the measurement in the clinic (15.43±5.16 mmHg) (P<0.05).The overall agreement between 24-hour IOP measurements made in the clinic and at home in diagnosis of primary open angle glaucoma was 85.0% (K coefficient: 0.68).CONCLUSION: The 24-hour IOP measured in the clinic was similar to that measured at home, and the method of measuring IOP in the clinic is acceptable in diagnosing primary open angle glaucoma.

A 1 270 bp full-length cDNA fragment was obtained from the Schistosoma japonicum (Chinese strain) adult cDNA library after the 3′ and 5′ ends of the incomplete expression sequence tag (EST) of hypoxanthine-guanine phosphoribosyltransferase of Schistosoma japonicum (SjHGPRT) were amplified by the anchored PCR with 2 pairs of primer that were designed according to the published incomplete SjHGPRT EST and the sequence of multiclone sites of library ?gt11 vector. Sequence analysis indicated that this fragment, with an identity of 82% to hypoxanthine-guanine phosphoribosyltransferase of Schistosoma mansoni (SmHGPRT), contained a complete open reading frame(ORF). The deduced amino acid sequence showed 83% identity to that of SmHGPRT. This fragment was cloned into the prokaryotic expression vector pQE30, and subsequently sequenced and expressed in Escherichia coli. SDS-PAGE revealed that M of the recombinant protein was about 28 ku. Western-blot analysis showed that the recombinant protein was recognized by the polyclonal antisera from rabbits immunized with Schistosoma japonicum adult worm antigen. Mice vaccinated with recombinant protein revealed significant worm burden, liver eggs per gram (LEPG), fecal eggs per gram (FEPG) and intrauterine eggs of the female worms reduction percentage, compared with the controls. Taken together, the SjHGPRT full-length cDNA can be cloned and expressed in E.coli as a recombinant protein that elicited immunity against the challenge infection with Schistosoma japonicum, indicating its potential as a partial protection vaccine candidate.

To investigate changes of 14-3-3beta from apoptosis induced by PrP106-126 polypeptide, HeLa cell was incubated with PrP106-126 for 4h or 8h. Nucleus changes and the expression of PARP were detected differently by Hoechst staining and Western blotting. Expressing of protein and mRNA from 14-3-3beta was determined by Western blotting and Real-time PCR. The results show that typical nucleus pyknosis and chip of apoptosis and degradation of PARP were induced by PrP106-126 peptide in HeLa cells. Degradation of 14-3-3beta appeared in apoptosis groups induced by PrP106-126 peptide. However, 14-3-3beta mRNA did not display any changes in apoptosis groups. This study indicated that degradation of antiapoptosis protein 143-3beta induced by PrP106-126 peptide may be one of pathogenesis mechanism of prion disease.
14-3-3 Proteins ; metabolism ; Apoptosis ; drug effects ; HeLa Cells ; Humans ; Peptide Fragments ; pharmacology ; Prions ; pharmacology ; Proteolysis ; drug effects

A 1 270 bp full-length cDNA fragment was obtained from the Schistosoma japonicum (Chinese strain) adult cDNA library after the '3' and 5' ends of the incomplete expression sequence tag (EST) of hypoxanthine-guanine phosphoribosyltransferase of Schistosoma japonicum (SjHGPRT) were amplified by the anchored PCR with 2 pairs of primer that were designed according to the published incomplete SjHGPRT EST and the sequence of multiclone sites of library λgt1 1 vector. Sequence analysis indicated that this fragment, with an identity of 82% to hypoxanthine-guanine phosphoribosyltransferase ofSchistosoma mansoni (SmHGPRT), contained a complete open reading frame(ORF). The deduced amino acid sequence showed 83% identity to that of SmHGPRT. This fragment was cloned into the prokaryotic expression vector pQE30, and subsequently sequenced and expressed in Escherichia coli. SDS-PAGE revealed that M of the recombinant protein was about 28 ku. Western-blot analysis showed that the recombinant protein was recognized by the polyclonal antisera from rabbits immunized with Schistosoma japonicum adult worm antigen. Mice vaccinated with recombinant protein revealed significant worm burden, liver eggs per gram (LEPG), fecal eggs per gram (FEPG) and intrauterine eggs of the female worms reduction percentage, compared with the controls. Taken together, the SjHGPRT full-length cDNA can be cloned and expressed in E. coli as a recombinant protein that elicited immunity against the challenge infection with Schistosoma japonicum, indicating its potential as a partia1 protection vaccine candidate.

ObjectiveTo evaluate the application of multi-slice CT (MSCT) perfusion scan technique in predicting renal function recovery after unilateral hydronephrosis treatment.MethodsThirtyeight patients with unilateral obstructive hydronephrosis not shown on intravenous urography (IVU) and a normal contralateral kidney were recruited for this study.Patients were divided into detected (D) and undetected (UD) groups depending on whether the IVU detected urinary tract obstruction.All patients underwent plain abdominal X-ray,gray-scale ultrasonography,excretory urography and MSCT perfusion scan before and after the treatment.Patients were followed-up at six months or more after the treatment for a mean duration of 12.5 months (range from 6 to 22 ).ResultsOf the 38 cases,22 cases were in group D,16 cases were in group UD.On MSCT,renal cortex blood flow (BF) and blood volume ( BV ) value after treatment in group D were 561.1 ± 165.4 ml/( 100 g · min) and 35.9 ± 11.3 ml/100 g compared with before treatment rates of 361.6 ±109.7 ml/(100g· min) and24.1 ±10.2 ml/100g,t=-3.38,-2.34,P＜0.01,0.05.In the UD group,the differences of these parameters were after treatment 38.7 ± 15.4 ml/(100 g · min),10.306 ± 4.925 ml/100 g and before treatment 39.1 ± 22.5 ml/( 100 g · min) and 8.7 ± 4.4 ml/100 g,P ＞ 0.05.In the aspects of BF and BV,there were statistically significant differences between group D and group U D both before and after the treatment,t=9.09,4.15,P ＜ 0.01.ConclusionsM SCT perfusion can provide a valuable prediction technique of the renal function recovery in patients with unilateral obstructive hydronephrosis.Improvement of renal function can be expected after relief of obstructive hydronephrosis if the patients have a BF 361.6 ml/( 100 g · min) and BV 24.1 ml/100 g or greater measured by MSCT perfusion.

Animals ; Cromolyn Sodium ; administration & dosage ; Disease Models, Animal ; Intestines ; blood supply ; Mast Cells ; drug effects ; Rats ; Rats, Sprague-Dawley ; Reperfusion Injury ; mortality ; pathology ; p-Methoxy-N-methylphenethylamine ; administration & dosage

The crude extracts of the fermentation broth from a marine sediment-derived actinomycete strain, Saccharothrix sp. 10-10, showed significant antibacterial activities against drug-resistant pathogens. A genome-mining PCR-based experiment targeting the genes encoding key enzymes involved in the biosynthesis of secondary metabolites indicated that the strain 10-10 showed the potential to produce tetracenomycin-like compounds. Further chemical investigation of the cultures of this strain led to the identification of two antibiotics, including a tetracenomycin (Tcm) analogs, Tcm X (1), and a tomaymycin derivative, oxotomaymycin (2). Their structures were identified by spectroscopic data analysis, including UV, 1D-NMR, 2D-NMR and MS spectra. Tcm X (1) showed moderate antibacterial activities against a number of drug-resistant pathogens, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococci (VRE) pathogens, with the MIC values in the range of 32-64 microg x mL(-1). In addition, 1 also displayed significant cytotoxic activities against human cancer cell lines, including HL60 (leukemia), HepG2 (liver), and MCF-7 (breast) with the IC 50 values of 5.1, 9.7 and 18.0 micromol x L(-1), respectively. Guided by the PCR-based gene sequence analysis, Tcm X (1) and oxotomaymycin (2) were identified from the genus of Saccharothrix and their 13C NMR data were correctly assigned on the basis of 2D NMR spectroscopic data analysis for the first time.
Actinomycetales ; chemistry ; genetics ; Anti-Bacterial Agents ; chemistry ; isolation & purification ; pharmacology ; Antineoplastic Agents ; chemistry ; isolation & purification ; pharmacology ; Benzodiazepinones ; chemistry ; isolation & purification ; pharmacology ; Cell Line, Tumor ; Data Mining ; methods ; Drug Resistance, Bacterial ; Enterococcus faecalis ; drug effects ; Fermentation ; Genomics ; Humans ; Inhibitory Concentration 50 ; Marine Biology ; Methicillin-Resistant Staphylococcus aureus ; drug effects ; Microbial Sensitivity Tests ; Molecular Structure ; Naphthacenes ; chemistry ; isolation & purification ; pharmacology ; Phylogeny ; Staphylococcus epidermidis ; drug effects