The synthesis of new 4-imino-4H-chromeno[2,3-d]pyrimidin-3(5H)-amine in four steps including one step under microwave dielectric heating is reported. The structural identity of the synthesized compounds was establishe...The synthesis of new 4-imino-4H-chromeno[2,3-d]pyrimidin-3(5H)-amine in four steps including one step under microwave dielectric heating is reported. The structural identity of the synthesized compounds was established according to their spectroscopic analysis, such as FT-IR, NMR and mass spectroscopy. These new compounds were tested for their antiproliferative activities on seven representative human tumoral cell lines (Huh7 D12, Caco2, MDA-MB231, MDA-MB468, HCT116, PC3 and MCF7) and also on fibroblasts. Among them, only the compounds 6c showed micromolar cytotoxic activity on tumor cell lines (1.8 50 50 > 25 μM). Finally, in silico ADMET studies ware performed to investigate the possibility of using of the identified compound 6c as potential anti-tumor compound.展开更多
AIM: To investigate the potential roles of enhancer of zeste homolog2(EZH2), Bmi-1 and mi R-203 in cell proliferation and invasion in hepatocellular carcinoma(HCC) cell line Hep3 B.METHODS: A total of 73 patients who ...AIM: To investigate the potential roles of enhancer of zeste homolog2(EZH2), Bmi-1 and mi R-203 in cell proliferation and invasion in hepatocellular carcinoma(HCC) cell line Hep3 B.METHODS: A total of 73 patients who underwent surgical resection at Fuzong Clinical Medical College of Fujian Medical University were enrolled in this study. Hep3 B cells were cultivated in RPMI 1640 medium supplemented with 10% fetal bovine serum at 37?℃. Vectors that containing c DNA of the EZH2 gene or mi R-203 targeted sh RNA plasmid were constructed, and then transfected into Hep3 B cells. The m RNA expression of mi R-203, EZH2, and Bmi-1 was analyzed using quantitative real-time polymerase chain reaction analysis, and the protein levels of EZH2 and Bmi-1 were detected by Western blot analysis. Effect of EZH2 or mi R-203 on cell proliferation was observed by methyl thiazolyl tetrazolium assay, and cell apoptosis was assessed using flow cytometry. Besides, effect of EZH2 or mi R-203 on tumor cell invasion was detected using Transwell assay.RESULTS: The m RNA levels of EZH2 and Bmi-1 in HCC tissues and in Hep3 B cells were significantly higher compared with those in normal samples(P < 0.01), while mi R-203 level was significantly lower in HCC tissues(P < 0.01). Hep3 B cells transfected with EZH2-sh RNA or mi R-203-sh RNA showed lower expression levels of EZH2 and Bmi-1(P < 0.05). Compared with controls, Hep3 B cells transfected with EZH2-sh RNA had relative slow cell proliferation, indicating that low expression of EZH2 and Bmi-1 and overexpression of mi R-203 could inhibit Hep3 B cell proliferation(P < 0.05). The average apoptosis rate of Hep3 B cells transfected with EZH2-sh RNA vector was about 18.631%, while that of Hep3 B cells transfected with sh RNA vector was about 5.33%, suggesting that EZH2 was down-regulated by transfecting with EZH2-sh RNA, and the down-regulated EZH2 contributed to the cell apoptosis. Low expression of EZH2 and Bmi-1 and overexpression of mi R-203 could reduce Hep3 B cell invasion(P < 0.05).CONCLUSION: Our study suggests that EZH2 and Bmi-1 are up-regulated while mi R-203 is downregulated in Hep3 B cells. Mi R-203 may contribute to the metastasis and enhance apoptosis of HCC cells by regulating EZH2 and Bmi-1. Our study may provide a theoretical basis for metastasis of HCC and targeted therapy of HCC.展开更多
In the design of building structures,joint efforts must be decided to resolve the depth of competent layers across the intended site to safeguard the durability of civil engineering structures and to avert the disastr...In the design of building structures,joint efforts must be decided to resolve the depth of competent layers across the intended site to safeguard the durability of civil engineering structures and to avert the disastrous consequences of structural failure and collapse.In this study,an integrated methodology that employed DC resistivity tomography involving 2-D and 3-D techniques and geotechnical-soil analysis was used to evaluate subsoil conditions for engineering site investigation at Okerenkoko primary school,in the Warri-southwest area of Delta State,to adduce the phenomena responsible for the visible cracks/structural failure observed in the buildings.The results obtained brought to light the geological structure beneath the subsurface,which consists of four geoelectric layers identified as topsoil,dry/lithified upper sandy layer,wet sand(water-saturated)and peat/clay/sandy clayey soil(highly water-saturated).The deeply-seated peat/clay materials(ρ≤20Ωm)were delineated in the study area to the depths of 17.1 m and 19.8 m from 2-D and 3-D tomography respectively.3-D images presented as horizontal depth slices revealed the dominance of very low resistivity materials i.e.peat/clay/sandy clay within the fourth,fifth and sixth layers at depths ranging from 8.68-12.5 m,12.5-16.9 m and 16.9-21.9 m respectively.The dominance of mechanically unstable peat/clay/sandy clay layers beneath the subsurface,which are highly mobile in response to volumetric changes,is responsible for the noticeable cracks/failure detected on structures within the study site.These observations were validated by a geotechnical test of soil samples in the study area.Atterberg’s limits of the samples revealed plasticity indices of zero.Thus,the soil samples within the depth analyzed were representatives of sandy soil that does not possess any plasticity.The methods justifiably provided relevant information on the subsurface geology beneath the study site and should be appropriated as major tools for engineering site assessment/geotechnical projects.展开更多
It is a research subject in computer vision to 3D reconstruction of an object represented by a single 2D line drawing. Previous works on 3D reconstruction from 2D line drawings focus on objects with lines, plane, view...It is a research subject in computer vision to 3D reconstruction of an object represented by a single 2D line drawing. Previous works on 3D reconstruction from 2D line drawings focus on objects with lines, plane, view, and so on. This paper mainly studies the 3D reconstruction from 2D line drawings. Besides, a new approach is proposed： it is that for the research of the point coordinates of 2D line drawings, so as to achieve the object reconstruction by the reconstruction of point coordinates. The reconstruction process includes： （1） the collection of point coordinates （X,Y） of 2D line drawings; （2） the derivation of mathematical formula about the reconstruction of the point of 2D line drawings, and calculating the corresponding point of the 3D coordinates; （3） the regeneration of 3D graphics with 3D points; （4） analyze error by the proportional of parallel of axonometric projection, in order to prove the accuracy of the method.展开更多
Cux Bi2Se3 is a superconductor that is a potential candidate for topological superconductors. We report our laser- based angle-resolved photoemission measurement on the electronic structure of the CuxBi2Se3 supercondu...Cux Bi2Se3 is a superconductor that is a potential candidate for topological superconductors. We report our laser- based angle-resolved photoemission measurement on the electronic structure of the CuxBi2Se3 superconductor, and a detailed magneto-resistance measurement in both normal and superconducting states. We find that the topological surface state of the pristine Bi2Se3 topological insulator remains robust after the Cu-intercalation, while the Dirae cone location moves downward due to electron doping. Detailed measurements on the magnetic field-dependence of the resistance in the superconducting state establishes an irreversibility line and gives a value of the upper critical field at zero temperature of ～4000 Oe for the Cu0.3Bi2Se3 superconductor with a middle point Tc of 1.g K. The relation between the upper critical field He2 and temperature T is different from the usual scaling relation found in cuprates and in other kinds of superconductors. Small positive magneto-resistance is observed in Cuo.3Bi2Se3 superconductors up to room temperature. These observations provide useful information for further study of this possible candidate for topological superconductors.展开更多
By means of improved ligand-field theory, the ＂pure electronic＂ pressure-induced shifts （PS＇s） and the PS＇s due to electron-phonon interaction （EPI） of R1 line and R2 line of YAG：Cr^3＋ have been calculated, ...By means of improved ligand-field theory, the ＂pure electronic＂ pressure-induced shifts （PS＇s） and the PS＇s due to electron-phonon interaction （EPI） of R1 line and R2 line of YAG：Cr^3＋ have been calculated, respectively. The calculated results are in very good agreement with the experimental data. It is demonstrated that the admixture of │t^2 2（^3T1）e^4T2〉 and │t^3 2 ^2E〉 bases in the wavefunction of RI level of YAG：Crs＋ and its change with pressure play a key role for the PS of RI line. The behaviors of the ＂pure electronic＂ PS of RI line and the PS of RI line due to EPI are different. It is the combined eEect of them that gives rise to the total PS of R1 line, which has satisfactorily explained the experimental results. The systematic analyses and comparisons between the feature of R1-line PS of YAG：Cr^3＋ and the ones of three laser crystals （GSGG：Cr^3＋, GGG：Cr^3＋ and ruby） have been made, and the origin of the difference between them has been revealed.展开更多
The human vision system can reconstruct a 3D object easily from single 2D line drawings even if the hidden lines of the object are invisible. Now, there are many methods have emulated this ability, but when the hidden...The human vision system can reconstruct a 3D object easily from single 2D line drawings even if the hidden lines of the object are invisible. Now, there are many methods have emulated this ability, but when the hidden lines of the object are invisible, these methods cannot reconstruct a complete 3D object. Therefore, we put forward a new algorithm to settle this hard problem. Our approach consists of two steps： （1） infer the invisible vertices and edges to complete the line drawing, （2） propose a vertex-based optimization method to reconstruct a 3D object.展开更多
文摘The synthesis of new 4-imino-4H-chromeno[2,3-d]pyrimidin-3(5H)-amine in four steps including one step under microwave dielectric heating is reported. The structural identity of the synthesized compounds was established according to their spectroscopic analysis, such as FT-IR, NMR and mass spectroscopy. These new compounds were tested for their antiproliferative activities on seven representative human tumoral cell lines (Huh7 D12, Caco2, MDA-MB231, MDA-MB468, HCT116, PC3 and MCF7) and also on fibroblasts. Among them, only the compounds 6c showed micromolar cytotoxic activity on tumor cell lines (1.8 50 50 > 25 μM). Finally, in silico ADMET studies ware performed to investigate the possibility of using of the identified compound 6c as potential anti-tumor compound.
文摘AIM: To investigate the potential roles of enhancer of zeste homolog2(EZH2), Bmi-1 and mi R-203 in cell proliferation and invasion in hepatocellular carcinoma(HCC) cell line Hep3 B.METHODS: A total of 73 patients who underwent surgical resection at Fuzong Clinical Medical College of Fujian Medical University were enrolled in this study. Hep3 B cells were cultivated in RPMI 1640 medium supplemented with 10% fetal bovine serum at 37?℃. Vectors that containing c DNA of the EZH2 gene or mi R-203 targeted sh RNA plasmid were constructed, and then transfected into Hep3 B cells. The m RNA expression of mi R-203, EZH2, and Bmi-1 was analyzed using quantitative real-time polymerase chain reaction analysis, and the protein levels of EZH2 and Bmi-1 were detected by Western blot analysis. Effect of EZH2 or mi R-203 on cell proliferation was observed by methyl thiazolyl tetrazolium assay, and cell apoptosis was assessed using flow cytometry. Besides, effect of EZH2 or mi R-203 on tumor cell invasion was detected using Transwell assay.RESULTS: The m RNA levels of EZH2 and Bmi-1 in HCC tissues and in Hep3 B cells were significantly higher compared with those in normal samples(P < 0.01), while mi R-203 level was significantly lower in HCC tissues(P < 0.01). Hep3 B cells transfected with EZH2-sh RNA or mi R-203-sh RNA showed lower expression levels of EZH2 and Bmi-1(P < 0.05). Compared with controls, Hep3 B cells transfected with EZH2-sh RNA had relative slow cell proliferation, indicating that low expression of EZH2 and Bmi-1 and overexpression of mi R-203 could inhibit Hep3 B cell proliferation(P < 0.05). The average apoptosis rate of Hep3 B cells transfected with EZH2-sh RNA vector was about 18.631%, while that of Hep3 B cells transfected with sh RNA vector was about 5.33%, suggesting that EZH2 was down-regulated by transfecting with EZH2-sh RNA, and the down-regulated EZH2 contributed to the cell apoptosis. Low expression of EZH2 and Bmi-1 and overexpression of mi R-203 could reduce Hep3 B cell invasion(P < 0.05).CONCLUSION: Our study suggests that EZH2 and Bmi-1 are up-regulated while mi R-203 is downregulated in Hep3 B cells. Mi R-203 may contribute to the metastasis and enhance apoptosis of HCC cells by regulating EZH2 and Bmi-1. Our study may provide a theoretical basis for metastasis of HCC and targeted therapy of HCC.
文摘In the design of building structures,joint efforts must be decided to resolve the depth of competent layers across the intended site to safeguard the durability of civil engineering structures and to avert the disastrous consequences of structural failure and collapse.In this study,an integrated methodology that employed DC resistivity tomography involving 2-D and 3-D techniques and geotechnical-soil analysis was used to evaluate subsoil conditions for engineering site investigation at Okerenkoko primary school,in the Warri-southwest area of Delta State,to adduce the phenomena responsible for the visible cracks/structural failure observed in the buildings.The results obtained brought to light the geological structure beneath the subsurface,which consists of four geoelectric layers identified as topsoil,dry/lithified upper sandy layer,wet sand(water-saturated)and peat/clay/sandy clayey soil(highly water-saturated).The deeply-seated peat/clay materials(ρ≤20Ωm)were delineated in the study area to the depths of 17.1 m and 19.8 m from 2-D and 3-D tomography respectively.3-D images presented as horizontal depth slices revealed the dominance of very low resistivity materials i.e.peat/clay/sandy clay within the fourth,fifth and sixth layers at depths ranging from 8.68-12.5 m,12.5-16.9 m and 16.9-21.9 m respectively.The dominance of mechanically unstable peat/clay/sandy clay layers beneath the subsurface,which are highly mobile in response to volumetric changes,is responsible for the noticeable cracks/failure detected on structures within the study site.These observations were validated by a geotechnical test of soil samples in the study area.Atterberg’s limits of the samples revealed plasticity indices of zero.Thus,the soil samples within the depth analyzed were representatives of sandy soil that does not possess any plasticity.The methods justifiably provided relevant information on the subsurface geology beneath the study site and should be appropriated as major tools for engineering site assessment/geotechnical projects.
文摘It is a research subject in computer vision to 3D reconstruction of an object represented by a single 2D line drawing. Previous works on 3D reconstruction from 2D line drawings focus on objects with lines, plane, view, and so on. This paper mainly studies the 3D reconstruction from 2D line drawings. Besides, a new approach is proposed： it is that for the research of the point coordinates of 2D line drawings, so as to achieve the object reconstruction by the reconstruction of point coordinates. The reconstruction process includes： （1） the collection of point coordinates （X,Y） of 2D line drawings; （2） the derivation of mathematical formula about the reconstruction of the point of 2D line drawings, and calculating the corresponding point of the 3D coordinates; （3） the regeneration of 3D graphics with 3D points; （4） analyze error by the proportional of parallel of axonometric projection, in order to prove the accuracy of the method.
基金the National Natural Science Foundation of China under Grant Nos 11190022,91021006 and 11374338the National Basic Research Program of China under Grant Nos 2011CB921703,2011CBA00110 and 2013CB921700the Strategic Priority Research Program(B) of the Chinese Academy of Sciences under Grant No XDB07020300
文摘Cux Bi2Se3 is a superconductor that is a potential candidate for topological superconductors. We report our laser- based angle-resolved photoemission measurement on the electronic structure of the CuxBi2Se3 superconductor, and a detailed magneto-resistance measurement in both normal and superconducting states. We find that the topological surface state of the pristine Bi2Se3 topological insulator remains robust after the Cu-intercalation, while the Dirae cone location moves downward due to electron doping. Detailed measurements on the magnetic field-dependence of the resistance in the superconducting state establishes an irreversibility line and gives a value of the upper critical field at zero temperature of ～4000 Oe for the Cu0.3Bi2Se3 superconductor with a middle point Tc of 1.g K. The relation between the upper critical field He2 and temperature T is different from the usual scaling relation found in cuprates and in other kinds of superconductors. Small positive magneto-resistance is observed in Cuo.3Bi2Se3 superconductors up to room temperature. These observations provide useful information for further study of this possible candidate for topological superconductors.
文摘By means of improved ligand-field theory, the ＂pure electronic＂ pressure-induced shifts （PS＇s） and the PS＇s due to electron-phonon interaction （EPI） of R1 line and R2 line of YAG：Cr^3＋ have been calculated, respectively. The calculated results are in very good agreement with the experimental data. It is demonstrated that the admixture of │t^2 2（^3T1）e^4T2〉 and │t^3 2 ^2E〉 bases in the wavefunction of RI level of YAG：Crs＋ and its change with pressure play a key role for the PS of RI line. The behaviors of the ＂pure electronic＂ PS of RI line and the PS of RI line due to EPI are different. It is the combined eEect of them that gives rise to the total PS of R1 line, which has satisfactorily explained the experimental results. The systematic analyses and comparisons between the feature of R1-line PS of YAG：Cr^3＋ and the ones of three laser crystals （GSGG：Cr^3＋, GGG：Cr^3＋ and ruby） have been made, and the origin of the difference between them has been revealed.
文摘The human vision system can reconstruct a 3D object easily from single 2D line drawings even if the hidden lines of the object are invisible. Now, there are many methods have emulated this ability, but when the hidden lines of the object are invisible, these methods cannot reconstruct a complete 3D object. Therefore, we put forward a new algorithm to settle this hard problem. Our approach consists of two steps： （1） infer the invisible vertices and edges to complete the line drawing, （2） propose a vertex-based optimization method to reconstruct a 3D object.
