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
Two-dimensional honeycomb lattices show great potential in the realization of Dirac nodal line fermions(DNLFs).Here,we successfully synthesized a gold telluride(AuTe)monolayer by direct tellurizing an Au(111)substrate...Two-dimensional honeycomb lattices show great potential in the realization of Dirac nodal line fermions(DNLFs).Here,we successfully synthesized a gold telluride(AuTe)monolayer by direct tellurizing an Au(111)substrate.Low energy electron diffraction measurements reveal that it is(2×2)AuTe layer stacked onto(3×3)Au(111)substrate.Moreover,scanning tunneling microscopy images show that the AuTe layer has a honeycomb structure.Scanning transmission electron microscopy reveals that it is a single-atom layer.In addition,first-principles calculations demonstrate that the honeycomb AuTe monolayer exhibits Dirac nodal line features protected by mirror symmetry,which is validated by angle-resolved photoemission spectra.Our results establish that monolayer AuTe can be a good candidate to investigate 2D DNLFs and provides opportunities to realize high-speed low-dissipation devices.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
In order to study the effect of 5, 6-Dichloro-l-13-D-ribofuranosyl-benzimidazole (DRB) on the biological characteristics of human laryngeal carcinoma Hep-2 cell line in vitro, Hep-2 cells cultured in vitro were trea...In order to study the effect of 5, 6-Dichloro-l-13-D-ribofuranosyl-benzimidazole (DRB) on the biological characteristics of human laryngeal carcinoma Hep-2 cell line in vitro, Hep-2 cells cultured in vitro were treated with different concentrations of DRB. Changes in cell proliferation, apoptotic rate and invasiveness were detected by MTT assay, flow cytometry (FCM) and matrigel in vitro invasion assay, respectively. It was found that DRB inhibited the proliferation of Hep-2 cells in a dose- and time-dependent manner. After being treated with 0, 10, 20, 40, 80 μmmol/L DRB for 24 h, the apoptotic rate in Hep-2 cells was (0.68±0.19)%, (1.95±0.12)%, (8.51±0.26)%, (11.26±0.17)% and (14.99±0.32)%, respectively. The matrigel in vitro invasion assay revealed that DRB began to inhibit the invasion of Hep-2 cells at the concentration of 5 μmmol/L, and with the increase of DRB concentration, the inhibitory effect was enhanced. It was suggested that DRB could influence the essential biological characteristics of Hep-2 cells, inhibit Hep-2 cells proliferation, reduce invasive ability and induce apoptosis of Hep-2 cells.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
In CSEM exploration, the receivers are generally located about three to five times the skin depth from the transmitter. In this paper, we study the effect of a conductor between the transmitter and the survey area on ...In CSEM exploration, the receivers are generally located about three to five times the skin depth from the transmitter. In this paper, we study the effect of a conductor between the transmitter and the survey area on the target conductor response using forward modeling and inversion. The 2D forward finite element calculations show that the conductor mainly affects the response at middle and low frequencies. The lower the resistivity and the larger the conductor, the larger the effect and the effect increases with decreasing frequency. The inversion results indicate that the calculated position of the target body can move towards the source, leading to an incorrect interpretation without considering the conductor. In order to reduce the effect of a conductor between the source and the survey area, CSEM acquisition should be conducted in three dimensions using multiple sources and 3D inversion should be used during interpretation.展开更多
Objective: This work aimed to study the inhibitory effect and the related mechanism of metformin (MET) on the proliferation of human hepatoma HepG2 cells. Methods: Human hepatoma HepG2 cells were treated with MET ...Objective: This work aimed to study the inhibitory effect and the related mechanism of metformin (MET) on the proliferation of human hepatoma HepG2 cells. Methods: Human hepatoma HepG2 cells were treated with MET (0, 2, 10, and 50 mM). The inhibitory effect of MET on the proliferation of HepG2 cells was determined by MTT method. The apoptosis of HepG2 cells was detected by flow cytornetry. The expression of cyclin D1 in HepG2 cells was examined by Western blot. ROS-DHE fluorescence probe was used to stain the reactive oxygen species (ROS) generated by HepG2 cells after treat- ment. Results: MET could inhibit the proliferation of HepG2 cells in a dose and time dependent manner. MET promoted the apoptosis of HepG2 cells. In addition, MET suppressed the expression of cell cycle protein cyclin D1 and induced the produc- tion of ROS in HepG2 cells. Conclusion: MET can inhibit the proliferation of human hepatoma HepG2 cells and induce cell apoptosis. Meanwhile, MET has the ability to decrease the expression of cyclin D1 and induce ROS generation, which may be involved in the mechanism of inhibiting hepatoma cells proliferation.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.
基金Project supported by the National Key R&D Program of China (Grant No.2018YFA0305800)the National Natural Science Foundation of China (Grant Nos.61925111,61888102,and 52102193)+2 种基金the Strategic Priority Research Program of Chinese Academy of Sciences (Grant Nos.XDB28000000 and XDB30000000)CAS Project for Young Scientists in Basic Research (Grant No.YSBR-003)the Fundamental Research Funds for the Central Universities。
文摘Two-dimensional honeycomb lattices show great potential in the realization of Dirac nodal line fermions(DNLFs).Here,we successfully synthesized a gold telluride(AuTe)monolayer by direct tellurizing an Au(111)substrate.Low energy electron diffraction measurements reveal that it is(2×2)AuTe layer stacked onto(3×3)Au(111)substrate.Moreover,scanning tunneling microscopy images show that the AuTe layer has a honeycomb structure.Scanning transmission electron microscopy reveals that it is a single-atom layer.In addition,first-principles calculations demonstrate that the honeycomb AuTe monolayer exhibits Dirac nodal line features protected by mirror symmetry,which is validated by angle-resolved photoemission spectra.Our results establish that monolayer AuTe can be a good candidate to investigate 2D DNLFs and provides opportunities to realize high-speed low-dissipation devices.
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This project was supported by a grant from the Teaching and Research Award Program for Outstanding Young Teacher in Higher Education Institution of Ministry of Education of China.
文摘In order to study the effect of 5, 6-Dichloro-l-13-D-ribofuranosyl-benzimidazole (DRB) on the biological characteristics of human laryngeal carcinoma Hep-2 cell line in vitro, Hep-2 cells cultured in vitro were treated with different concentrations of DRB. Changes in cell proliferation, apoptotic rate and invasiveness were detected by MTT assay, flow cytometry (FCM) and matrigel in vitro invasion assay, respectively. It was found that DRB inhibited the proliferation of Hep-2 cells in a dose- and time-dependent manner. After being treated with 0, 10, 20, 40, 80 μmmol/L DRB for 24 h, the apoptotic rate in Hep-2 cells was (0.68±0.19)%, (1.95±0.12)%, (8.51±0.26)%, (11.26±0.17)% and (14.99±0.32)%, respectively. The matrigel in vitro invasion assay revealed that DRB began to inhibit the invasion of Hep-2 cells at the concentration of 5 μmmol/L, and with the increase of DRB concentration, the inhibitory effect was enhanced. It was suggested that DRB could influence the essential biological characteristics of Hep-2 cells, inhibit Hep-2 cells proliferation, reduce invasive ability and induce apoptosis of Hep-2 cells.
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.
基金supported by the Project kzcx2-yw-113,kzcx2-yw-121 and kzcx1-yw-15-4,CAS
文摘In CSEM exploration, the receivers are generally located about three to five times the skin depth from the transmitter. In this paper, we study the effect of a conductor between the transmitter and the survey area on the target conductor response using forward modeling and inversion. The 2D forward finite element calculations show that the conductor mainly affects the response at middle and low frequencies. The lower the resistivity and the larger the conductor, the larger the effect and the effect increases with decreasing frequency. The inversion results indicate that the calculated position of the target body can move towards the source, leading to an incorrect interpretation without considering the conductor. In order to reduce the effect of a conductor between the source and the survey area, CSEM acquisition should be conducted in three dimensions using multiple sources and 3D inversion should be used during interpretation.
文摘目的:探讨不同分子靶向药物对高表达与低表达ATP结合转运蛋白G超家族成员2(ATP-binding cassette super-family Gmember 2,ABCG2)的人耐药鼻咽癌CNE2/DDP细胞(分别简写为ABCG2highCNE2/DDP和ABCG2lowCNE2/DDP)表面NKG2D配体(natural killer group 2 member Dligands,NKG2DLs)表达的诱导作用及其对NK细胞杀伤敏感性的影响。方法:免疫磁珠法分选ABCG2highCNE2/DDP、ABCG2lowCNE2/DDP细胞及NK细胞。流式细胞术检测分选细胞的纯度和不同分子靶向药物(硼替佐米、索拉非尼、舒尼替尼)处理前后ABCG2highCNE2/DDP和ABCG2lowCNE2/DDP细胞NKG2DLs的表达率。LDH释放法检测不同药物处理前后ABCG2highCNE2/DDP和ABCG2lowCNE2/DDP细胞对NK细胞杀伤的敏感性。结果:ABCG2highCNE2/DDP和ABCG2lowCNE2/DDP细胞表面ABCG2的表达率分别为(91.40±2.32)%和(1.70±0.24)%。分选后NK细胞中CD3-CD16+CD56+细胞的比例达90%以上。药物处理前,ABCG2highCNE2/DDP和ABCG2lowCNE2/DDP细胞MICA、MICB、ULBP1、ULBP2和ULBP3呈弱表达;经不同分子靶向药物处理后,5种NKG2DLs的表达率均明显上升(P<0.01),以舒尼替尼处理后NKG2DLs的表达率升高最明显。随着NKG2DLs表达的上调,ABCG2highCNE2/DDP和ABCG2lowCNE2/DDP细胞对NK细胞杀伤的敏感性也随之升高。结论:不同分子靶向药物可诱导耐药鼻咽癌CNE2/DDP细胞NKG2DLs的表达,以舒尼替尼的诱导作用最强,且肿瘤细胞NKG2DLs的表达与其对NK细胞杀伤敏感性之间存在线性关系。
文摘Objective: This work aimed to study the inhibitory effect and the related mechanism of metformin (MET) on the proliferation of human hepatoma HepG2 cells. Methods: Human hepatoma HepG2 cells were treated with MET (0, 2, 10, and 50 mM). The inhibitory effect of MET on the proliferation of HepG2 cells was determined by MTT method. The apoptosis of HepG2 cells was detected by flow cytornetry. The expression of cyclin D1 in HepG2 cells was examined by Western blot. ROS-DHE fluorescence probe was used to stain the reactive oxygen species (ROS) generated by HepG2 cells after treat- ment. Results: MET could inhibit the proliferation of HepG2 cells in a dose and time dependent manner. MET promoted the apoptosis of HepG2 cells. In addition, MET suppressed the expression of cell cycle protein cyclin D1 and induced the produc- tion of ROS in HepG2 cells. Conclusion: MET can inhibit the proliferation of human hepatoma HepG2 cells and induce cell apoptosis. Meanwhile, MET has the ability to decrease the expression of cyclin D1 and induce ROS generation, which may be involved in the mechanism of inhibiting hepatoma cells proliferation.