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供应链金融对中小企业R&D投资效率的影响:基于融资约束视角
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作者 胡海青 原敏倩 薛萌 《科技进步与对策》 北大核心 2025年第1期102-112,共11页
创新是中小企业保持竞争力、适应市场变化和实现可持续发展的关键。基于2016-2022年创业板中小企业相关数据,运用三阶段DEA分析、面板Tobit模型回归、二元Logistic回归等方法,探究供应链金融对中小企业R&D投资效率的影响。结果表明... 创新是中小企业保持竞争力、适应市场变化和实现可持续发展的关键。基于2016-2022年创业板中小企业相关数据,运用三阶段DEA分析、面板Tobit模型回归、二元Logistic回归等方法,探究供应链金融对中小企业R&D投资效率的影响。结果表明,供应链金融能够显著提高中小企业R&D投资效率,融资约束在二者间发挥遮掩效应。进一步分析发现,上述效应对供应链集中度较高的企业更为显著。结论可为发挥供应链金融筹资优势,促进供应链生态系统资源互补、信息共享的协同创新网络形成,进而支持中小企业创新活动提供理论支持。 展开更多
关键词 供应链金融 r&d投资效率 三阶段dEA 面板Tobit模型 遮掩效应
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Effects of Glycidamide on Activity and Progesterone Biosynthesis of Rat R2C Leydig Cells
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作者 许伟 孙建霞 +6 位作者 白顺 李名薇 文罗娜 刘洁生 李宏业 黄亚东 白卫滨 《Agricultural Science & Technology》 CAS 2015年第6期1187-1190,共4页
Objective] This study aimed to investigate the effects of glycidamide (GA) on growth and progesterone biosynthesis of rat R2C Leydig cel s cultured in vitro. [Method] The R2C Leydig cel s were treated with GA with c... Objective] This study aimed to investigate the effects of glycidamide (GA) on growth and progesterone biosynthesis of rat R2C Leydig cel s cultured in vitro. [Method] The R2C Leydig cel s were treated with GA with concentrations of 0.25, 0.5, 0.75, 1, 2, 4 and 6 mmol/L respectively for 48 h. The IC25, IC50 and IC75 values of GA were al detected by MTT assay. The Leydig cel s were treated with GA at concentrations of IC25, IC50 and IC75 respectively for 48 h, and then the morphology of Leydig cel s was observed. After the Leydig cel s were treated with GA for 4 h, the cel ular DNA damage was measured by the comet assay technique; and after the Leydig cel s were with treated with GA for 24 h, the progesterone biosynthesis amount was detected by radioimmunoassay (RIA). [Result] GA could inhibit the via-bility of R2C Leydig cel s, and its IC25, IC50 and IC75 were 0.635, 0.872 and 1.198 mmol/L, respectively. The GA at concentrations of IC25, IC50 and IC75 affected the growth and morphology of rat R2C Leydig cel s in varying degrees. The 4-h treat-ment of GA could significantly damage the DNA of R2C Leydig cel s, and the 24-h treatment of GA at concentrations of IC25, IC50 and IC75 al reduced the progesterone biosynthesis amount. [Conclusion] GA could inhibit the growth and progesterone biosynthesis of rat R2C Leydig cel s. 展开更多
关键词 GLYCIdAMIdE r2C Leydig cel s Cel activity dNA damage Proges-terone
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Synthesis,Bioactivity and Crystal Structure Analysis of Novel Benzo[d]isothiazol-3(2H)-ones 被引量:7
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作者 王向辉 林强 +2 位作者 尹学琼 游诚航 杨建新 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2012年第8期1170-1174,共5页
Two compounds,3-oxo-N-o-tolylbenzo[d]isothiazole-2(3H)-carboxamide (1) and N-(2-methoxyphenyl)-3-oxobenzo[d]isothiazole-2(3H)-carboxamide (2),were synthesized from the initial compound benzo[d]isothiazol-3... Two compounds,3-oxo-N-o-tolylbenzo[d]isothiazole-2(3H)-carboxamide (1) and N-(2-methoxyphenyl)-3-oxobenzo[d]isothiazole-2(3H)-carboxamide (2),were synthesized from the initial compound benzo[d]isothiazol-3(2H)-one (BIT) and characterized by 1 H NMR,IR and elemental analysis,respectively.The single crystals of compounds 1 and 2 were obtained and determined by X-ray diffraction analysis.The preliminary results of biological activity experiment show that some of the title compounds exhibited a favorable antimicrobial activity. 展开更多
关键词 benzo[d]isothiazol-3(2H)-one (BIT) crystal structure antimicrobial activity
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Measurable surface d charge of Pd as a descriptor for the selective hydrogenation activity of quinoline 被引量:3
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作者 Shunlin Li Lili Wang +3 位作者 Mengmeng Wu Yafei Sun Xiaojuan Zhu Ying Wan 《Chinese Journal of Catalysis》 SCIE EI CAS CSCD 北大核心 2020年第9期1337-1347,共11页
Au Pd nanoalloys with tunable Pd concentrations have been synthesized and used as model catalysts. They have been directly imaged by high-angle annular dark-field scanning transmission electron microscopy and investig... Au Pd nanoalloys with tunable Pd concentrations have been synthesized and used as model catalysts. They have been directly imaged by high-angle annular dark-field scanning transmission electron microscopy and investigated by thorough analyses of their extended X-ray absorption fine structure, X-ray absorption near-edge structure, X-ray diffraction and X-ray photoelectron spectroscopy measurements. The bimetallic nanoparticles are embedded in a carbonaceous matrix and have almost an identical structure at the atomic level and the same electronic properties as Au Pd bulk alloys with the same compositions. The d-electron increase at surface Pd sites is determined by the Pd concentration of the alloy. Similarly, their activation entropy and catalytic activity for the hydrogenation of quinoline is related to the Pd concentration, with Au50 Pd50 the most active of the alloys investigated. An almost 11 times higher activity was achieved compared to a pure Pd catalyst. The experimentally measurable surface d charge at the Pd sites in the Au Pd was found to linearly correlate with the activation entropy and catalytic activity for the hydrogenation of quinoline. The alloy structure is stable, showing negligible metal segregation, dissolution-redeposition and aggregation during the hydrogenation process which involves strong adsorption. 展开更多
关键词 Surface d charge Au Pd alloy activation entropy QUINOLINE HYdrOGENATION
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Crystal Structure and Antiproliferative Activity of Ethyl 3,9-Dihydroxy-9-methyl-7-phenyl-7,8,10-trihydro-6Hdibenzo[b,d]pyran-6-one-8-carboxylate 被引量:1
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作者 CHEN Chao-Yue HE Qin-Ting +1 位作者 SUN Da-Dong HU Jin-Song 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2016年第2期199-204,共6页
Ethyl 3,9-dihydroxy-9-methyl-7-phenyl-7,8,10-trihydro-6H-dibenzo[b,d]pyran-6-one-8-carboxylate(C(23)H(22)O6,Mr = 394.42) has been synthesized and its structure was determined by ~1H and ^(13)C NMR,ESI-MS,eleme... Ethyl 3,9-dihydroxy-9-methyl-7-phenyl-7,8,10-trihydro-6H-dibenzo[b,d]pyran-6-one-8-carboxylate(C(23)H(22)O6,Mr = 394.42) has been synthesized and its structure was determined by ~1H and ^(13)C NMR,ESI-MS,elemental analysis,and X-ray single-crystal diffraction.The crystal belongs to the triclinic system,space group P1,with a = 8.8220(17),b = 9.881(2),c = 12.157(2) A,α= 90.488(3),β= 102.664(4),γ= 98.799(3)°,V= 1020.8(3) A^3,Z= 2,Dc = 1.342 g/cm^3,μ= 0.099mm^(-1),F(000) = 436,R = 0.0615 and wR = 0.2501 for 2592 observed reflections with(I2σ(I)).In the crystal structure,the coumarin ring system is planar and the 3:4 fused cyclohexane ring adopts distorted half-chair conformation.Rich hydrogen bonding interactions are formed between compound 2 and lattice water molecules.These interactions assemble molecules of 2 into 2D layered networks in an AB stacking sequence.Its in vitro antiproliferative activities against three human cancer cell lines were evaluated by MTT assay. 展开更多
关键词 COUMArIN 6H-dibenzo[b d]pyran-6-one crystal structure antiproliferative activity
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The Hydroxylation of Vitamin D on C25 in Thyrotoxicosis The Role of the Activity of Microsomal Liver Enzymes 被引量:1
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作者 Chris G. Velentzas 《International Journal of Clinical Medicine》 2012年第4期295-299,共5页
Vitamin D3 after its entrance in the organism undergoes hydroxylation on C-25 carbon atom by the action of microsomal liver enzymes giving the metabolite 25 hydroxyvitamin D3 (25OHD3). The function of microsomal liver... Vitamin D3 after its entrance in the organism undergoes hydroxylation on C-25 carbon atom by the action of microsomal liver enzymes giving the metabolite 25 hydroxyvitamin D3 (25OHD3). The function of microsomal liver enzymes is influenced in some specified states by hormones or drugs. It has approved that thyroxin is a potent stimulator of these enzymes while allopurinol suppresses their function. The aim of this issue is to examine 25OHD3 plasma levels in thyrotoxic subjects and in those pretreated with allopurinol on the base of the afford mentioned data. In a first phase 25OHD3 plasma levels were estimated in thyrotoxic subjects against euthytoid healthy controls. In a second phase lmg vitamin D3 was injected intravenously (i.v.) in thyrotoxic subjects and in healthy euthyroid controls. 25OHD3 plasma levels were measured before and in post injection period in six hours intervals for 48 hours. In a third phase a couple of subjects one thyrotoxic and one euthyroid healthy control pretreated both with allopurinol injected lmg of vitamin D3 i.v. In all studied subjects 25OHD3 plasma levels were measured before and in post injection period in six hours intervals for 48 hours. The pre and post injection 25OHD3 plasma levels measured the size of activity of liver enzyme responsible for bioactivation of vitamin D3. In the first phase was indicated that 25OHD3 plasma levels were lower in thyrotoxic subjects comparing with that of euthyroid healthy controls (p 3 in thyrotoxic subjects was 2,5 to 8 times faster comparing with euthyroid healthy controls. In the third phase was shown that allopurinol decreases the activity of liver enzymes function as regard the bioactivation of vitamin D3. The bioactivation of vitamin D3 is accelerated in thyrotoxicosis compared with that in euthyroid state. This phenomenon produces low 25OHD3 plasma levels in thyrotoxic subjects which initially may be normal or slightly increased depended from the vitamin D3 status in the thyrotoxic subjects. By continuous stimulatory action of increased thyroid hormones on liver enzymes the 25OHD3 plasma levels earlier or later decline in levels of hypo-or avitaminosis D3. The previously described biological events may explain the decreased intestinal calcium absorption of vitamin D3 and the osteomalacic component found in a percentage of thyrotoxic bone histology. For the blocking effects of allopurinol on liver enzymes function and possibly of other pharmaceutical products in relation to vitamin D3 bioactivation, available data are still lacking. 展开更多
关键词 25-Hydroxyvitamin d THYrOXIN ALLOPUrINOL Microsomal Liver Enzyme’S activity
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Colonic vitamin D receptor expression is inversely associated with disease activity and jumonji domain-containing 3 in active ulcerative colitis 被引量:1
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作者 Hong-Qian Wang Wen-Hui Zhang +6 位作者 Ya-Qi Wang Xiao-Pan Geng Ming-Wei Wang Yuan-Yuan Fan Jing Guan Ji-Long Shen Xi Chen 《World Journal of Gastroenterology》 SCIE CAS 2020年第46期7352-7366,共15页
BACKGROUND The expression of jumonji domain-containing 3(Jmjd3)and trimethylated H3 lysine 27(H3K27me3)in active ulcerative colitis(UC)and the correlation between vitamin D receptor(VDR)and the Jmjd3 pathway are unkno... BACKGROUND The expression of jumonji domain-containing 3(Jmjd3)and trimethylated H3 lysine 27(H3K27me3)in active ulcerative colitis(UC)and the correlation between vitamin D receptor(VDR)and the Jmjd3 pathway are unknown.AIM To study the relationship between VDR,Jmjd3 and H3K27me3 in patients with active UC.METHODS One hundred patients with active UC and 56 healthy controls were enrolled in this study.The patients with active UC were divided into groups according to mild(n=29),moderate(n=32)and severe(n=29)disease activity based on the modified Mayo score.Vitamin D levels were measured by radioimmunoassay.Colonic mucosal tissues from UC patients and controls were collected by colonoscopy.The expression of VDR,Jmjd3 and H3K27me3 in the intestinal mucosa was determined by immunohistochemistry staining.RESULTS Patients with active UC had lower levels of serum vitamin D(13.7±2.8 ng/mL,P<0.001)than the controls(16.2±2.5 ng/mL).In the UC cohort,serum vitamin D level was negatively correlated with disease activity(r=-0.323,P=0.001).VDR expression in the mucosa of UC patients was reduced compared to that in normal tissues(P<0.001)and negatively correlated with disease activity(r=-0.868,P<0.001).Similar results for VDR expression were noted in the most serious lesion(defined as UC diseased)and 20 cm proximal to the anus(defined as UC normal)(P<0.05).Simultaneously,Jmjd3 expression significantly increased in UC patients(P<0.001),but no difference was found between the different sites in UC patients.H3K27me3 expression in UC patients was significantly down-regulated when compared with normal tissues(P<0.001),but up-regulated in the mild disease activity group in comparison with the moderate disease activity group of UC patients(P<0.05).Jmjd3 Level was negatively correlated with the level of VDR(r=-0.342,P=0.002)and H3K27me3(r=-0.341,P=0.002),while VDR level was positively correlated with H3K27me3(r=0.473,P<0.001).CONCLUSION Serum vitamin D and VDR were inversely correlated with disease activity in active UC.Jmjd3 expression increased in the colonic mucosa of active UC patients and was negatively associated with VDR and H3K27me3 level. 展开更多
关键词 Vitamin d Ulcerative colitis disease activity Vitamin d receptor Jumonji domain-containing 3 Trimethylated H3 lysine 27
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Synthesis, Crystal Structure, and Biological Activity of 4-Chlorobenzaldehyde (2-trifluoromethylTrifluoromethyl-5,6,7,8-tetrahydrobenzo[4 ,5]-thieno[2,3-d]pyrimidin-4-yl)hydrazone Monohydrate 被引量:3
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作者 杨平 王艳 +4 位作者 段正超 邵 宇 聂光华 宋新建 田大听 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2013年第7期1023-1030,共8页
The novel title compound 4-chlorobenzaldehyde (2-trifluoromethyl-5,6,7,8- tetrahydro- benzo[4,5]thieno[2,3-d]pyrimidin-4-yl)hydrazone monohydrate (C18H14C1F3N4S.H20, Mr = 428.86) has been synthesized by a condensa... The novel title compound 4-chlorobenzaldehyde (2-trifluoromethyl-5,6,7,8- tetrahydro- benzo[4,5]thieno[2,3-d]pyrimidin-4-yl)hydrazone monohydrate (C18H14C1F3N4S.H20, Mr = 428.86) has been synthesized by a condensation reaction of 4-chlorobenzaldehyde with (2-trifuoromethyl-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-yl)hydrazine, and its crystal structure was determined by single-crystal X-ray diffraction. The crystal belongs to monoclinic, space group P21/c with a = 7.4252(7), b = 26.344(2), c = 10.3095(9) A, /3 = 109.407(2)~, V= 1902.0(3) A3, Z = 4, Dc = 1.498 g/cm^3, p = 0.356 mm-1, F(000) = 880, the final R = 0.0564 and wR = 0.1681 for 2343 observed reflections with I 〉 2o(/). X-ray diffraction analysis reveals that the title hydrazone molecule is nearly planar except for the cyclohexene and trifluoromethyl moieties. In the crystal packing, the molecules form stacks by a three-dimensional framework, which results from intermolecular N(3)-H(3)...O(1), O(1)-H(1B)...N(2), O(1)- H(1B)...N(4) and O(1)-H(1A)...F(1) hydrogen bonds via water molecules together with π-π stacking interactions. Molecular geometry of the title compound in the ground state optimized by B3LYP functional with 6-311G** basis sets indicates that the calculations are in agreement with the experimental data. The preliminary bioassay suggested that the title compound exhibits relatively good fungicidal activity against Fusarium oxysporium fsp.vasinfectum and Dothiorella gregaria. 展开更多
关键词 thieno[2 3-d]pyrimidine hydrazone TrIFLUOrOMETHYL dFT calculation biological activity
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Synthesis, Crystal Structure, and Antitumor Activity of 1-(4-Methoxybenzylidene)-2-(1-phenyl-6-trifluoromethyl-1H-pyrazolo[3,4-d]pyrimidin-4-yl)hydrazine Monohydrate 被引量:2
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作者 杨平 高慧 宋新建 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2014年第8期1129-1134,共6页
The novel title compound 1-(4-methoxybenzylidene)-2-(1-phenyl-6-trifluoromethyl- 1H-pyrazolo[3,4-d]pyrimidin-4-yl)hydrazine monohydrate (C20HisF3N60-H20, Mr = 430.40) has been synthesized by a four-step procedur... The novel title compound 1-(4-methoxybenzylidene)-2-(1-phenyl-6-trifluoromethyl- 1H-pyrazolo[3,4-d]pyrimidin-4-yl)hydrazine monohydrate (C20HisF3N60-H20, Mr = 430.40) has been synthesized by a four-step procedure including the cyclization, chlorination, hydrazinolysis and condensation reaction, and its crystal structure was determined by single-crystal X-ray diffraction. The crystal belongs to orthorhombic, space groupPbca with a = 8.3779(13), b = 17.607(3), c = 26.774(4) A, V= 3949.2(11) A3, Z=8, Dc = 1.448 g/cm3, μ = 0.117 mm-l, F(000) = 1776, the final R = 0.0553 and wR = 0.1516 for 2354 observed reflections with 1 〉 2σ(/). X-ray diffraction analysis reveals that the title compound is almost coplanar except for the trifluoromethyl and phenyl moieties. In the crystal packing, the molecules are linked by intermolecular O(lW)-H(1WA)-"N(2), O(1W)-H(1WA).--N(4) and N(5)-H(5A)...O(lW) hydrogen bonds via water molecules and stacked through π-π stacking interactions. The preliminary bioassay suggested that the title compound exhibits relatively good antitumor activity against HepG2 and BCG-823. 展开更多
关键词 pyrazolo[3 4-d]pyrimidine hydrazone TrIFLUOrOMETHYL antitumor activity
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Synthesis, Structure and Biological Activity of 2-[2-(4-Fluorobenzylidene)hydrazinyl]-4-(1-methyl-1H-indol-3-yl)thieno[3,2-d]pyrimidine 被引量:3
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作者 SHI Jian-Tao GONG Yi-Lin +4 位作者 LI Jun WANG Yang CHEN Ye DING Shi LIU Ju 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2019年第9期1530-1536,共7页
The title compound 2-[2-(4-fluorobenzylidene)hydrazinyl]-4-(1-methyl-1 H-indol-3-yl)thieno[3,2-d] pyrimidine(8) was synthesized by the condensation of 4-fluorobenzaldehyde(7) with 2-hydrazinyl-4-(1-methyl-1 H-indol-3-... The title compound 2-[2-(4-fluorobenzylidene)hydrazinyl]-4-(1-methyl-1 H-indol-3-yl)thieno[3,2-d] pyrimidine(8) was synthesized by the condensation of 4-fluorobenzaldehyde(7) with 2-hydrazinyl-4-(1-methyl-1 H-indol-3-yl)thieno[3,2-d]pyrimidine(6). This intermediate was prepared from methyl 3-aminothiophene-2-carboxylate(1) by the condensation with urea, chlorination with phosphorus oxychloride and then condensation with hydrazine hydrate. The crystal of 8 belongs to monoclinic system, space group P21/c with a = 14.0453(18), b = 17.436(2), c = 18.0982(17) ? and β = 122.969(7)°. In addition, 8 possesses marked inhibition against the proliferation of human colon cancer cell line HT-29(IC50 = 6.09 μM) and human gastric cancer cell line MKN45(IC50 = 3.04 μM), displaying promising anticancer activity. 展开更多
关键词 thieno[3 2-d] PYrIMIdINE SYNTHESIS X-ray dIFFrACTION ANTITUMOr activity
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Effects of nitrogen ion irradiation on endoglucanase activity and gene mutation of Bacillus subtilis Bac01 被引量:2
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作者 LU Jie MAO Peihong +2 位作者 JIN Xiang YU Long YING Hanjie 《Nuclear Science and Techniques》 SCIE CAS CSCD 2009年第5期271-276,共6页
Bacillus subtilis Bac01 was mutated by 15 keV N+ ions of 1.5×1016 cm-2. The mutant strain Bac11 with high yield of endoglucanase was isolated using carboxymethylcellulose sodium and congo red indicative plates. I... Bacillus subtilis Bac01 was mutated by 15 keV N+ ions of 1.5×1016 cm-2. The mutant strain Bac11 with high yield of endoglucanase was isolated using carboxymethylcellulose sodium and congo red indicative plates. It exhibited higher endoglucanase activitiy (381.89IU) than the original strain Bac01 (93.33IU). Two 1,500 bp endoglucanase gene fragments were obtained with PCR amplification from B. subtilis Bac01 and mutant strain Bac11. BLAST comparison result indicated that 10 nucleotides mutated. Bioinformatics methods were used to analyze the two predicted amino acid sequences, and it was found that 5 amino acid residues changed, being all in the cellulose-binding domain of endoglucanase. 展开更多
关键词 放射性 能级 核技术 研究 氮离子
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Pharmarcogenetic Mechanism of ACE liD Polymorphism Adversely Responding to ACE Inhibitors in Regulating the ACE Promoter Activity in Neurons 被引量:1
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作者 Yuan-Han Yang Hsueh-Wei Chang +4 位作者 Wei-Chiao Chang Yu-Cheng Shih Ke-Li Tsai I Chien Shyh-Jong Wu 《Journal of Pharmacy and Pharmacology》 2016年第8期419-431,共13页
The ACE (angiotensin converting enzyme) inhibitors are not only drugs widely prescribed drugs in cardiovascular diseases, but also potentially therapeutic agents in dementia. Based on the findings that the ACE inhib... The ACE (angiotensin converting enzyme) inhibitors are not only drugs widely prescribed drugs in cardiovascular diseases, but also potentially therapeutic agents in dementia. Based on the findings that the ACE inhibitors could activate the c-Jun N-terminal kinase signal to increase the ACE gene expression and that the Alu element of the human ACE gene involved in regulating ACE promoter activity, we aimed to investigate whether there are different pharmacogenetic responses of ACE I/D polymorphism to the ACE inhibitors in neurons. The three reporter vectors, pACEpro(0-SEAP, p-I-ACEpro-SEAP, and p-D-ACEpro-SEAP were used to examine the transcriptional activity of the vectors responding to the lisinopril treatment using a transient-transfection method in SH-SY5Y cells. Our results showed that lisinopril increased the promoter activity of an ACE gene by 16.7%. Additionally, we found the lisinopril enhanced the ACE promoter activity of the I-form vector by 17.2%, but adversely reduced that of the D-form vector by 16.8%, as compared with the respective control without the lisinopril treatment. Firstly, our findings had proved that the UD polymorphism of ACE gene contrarily responds to the ACE inhibitors in regulating the ACE expression in neurons, which provide a novel insight suggesting genetic testing to tailor the treatment regimens in AD (Alzheimer's disease) patients. 展开更多
关键词 ACE inhibitors ACE I/d polymorphism Aizheimer's disease PHArMACOGENETICS promoter activity.
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Vitamin D<sub>3</sub>Receptor Activation Rescued Corticostriatal Neural Activity and Improved Motor Function in –D<sub>2</sub>R Tardive Dyskinesia Mice Model
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作者 Oluwamolakun O. Bankole Babafemi J. Laoye +7 位作者 Mujittapha U. Sirjao Azeez O. Ishola Damilola E. Oyeleke Wasiu G. Balogun Amin Abdulbasit Ansa E. Cobham Ibukun D. Akinrinade Olalekan M. Ogundele 《Journal of Biomedical Science and Engineering》 2015年第8期520-530,共11页
Haloperidol-induced dyskinesia has been linked to a reduction in dopamine activity characterized by the inhibition of dopamine receptive sites on D2-receptor (D2R). As a result of D2R inhibition, calcium-linked neural... Haloperidol-induced dyskinesia has been linked to a reduction in dopamine activity characterized by the inhibition of dopamine receptive sites on D2-receptor (D2R). As a result of D2R inhibition, calcium-linked neural activity is affected and seen as a decline in mo-tor-cognitive function after prolonged haloperidol use in the treatment of psychotic disorders. In this study, we have elucidated the relationship between haloperidol-induced tardive dyskinesia and the neural activity in motor cortex (M1), basal nucleus (CPu), prefrontal cortex (PFC) and hippocampus (CA1). Also, we explored the role of Vitamin D3 receptor (VD3R) activation as a therapeutic target in improving motor-cognitive functions in dyskinetic mice. Dyskinesia was induced in adult BALB/c mice after 28 days of haloperidol treatment (10 mg/Kg;intraperitoneal). We established the presence of abnormal involuntary movements (AIMs) in the haloperidol treated mice (-D2) through assessment of the threshold and amplitude of abnormal involuntary movements (AIMs) for the Limbs (Li) and Orolingual (Ol) area (Li and Ol AIMs). As a confirmatory test, the dyskinetic mice (-D2) showed high global AIMs score when compared with the VD3RA intervention group (-D2/+VDR) for Li and Ol AIMs. Furthermore, in the behavioral tests, the dyskinetic mice exhibited a decrease in latency of fall (LOF;Rotarod-P 2/+VDR), 100 mg/Kg for 7 days, CPu-CA1 burst activity was restored leading to a decrease in abnormal movement, and an increase in motor function. Ultimately, we deduced that VD3RA activation reduced the threshold of abnormal movement in haloperidol induced dyskinesia. 展开更多
关键词 HALOPErIdOL Vd3r dYSKINESIA d2r NEUrAL activity COrTICOSTrIATAL
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Synthesis,Characterization and Antibacterial Activity of 3-(2-(Heterocyclo-2-ylthio)-ethoxy)benzo[d]isothiazoles
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作者 冯文 谢灵杰 +3 位作者 宋煌旺 史载锋 王向辉 林强 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2017年第6期911-917,共7页
Seven novel 3-(2-(heterocyclo-2-ylthio)ethoxy)benzo[d]isothiazoles(3a^3g) have been synthesized and characterized by ESI-MS and 1H and 13 C NMR spectra. The crystal structures of 3a and 3g have been determined. ... Seven novel 3-(2-(heterocyclo-2-ylthio)ethoxy)benzo[d]isothiazoles(3a^3g) have been synthesized and characterized by ESI-MS and 1H and 13 C NMR spectra. The crystal structures of 3a and 3g have been determined. Compound 3a(C(11)H(11)N5O1S2) belongs to the monoclinic system and 3g(C(12)H(11)N3OS3) to the triclinic system. The title compounds show excellent in vitro antibacterial activities, with the minimum inhibitory concentrations varying from 4 to 32 ug/m L. 展开更多
关键词 3-(2-(heterocyclo-2-ylthio)ethoxy)benzo[d]isothiazoles SYNTHESIS crystal structure antibacterial activity
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Electron Donating Property and Catalytic Activity ofPerovskite-type Mixed Oxides (ABO_3) Consisting of Rare Earth and 3d Transition Metals
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作者 S.Sugunant and V.Meera(Dept. of Applied Chemistry, Cochin University of Science and Technology, Kochi-682022, India) 《Journal of Materials Science & Technology》 SCIE EI CAS CSCD 1995年第3期229-231,共3页
The catalytic activity of Perovskite-type mixed oxides (LaCoO3, PrCoO3 and SmCoO3) for the reduction of cyclohexanone to cyclohexanol with 2-propanol (Meerwein-PonndorfVerley reduction) has been studied. The data have... The catalytic activity of Perovskite-type mixed oxides (LaCoO3, PrCoO3 and SmCoO3) for the reduction of cyclohexanone to cyclohexanol with 2-propanol (Meerwein-PonndorfVerley reduction) has been studied. The data have been correlated with the surface electron donor properties of these mixed oxides 展开更多
关键词 activity type ABO3 Consisting of rare Earth and 3d Transition Metals Electron donating Property and Catalytic activity ofPerovskite-type Mixed Oxides
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Three-dimensional crustal velocity structure and activity characteristics of the Madoi Ms7.4 earthquake in 2021
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作者 Ma Yong Zhang Hai-Jiang +1 位作者 Gao Lei and Chen Zhi-Gang 《Applied Geophysics》 SCIE CSCD 2022年第4期590-602,605,共14页
In this paper,using natural earthquake P-wave arrival time data recorded by the seismic network in the surrounding area of Madoi,the three-dimensional fine P-wave crustal velocity structure at depths above 60 km in th... In this paper,using natural earthquake P-wave arrival time data recorded by the seismic network in the surrounding area of Madoi,the three-dimensional fine P-wave crustal velocity structure at depths above 60 km in the epicenter of the Madoi Ms7.4 earthquake was inverted using the double-difference seismic tomography method.On the basis of the relocation of the source of the aftershock sequence,we summarized the strip-shaped distribution characteristics along the strike of the Jiangcuo fault,revealing the significant heterogeneity of the crustal velocity structure in the source area.Research has found that most of the Madoi Ms7.4 aftershocks were located in the weak area of the high-speed anomaly in the upper crust.The focal depth changed with the velocity structure,showing obvious fluctuation and segmentation characteristics.There was a good correspondence between the spatial distribution and the velocity structure.The high-velocity bodies of the upper crust in the hypocenter area provided a medium environment for earthquake rupture,the low-velocity bodies of the middle crust formed the deep material,and the migration channel and the undulating shape of the high-speed body in the lower crust corroborated the strong pushing action in the region.The results confirmed that under the continuous promotion of tectonic stress in the Madoi area,the high-speed body of the Jiangcuo fault blocked the migration of weak materials in the middle crust.When the stress accumulation exceeded the limit,the Madoi Ms7.4 earthquake occurred.Meanwhile,the nonuniform velocity structure near the fault plane determined the location of the main shock and the spatiotemporal distribution of the aftershock sequence. 展开更多
关键词 Madoi Ms7.4 earthquake double-difference tomography 3d velocity structure seismic activity characteristics
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<i>Vitamin</i>D<sub>3</sub>Receptor Activation Rescued Corticostriatal Neural Activity and Improved Motor-Cognitive Function in -D<sub>2</sub>R Parkinsonian Mice Model
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作者 Azeez O. Ishola Babafemi J. Laoye +7 位作者 Damilola E. Oyeleke Oluwamolakun O. Bankole Mujittapha U. Sirjao Ansa E. Cobham Wasiu G. Balogun Amin Abdulbasit Ibukun D. Akinrinade Olalekan M. Ogundele 《Journal of Biomedical Science and Engineering》 2015年第9期601-615,共15页
Background: fourth generation antipsychotics have been implicated in the blockade of calcium signalling through inhibition of dopamine receptive sites on dopaminergic D2 Receptor (D3R). As a result of the abnormal cal... Background: fourth generation antipsychotics have been implicated in the blockade of calcium signalling through inhibition of dopamine receptive sites on dopaminergic D2 Receptor (D3R). As a result of the abnormal calcium signalling associated with D2R inhibition, changes occur in the motor and memory neural axis leading to the observed behavioural deficits after prolonged haloperidol. Thus, Vitamin D3 receptor (VD3R), a calcium controlling receptor in the striatum can be targeted to relief the neurological symptoms associated with haloperidol (-D2R) induced PD. Aim: This study sets to investigate the role of VD3R activation in vitro and in vivo after haloperidol-induced Dopaminergic (D2R) blockade. In addition, we examined the associated neural activity and behavioural changes in parkinsonian and VDRA intervention mice. Methods: Dopaminergic D2R inhibition was investigated in vitro using Melanocytes isolated from the scale of a Tilapia. In four separate set ups, the cells were cultured in calcium free Ringer’s solution as follows;300 μM haloperidol, 100 μM VD3, 100 mM calcium chloride and a combination of 300 μM haloperidol and 100 μM VD3. Subsequently, dopaminergic vesicle accumulation and calcium signalling were observed in bright field microscopy using blue and green fluorescence probes. In the second phase, PD was induced in adult BALB/c mice (-D2;n = 8) after 14 days of intraperitoneal haloperidol treatment (10 mg/Kg). A set of n = 4 mice were untreated (-D2) while the other group (n = 4) received 100 mg/Kg of VD3 for 7 days (-D2/+VDR). The control groups (n = 4 each) were treated with normal saline (NS) and VD3 (+VDR) for 14 days. At the end of the treatment phase, the animals were assessed in Rotarod, parallel bar-, cylinder-, Y-Maze-, one trial place recognition- and novel object recognition-(NOR) tests. Neural activity was measured using chronic electrode implants placed in the M1 (motor cortex), CPu (striatum), CA1 (hippocampus) and PFC (prefrontal cortex). Neural activity was compared with the outcomes of behavioural tests for memory and motor functions and data was expressed as mean ± SEM (analysed using ANOVA with Tukey post-hoc test, significant level was set at 0.05). Results/Discussion: in vitro outcomes show that VDR increase calcium signalling and reverses the effect of haloperidol;specifically by reducing dopaminergic vesicle accumulation in the cell body. Similarly, in vivo neural recordings suggest an increase in calcium hyperpolarization currents in the CPu and PFC of intervention mice (-D2/+VDR) when compared with the parkinsonian mice (-D2). These animals (-D2/+VDR) also recorded an improvement in spatial working memory and motor function versus the Parkinsonian mice (-D2). These outcomes suggest the role of CPu-PFC corticostriatal outputs in the motor-cognitive decline seen in parkinsonian mice. Similarly, VDRA reduced the neural deficits through restoration of calcium currents (burst activities) in the intervention mice (-D2/+VDR). Conclusion: VDRA treatment reduced the motor-cognitive defects observed in haloperidol induced PD. Our findings suggest the role of VDRA in restoration of calcium currents associated with PFC and CPu corticostriatal outputs seen as burst frequencies in in vivo neural recording. 展开更多
关键词 dOPAMINE Calcium Signalling d2r Vd3r COrTICOSTrIATAL Neural System
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Evaluation of Activity Patterns in Quinpirole-Treated Rats
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作者 Carlos L. Paíno 《Journal of Behavioral and Brain Science》 2014年第7期291-296,共6页
The present study aims to evaluate in rats the activity changes associated to treatments with D2-like receptor agonists using a simple behavioral procedure. Rats receiving a single dose of 1 mg/kg quinpirole or vehicl... The present study aims to evaluate in rats the activity changes associated to treatments with D2-like receptor agonists using a simple behavioral procedure. Rats receiving a single dose of 1 mg/kg quinpirole or vehicle were scored for 6 spontaneous behaviors at different post-injection times. In each time point, the animals were placed in testing cages for 12 min and video-recorded during the last 2 min. The number of forelimb steps and the time spent sniffing were significantly increased by 15 min post-injection in the quinpirole group. Forelimb steps remained increased for at least 24 h. Scores of time spent sniffing, as well as time inactive and number of hindlimb steps appeared greatly altered at 90 and 180 min, but not at later time points. By 48 h, no differences between control and quinpirole-treated rats were observed. In conclusion, the simple behavioral procedure here proposed—or adaptations of it—provides a sensitive test to evaluate the time course of the effects of D2-like receptor agonists on rat spontaneous activity. Additionally, this test takes into account context-dependent sensitization. It can be adapted to different treatment conditions. This methodology would be useful for the preclinical screening of D2-like receptor drugs, using reduced numbers of animals to test those doses and treatment schedules producing less side-effects. 展开更多
关键词 BEHAVIOrAL activity d2-Like receptor AGONIST SPONTANEOUS Behavior STEPPING SNIFFING
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Synthesis and Antitumor Activity of 3-[2-(4-Hydroxy-Phenyl)-Ethyl]-Benzo[d] Isoxazole-4,6-Diol
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作者 Li Wang 《International Journal of Organic Chemistry》 CAS 2023年第1期1-6,共6页
A new phloretin derivative 1 3-[2-(4-hydroxy-phenyl)-ethyl]-benzo[d] isoxazole-4,6-diol (yield 63%) was synthesized from phloretin by carbonyl nucleophilic addition condensation reaction. Its structure was characteriz... A new phloretin derivative 1 3-[2-(4-hydroxy-phenyl)-ethyl]-benzo[d] isoxazole-4,6-diol (yield 63%) was synthesized from phloretin by carbonyl nucleophilic addition condensation reaction. Its structure was characterized by 1H NMR, 13C NMR and HR-MS. The phloretin, compound 1, resveratrol and acetylated resveratrol were determined by comparing them with paclitaxel. Anti-tumor activity of alcohol on SPC-A1, EC109, A549, MCF-7 and MDA-MB-231 cell lines. Compound 1 showed better antitumor activity than docetaxel against A549 tumor cells. 展开更多
关键词 3-[2-(4-Hydroxy-Phenyl)-Ethyl]-Benzo[d] Isoxazole-4 6-diol SYNTHESIS Antitumor activity
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The Effect of Fabrication Conditions on the Morphology and Photocatalytic Activity of Bismutite Bi<sub>2</sub>O<sub>2</sub>CO<sub>3</sub>Particles
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作者 Hong Hu Changlong Xiao 《Open Journal of Physical Chemistry》 2017年第1期1-8,共8页
In this study, three-dimensional bismutite Bi2O2CO3 nanoparticels (BSC NPs) have been synthesized through a facile hydrothermal treatment under mild conditions. The reaction temperatures and NaOH concentration have a ... In this study, three-dimensional bismutite Bi2O2CO3 nanoparticels (BSC NPs) have been synthesized through a facile hydrothermal treatment under mild conditions. The reaction temperatures and NaOH concentration have a vital influence on the physical and photocatalytic properties of the obtained BSC NPs. The crystal structure, morphology, chemical composition, specific surface area and photoresponse of as-obtained catalysts were characterized by X-ray diffraction, Scanning electron microsprctrosopy, Energy-dispersive spectroscopy, N2 adsorption/desorption isotherms and UV-Vis spectra, respectively. Furthermore, Rhodamine 6G was used as model reaction to evaluate the photocatalytic activity of BSC NPs. As a result, there was no obvious effect of hydrothermal reaction temperature and NaOH concentration on phase structure and UV-visible light response;while the morphology, BET surface area and photoactivity were affected by hydrothermal reaction temperature and NaOH concentration. 展开更多
关键词 Bi2O2CO3 PArTICLES r6G degradation Photocatalytic activity HYdrOXYL radical
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