Based on the structure-activity relationships and antiangiogenic mechanism of RGD-containing peptides, a series of 5-amino- 1,3-dihydro-1,3-dioxo-2H-isoindole derivatives were synthesized. The structures were characte...Based on the structure-activity relationships and antiangiogenic mechanism of RGD-containing peptides, a series of 5-amino- 1,3-dihydro-1,3-dioxo-2H-isoindole derivatives were synthesized. The structures were characterized by ^1H NMR, MS and elementary analysis. There ability to inhibit angiogenesis were evaluated by chick embryo chorioallantoic membrane assay at 10^-5 mol/L. Compounds 7a and 7b displayed obvious antiangiogenic activity.展开更多
A coordination polymer [Mn2（ctpt）2（aic）2]n （1, ctpt = 2-（4-chloro-phenyl）-1H- 1,3,7,8-tetraaza-cyclopenta[l]phenanthrene, H2aic = 5-amino-isophthalic acid） was hydrother- mally designed and synthesized. The co...A coordination polymer [Mn2（ctpt）2（aic）2]n （1, ctpt = 2-（4-chloro-phenyl）-1H- 1,3,7,8-tetraaza-cyclopenta[l]phenanthrene, H2aic = 5-amino-isophthalic acid） was hydrother- mally designed and synthesized. The complex was characterized by elemental analysis, IR spectro- scopy, single-crystal X-ray diffraction, and thermogravimetric analysis （TGA）. Each Mn（II） atom is linked by the aic ligands with neighbor Mn（II） atoms, forming an infinite one-dimensional （1D） double-chain structure. Complex 1 crystallizes in monoclinic, space group C2/c, with a = 18.23（1）, b = 17.27（1）, c = 16.69（1） ？, V = 4814.0（7） ？3, C27H16ClMnN5O4, Mr = 564.84, Dc = 1.559 g/cm3, μ（MoKα） = 0.706 mm-1, F（000） = 2296, Z = 8, the final R = 0.0487 and wR = 0.1269 （I 〉 2σ（I））. The 1D chain structure of complex 1 is stable below 458 ℃. In addition, to elucidate the essential electronic characters of this complex, theoretical calculation analysis of 1 was performed by the PBE0/LANL2DZ method in Gaussian 03 Program.展开更多
Ten new rare earth solid complexes were synthesized by the reaction of sodium 5-aminosalicyliate with rare earth chloride. The structure character, physical and chemical properties of these complexes were studied by I...Ten new rare earth solid complexes were synthesized by the reaction of sodium 5-aminosalicyliate with rare earth chloride. The structure character, physical and chemical properties of these complexes were studied by IR, UV, ()~1H NMR spectra, TG-DTA, fluorescence, elemental analyses, molar conductance and magnetic susceptibility. The ten rare earth complexes exist in dimeric form probably and the coordination number is seven. The antibacterial activity of the ligand and six complexes was also tested against Staphylococcus aureus, Escherichia coli and Bacillus subtilis, and the effect of Yb complex at 20 mg·ml^(-1) against Staphylococcus aureus is most significant.展开更多
Objective To study the adsorption of 5-Amino-2-chlorotoluene-4-sulfonic (CLT) and chlorhydric (HCl) acids from wastewater by weakly basic resin. Methods The kinetics and isotherm were studied. Thermodynamic parameters...Objective To study the adsorption of 5-Amino-2-chlorotoluene-4-sulfonic (CLT) and chlorhydric (HCl) acids from wastewater by weakly basic resin. Methods The kinetics and isotherm were studied. Thermodynamic parameters for the adsorption of acids were calculated and discussed. Results The adsorption of CLT and HCl acids followed Langmuir isotherm and the first-order kinetics model. Conclusion The adsorptive affinity of the two acids on D301R is in the order of CLT acid 〉 HCl acid. CLT and HCl acids can be separated.展开更多
Based on a systemic analysis for the globa1 burden of disease study from 1990 to 2016,the Global Burden of Diseases(GBD)2016 Alcohol Collaborators reported that alcohol use was a 1eading nisk factor for globa1 disease...Based on a systemic analysis for the globa1 burden of disease study from 1990 to 2016,the Global Burden of Diseases(GBD)2016 Alcohol Collaborators reported that alcohol use was a 1eading nisk factor for globa1 disease burden and caused substantial health loss.However,alcoholic dnink(wines and sakes)contains abundant nutrients,particularly fermentable amino acids denived from grapes and rice.Amino acid nutrition and metabolism is strongly associated with health and preventiom against various diseases.The purpose of this study was to elucidate 40 kinds of free amino acid(FAA)profles in wines and sakes.In addition,the present study also provided the contents of 5-aminolevulinic acid(5-AI A)involved in the vital functionality of mitochondria.FAAs were detected and analyzed by use of an automatic amino acid analyzer.Aromatic amino acid,branched chain amino acid and Fischer ratio were calculated for each beverage.Individua1 FAAs showed significant differences between wines and sakes.Sakes abundantly contained almost all FAAs whereas wines had just a lttle content in some FAAs.Sakse were rich in arginine,glycine,alanine,valine,glutamic acid and leucine,while wines were remarkably nich in proline(Pro).Wines showed increased FAA levels in 6 kinds of variables(4-hydroxyproline,3-methy1 histidine,B-alanine,a-aminobutyric acid,Pro and a.-aminoadipic acid).In functionally characteristic FAAs,both wines and sakes were considerably abundant in y aminobutynic acid and 5-AI A The total amount of aromatic amino acid and branched chain amino acid were markedly higher in sakes than in wines.These results revealed that there were the apparent different characteristics in FAA profiles between wines and sakes.This difference resulted from fermentation process in wines(single fermentation)and sakes(paralle1 double fermentation).Forty kinds of FAA profiles are more usefu1 in investigating characteristics of the taste of wines and sakes.In future,detailed FAA analysis has the potential to find functional nutrients such as 5-AI A,whereas other foods generally contain ittle amount of these FAAs.展开更多
Background Complete tumour resection is important for improving the prognosis of brain tumour patients. However, extensive resection remains controversial because the tumour margin is difficult to be distinguished fro...Background Complete tumour resection is important for improving the prognosis of brain tumour patients. However, extensive resection remains controversial because the tumour margin is difficult to be distinguished from surrounding brain tissue. It has been established that 5-amino-4-0xopentanoic acid （5-aminolevulinic acid, ALA） can be used as a photodynamic diagnostic marker and a photosensitizer for photodynamic therapy in surgical treatment of brain tumours. We investigated the efficacy of ALA photodynamically guided microsurgery and photodynamic therapy on VX2 brain tumour implanted in a rabbit model. Methods Eighty New Zealand rabbits implanted with VX2 brain tumours were randomly assigned to five groups： control, conventional white light microsurgery, a photodynamic therapy group, a photodynamically guided microsurgery group and a group in which guided microsurgery was followed by photodynamic therapy. The VX2 tumour was resected under a surgical microscope. The tumour resection was confirmed with histological analysis. All animals were examined with MRI for presence of any residual tumour tissue. The survival time of each rabbit was recorded. Results All treatment groups showed a significantly extended survival time compared with the control group. Photodynamically guided microsurgery combined with photodynamic therapy significantly prolonged survival time, compared with guided microsurgery alone. MRI and the autopsy results confirmed removal of most of the tumours. Conclusions Our results suggest that photodynamically guided surgery and photodynamic therapy significantly reduce or delay local recurrence, increase the effectiveness of radical resection and prolong the survival time of tumour bearing rabbits. Their combination has the potential to be used as a rapid and highly effective treatment of metastatic brain tumours.展开更多
The utilization of poly （2-hydroxyethylmetha- crylate） grafted agar （Ag-g-P（HEMA）） as a matrix for the controlled release of 5-aminosalicylic acid was investi- gated. Grafted copolymers of 2-hydroxyethylmethacry...The utilization of poly （2-hydroxyethylmetha- crylate） grafted agar （Ag-g-P（HEMA）） as a matrix for the controlled release of 5-aminosalicylic acid was investi- gated. Grafted copolymers of 2-hydroxyethylmethacrylate （HEMA） monomers on agar were synthesized by micro- wave assisted method. In vitro drug release studies were performed at pH values of 2 and 7 in order to investigate the possibility of pH triggered release for colon targeted drug delivery. Further, the percent grafting vs. tso （the time taken for release of 50% of the enclosed drug） value was studied and the results indicate that it may be possible to develop a programmable drug release matrix based on grafted polysaccharide. Ag-g-P（HEMA） appears to be a useful matrix for controlled release.展开更多
5-Amino-3-methylthio-1H-pyrazoles are very important building blocks from which a wide variety of pyrazole de-rivatives can be prepared. When substituted 5-amino-3-methylthio-1H-pyrazole was treated with CH3I, the met...5-Amino-3-methylthio-1H-pyrazoles are very important building blocks from which a wide variety of pyrazole de-rivatives can be prepared. When substituted 5-amino-3-methylthio-1H-pyrazole was treated with CH3I, the methy-lation occurres at endocyclic two nitrogens at the same time. The ratio of isomers in products was depended upon the nature of 4-position substituent in the pyrazole ring. The products were characterized by X-ray diffraction analysis, and the ratios of isomer were explained by means of the results of ab inito calculation.展开更多
A newly synthesized reagent 2-amino-5-mercapto-[1, 3, 4]triazole (MATZ) has been usedto fabricate self-assembled monolayers (SAMs) on gold electrode for the first time. The SAMselectrode was characterized by electroch...A newly synthesized reagent 2-amino-5-mercapto-[1, 3, 4]triazole (MATZ) has been usedto fabricate self-assembled monolayers (SAMs) on gold electrode for the first time. The SAMselectrode was characterized by electrochemical methods and scanning electronic microscopy (SEM),the SAMs electrode can be used to determinate dopamine (DA) and uric acid (UA) simultaneouslywith a detection limit of 8×10-7 mol/L for DA and 1×10-6 mol/L for UA respectively. The SAMscan also be used to detect the contents of DA and UA in synthetic urine sample with satisfactoryresults.展开更多
Seven optimized configurations and their electronic structures of 4-amino-5-nitro- 1,2,3-triazole dimers on their potential energy surface have been obtained by using density functional theory （DPT） method at the B3...Seven optimized configurations and their electronic structures of 4-amino-5-nitro- 1,2,3-triazole dimers on their potential energy surface have been obtained by using density functional theory （DPT） method at the B3LYP/6-311＋＋G＊＊ level. The maximum intermolecular interaction energy is -35.42 kJ/mol via the basis set superposition error-correction （BSSE） and zero point energy-correction （ZPE）. Charge transfers between the two subsystems are small. The vibration analysis of optimized configurations was performed, and the thermodynamic property changes from monomer to dimer have been obtained with the temperature ranging from 200 to 800 K on the basis of statistical thermodynamics. It is found that the hydrogen bonds contribute to the dimers dominantly, and the extent of intermolecular interaction is mainly determined by the hydrogen bonds＇ strength rather than their number. The dimerization processes of Ⅳ, Ⅴand Ⅵ can occur spontaneously at 200 K.展开更多
文摘Based on the structure-activity relationships and antiangiogenic mechanism of RGD-containing peptides, a series of 5-amino- 1,3-dihydro-1,3-dioxo-2H-isoindole derivatives were synthesized. The structures were characterized by ^1H NMR, MS and elementary analysis. There ability to inhibit angiogenesis were evaluated by chick embryo chorioallantoic membrane assay at 10^-5 mol/L. Compounds 7a and 7b displayed obvious antiangiogenic activity.
基金supported by the National Natural Science Foundation of China(No.21406085)
文摘A coordination polymer [Mn2（ctpt）2（aic）2]n （1, ctpt = 2-（4-chloro-phenyl）-1H- 1,3,7,8-tetraaza-cyclopenta[l]phenanthrene, H2aic = 5-amino-isophthalic acid） was hydrother- mally designed and synthesized. The complex was characterized by elemental analysis, IR spectro- scopy, single-crystal X-ray diffraction, and thermogravimetric analysis （TGA）. Each Mn（II） atom is linked by the aic ligands with neighbor Mn（II） atoms, forming an infinite one-dimensional （1D） double-chain structure. Complex 1 crystallizes in monoclinic, space group C2/c, with a = 18.23（1）, b = 17.27（1）, c = 16.69（1） ？, V = 4814.0（7） ？3, C27H16ClMnN5O4, Mr = 564.84, Dc = 1.559 g/cm3, μ（MoKα） = 0.706 mm-1, F（000） = 2296, Z = 8, the final R = 0.0487 and wR = 0.1269 （I 〉 2σ（I））. The 1D chain structure of complex 1 is stable below 458 ℃. In addition, to elucidate the essential electronic characters of this complex, theoretical calculation analysis of 1 was performed by the PBE0/LANL2DZ method in Gaussian 03 Program.
文摘Ten new rare earth solid complexes were synthesized by the reaction of sodium 5-aminosalicyliate with rare earth chloride. The structure character, physical and chemical properties of these complexes were studied by IR, UV, ()~1H NMR spectra, TG-DTA, fluorescence, elemental analyses, molar conductance and magnetic susceptibility. The ten rare earth complexes exist in dimeric form probably and the coordination number is seven. The antibacterial activity of the ligand and six complexes was also tested against Staphylococcus aureus, Escherichia coli and Bacillus subtilis, and the effect of Yb complex at 20 mg·ml^(-1) against Staphylococcus aureus is most significant.
基金The study was supported by the Nature Science Foundation of Jilin Province (No. 990337).
文摘Objective To study the adsorption of 5-Amino-2-chlorotoluene-4-sulfonic (CLT) and chlorhydric (HCl) acids from wastewater by weakly basic resin. Methods The kinetics and isotherm were studied. Thermodynamic parameters for the adsorption of acids were calculated and discussed. Results The adsorption of CLT and HCl acids followed Langmuir isotherm and the first-order kinetics model. Conclusion The adsorptive affinity of the two acids on D301R is in the order of CLT acid 〉 HCl acid. CLT and HCl acids can be separated.
文摘Based on a systemic analysis for the globa1 burden of disease study from 1990 to 2016,the Global Burden of Diseases(GBD)2016 Alcohol Collaborators reported that alcohol use was a 1eading nisk factor for globa1 disease burden and caused substantial health loss.However,alcoholic dnink(wines and sakes)contains abundant nutrients,particularly fermentable amino acids denived from grapes and rice.Amino acid nutrition and metabolism is strongly associated with health and preventiom against various diseases.The purpose of this study was to elucidate 40 kinds of free amino acid(FAA)profles in wines and sakes.In addition,the present study also provided the contents of 5-aminolevulinic acid(5-AI A)involved in the vital functionality of mitochondria.FAAs were detected and analyzed by use of an automatic amino acid analyzer.Aromatic amino acid,branched chain amino acid and Fischer ratio were calculated for each beverage.Individua1 FAAs showed significant differences between wines and sakes.Sakes abundantly contained almost all FAAs whereas wines had just a lttle content in some FAAs.Sakse were rich in arginine,glycine,alanine,valine,glutamic acid and leucine,while wines were remarkably nich in proline(Pro).Wines showed increased FAA levels in 6 kinds of variables(4-hydroxyproline,3-methy1 histidine,B-alanine,a-aminobutyric acid,Pro and a.-aminoadipic acid).In functionally characteristic FAAs,both wines and sakes were considerably abundant in y aminobutynic acid and 5-AI A The total amount of aromatic amino acid and branched chain amino acid were markedly higher in sakes than in wines.These results revealed that there were the apparent different characteristics in FAA profiles between wines and sakes.This difference resulted from fermentation process in wines(single fermentation)and sakes(paralle1 double fermentation).Forty kinds of FAA profiles are more usefu1 in investigating characteristics of the taste of wines and sakes.In future,detailed FAA analysis has the potential to find functional nutrients such as 5-AI A,whereas other foods generally contain ittle amount of these FAAs.
文摘Background Complete tumour resection is important for improving the prognosis of brain tumour patients. However, extensive resection remains controversial because the tumour margin is difficult to be distinguished from surrounding brain tissue. It has been established that 5-amino-4-0xopentanoic acid （5-aminolevulinic acid, ALA） can be used as a photodynamic diagnostic marker and a photosensitizer for photodynamic therapy in surgical treatment of brain tumours. We investigated the efficacy of ALA photodynamically guided microsurgery and photodynamic therapy on VX2 brain tumour implanted in a rabbit model. Methods Eighty New Zealand rabbits implanted with VX2 brain tumours were randomly assigned to five groups： control, conventional white light microsurgery, a photodynamic therapy group, a photodynamically guided microsurgery group and a group in which guided microsurgery was followed by photodynamic therapy. The VX2 tumour was resected under a surgical microscope. The tumour resection was confirmed with histological analysis. All animals were examined with MRI for presence of any residual tumour tissue. The survival time of each rabbit was recorded. Results All treatment groups showed a significantly extended survival time compared with the control group. Photodynamically guided microsurgery combined with photodynamic therapy significantly prolonged survival time, compared with guided microsurgery alone. MRI and the autopsy results confirmed removal of most of the tumours. Conclusions Our results suggest that photodynamically guided surgery and photodynamic therapy significantly reduce or delay local recurrence, increase the effectiveness of radical resection and prolong the survival time of tumour bearing rabbits. Their combination has the potential to be used as a rapid and highly effective treatment of metastatic brain tumours.
文摘The utilization of poly （2-hydroxyethylmetha- crylate） grafted agar （Ag-g-P（HEMA）） as a matrix for the controlled release of 5-aminosalicylic acid was investi- gated. Grafted copolymers of 2-hydroxyethylmethacrylate （HEMA） monomers on agar were synthesized by micro- wave assisted method. In vitro drug release studies were performed at pH values of 2 and 7 in order to investigate the possibility of pH triggered release for colon targeted drug delivery. Further, the percent grafting vs. tso （the time taken for release of 50% of the enclosed drug） value was studied and the results indicate that it may be possible to develop a programmable drug release matrix based on grafted polysaccharide. Ag-g-P（HEMA） appears to be a useful matrix for controlled release.
基金Project supported by the National Natural Science Foundation of China (No. 20172031) and the Research Fund for the Doctoral Program of Higher Education China.
文摘5-Amino-3-methylthio-1H-pyrazoles are very important building blocks from which a wide variety of pyrazole de-rivatives can be prepared. When substituted 5-amino-3-methylthio-1H-pyrazole was treated with CH3I, the methy-lation occurres at endocyclic two nitrogens at the same time. The ratio of isomers in products was depended upon the nature of 4-position substituent in the pyrazole ring. The products were characterized by X-ray diffraction analysis, and the ratios of isomer were explained by means of the results of ab inito calculation.
文摘A newly synthesized reagent 2-amino-5-mercapto-[1, 3, 4]triazole (MATZ) has been usedto fabricate self-assembled monolayers (SAMs) on gold electrode for the first time. The SAMselectrode was characterized by electrochemical methods and scanning electronic microscopy (SEM),the SAMs electrode can be used to determinate dopamine (DA) and uric acid (UA) simultaneouslywith a detection limit of 8×10-7 mol/L for DA and 1×10-6 mol/L for UA respectively. The SAMscan also be used to detect the contents of DA and UA in synthetic urine sample with satisfactoryresults.
基金Project of National Natural Science Foundation of China (No. 10576030, 20173028)
文摘Seven optimized configurations and their electronic structures of 4-amino-5-nitro- 1,2,3-triazole dimers on their potential energy surface have been obtained by using density functional theory （DPT） method at the B3LYP/6-311＋＋G＊＊ level. The maximum intermolecular interaction energy is -35.42 kJ/mol via the basis set superposition error-correction （BSSE） and zero point energy-correction （ZPE）. Charge transfers between the two subsystems are small. The vibration analysis of optimized configurations was performed, and the thermodynamic property changes from monomer to dimer have been obtained with the temperature ranging from 200 to 800 K on the basis of statistical thermodynamics. It is found that the hydrogen bonds contribute to the dimers dominantly, and the extent of intermolecular interaction is mainly determined by the hydrogen bonds＇ strength rather than their number. The dimerization processes of Ⅳ, Ⅴand Ⅵ can occur spontaneously at 200 K.
