Aromatic aldehydes are the most fundamentally important compounds used in organic synthesis.The development of new synthetic methods for introduction of a formyl group into an organic scaffold is highly desirable.In t...Aromatic aldehydes are the most fundamentally important compounds used in organic synthesis.The development of new synthetic methods for introduction of a formyl group into an organic scaffold is highly desirable.In this report,a nickel-catalyzed reductive coupling between aryl halides andα–chloro N-methoxyphthalimide has been documented for the synthesis of a diverse array of aromatic aldehydes.Because of mild reductive coupling conditions,excellent functional group tolerance,especially for substrates containing free-OH and-NH_(2),was observed.Due to the simple operation mode,a large library of aromatic aldehydes can be quickly constructed by this process.Moreover,the present protocol is amenable for late-stage functionalization of bioactive compound.A combined computational and experimental investigation suggested the reaction may undergo a reaction mechanism of active Ni(I)catalyst formation and the formation of key formyl radical intermediate under zinc reductive conditions.展开更多
A series of novel polyphosphonates containing 5-flouro- N1-furanyl-N3- glyceroalkyl-uracil and formyl groups was synthesized by the condensation of 3-(w- (1-furanyl-5-flourouracil-3-yl) alkoxy)-1, 2-dihydroxy propane ...A series of novel polyphosphonates containing 5-flouro- N1-furanyl-N3- glyceroalkyl-uracil and formyl groups was synthesized by the condensation of 3-(w- (1-furanyl-5-flourouracil-3-yl) alkoxy)-1, 2-dihydroxy propane with phosphonyl dichloride. The products were characterized by IR, 1H NMR, 31P NMR, M, and elemental analysis. The results of bioassay show that compound 8a possesses potential anticancer activity.展开更多
The mechanisms and kinetics of the gas phase reactions that the hydrogen atom in formyl fluoride （FCHO） abstracted by OH in the presence of water, formic acid （FA）, or sulfuric acid （SA） are theoretically invest...The mechanisms and kinetics of the gas phase reactions that the hydrogen atom in formyl fluoride （FCHO） abstracted by OH in the presence of water, formic acid （FA）, or sulfuric acid （SA） are theoretically investigated at the CCSD（T）/6-311＋＋G（3df, 3pd）//MO6-2X/6- 311＋＋G（3df, 3pd） level of theory. The calculated results show that the barriers of the transition states involving catalysts are lowered to -2.89, -6.25, and -7.76 kcal/mol from 3.64 kcal/mol with respect to the separate reactants, respectively, which reflects that those catalysts play an important role in reducing the barrier of the hydrogen abstraction reaction of FCHO with OH. Additionally, using conventional transition state theory with Eckart tun- neling correction, the kinetic data demonstrate that the entrance channel X…FCHO＋OH （X=H2O, FA, or SA） is significantly more favorable than the pathway X…OH＋FCHO. More- over, the rate constants of the reactions of FCHO with OH radical with H2O, FA, or SA introduced are computed to be smaller than that of the naked OH＋FCHO reaction because the concentration of the formed X…FCHO or X…OH complex is quite low in the atmosphere.展开更多
For the first time, Pd supported on natural palygorskite was developed for amine formylation with CO2 and H2. Both secondary and primary amines with diverse structures could be converted into the desired formamides at...For the first time, Pd supported on natural palygorskite was developed for amine formylation with CO2 and H2. Both secondary and primary amines with diverse structures could be converted into the desired formamides at < 100 °C, and good to excellent yields were obtained.展开更多
Formyl peptide receptors (FPRs) were observed to expand in rodents and were recently suggested as candidate vomeronasal chemo-sensory receptors. Since vomeronasal chemosensory receptors usually underwent positive sele...Formyl peptide receptors (FPRs) were observed to expand in rodents and were recently suggested as candidate vomeronasal chemo-sensory receptors. Since vomeronasal chemosensory receptors usually underwent positive selection and evolved concordantly with the vomeronasal organ (VNO) morphology, we surveyed FPRs in primates in which VNO morphology is greatly diverse and thus it would provide us a clearer view of VNO-FPRs evolution. By screening available primate genome sequences, we obtained the FPR repertoires in representative primate species. As a result, we did not find FPR family size expansion in primates. Further analyses showed no evolution-ary force variance between primates with or without VNO structure, which indicated that there was no functional divergence among pri-mates FPRs. Our results suggest that primates lack the VNO-specific FPRs and the FPR expansion is not a common phenomenon in mammals outside rodent lineage, regardless of VNO complexity.展开更多
Trimethylsilylation of alcohols was achieved using 1,1,1,3,3,3-hexamethyldisilazane（HMDS） as silylating agent,in the presence of polyvinylpolypyrrolidonium tribromide in acetonitrile at room temperature.Also a varie...Trimethylsilylation of alcohols was achieved using 1,1,1,3,3,3-hexamethyldisilazane（HMDS） as silylating agent,in the presence of polyvinylpolypyrrolidonium tribromide in acetonitrile at room temperature.Also a variety of alcohols were converted into alkyl formates by ethyl formate and a catalytic amount of polyvinylpolypyrrolidonium tribromide under solvent free conditions at room temperature.展开更多
AIM:To solidify the involvement of Saa-related pathway in corneal neovascularization(CorNV).The pathogenesis of inflammatory CorNV is not fully understood yet,and our previous study implicated that serum amyloid A(Saa...AIM:To solidify the involvement of Saa-related pathway in corneal neovascularization(CorNV).The pathogenesis of inflammatory CorNV is not fully understood yet,and our previous study implicated that serum amyloid A(Saa)1(Saa1)and Saa3 were among the genes up-regulated upon CorNV induction in mice.METHODS:Microarray data obtained during our profiling project on CorNV were analyzed for the genes encoding the four SAA family members(Saa1-4),six reported SAA receptors(formyl peptide receptor 2,Tlr2,Tlr4,Cd36,Scarb1,P2rx7)and seven matrix metallopeptidases(Mmp)1a,1b,2,3,9,10,13reportedly to be expressed upon SAA pathway activation.The baseline expression or changes of interested genes were further confirmed in animals with CorNV using molecular or histological methods.CorNV was induced in Balb/c and C57BL/6 mice by placing either three interrupted 10-0 sutures or a 2 mm filter paper soaked with sodium hydroxide in the central area of the cornea.At desired time points,the corneas were harvested for histology examination or for extraction of mRNA and protein.The mRNA levels of Saa1,Saa3,Fpr2,Mmp2and Mmp3 in corneas were detected using quantitative reverse transcription-PCR,and SAA3 protein in tissues detected using immunohistochemistry or western blotting.RESULTS:Microarray data analysis revealed that Saa1,Saa3,Fpr2,Mmp2,Mmp3 messengers were readily detected in normal corneas and significantly upregulated upon CorNV induction.The changes of these five genes were confirmed with real-time PCR assay.Onthe contrary,other SAA members(Saa2,Saa4),other SAA receptors(Tlr2,Tlr4,Cd36,P2rx7,etc),or other Mmps(Mmp1a,Mmp1b,Mmp9,Mmp10,Mmp13)did not show consistent changes.Immunohistochemistry study and western blotting further confirmed the expression of SAA3 products in normal corneas as well as their upregulation in corneas with CorNV.CONCLUSION:SAA-FPR2 pathway composing genes were expressed in normal murine corneas and,upon inflammatory stimuli challenge to the corneas,their expressions were up-regulated,suggesting their roles in pathogenesis of CorNV.The potential usefulness of SAA-FPR2 targets in future management of CorNVrelated diseases deserves investigation.展开更多
2-（Sulfooxy）propane-1,2,3-tricarboxylic acid（supported on silica gel） has been introduced as novel and green catalyst for the formylation of alcohols and amines with ethyl formate,as mild formylation agent,under n...2-（Sulfooxy）propane-1,2,3-tricarboxylic acid（supported on silica gel） has been introduced as novel and green catalyst for the formylation of alcohols and amines with ethyl formate,as mild formylation agent,under neat conditions at room temperature.展开更多
Two metal-organic frameworks [（Zn0.5L）·（H2O）]n （1） and [（Ni0.5L）？（H2O）]n （2） constructed by the 3-formyl-4-（pyridin-4-yl） benzoic acid ligand （HL） were synthesized and characterized by single-cry...Two metal-organic frameworks [（Zn0.5L）·（H2O）]n （1） and [（Ni0.5L）？（H2O）]n （2） constructed by the 3-formyl-4-（pyridin-4-yl） benzoic acid ligand （HL） were synthesized and characterized by single-crystal X-ray diffraction. 1 crystallizes in orthorhombic space group Pnna with a = 16.6152（8）, b = 12.6825（6）, c = 15.3908（8） A, V = 3243.2（3） ？3, Z = 4, Mr = 511.12, Dc = 1.047 g/cm3, F（000） = 1048, μ = 1.144 mm-1, GOOF = 1.061, the final R = 0.0471 and wR = 0.1262 for 12168 observed reflections with I 〉 2σ（I）. 2 is isostructural to 1, which also crystallizes in orthorhombic space group Pnna with a = 16.6152（8）, b = 12.6825（6）, c = 15.3908（8） ？, V = 3243.2（3） ？3, Z = 4, Mr = 511.12, Dc = 1.047 g/cm3, F（000） = 1048, μ = 1.144 mm-1, GOOF = 1.061, the final R = 0.0471 and wR = 0.1262 for 12168 observed reflections with I 〉 2σ（I）. Additionally, thermogravimetric analysis, FT-IR spectroscopy and powder X-ray diffraction were discussed.展开更多
An environmental benign procedure for synthesis of 2-(N-formyl)-5-aryl/aryloxymethyl-1,3,4-thiadiazoles has been developed by reaction of 2-amino-5-aryl/aryloxymethyl-1,3,4-thiadiazoles with formic acid in PEG-400.The...An environmental benign procedure for synthesis of 2-(N-formyl)-5-aryl/aryloxymethyl-1,3,4-thiadiazoles has been developed by reaction of 2-amino-5-aryl/aryloxymethyl-1,3,4-thiadiazoles with formic acid in PEG-400.The key advantages of this protocol are the shorter reaction time,higher yields,lower cost,simple workup,and environment-friendly compared to conventional organic solvent reaction.The present method does not involve any hazardous organic solvent or catalyst.展开更多
N-formyl peptide receptors(FPRs)were first identified upon phagocytic leukocytes,but more than four decades of research has unearthed a plethora of non-myeloid roles for this receptor family.FPRs are expressed within ...N-formyl peptide receptors(FPRs)were first identified upon phagocytic leukocytes,but more than four decades of research has unearthed a plethora of non-myeloid roles for this receptor family.FPRs are expressed within neuronal tissues and markedly in the central nervous system,where FPR interactions with endogenous ligands have been implicated in the pathophysiology of several neurodegenerative diseases including Alzheimer's disease and Parkinson's disease,as well as neurological cancers such as neuroblastoma.Whilst the homeostatic function of FPRs in the nervous system is currently undefined,a variety of novel physiological roles for this receptor family in the neuronal context have been posited in both human and animal settings.Rapid developments in recent years have implicated FPRs in the process of neurogenesis and neuronal differentiation which,upon greater characterisation,could represent a novel pharmacological target for neuronal regeneration therapies that may be used in the treatment of brain/spinal cord injury,stroke and neurodegeneration.This review aims to summarize the recent progress made to determine the physiological role of FPRs in a neuronal setting,and to put forward a case for FPRs as a novel pharmacological target for conditions of the nervous system,and for their potential to open the door to novel neuronal regeneration therapies.展开更多
Two species of N-arylpyrazoles containing active amino group were synthesized.And formylations of N-arylpyazoles containing amino in different position of pyrazole rings using Vilsmeier-Haack reaction gave a series of...Two species of N-arylpyrazoles containing active amino group were synthesized.And formylations of N-arylpyazoles containing amino in different position of pyrazole rings using Vilsmeier-Haack reaction gave a series of useful pyrazole intermediates.The important features of this protocol were cheap materials,easy process,mild reaction conditions and good yield of products.展开更多
The title compound 5,17-diformyl-11,23-di（tert-butyl）-25,26,27,28-tetrapropoxycalix[4]arene has been synthesized by selective formylation of 5,11,17,23-tetra（tert-butyl）25,26,27,28-tetrahydroxycalix[4]arene in thr...The title compound 5,17-diformyl-11,23-di（tert-butyl）-25,26,27,28-tetrapropoxycalix[4]arene has been synthesized by selective formylation of 5,11,17,23-tetra（tert-butyl）25,26,27,28-tetrahydroxycalix[4]arene in three steps and characterized by1H NMR and X-ray single-crystal diffraction.The crystal belongs to the monoclinic system,space group C2/c with a = 25.760（3）,b = 10.9952（10）,c = 18.630（2）,β = 119.985（4）°,V = 4570.4（9）3,Z = 4,Dc = 1.106 g/cm3,Mr = 761.01,F（000） = 1648,μ = 0.071 mm-1,MoKa radiation（λ = 0.71073）,R = 0.0710 and wR = 0.2411 for 3234 observed reflections with I 2σ（I）.X-ray analysis reveals that the title compound adopts a pinched cone conformation which leads to an open cavity.Intermolecular C–H O weak interactions link the molecules along the bc plane,which are effective in the stabilization of the crystal structure.展开更多
BACKGROUND Formyl peptide receptor 2(Fpr2)is an important receptor in host resistance to bacterial infections.In previous studies,we found that the liver of Fpr2-/-mice is the most severely damaged target organ in blo...BACKGROUND Formyl peptide receptor 2(Fpr2)is an important receptor in host resistance to bacterial infections.In previous studies,we found that the liver of Fpr2-/-mice is the most severely damaged target organ in bloodstream infections,although the reason for this is unclear.AIM To investigate the role of Fpr2 in liver homeostasis and host resistance to bacterial infections.METHODS Transcriptome sequencing was performed on the livers of Fpr2-/-and wild-type(WT)mice.Differentially expressed genes(DEGs)were identified in the Fpr2-/-and WT mice,and the biological functions of DEGs were analyzed by Gene Ontology(GO)and Kyoto Encyclopedia of Genes and Genomes(KEGG)enrichment analysis.Quantitative real time-polymerase chain reaction(qRT-PCR)and western blot(WB)analyses were used to further validate the expression levels of differential genes.Cell counting kit-8 assay was employed to investigate cell survival.The cell cycle detection kit was used to measure the distribution of cell cycles.The Luminex assay was used to analyze cytokine levels in the liver.The serum biochemical indices and the number of neutrophils in the liver were measured,and hepatic histopathological analysis was performed.RESULTS Compared with the WT group,445 DEGs,including 325 upregulated genes and 120 downregulated genes,were identified in the liver of Fpr2-/-mice.The enrichment analysis using GO and KEGG showed that these DEGs were mainly related to cell cycle.The qRT-PCR analysis confirmed that several key genes(CycA,CycB1,Cdc20,Cdc25c,and Cdk1)involved in the cell cycle had significant changes.The WB analysis confirmed a decrease in the expression of CDK1 protein.WRW4(an antagonist of Fpr2)could inhibit the proliferation of HepG2 cells in a concentration dependent manner,with an increase in the number of cells in the G0/G1 phase,and a decrease in the number of cells in the S phase.Serum alanine aminotransferase levels increased in Fpr2-/-mice.The Luminex assay measurements showed that interleukin(IL)-10 and chemokine(C-X-C motif)ligand(CXCL)-1 levels were significantly reduced in the liver of Fpr2-/-mice.There was no difference in the number of neutrophils,serum C-reactive protein levels,and liver pathology between WT and Fpr2-/-mice.CONCLUSION Fpr2 participates in the regulation of cell cycle and cell proliferation,and affects the expression of IL-10 and CXCL-1,thus playing an important protective role in maintaining liver homeostasis.展开更多
OBJECTIVE To identify the mechanisms by which the formyl peptide receptor 2(FPR2)mediates both inflammatory and anti-inflammatory signaling in an agonist-dependent manner.METHODS Cells expressing FPR2 were incubated w...OBJECTIVE To identify the mechanisms by which the formyl peptide receptor 2(FPR2)mediates both inflammatory and anti-inflammatory signaling in an agonist-dependent manner.METHODS Cells expressing FPR2 were incubated with weak agonists,Aβ42 and Ac2-26,before stimulation with a strong agonist,WKYMVm.Calcium mobilization,c AMP inhibition and MAP kinase activation were measured.Intramolecular FRET were determined using FPR2 constructs with an ECFP attached to the C-terminus and a Fl As H binding motif embedded in the first or third intracellular loop(IL1 or IL3,respectively).RESULTS Aβ42 did not induce significant Ca^(2+) mobilization,but positively modulated WKYMVm-induced Ca^(2+) mobilization and c AMP reduction in a dose-variable manner within a narrow range of ligand concentrations.Treating FPR2-expressing cells with Ac2-26,a peptide with anti-inflammatory activity,negatively modulated WKYMVm-induced Ca^(2+) mobilization and c AMP reduction.Intramolecular FRET assay showed that stimulation of the receptor constructs with Aβ42 brought the C-terminal domain closer to IL1 but away from IL3.An opposite conformational change was induced by Ac2-26.The FPR2 conformation induced by Aβ42 corresponded to enhanced ERK phosphorylation and attenuated p38 MAPK phosphorylation,whereas Ac2-26 induced FPR2 conformational change corresponding to elevated p38 MAPK phosphorylation and reduced ERK phosphorylation.CONCLUSION Aβ42 and Ac2-26 induce different conformational changes in FPR2.These findings provide a structural basis for FPR2 mediation of inflammatory vs anti-inflammatory functions and identify a type of receptor modulation that differs from the classic positive and negative allosteric modulation.展开更多
We compute the thermodynamic and the kinetic properties for the reaction: HCOCN→HCH+CO using the statistical theory and the transition-state theory.The equi- librium constants and the rate coefficients of this reacti...We compute the thermodynamic and the kinetic properties for the reaction: HCOCN→HCH+CO using the statistical theory and the transition-state theory.The equi- librium constants and the rate coefficients of this reaction are also reported here,and the half lives of formyl cyanide at different temperatures are first estimated in this work.展开更多
基金financial support from the National Natural Science Foundation of China(No.22001147)Taishan Scholars Project of Shandong Province(No.tsqn202103027)+1 种基金Distinguished Young Scholars of Shandong Province(Overseas)(No.2022HWYQ-001)Qilu Youth Scholar Funding of Shandong University。
文摘Aromatic aldehydes are the most fundamentally important compounds used in organic synthesis.The development of new synthetic methods for introduction of a formyl group into an organic scaffold is highly desirable.In this report,a nickel-catalyzed reductive coupling between aryl halides andα–chloro N-methoxyphthalimide has been documented for the synthesis of a diverse array of aromatic aldehydes.Because of mild reductive coupling conditions,excellent functional group tolerance,especially for substrates containing free-OH and-NH_(2),was observed.Due to the simple operation mode,a large library of aromatic aldehydes can be quickly constructed by this process.Moreover,the present protocol is amenable for late-stage functionalization of bioactive compound.A combined computational and experimental investigation suggested the reaction may undergo a reaction mechanism of active Ni(I)catalyst formation and the formation of key formyl radical intermediate under zinc reductive conditions.
基金This project was supported by the National Natural Science Foundation of China.
文摘A series of novel polyphosphonates containing 5-flouro- N1-furanyl-N3- glyceroalkyl-uracil and formyl groups was synthesized by the condensation of 3-(w- (1-furanyl-5-flourouracil-3-yl) alkoxy)-1, 2-dihydroxy propane with phosphonyl dichloride. The products were characterized by IR, 1H NMR, 31P NMR, M, and elemental analysis. The results of bioassay show that compound 8a possesses potential anticancer activity.
文摘The mechanisms and kinetics of the gas phase reactions that the hydrogen atom in formyl fluoride （FCHO） abstracted by OH in the presence of water, formic acid （FA）, or sulfuric acid （SA） are theoretically investigated at the CCSD（T）/6-311＋＋G（3df, 3pd）//MO6-2X/6- 311＋＋G（3df, 3pd） level of theory. The calculated results show that the barriers of the transition states involving catalysts are lowered to -2.89, -6.25, and -7.76 kcal/mol from 3.64 kcal/mol with respect to the separate reactants, respectively, which reflects that those catalysts play an important role in reducing the barrier of the hydrogen abstraction reaction of FCHO with OH. Additionally, using conventional transition state theory with Eckart tun- neling correction, the kinetic data demonstrate that the entrance channel X…FCHO＋OH （X=H2O, FA, or SA） is significantly more favorable than the pathway X…OH＋FCHO. More- over, the rate constants of the reactions of FCHO with OH radical with H2O, FA, or SA introduced are computed to be smaller than that of the naked OH＋FCHO reaction because the concentration of the formed X…FCHO or X…OH complex is quite low in the atmosphere.
基金supported by the National Natural Science Foundation of China(91745106,21633013)the Major Projects of the National Natural Science Foundation of Gansu,China(18JR4RA001)+1 种基金the Youth Innovation Promotion Association CAS(2019409)Fujian Institute of Innovation,CAS and Key Research Program of Frontier Sciences of CAS(QYZDJ-SSW-SLH051)~~
文摘For the first time, Pd supported on natural palygorskite was developed for amine formylation with CO2 and H2. Both secondary and primary amines with diverse structures could be converted into the desired formamides at < 100 °C, and good to excellent yields were obtained.
基金supported by grants from National Natural Science Foundation of China (No. 30900793)a grant from Key Project from National Natural Science Foundation of China (No. 30930015) to P.S.+1 种基金West Light Foundation of the Chinese Academy of Sciences to H.Y.by a start-up fund of "Hundreds Talent Program" from Chinese Academy of Sciences
文摘Formyl peptide receptors (FPRs) were observed to expand in rodents and were recently suggested as candidate vomeronasal chemo-sensory receptors. Since vomeronasal chemosensory receptors usually underwent positive selection and evolved concordantly with the vomeronasal organ (VNO) morphology, we surveyed FPRs in primates in which VNO morphology is greatly diverse and thus it would provide us a clearer view of VNO-FPRs evolution. By screening available primate genome sequences, we obtained the FPR repertoires in representative primate species. As a result, we did not find FPR family size expansion in primates. Further analyses showed no evolution-ary force variance between primates with or without VNO structure, which indicated that there was no functional divergence among pri-mates FPRs. Our results suggest that primates lack the VNO-specific FPRs and the FPR expansion is not a common phenomenon in mammals outside rodent lineage, regardless of VNO complexity.
文摘Trimethylsilylation of alcohols was achieved using 1,1,1,3,3,3-hexamethyldisilazane（HMDS） as silylating agent,in the presence of polyvinylpolypyrrolidonium tribromide in acetonitrile at room temperature.Also a variety of alcohols were converted into alkyl formates by ethyl formate and a catalytic amount of polyvinylpolypyrrolidonium tribromide under solvent free conditions at room temperature.
基金Supported by National Natural Science Foundation of China(No.8120066481271050)
文摘AIM:To solidify the involvement of Saa-related pathway in corneal neovascularization(CorNV).The pathogenesis of inflammatory CorNV is not fully understood yet,and our previous study implicated that serum amyloid A(Saa)1(Saa1)and Saa3 were among the genes up-regulated upon CorNV induction in mice.METHODS:Microarray data obtained during our profiling project on CorNV were analyzed for the genes encoding the four SAA family members(Saa1-4),six reported SAA receptors(formyl peptide receptor 2,Tlr2,Tlr4,Cd36,Scarb1,P2rx7)and seven matrix metallopeptidases(Mmp)1a,1b,2,3,9,10,13reportedly to be expressed upon SAA pathway activation.The baseline expression or changes of interested genes were further confirmed in animals with CorNV using molecular or histological methods.CorNV was induced in Balb/c and C57BL/6 mice by placing either three interrupted 10-0 sutures or a 2 mm filter paper soaked with sodium hydroxide in the central area of the cornea.At desired time points,the corneas were harvested for histology examination or for extraction of mRNA and protein.The mRNA levels of Saa1,Saa3,Fpr2,Mmp2and Mmp3 in corneas were detected using quantitative reverse transcription-PCR,and SAA3 protein in tissues detected using immunohistochemistry or western blotting.RESULTS:Microarray data analysis revealed that Saa1,Saa3,Fpr2,Mmp2,Mmp3 messengers were readily detected in normal corneas and significantly upregulated upon CorNV induction.The changes of these five genes were confirmed with real-time PCR assay.Onthe contrary,other SAA members(Saa2,Saa4),other SAA receptors(Tlr2,Tlr4,Cd36,P2rx7,etc),or other Mmps(Mmp1a,Mmp1b,Mmp9,Mmp10,Mmp13)did not show consistent changes.Immunohistochemistry study and western blotting further confirmed the expression of SAA3 products in normal corneas as well as their upregulation in corneas with CorNV.CONCLUSION:SAA-FPR2 pathway composing genes were expressed in normal murine corneas and,upon inflammatory stimuli challenge to the corneas,their expressions were up-regulated,suggesting their roles in pathogenesis of CorNV.The potential usefulness of SAA-FPR2 targets in future management of CorNVrelated diseases deserves investigation.
基金Financial support for this work by the Ilam University,Ilam,Iran is gratefully acknowledged
文摘2-（Sulfooxy）propane-1,2,3-tricarboxylic acid（supported on silica gel） has been introduced as novel and green catalyst for the formylation of alcohols and amines with ethyl formate,as mild formylation agent,under neat conditions at room temperature.
基金supported by the National Natural Science Foundation of China(No.21371119,21431004,21401128,21522104,and 21620102001)the National Key Basic Research Program of China(No.2014CB932102 and 2016YFA0203400)the Shanghai“Eastern Scholar”Program
文摘Two metal-organic frameworks [（Zn0.5L）·（H2O）]n （1） and [（Ni0.5L）？（H2O）]n （2） constructed by the 3-formyl-4-（pyridin-4-yl） benzoic acid ligand （HL） were synthesized and characterized by single-crystal X-ray diffraction. 1 crystallizes in orthorhombic space group Pnna with a = 16.6152（8）, b = 12.6825（6）, c = 15.3908（8） A, V = 3243.2（3） ？3, Z = 4, Mr = 511.12, Dc = 1.047 g/cm3, F（000） = 1048, μ = 1.144 mm-1, GOOF = 1.061, the final R = 0.0471 and wR = 0.1262 for 12168 observed reflections with I 〉 2σ（I）. 2 is isostructural to 1, which also crystallizes in orthorhombic space group Pnna with a = 16.6152（8）, b = 12.6825（6）, c = 15.3908（8） ？, V = 3243.2（3） ？3, Z = 4, Mr = 511.12, Dc = 1.047 g/cm3, F（000） = 1048, μ = 1.144 mm-1, GOOF = 1.061, the final R = 0.0471 and wR = 0.1262 for 12168 observed reflections with I 〉 2σ（I）. Additionally, thermogravimetric analysis, FT-IR spectroscopy and powder X-ray diffraction were discussed.
基金support from the Natural Science Foundation of Gansu Province(No.3ZS061- A25-019)the Scientific Research fund of Gansu Provincial Education Department(No.0601-25)
文摘An environmental benign procedure for synthesis of 2-(N-formyl)-5-aryl/aryloxymethyl-1,3,4-thiadiazoles has been developed by reaction of 2-amino-5-aryl/aryloxymethyl-1,3,4-thiadiazoles with formic acid in PEG-400.The key advantages of this protocol are the shorter reaction time,higher yields,lower cost,simple workup,and environment-friendly compared to conventional organic solvent reaction.The present method does not involve any hazardous organic solvent or catalyst.
文摘N-formyl peptide receptors(FPRs)were first identified upon phagocytic leukocytes,but more than four decades of research has unearthed a plethora of non-myeloid roles for this receptor family.FPRs are expressed within neuronal tissues and markedly in the central nervous system,where FPR interactions with endogenous ligands have been implicated in the pathophysiology of several neurodegenerative diseases including Alzheimer's disease and Parkinson's disease,as well as neurological cancers such as neuroblastoma.Whilst the homeostatic function of FPRs in the nervous system is currently undefined,a variety of novel physiological roles for this receptor family in the neuronal context have been posited in both human and animal settings.Rapid developments in recent years have implicated FPRs in the process of neurogenesis and neuronal differentiation which,upon greater characterisation,could represent a novel pharmacological target for neuronal regeneration therapies that may be used in the treatment of brain/spinal cord injury,stroke and neurodegeneration.This review aims to summarize the recent progress made to determine the physiological role of FPRs in a neuronal setting,and to put forward a case for FPRs as a novel pharmacological target for conditions of the nervous system,and for their potential to open the door to novel neuronal regeneration therapies.
基金Project supported by the National Natural Science Foundation of China(No.20572079)the Natural Science Foundation of Zhejiang Province(No.Y407079)the Foundation of Science and Technology Department of Zhejiang Province(No.2007C21116).
文摘Two species of N-arylpyrazoles containing active amino group were synthesized.And formylations of N-arylpyazoles containing amino in different position of pyrazole rings using Vilsmeier-Haack reaction gave a series of useful pyrazole intermediates.The important features of this protocol were cheap materials,easy process,mild reaction conditions and good yield of products.
基金Supported by the National Natural Science Foundation of China(No.21002009)Major Program for the Natural Science Research of Jiangsu Colleges and Universities(12KJA150002)+3 种基金Jiangsu Key Laboratory of Advanced Catalytic Materials and Technology(BM2012110)the Scientific and Technological Project of Changzhou(CJ20115019)Priority Academic Program Development of Jiangsu Higher Education Institutionsthe Qing-Lan Project of Jiangsu Province
文摘The title compound 5,17-diformyl-11,23-di（tert-butyl）-25,26,27,28-tetrapropoxycalix[4]arene has been synthesized by selective formylation of 5,11,17,23-tetra（tert-butyl）25,26,27,28-tetrahydroxycalix[4]arene in three steps and characterized by1H NMR and X-ray single-crystal diffraction.The crystal belongs to the monoclinic system,space group C2/c with a = 25.760（3）,b = 10.9952（10）,c = 18.630（2）,β = 119.985（4）°,V = 4570.4（9）3,Z = 4,Dc = 1.106 g/cm3,Mr = 761.01,F（000） = 1648,μ = 0.071 mm-1,MoKa radiation（λ = 0.71073）,R = 0.0710 and wR = 0.2411 for 3234 observed reflections with I 2σ（I）.X-ray analysis reveals that the title compound adopts a pinched cone conformation which leads to an open cavity.Intermolecular C–H O weak interactions link the molecules along the bc plane,which are effective in the stabilization of the crystal structure.
基金the State Key Laboratory of Pathogen and Biosecurity,No.SKLPBS2119 and SKLPBS2212the Medical Science Research Project of Dalian,No.2112015。
文摘BACKGROUND Formyl peptide receptor 2(Fpr2)is an important receptor in host resistance to bacterial infections.In previous studies,we found that the liver of Fpr2-/-mice is the most severely damaged target organ in bloodstream infections,although the reason for this is unclear.AIM To investigate the role of Fpr2 in liver homeostasis and host resistance to bacterial infections.METHODS Transcriptome sequencing was performed on the livers of Fpr2-/-and wild-type(WT)mice.Differentially expressed genes(DEGs)were identified in the Fpr2-/-and WT mice,and the biological functions of DEGs were analyzed by Gene Ontology(GO)and Kyoto Encyclopedia of Genes and Genomes(KEGG)enrichment analysis.Quantitative real time-polymerase chain reaction(qRT-PCR)and western blot(WB)analyses were used to further validate the expression levels of differential genes.Cell counting kit-8 assay was employed to investigate cell survival.The cell cycle detection kit was used to measure the distribution of cell cycles.The Luminex assay was used to analyze cytokine levels in the liver.The serum biochemical indices and the number of neutrophils in the liver were measured,and hepatic histopathological analysis was performed.RESULTS Compared with the WT group,445 DEGs,including 325 upregulated genes and 120 downregulated genes,were identified in the liver of Fpr2-/-mice.The enrichment analysis using GO and KEGG showed that these DEGs were mainly related to cell cycle.The qRT-PCR analysis confirmed that several key genes(CycA,CycB1,Cdc20,Cdc25c,and Cdk1)involved in the cell cycle had significant changes.The WB analysis confirmed a decrease in the expression of CDK1 protein.WRW4(an antagonist of Fpr2)could inhibit the proliferation of HepG2 cells in a concentration dependent manner,with an increase in the number of cells in the G0/G1 phase,and a decrease in the number of cells in the S phase.Serum alanine aminotransferase levels increased in Fpr2-/-mice.The Luminex assay measurements showed that interleukin(IL)-10 and chemokine(C-X-C motif)ligand(CXCL)-1 levels were significantly reduced in the liver of Fpr2-/-mice.There was no difference in the number of neutrophils,serum C-reactive protein levels,and liver pathology between WT and Fpr2-/-mice.CONCLUSION Fpr2 participates in the regulation of cell cycle and cell proliferation,and affects the expression of IL-10 and CXCL-1,thus playing an important protective role in maintaining liver homeostasis.
基金supported by National Natural Science Foundation of China(31470856 to RDY)the Science and Technology Development Fund of Macao(FDCT 072/2015/A2)the University of Macao(SRG2015-00047-ICMS-QRCM)
文摘OBJECTIVE To identify the mechanisms by which the formyl peptide receptor 2(FPR2)mediates both inflammatory and anti-inflammatory signaling in an agonist-dependent manner.METHODS Cells expressing FPR2 were incubated with weak agonists,Aβ42 and Ac2-26,before stimulation with a strong agonist,WKYMVm.Calcium mobilization,c AMP inhibition and MAP kinase activation were measured.Intramolecular FRET were determined using FPR2 constructs with an ECFP attached to the C-terminus and a Fl As H binding motif embedded in the first or third intracellular loop(IL1 or IL3,respectively).RESULTS Aβ42 did not induce significant Ca^(2+) mobilization,but positively modulated WKYMVm-induced Ca^(2+) mobilization and c AMP reduction in a dose-variable manner within a narrow range of ligand concentrations.Treating FPR2-expressing cells with Ac2-26,a peptide with anti-inflammatory activity,negatively modulated WKYMVm-induced Ca^(2+) mobilization and c AMP reduction.Intramolecular FRET assay showed that stimulation of the receptor constructs with Aβ42 brought the C-terminal domain closer to IL1 but away from IL3.An opposite conformational change was induced by Ac2-26.The FPR2 conformation induced by Aβ42 corresponded to enhanced ERK phosphorylation and attenuated p38 MAPK phosphorylation,whereas Ac2-26 induced FPR2 conformational change corresponding to elevated p38 MAPK phosphorylation and reduced ERK phosphorylation.CONCLUSION Aβ42 and Ac2-26 induce different conformational changes in FPR2.These findings provide a structural basis for FPR2 mediation of inflammatory vs anti-inflammatory functions and identify a type of receptor modulation that differs from the classic positive and negative allosteric modulation.
文摘We compute the thermodynamic and the kinetic properties for the reaction: HCOCN→HCH+CO using the statistical theory and the transition-state theory.The equi- librium constants and the rate coefficients of this reaction are also reported here,and the half lives of formyl cyanide at different temperatures are first estimated in this work.
