The two diarylheptanoids (E)-1-(4-hydroxy-3-methoxyphenyl)-7-(4-hydroxyphenyl) hept-4-en-3-one 1 (Gingerenone C) and (±)-5-hydroxy-1-(4-hydroxy-3-methoxyphenyl)-7-(4- hydroxyphenyl)-3-heptanone 2 were synthesized...The two diarylheptanoids (E)-1-(4-hydroxy-3-methoxyphenyl)-7-(4-hydroxyphenyl) hept-4-en-3-one 1 (Gingerenone C) and (±)-5-hydroxy-1-(4-hydroxy-3-methoxyphenyl)-7-(4- hydroxyphenyl)-3-heptanone 2 were synthesized from vanillin 3 and 4-hydroxybenzaldehyde 9.展开更多
A rabbit model of traumatic optic nerve injury, established by occlusion of the optic nerve using a vascular clamp, was used to investigate the effects of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid recep...A rabbit model of traumatic optic nerve injury, established by occlusion of the optic nerve using a vascular clamp, was used to investigate the effects of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor antagonist GYKI 52466 on apoptosis of retinal ganglion cells following nerve injury. Hematoxylin-eosin staining and a terminal deoxynucleotidyl transferase dUTP nick end labeling assay showed that retinal ganglion cells gradually decreased with increasing time of optic nerve injury, while GYKI 52466 could inhibit this process. The results demonstrate that following acute optic nerve injury, apoptosis of retinal ganglion cells is a programmed process, which can be inhibited by the alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor antagonist.展开更多
2-Benzyl-5-hydroxy-4-oxopentanoic acid 1 and its enantiomers were designed,synthesized and assayed for inhibitory activity against carboxypeptidase A(CPA,EC 3.4.17.1).To verify the role of the terminal hydroxyl group ...2-Benzyl-5-hydroxy-4-oxopentanoic acid 1 and its enantiomers were designed,synthesized and assayed for inhibitory activity against carboxypeptidase A(CPA,EC 3.4.17.1).To verify the role of the terminal hydroxyl group in 1 binding to CPA,2-benzyl-5- benzyloxy-4-oxopentanoic acid 2 was also synthesized and evaluated.The inhibition constants show that both L-1 and D-1 were shown to have strong binding affinity with L-1 being more potent than its enantiomer by 165-fold.On the other hand,the inhibition constant ...展开更多
The title compound, 4-（tert-butyl）-5-（1 H- 1,2,4-triazol- 1 -yl）-N-（2-hydroxy-3,5-diio- dinebenzyl）thiazol-2-amine, was synthesized via the reduction of 4-（tert-butyl）-5-（1H-l,2,4- triazol-l-yl）-N-benzyliden...The title compound, 4-（tert-butyl）-5-（1 H- 1,2,4-triazol- 1 -yl）-N-（2-hydroxy-3,5-diio- dinebenzyl）thiazol-2-amine, was synthesized via the reduction of 4-（tert-butyl）-5-（1H-l,2,4- triazol-l-yl）-N-benzylidene-thiazol-2-amine with NaBH4, and its crystal structure was determined by single-crystal X-ray diffraction. The compound crystallizes in monoclinic system, space group P21/c with a = 7.91944（19）, b = 10.5250（3）, c = 24.4985（6） A, Z = 4, V = 2041.66（9） A3, Mr = 599.22, Dc = 1,949 Mg/m3, S = 1.120, p = 3.203 mm-1, F（000） = 1152, the final R = 0.0283 and wR = 0.0592 for 3490 observed reflections （I 〉 2σ（I））. X-ray analysis displays that the crystal water takes part in three intermolecular hydrogen bonds of O（2）-H（2A）…O（1）, O（2）-H（2B）…N（I） and N（5）-H（5）…O（2）, and an octatomic ring R^（8） is formed via intramolecular hydrogen bond of O（I）-H（IA）…N（4）. Furthermore, the I…I contacts are involved in stabilizing the overall three-dimensional network structure. The preliminary biological test shows the title compound has good antitumor activity with the IC50 value of 26 μM against the Hela cell line.展开更多
（＋）-（4S,5R）-and （-）-（4R,5S）-osmundalactones as well as （＋）-（4R,5S）- and （-）-（4S,5R）- 5-hydroxy-2-hexen-4-olides were synthesized by a concise and efficient synthesis method starting from 4-benzyloxy-...（＋）-（4S,5R）-and （-）-（4R,5S）-osmundalactones as well as （＋）-（4R,5S）- and （-）-（4S,5R）- 5-hydroxy-2-hexen-4-olides were synthesized by a concise and efficient synthesis method starting from 4-benzyloxy-5-hydroxy-2（E）-hexenoate in good yield with over 99% e.e..展开更多
A study on catalytic dehydration of 4-hydroxy-3-hexanone （HH） to 4-hexen-3-one （HO） was carried out through conversion of HH over HZSM-5 zeolite catalyst in a fixed-bed reactor （FBR） operating under almospheric ...A study on catalytic dehydration of 4-hydroxy-3-hexanone （HH） to 4-hexen-3-one （HO） was carried out through conversion of HH over HZSM-5 zeolite catalyst in a fixed-bed reactor （FBR） operating under almospheric pressure. The test indicated a relatively high activity of the HZSM-5 zeolite capable of achieving a HH conversion of 99.2% and a HO yield of 83.5%. Catalyst deactivation could be prevented by increasing the reaction temperature by 10 ＂C for every 20 h and adding 2.0% of piperidine in the feed. A catalyst stability test （for 100 h） in FBR showed that the catalyst was active even after 100 h of time-on-stream with HH conversion remaining at 99.2% and HO yield still reaching over 83.5%. Regenera- tion experiment showed that the regenerated catalyst demonstrated a catalytic performance comparable to the fresh one.展开更多
The title compound [2-hydroxy-5-（4-hydroxy-3-phenyliminomethyl-benzyl）-benzylidene]-phenyl-amine （C27H22N2O2, Mr = 406.47） was synthesized by 5,5′-methylene-bissalicylal- dehyde with aminobenezene, and its crysta...The title compound [2-hydroxy-5-（4-hydroxy-3-phenyliminomethyl-benzyl）-benzylidene]-phenyl-amine （C27H22N2O2, Mr = 406.47） was synthesized by 5,5′-methylene-bissalicylal- dehyde with aminobenezene, and its crystal structure was determined by single-crystal X-ray diffraction. The crystal belongs to the monoclinic system, space group C2/c with a = 4.4026（6）, b = 1.501（13）, c = 0.95818（12） nm, β = 90.868（2）°, V= 4.2813（9） nm^3, Z= 8, Dc= 1.292 g/cm^3,μ = 0.010, F（000） = 1744, R = 0.0576 and wR = 0.1450 for 3766 observed reflections with I 〉 2σ（I）. X-ray analysis reveals that the molecule has a pair of intramolecular OH…N hydrogen bonds.展开更多
A facile synthesis of the analog of curcumin. 1,7-bis (4-hydroxyphenyl)-3-hydroxy-1.3-heptadien-5-one 1 was achieved. The key step was completed through the regioselective condensation of ketone 5 and acyl chloride 7.
A new coordination polymer, {[CdL（en）]＇DMF}n （1, H2L = 4-[（8-hydroxy-5- quinolinyl）azo]-benzenesulfonic acid, en = ethylenediamine, DMF = N,N-dimethylformamide）, has been solvothermally synthesized and structur...A new coordination polymer, {[CdL（en）]＇DMF}n （1, H2L = 4-[（8-hydroxy-5- quinolinyl）azo]-benzenesulfonic acid, en = ethylenediamine, DMF = N,N-dimethylformamide）, has been solvothermally synthesized and structurally characterized by single-crystal X-ray diffrac- tion, infrared （IR） spectra, elemental analysis, powder X-ray diffractions （PXRD） and thermo- gravimetric analysis （TGA）. Compound 1 crystallizes in monoclinic, space group P2Jc with a = 14.6525（9）, b = 13.3917（9）, c = 11.8838（8） A, β = 101.2290（10）°, V = 2287.2（3） A3, Z = 4, C20H24CdN6OsS, Mr = 572.91, Dc. = 1.664 mg-mm-3, F（000） = 1160, p = 1.091 mm-1, R = 0.0232 and wR = 0.0587 for 3597 observed reflections （I 〉 2σ（I））. Compound 1 exhibits a one-dimensional （1D） double-chain structure which is further connected through hydrogen bonding and π-π interactions into a three-dimensional （3D） supramolecular network. In addition, it exhibits blue fluorescence at room temperature in the solid state.展开更多
The reaction of 5-hydroxyl-7-methoxyflavone（tectochrysin） with bromine obtained 3,6,8-tribromo-5-hydroxy-2,7-dimethoxy-2,3-dihydrochromen-4-one（1）, which was characterized by FT-IR, 1 H-NMR, 13C-NMR, elemental ana...The reaction of 5-hydroxyl-7-methoxyflavone（tectochrysin） with bromine obtained 3,6,8-tribromo-5-hydroxy-2,7-dimethoxy-2,3-dihydrochromen-4-one（1）, which was characterized by FT-IR, 1 H-NMR, 13C-NMR, elemental analysis and X-ray single-crystal diffraction. Complex 1 belongs to the monoclinic system, space group pbca with a = 9.4673（8）, b = 17.9938（15）, c = 21.2004（17） A, V = 3611.5（5） A3, Z = 8, μ = 0.6726 mm^（-1）, Dc = 1.795 g/cm3, F（000） = 2080, the final R = 0.0358 and wR = 0.0644 with I 2σ（I）. The results show that the addition reaction occurs at the carbon-carbon double bond（C2 and C3） of tectochrysin and 1 belongs to dihydroflavone. The reaction mechanism was discussed and the structure revealed that the crystal structure of 1 is stabilized by intramolecular hydrogen bonds and C–Br···π interactions. The antitumor ability of 1 was evaluated against human leukemia cells（K562）, human breast cancer cells（MCF-7） and human lung cancer cells（A549）. 1 exhibited potent antitumor activities against human leukemia cells（K562） with the IC50 values of 18.9 μmol/L.展开更多
Persistent postsurgical pain is a serious issue in public health, which has received increased interest in recent years. Previous studies have reported that psychological factors promote the development of chronic pos...Persistent postsurgical pain is a serious issue in public health, which has received increased interest in recent years. Previous studies have reported that psychological factors promote the development of chronic postsurgical pain. However, it is unclear how chronification of postsurgical pain occurs. The α-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid receptor(AMPA) phosphorylation in the central nervous system plays a critical role in synaptic plasticity and contributes to central sensitization and chronic pain development. Here, we discuss the role of AMPA receptor regulation in stress-induced pain chronification after surgery.展开更多
Phytochemical studies and antioxidant activities were carried out on n-hexane, ethyl acetate, ethanol and methanol extracts of the leaves of Lippia rugosa A. Chev (Verbenaceae), a medicinal plant used traditionally in...Phytochemical studies and antioxidant activities were carried out on n-hexane, ethyl acetate, ethanol and methanol extracts of the leaves of Lippia rugosa A. Chev (Verbenaceae), a medicinal plant used traditionally in the Cameroonian savannah’s region to protect foodstuffs and to cure degenerative diseases. Results indicated that theses extracts contain terpenoids, phenolic and flavonoid compounds. Except the n-hexane extract, all of the obtained extracts exhibit antioxidant activities with the ethanol extract being the most effective with an inhibition percentage of 85.668% ± 1.233% and an inhibition concentration (IC<sub>50</sub>) of 58 μg/ml (R<sup>2</sup> = 0.987, P < 0.01) at a concentration of 100 mg/ml. Chromatographic separation on silica gel of the ethanol extract led to the isolation of a pure organic compound which was characterized as 7-hydroxy-5,6,4'-trimethox- yflavone by extensive 1D and 2D NMR spectroscopy, a flavonoid exhibiting antioxidative activity with an inhibitory percentage of 25.506% ± 0.205% and inhibition concentration (IC<sub>50</sub>) of 221 μg/ml (R<sup>2</sup> = 0.966, P < 0.01). This is the first time that 7-hydroxy-5,6,4'-trimethoxyflavone is being isolated from L. rugosa and its antioxidant activity evaluated.展开更多
Two N-donor ligands mediated Cd（Ⅱ） coordination polymers, namely,[Cd（L）（dmpz）2]n （1） and {[Cd（L）（atr）05（H20）]（H2O）}n （2） （H2L = methyl-3-hydroxy-5-carboxy-2-thiophenecarboxylate, dmpz = 3,5-dimethy...Two N-donor ligands mediated Cd（Ⅱ） coordination polymers, namely,[Cd（L）（dmpz）2]n （1） and {[Cd（L）（atr）05（H20）]（H2O）}n （2） （H2L = methyl-3-hydroxy-5-carboxy-2-thiophenecarboxylate, dmpz = 3,5-dimethylpyrazole, and atr= 4-amino-l,2,4-triazole）, havebeen produced. Their structures were characterized by single-crystal X-ray diffraction analysis,elemental analyses and infrared spectra. Compound 1 possesses a one-dimensional （1D） chainstructure and is finally extended into a three-dimensional （3D） supramolecular architecturethough hydrogen bonding interactions. Compound 2 features a two-dimensional （2D） networkwith 4-connected sql topology based on dinuclear Cd（Ⅱ） clusters as nodes, which is alsoassembled into a 3D supramolecular architecture through hydrogen bonding interactions.Furthermore, compounds 1 and 2 exhibit high thermal stabilities and intense fluorescent emissionin the solid, and can be explored as potential luminescent materials.展开更多
The thermal decomposition behavior and kinetic parameters of the exothermic decomposition reactions of the title compound in a temperature-programmed mode have been investigated by means of DSC, TG-DTG and lower rate ...The thermal decomposition behavior and kinetic parameters of the exothermic decomposition reactions of the title compound in a temperature-programmed mode have been investigated by means of DSC, TG-DTG and lower rate thermolysis/FTIR. The possible reaction mechanism was proposed. The critical temperature of thermal explo-sion was calculated. The influence of the title compound on the combustion characteristic of composite modified double base propellant containing RDX has been explored with the strand burner. The results show that the kinetic model function in differential form, apparent activation energy Ea and pre-exponential factor A of the major exo-thermic decomposition reaction are 1-a, 207.98 kJmol-1 and 1015.64 s-1, respectively. The critical temperature of thermal explosion of the compound is 312.87 ℃. The kinetic equation of the major exothermic decomposition process of the title compound at 0.1 MPa could be expressed as: ()416.422.502?d101 edTTaa-10=-. As an auxiliary catalyst, the title compound can help the main catalyst lead salt of 4-hydroxy-3,5-dinitropyridine oxide to en-hance the burning rate and reduce the pressure exponent of RDX-CMDB propellant.展开更多
In order to improve the water solubility and bioavailability of 5-hydroxy-7-methoxyflavone,argentum 5-hydroxy-7-methoxy-2-phenyl-4H-chromen-4-one-6-sulfonate[Ag4(H2O)6](C(16)H(11)O4SO3)4·H2O(1,C(16)H(11)O4SO3=5-h...In order to improve the water solubility and bioavailability of 5-hydroxy-7-methoxyflavone,argentum 5-hydroxy-7-methoxy-2-phenyl-4H-chromen-4-one-6-sulfonate[Ag4(H2O)6](C(16)H(11)O4SO3)4·H2O(1,C(16)H(11)O4SO3=5-hydroxy-7-methoxy-2-phenyl-4H-chromen-4-one-6-sulfonate)was synthesized by sulfonation reaction.The structure of 1 was characterized by FT-IR,elemental analysis and X-ray single-crystal diffraction.Complex 1 belongs to the triclinic system,space group P1,a=8.077(4),b=12.365(4),c=17.735(7)A,V=1685.0(12)A3,Z=1,μ=1.372 mm^–1,Dc=1.936 g/cm^3,F(000)=984,the final R=0.0819 and wR=0.2332 with I>2σ(I).3D structure of 1 exhibits alternating organic and inorganic regions.O–H×××O hydrogen bonds and Ag–O coordination interactions exist among crystal water,coordinated water and sulfo group,which constructed an organic zone.Flavone skeletons form organic region of 1.Sulfo group is the bridge linking these two regions.The in vitro antitumor activity of 1 against human lymphoma cells U937 and human breast cancer cells MCF-7 were evaluated with CCK-8 assay.The result shows that 1 showed inhibitory activity against tumour cell U937 and MCF-7,and indicated that flavone sulfonate derivatives may be potential leads for further biological screenings and may generate drug-like molecules.展开更多
Two novel compounds, clemaphenol A and dihydro-4-hydroxy-5-hyroxymethyl-2(3H)-fura-none were isolated together with eight known compounds, isoferulic acid, b-sitosterol, daucosterol, 5-hy-droxymethyl-2-furancarboxalde...Two novel compounds, clemaphenol A and dihydro-4-hydroxy-5-hyroxymethyl-2(3H)-fura-none were isolated together with eight known compounds, isoferulic acid, b-sitosterol, daucosterol, 5-hy-droxymethyl-2-furancarboxaldehyde, 5-hydroxy-4-oxo-pentanoic acid, palmitic acid, linoleic acid and anemonin from the root of Clematis chinensis Osbeck.展开更多
文摘The two diarylheptanoids (E)-1-(4-hydroxy-3-methoxyphenyl)-7-(4-hydroxyphenyl) hept-4-en-3-one 1 (Gingerenone C) and (±)-5-hydroxy-1-(4-hydroxy-3-methoxyphenyl)-7-(4- hydroxyphenyl)-3-heptanone 2 were synthesized from vanillin 3 and 4-hydroxybenzaldehyde 9.
基金The Foundation of Xinjiang Uygur Autonomous Region in China, No. 200821137the National Natural Science Foundation of China, No. 81160153
文摘A rabbit model of traumatic optic nerve injury, established by occlusion of the optic nerve using a vascular clamp, was used to investigate the effects of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor antagonist GYKI 52466 on apoptosis of retinal ganglion cells following nerve injury. Hematoxylin-eosin staining and a terminal deoxynucleotidyl transferase dUTP nick end labeling assay showed that retinal ganglion cells gradually decreased with increasing time of optic nerve injury, while GYKI 52466 could inhibit this process. The results demonstrate that following acute optic nerve injury, apoptosis of retinal ganglion cells is a programmed process, which can be inhibited by the alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor antagonist.
文摘2-Benzyl-5-hydroxy-4-oxopentanoic acid 1 and its enantiomers were designed,synthesized and assayed for inhibitory activity against carboxypeptidase A(CPA,EC 3.4.17.1).To verify the role of the terminal hydroxyl group in 1 binding to CPA,2-benzyl-5- benzyloxy-4-oxopentanoic acid 2 was also synthesized and evaluated.The inhibition constants show that both L-1 and D-1 were shown to have strong binding affinity with L-1 being more potent than its enantiomer by 165-fold.On the other hand,the inhibition constant ...
基金supported by the National Undergraduate Training Programs for Innovation and Entrepreneurship of Hunan Universitythe Natural Science Foundation of Hunan Province(No.12jj3012)
文摘The title compound, 4-（tert-butyl）-5-（1 H- 1,2,4-triazol- 1 -yl）-N-（2-hydroxy-3,5-diio- dinebenzyl）thiazol-2-amine, was synthesized via the reduction of 4-（tert-butyl）-5-（1H-l,2,4- triazol-l-yl）-N-benzylidene-thiazol-2-amine with NaBH4, and its crystal structure was determined by single-crystal X-ray diffraction. The compound crystallizes in monoclinic system, space group P21/c with a = 7.91944（19）, b = 10.5250（3）, c = 24.4985（6） A, Z = 4, V = 2041.66（9） A3, Mr = 599.22, Dc = 1,949 Mg/m3, S = 1.120, p = 3.203 mm-1, F（000） = 1152, the final R = 0.0283 and wR = 0.0592 for 3490 observed reflections （I 〉 2σ（I））. X-ray analysis displays that the crystal water takes part in three intermolecular hydrogen bonds of O（2）-H（2A）…O（1）, O（2）-H（2B）…N（I） and N（5）-H（5）…O（2）, and an octatomic ring R^（8） is formed via intramolecular hydrogen bond of O（I）-H（IA）…N（4）. Furthermore, the I…I contacts are involved in stabilizing the overall three-dimensional network structure. The preliminary biological test shows the title compound has good antitumor activity with the IC50 value of 26 μM against the Hela cell line.
文摘（＋）-（4S,5R）-and （-）-（4R,5S）-osmundalactones as well as （＋）-（4R,5S）- and （-）-（4S,5R）- 5-hydroxy-2-hexen-4-olides were synthesized by a concise and efficient synthesis method starting from 4-benzyloxy-5-hydroxy-2（E）-hexenoate in good yield with over 99% e.e..
基金supported by the Science and Technology Planning Program of Tianjin(Project No.12ZXCXGX21900)
文摘A study on catalytic dehydration of 4-hydroxy-3-hexanone （HH） to 4-hexen-3-one （HO） was carried out through conversion of HH over HZSM-5 zeolite catalyst in a fixed-bed reactor （FBR） operating under almospheric pressure. The test indicated a relatively high activity of the HZSM-5 zeolite capable of achieving a HH conversion of 99.2% and a HO yield of 83.5%. Catalyst deactivation could be prevented by increasing the reaction temperature by 10 ＂C for every 20 h and adding 2.0% of piperidine in the feed. A catalyst stability test （for 100 h） in FBR showed that the catalyst was active even after 100 h of time-on-stream with HH conversion remaining at 99.2% and HO yield still reaching over 83.5%. Regenera- tion experiment showed that the regenerated catalyst demonstrated a catalytic performance comparable to the fresh one.
基金supported by the Project for Distinguished Young Scholars from Hubei Provincial Department of Education (No. Q20082601)
文摘The title compound [2-hydroxy-5-（4-hydroxy-3-phenyliminomethyl-benzyl）-benzylidene]-phenyl-amine （C27H22N2O2, Mr = 406.47） was synthesized by 5,5′-methylene-bissalicylal- dehyde with aminobenezene, and its crystal structure was determined by single-crystal X-ray diffraction. The crystal belongs to the monoclinic system, space group C2/c with a = 4.4026（6）, b = 1.501（13）, c = 0.95818（12） nm, β = 90.868（2）°, V= 4.2813（9） nm^3, Z= 8, Dc= 1.292 g/cm^3,μ = 0.010, F（000） = 1744, R = 0.0576 and wR = 0.1450 for 3766 observed reflections with I 〉 2σ（I）. X-ray analysis reveals that the molecule has a pair of intramolecular OH…N hydrogen bonds.
文摘A facile synthesis of the analog of curcumin. 1,7-bis (4-hydroxyphenyl)-3-hydroxy-1.3-heptadien-5-one 1 was achieved. The key step was completed through the regioselective condensation of ketone 5 and acyl chloride 7.
基金National Basic Research Program of China(973 Program,No.2012CB821700)Major International(Regional)Joint Research Project of National Natural Science Foundation(No.21120102034)+2 种基金National Natural Science Foundation(No.2083100251108122)Education Department of Jilin Province(No.2013-328)
文摘A new coordination polymer, {[CdL（en）]＇DMF}n （1, H2L = 4-[（8-hydroxy-5- quinolinyl）azo]-benzenesulfonic acid, en = ethylenediamine, DMF = N,N-dimethylformamide）, has been solvothermally synthesized and structurally characterized by single-crystal X-ray diffrac- tion, infrared （IR） spectra, elemental analysis, powder X-ray diffractions （PXRD） and thermo- gravimetric analysis （TGA）. Compound 1 crystallizes in monoclinic, space group P2Jc with a = 14.6525（9）, b = 13.3917（9）, c = 11.8838（8） A, β = 101.2290（10）°, V = 2287.2（3） A3, Z = 4, C20H24CdN6OsS, Mr = 572.91, Dc. = 1.664 mg-mm-3, F（000） = 1160, p = 1.091 mm-1, R = 0.0232 and wR = 0.0587 for 3597 observed reflections （I 〉 2σ（I））. Compound 1 exhibits a one-dimensional （1D） double-chain structure which is further connected through hydrogen bonding and π-π interactions into a three-dimensional （3D） supramolecular network. In addition, it exhibits blue fluorescence at room temperature in the solid state.
基金supported by Youth Backbone Teachers Project Funded by Xianyang Normal University(No.XSYGG201606)Scientific Research Program Funded by Shaanxi Provincial Education Department(No.16JK1822)+3 种基金Natural Science Basic Research Plan Funded by Shaanxi Province of China(No.2016JM5024)Science and Technology Projects of Xianyang City(No.2017k02-19)University Students Research and Innovation Training Program of Xianyang Normal University(No.2017060&201710722003)University Students Research and Innovation Training Program of Shaanxi Province(No.2490)
文摘The reaction of 5-hydroxyl-7-methoxyflavone（tectochrysin） with bromine obtained 3,6,8-tribromo-5-hydroxy-2,7-dimethoxy-2,3-dihydrochromen-4-one（1）, which was characterized by FT-IR, 1 H-NMR, 13C-NMR, elemental analysis and X-ray single-crystal diffraction. Complex 1 belongs to the monoclinic system, space group pbca with a = 9.4673（8）, b = 17.9938（15）, c = 21.2004（17） A, V = 3611.5（5） A3, Z = 8, μ = 0.6726 mm^（-1）, Dc = 1.795 g/cm3, F（000） = 2080, the final R = 0.0358 and wR = 0.0644 with I 2σ（I）. The results show that the addition reaction occurs at the carbon-carbon double bond（C2 and C3） of tectochrysin and 1 belongs to dihydroflavone. The reaction mechanism was discussed and the structure revealed that the crystal structure of 1 is stabilized by intramolecular hydrogen bonds and C–Br···π interactions. The antitumor ability of 1 was evaluated against human leukemia cells（K562）, human breast cancer cells（MCF-7） and human lung cancer cells（A549）. 1 exhibited potent antitumor activities against human leukemia cells（K562） with the IC50 values of 18.9 μmol/L.
基金Supported by The National Institute of Dental and Craniofacial Research Grants,Nos.R01 DE022880 and K02 DE023551
文摘Persistent postsurgical pain is a serious issue in public health, which has received increased interest in recent years. Previous studies have reported that psychological factors promote the development of chronic postsurgical pain. However, it is unclear how chronification of postsurgical pain occurs. The α-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid receptor(AMPA) phosphorylation in the central nervous system plays a critical role in synaptic plasticity and contributes to central sensitization and chronic pain development. Here, we discuss the role of AMPA receptor regulation in stress-induced pain chronification after surgery.
文摘Phytochemical studies and antioxidant activities were carried out on n-hexane, ethyl acetate, ethanol and methanol extracts of the leaves of Lippia rugosa A. Chev (Verbenaceae), a medicinal plant used traditionally in the Cameroonian savannah’s region to protect foodstuffs and to cure degenerative diseases. Results indicated that theses extracts contain terpenoids, phenolic and flavonoid compounds. Except the n-hexane extract, all of the obtained extracts exhibit antioxidant activities with the ethanol extract being the most effective with an inhibition percentage of 85.668% ± 1.233% and an inhibition concentration (IC<sub>50</sub>) of 58 μg/ml (R<sup>2</sup> = 0.987, P < 0.01) at a concentration of 100 mg/ml. Chromatographic separation on silica gel of the ethanol extract led to the isolation of a pure organic compound which was characterized as 7-hydroxy-5,6,4'-trimethox- yflavone by extensive 1D and 2D NMR spectroscopy, a flavonoid exhibiting antioxidative activity with an inhibitory percentage of 25.506% ± 0.205% and inhibition concentration (IC<sub>50</sub>) of 221 μg/ml (R<sup>2</sup> = 0.966, P < 0.01). This is the first time that 7-hydroxy-5,6,4'-trimethoxyflavone is being isolated from L. rugosa and its antioxidant activity evaluated.
基金supported by the National Natural Science of Foundation of China(No.21671094)
文摘Two N-donor ligands mediated Cd（Ⅱ） coordination polymers, namely,[Cd（L）（dmpz）2]n （1） and {[Cd（L）（atr）05（H20）]（H2O）}n （2） （H2L = methyl-3-hydroxy-5-carboxy-2-thiophenecarboxylate, dmpz = 3,5-dimethylpyrazole, and atr= 4-amino-l,2,4-triazole）, havebeen produced. Their structures were characterized by single-crystal X-ray diffraction analysis,elemental analyses and infrared spectra. Compound 1 possesses a one-dimensional （1D） chainstructure and is finally extended into a three-dimensional （3D） supramolecular architecturethough hydrogen bonding interactions. Compound 2 features a two-dimensional （2D） networkwith 4-connected sql topology based on dinuclear Cd（Ⅱ） clusters as nodes, which is alsoassembled into a 3D supramolecular architecture through hydrogen bonding interactions.Furthermore, compounds 1 and 2 exhibit high thermal stabilities and intense fluorescent emissionin the solid, and can be explored as potential luminescent materials.
基金the National Defense Industry Foundation (No. BZJ030901) and the Science and Technology Foundation of the National De-fense Key Laboratory of Propellant and Explosive Combustion of China (No. 51455010).
文摘The thermal decomposition behavior and kinetic parameters of the exothermic decomposition reactions of the title compound in a temperature-programmed mode have been investigated by means of DSC, TG-DTG and lower rate thermolysis/FTIR. The possible reaction mechanism was proposed. The critical temperature of thermal explo-sion was calculated. The influence of the title compound on the combustion characteristic of composite modified double base propellant containing RDX has been explored with the strand burner. The results show that the kinetic model function in differential form, apparent activation energy Ea and pre-exponential factor A of the major exo-thermic decomposition reaction are 1-a, 207.98 kJmol-1 and 1015.64 s-1, respectively. The critical temperature of thermal explosion of the compound is 312.87 ℃. The kinetic equation of the major exothermic decomposition process of the title compound at 0.1 MPa could be expressed as: ()416.422.502?d101 edTTaa-10=-. As an auxiliary catalyst, the title compound can help the main catalyst lead salt of 4-hydroxy-3,5-dinitropyridine oxide to en-hance the burning rate and reduce the pressure exponent of RDX-CMDB propellant.
基金Scientific Research Program Funded by Shaanxi Provincial Education Department(No.18JK0837)Natural Science Basic Research Plan Funded by Shaanxi Province of China(No.2018JM2045)+2 种基金Science and Technology Projects of Xianyang City(No.2017k02-19)Scientific Research Project Funded by Xianyang Normal University(No.XSYK18006)Qing-Lan Talents Project Funded by Xianyang Normal University(No.XSYQL201904)。
文摘In order to improve the water solubility and bioavailability of 5-hydroxy-7-methoxyflavone,argentum 5-hydroxy-7-methoxy-2-phenyl-4H-chromen-4-one-6-sulfonate[Ag4(H2O)6](C(16)H(11)O4SO3)4·H2O(1,C(16)H(11)O4SO3=5-hydroxy-7-methoxy-2-phenyl-4H-chromen-4-one-6-sulfonate)was synthesized by sulfonation reaction.The structure of 1 was characterized by FT-IR,elemental analysis and X-ray single-crystal diffraction.Complex 1 belongs to the triclinic system,space group P1,a=8.077(4),b=12.365(4),c=17.735(7)A,V=1685.0(12)A3,Z=1,μ=1.372 mm^–1,Dc=1.936 g/cm^3,F(000)=984,the final R=0.0819 and wR=0.2332 with I>2σ(I).3D structure of 1 exhibits alternating organic and inorganic regions.O–H×××O hydrogen bonds and Ag–O coordination interactions exist among crystal water,coordinated water and sulfo group,which constructed an organic zone.Flavone skeletons form organic region of 1.Sulfo group is the bridge linking these two regions.The in vitro antitumor activity of 1 against human lymphoma cells U937 and human breast cancer cells MCF-7 were evaluated with CCK-8 assay.The result shows that 1 showed inhibitory activity against tumour cell U937 and MCF-7,and indicated that flavone sulfonate derivatives may be potential leads for further biological screenings and may generate drug-like molecules.
基金This project was sponsored by Shanghai Science Committee (97541900-7)
文摘Two novel compounds, clemaphenol A and dihydro-4-hydroxy-5-hyroxymethyl-2(3H)-fura-none were isolated together with eight known compounds, isoferulic acid, b-sitosterol, daucosterol, 5-hy-droxymethyl-2-furancarboxaldehyde, 5-hydroxy-4-oxo-pentanoic acid, palmitic acid, linoleic acid and anemonin from the root of Clematis chinensis Osbeck.
