Sodium deoxycholate (NaDOC) could induce 1-bromo-4-(bromoacetyl) naphthalene (BBAN) to emit strong room temperature phosphorescence (RTP). Measurements of phosphore- scence spectra, peak intensity and polarization we...Sodium deoxycholate (NaDOC) could induce 1-bromo-4-(bromoacetyl) naphthalene (BBAN) to emit strong room temperature phosphorescence (RTP). Measurements of phosphore- scence spectra, peak intensity and polarization were used to investigate the solubilization of BBAN as a function of NaDOC concentration.展开更多
The purpose of this study is to use the newly synthesized molecule Sodium 8-(((carboxymethyl)amino)methyl)-4',7-bishydroxy-isoflavone-3'-sulfonate(M)as a research object,the pharmacological mechanism of the mo...The purpose of this study is to use the newly synthesized molecule Sodium 8-(((carboxymethyl)amino)methyl)-4',7-bishydroxy-isoflavone-3'-sulfonate(M)as a research object,the pharmacological mechanism of the molecule was analyzed by using a series of Systematic pharmacology methods.The results show that the M molecule has a higher drug-like DL value of 0.59 and better molecular property parameters,namely Hdon=4,Hacc=10 and AlogP=0.94;A total of 11 M molecules related targets,namely F2,ESR1,AR,F10,CA2,DPP4,CCNA2,PRSS1,CDK2,GSK3B and PTPN1;A total of 140 diseases are associated with M molecule targets,and these diseases are mainly related to cancer and cardiovascular diseases;A total of 52 pathways involve the pharmacological mechanisms of M molecules,which are mainly related to cancer and other related diseases;GO-enriched analysis showed that these targets are closely related to the regulation of peptidase activity and biological processes such as blood coagulation and hemostasis.This article clearly demonstrated the pharmacological mechanism of M molecule,which provides references for exploring the pharmacological mechanism of new compounds.展开更多
Sodium 3,5-bis(hydroxyimino)-1-methyl-2,4,6-trioxocyclohexanide C7H5N2NaO5 (I) has been isolated as the only product of the reaction of nitrosation of methylphloroglucinol. The structure of the titled compound has bee...Sodium 3,5-bis(hydroxyimino)-1-methyl-2,4,6-trioxocyclohexanide C7H5N2NaO5 (I) has been isolated as the only product of the reaction of nitrosation of methylphloroglucinol. The structure of the titled compound has been determined from single crystal X-ray diffraction data. The hydrated C7H5N2NaO52.5H2O crystallizes in the monoclinic space group C2/c, with a(?) 16.408(3);b(?) 12.446(3);c(?) 13.716(3);(o) 126.34(3). The planar organic anion exists in a triketo-dihydroxyimino form with the C–O and C–N distances from 1.220(2) to 1.271(2)?? and from 1.292(2) to 1.293?? respectively. In the IR spectrum of I, the sharp absorption band occurred at 1681 cm-1 due to C=O stretching indicating the strong H-interactions. The correlations of theoretical (DFT-B3LYP/aug-cc-pVDZ) and experimental UV-vis absorption spectra in neutral and alkaline ethanolic solutions showed the existence of hydroxyimino-nitroso tautomerism while ionization of I.展开更多
This paper reports the ultrastructural changes of trichomonas vaginaiis (T. vag. ) under the action of s-(-)usnic acid sodium in vitro. These changes can be shown by the following results:At first, the degranulation o...This paper reports the ultrastructural changes of trichomonas vaginaiis (T. vag. ) under the action of s-(-)usnic acid sodium in vitro. These changes can be shown by the following results:At first, the degranulation of the rough endoplasmic reticulum (RER) took place, the polyribosomes disaggregated. And then, the Golgi complex and the endoplasmic reticulum dilated. The cytoplasmic matrix presented and inhomogeneous apperance. Finally, the biomembrane loosed and fractured.The cell nuclei presented the karyorrhexis.展开更多
AIM: To investigate anti-hypersensitive effects of α2δ-1 ligands in non-inflammatory and inflammationassociated colonic hypersensitivity(CHS) mouse models.METHODS: To induce an inflammation-associated CHS, 1% dextra...AIM: To investigate anti-hypersensitive effects of α2δ-1 ligands in non-inflammatory and inflammationassociated colonic hypersensitivity(CHS) mouse models.METHODS: To induce an inflammation-associated CHS, 1% dextran sulfate sodium(DSS) was administered to C57Bl/6J male mice, in drinking water, for 14 d. Regarding the non-inflammatory neonatal maternal separation(NMS)-induced CHS model, wild-type C57BI/6J pups were isolated from their mother from day 2 to day 14(P2 to P14), three hours per day(from 9:00 a.m. to 12:00 p.m.). Colorectal distension was performed by inflating distension probe from 20 μL to 100 μL by 20 μL increment step every 10 s. After a first colorectal distension(CRD), drugs were administered subcutaneously, in a cumulative manner,(Gabapentin at 30 mg/kg and 100 mg/kg; Pregabalin at 10 mg/kg and 30 mg/kg; Carbamazepine at 10 mg/kg and 30 mg/kg) and a second CRD was performed one hour after each injection.RESULTS: The visceromotor response(VMR) to CRD was increased by our NMS paradigm protocol in comparison to non-handled(NH) mice, considering the highest distension volumes(80 μL: 0.783 ± 0.056 mV /s vs 0.531 ± 0.034 m V/s, P < 0.05 and 100 μL: 1.087 ± 0.056 m V/s vs 0.634 ± 0.038 m V/s, P < 0.05 for NMS and NH mice, respectively). In the inflammationassociated CHS, DSS-treated mice showed a dramatic and significant increase in VMR at 60 and 80 μL distension volumes when compared to control mice(60 μL: 0.920 ± 0.079 m V/s vs 0.426 ± 0.100 m V/s P < 0.05 and 80 μL: 1.193 ± 0.097 mV /s vs 0.681 ± 0.094 mV /s P < 0.05 for DSS- and Water-treated mice, respectively). Carbamazepine failed to significantly reduce CHS in both models. Gabapentin significantly reduced CHS in the DSS-induced model for both subcutaneous injections at 30 or 100 mg/kg. Pregabalin s i g n i f i c a n t l y r e d u c e d V M R t o C R D i n t h e n o n-inflammatory NMS-induced CHS model for the acute subcutaneous administration of the highest cumulative dose(30 mg/kg) and significantly reduced CHS in lowdose DSS-treated mice in a dose-dependent manner. Finally, the percent decrease of AUC induced by acute GBP or Pregabalin treatment were higher in the inflammatory DSS-induced CHS model in comparison to the non-inflammatory NMS-induced CHS model.CONCLUSION: This preclinical study demonstrates α2δ-1 ligands efficacy on inflammation-associated CHS, highlighting their potential clinical interest in patients with chronic abdominal pain and moderate intestinal inflammation.展开更多
A single phrase Na - X zeolite was synthesized from pretreated oil shale ash by alkaline fusion and hydrotherreal treatment. Eff3cts of the NaOH concentration, crystallization time ant temperature on the formation of ...A single phrase Na - X zeolite was synthesized from pretreated oil shale ash by alkaline fusion and hydrotherreal treatment. Eff3cts of the NaOH concentration, crystallization time ant temperature on the formation of Na-X zeolite were studied in detail. The single phase Na- X zeolite powders can. be prepared by alkaline fusion o.f pretreated oil shale ash at 600 ℃ .for 1 h, and crystalli-zation at 80 - 100 ℃ .for 8 - 10 h with NaOH concentration of 3 -3. 5 tool · L-1. Na - A zeolite appears when decreasing NaOH concentration, crystallization time or temperature, ant an unnamed zeolite emerges when prolonging crystallization time or raising crystalli-zation, temperature. SEM micrographs suggest that the aggregates of Na-X zeolite particles have perfect dispersity and uniform granular with about 1.5 μm in size, and most of the Na-X zeolite crystals display a regular octahedral structure with the size of about 500 nm. The specific surface area of the powders with single Na-X zeolite phase reaches the maximum value of 488. 163 2 m2· g -1, larger than that of multiple zeolite powders.展开更多
[Objective]The paper was to study a synthetic method suitable for industrial production of intermediate N-Chloroformyl-N-[4-(trifluoromethoxy)phenyl]methyl carbamate of indoxacarb.[Method]Using 4-trifluoromethoxy anil...[Objective]The paper was to study a synthetic method suitable for industrial production of intermediate N-Chloroformyl-N-[4-(trifluoromethoxy)phenyl]methyl carbamate of indoxacarb.[Method]Using 4-trifluoromethoxy aniline as the starting material,[4-(trifluoromethoxy)phenyl]carbamate was synthesized by homogeneous formylation method without acid-binding agent.Subsequently,it was reacted with sodium methoxide/potassium methoxide by reactive distillation to obtain[4-(trifluoromethoxy)phenyl]carbamate ammonium sodium/potassium,then directly reacted with triphosgene to obtain crude products of N-carbonochloridoyl-N-[4-(trifluoromethoxy)phenyl]carbamate;finally,competing product was obtained by recrystallization.[Result]The intermediate N-chloroformyl-N-[4-(trifluoromethoxy)phenyl]carbamate was synthesized by the method.The content of products was higher than 98%.The yield of product reached above 96%(calculated by 4-trifluoromethoxy aniline).[Conclusion]The method used for the synthesis of intermediate N-chloroformyl-N-[4-(trifluoromethoxy)phenyl]methyl carbamate was simple,with less three wastes,higher safety and lower cost.展开更多
We report a one-pot three-component synthesis of N-arylmethyl-4-(7-cyclohepta-1,3,5-trienyl)anilines by using various aromatic imines, tropylium tetrafluoroborate, and sodium tetrahydroborate in the presence of imidaz...We report a one-pot three-component synthesis of N-arylmethyl-4-(7-cyclohepta-1,3,5-trienyl)anilines by using various aromatic imines, tropylium tetrafluoroborate, and sodium tetrahydroborate in the presence of imidazole as activator.展开更多
Objective To investigate the influence of captoprial and SNP on the release of ET -1 in cultured VSMC of rats. Methods Measurement of endothelin - 1 levels by radioimmljnoassay in various concentrations of captopril a...Objective To investigate the influence of captoprial and SNP on the release of ET -1 in cultured VSMC of rats. Methods Measurement of endothelin - 1 levels by radioimmljnoassay in various concentrations of captopril and/or sodium nitroprusside in cultured vascular smooth muscle cell (VSMC) of rats. Results Both captopril and SNP could reduce the high ET - 1 levels of VSMC which were caused by Ang Ⅱ. There was a linear relationship between Ang Ⅱlevels and ET -1 production ( r = 0. 760, P <0. 001 ) . Conclusion Endothelin - 1 may accelerate the formation and development of atherosclerosis through inhibiting endogenous NO production by VSMC. ACEI or NO inhibition of ET -1 release could reduce atherosclerosis formation.展开更多
β-β″-Al2O3precursor powder was successfully prepared by a solid-phase sintering method with Li2CO3, Na2CO3 （as the sources of Li20 and Na20, respectively） and β″-Al2O3 powder as the raw materials. The precursor...β-β″-Al2O3precursor powder was successfully prepared by a solid-phase sintering method with Li2CO3, Na2CO3 （as the sources of Li20 and Na20, respectively） and β″-Al2O3 powder as the raw materials. The precursor was characterized by X-ray diffraction （XRD） and scan- ning electron microscope （SEM）. The results indicate that the amount of Na20 in the raw materials has a great effect on the formation of β″-Al2O3 in the β-β″-Al2O3 precursor. When Na20 content is 10 wt%, the content of β″-Al2O3 phase reaches the maximum value of 86.24 wt% in the precursor. The β-β″-Al2O3 ceramic was prepared from β-β″-Al2O3 precursor powder by isostatic pressing and burying sintering process. The conductive property of the β-β″-Al2O3 ceramic was examined by electrochemical impedance spectroscopy （EIS） method, and the density was measured by the Archimedes method. The results reveal that when 10 wt% Na20 was added, the sample exhibits the best performance with the lowest resistivity of 4.51.cm and the highest density of 3.25 g.cm 3. A solid electrolyte battery of PtlSnQ, Na2SnO3113 β-β″-Al2O3 Na CrO2, Cr2lO3 Pt was assembled by the β-β″-Al2O3 electrolyte tube to measure the open potential of the resulting battery, and the formation free energy of sodium stannate was calculated In the temperature range of 1273-773 K, the relationship between formation free energy of sodiumstannate and temperature was generated as follows：△GNa2SnO3 0=-1040.83＋0.2221T±7.54.展开更多
文摘Sodium deoxycholate (NaDOC) could induce 1-bromo-4-(bromoacetyl) naphthalene (BBAN) to emit strong room temperature phosphorescence (RTP). Measurements of phosphore- scence spectra, peak intensity and polarization were used to investigate the solubilization of BBAN as a function of NaDOC concentration.
基金The study was funded by the Middle-Aged and Young Teachers in Colleges and Universities in Guangxi Basic Ability Promotion Project(No.2017KY0581)and Natural Science Foundation of Guangxi Province(No.2018GXNSFAA138140).
文摘The purpose of this study is to use the newly synthesized molecule Sodium 8-(((carboxymethyl)amino)methyl)-4',7-bishydroxy-isoflavone-3'-sulfonate(M)as a research object,the pharmacological mechanism of the molecule was analyzed by using a series of Systematic pharmacology methods.The results show that the M molecule has a higher drug-like DL value of 0.59 and better molecular property parameters,namely Hdon=4,Hacc=10 and AlogP=0.94;A total of 11 M molecules related targets,namely F2,ESR1,AR,F10,CA2,DPP4,CCNA2,PRSS1,CDK2,GSK3B and PTPN1;A total of 140 diseases are associated with M molecule targets,and these diseases are mainly related to cancer and cardiovascular diseases;A total of 52 pathways involve the pharmacological mechanisms of M molecules,which are mainly related to cancer and other related diseases;GO-enriched analysis showed that these targets are closely related to the regulation of peptidase activity and biological processes such as blood coagulation and hemostasis.This article clearly demonstrated the pharmacological mechanism of M molecule,which provides references for exploring the pharmacological mechanism of new compounds.
文摘Sodium 3,5-bis(hydroxyimino)-1-methyl-2,4,6-trioxocyclohexanide C7H5N2NaO5 (I) has been isolated as the only product of the reaction of nitrosation of methylphloroglucinol. The structure of the titled compound has been determined from single crystal X-ray diffraction data. The hydrated C7H5N2NaO52.5H2O crystallizes in the monoclinic space group C2/c, with a(?) 16.408(3);b(?) 12.446(3);c(?) 13.716(3);(o) 126.34(3). The planar organic anion exists in a triketo-dihydroxyimino form with the C–O and C–N distances from 1.220(2) to 1.271(2)?? and from 1.292(2) to 1.293?? respectively. In the IR spectrum of I, the sharp absorption band occurred at 1681 cm-1 due to C=O stretching indicating the strong H-interactions. The correlations of theoretical (DFT-B3LYP/aug-cc-pVDZ) and experimental UV-vis absorption spectra in neutral and alkaline ethanolic solutions showed the existence of hydroxyimino-nitroso tautomerism while ionization of I.
文摘This paper reports the ultrastructural changes of trichomonas vaginaiis (T. vag. ) under the action of s-(-)usnic acid sodium in vitro. These changes can be shown by the following results:At first, the degranulation of the rough endoplasmic reticulum (RER) took place, the polyribosomes disaggregated. And then, the Golgi complex and the endoplasmic reticulum dilated. The cytoplasmic matrix presented and inhomogeneous apperance. Finally, the biomembrane loosed and fractured.The cell nuclei presented the karyorrhexis.
文摘AIM: To investigate anti-hypersensitive effects of α2δ-1 ligands in non-inflammatory and inflammationassociated colonic hypersensitivity(CHS) mouse models.METHODS: To induce an inflammation-associated CHS, 1% dextran sulfate sodium(DSS) was administered to C57Bl/6J male mice, in drinking water, for 14 d. Regarding the non-inflammatory neonatal maternal separation(NMS)-induced CHS model, wild-type C57BI/6J pups were isolated from their mother from day 2 to day 14(P2 to P14), three hours per day(from 9:00 a.m. to 12:00 p.m.). Colorectal distension was performed by inflating distension probe from 20 μL to 100 μL by 20 μL increment step every 10 s. After a first colorectal distension(CRD), drugs were administered subcutaneously, in a cumulative manner,(Gabapentin at 30 mg/kg and 100 mg/kg; Pregabalin at 10 mg/kg and 30 mg/kg; Carbamazepine at 10 mg/kg and 30 mg/kg) and a second CRD was performed one hour after each injection.RESULTS: The visceromotor response(VMR) to CRD was increased by our NMS paradigm protocol in comparison to non-handled(NH) mice, considering the highest distension volumes(80 μL: 0.783 ± 0.056 mV /s vs 0.531 ± 0.034 m V/s, P < 0.05 and 100 μL: 1.087 ± 0.056 m V/s vs 0.634 ± 0.038 m V/s, P < 0.05 for NMS and NH mice, respectively). In the inflammationassociated CHS, DSS-treated mice showed a dramatic and significant increase in VMR at 60 and 80 μL distension volumes when compared to control mice(60 μL: 0.920 ± 0.079 m V/s vs 0.426 ± 0.100 m V/s P < 0.05 and 80 μL: 1.193 ± 0.097 mV /s vs 0.681 ± 0.094 mV /s P < 0.05 for DSS- and Water-treated mice, respectively). Carbamazepine failed to significantly reduce CHS in both models. Gabapentin significantly reduced CHS in the DSS-induced model for both subcutaneous injections at 30 or 100 mg/kg. Pregabalin s i g n i f i c a n t l y r e d u c e d V M R t o C R D i n t h e n o n-inflammatory NMS-induced CHS model for the acute subcutaneous administration of the highest cumulative dose(30 mg/kg) and significantly reduced CHS in lowdose DSS-treated mice in a dose-dependent manner. Finally, the percent decrease of AUC induced by acute GBP or Pregabalin treatment were higher in the inflammatory DSS-induced CHS model in comparison to the non-inflammatory NMS-induced CHS model.CONCLUSION: This preclinical study demonstrates α2δ-1 ligands efficacy on inflammation-associated CHS, highlighting their potential clinical interest in patients with chronic abdominal pain and moderate intestinal inflammation.
文摘A single phrase Na - X zeolite was synthesized from pretreated oil shale ash by alkaline fusion and hydrotherreal treatment. Eff3cts of the NaOH concentration, crystallization time ant temperature on the formation of Na-X zeolite were studied in detail. The single phase Na- X zeolite powders can. be prepared by alkaline fusion o.f pretreated oil shale ash at 600 ℃ .for 1 h, and crystalli-zation at 80 - 100 ℃ .for 8 - 10 h with NaOH concentration of 3 -3. 5 tool · L-1. Na - A zeolite appears when decreasing NaOH concentration, crystallization time or temperature, ant an unnamed zeolite emerges when prolonging crystallization time or raising crystalli-zation, temperature. SEM micrographs suggest that the aggregates of Na-X zeolite particles have perfect dispersity and uniform granular with about 1.5 μm in size, and most of the Na-X zeolite crystals display a regular octahedral structure with the size of about 500 nm. The specific surface area of the powders with single Na-X zeolite phase reaches the maximum value of 488. 163 2 m2· g -1, larger than that of multiple zeolite powders.
文摘[Objective]The paper was to study a synthetic method suitable for industrial production of intermediate N-Chloroformyl-N-[4-(trifluoromethoxy)phenyl]methyl carbamate of indoxacarb.[Method]Using 4-trifluoromethoxy aniline as the starting material,[4-(trifluoromethoxy)phenyl]carbamate was synthesized by homogeneous formylation method without acid-binding agent.Subsequently,it was reacted with sodium methoxide/potassium methoxide by reactive distillation to obtain[4-(trifluoromethoxy)phenyl]carbamate ammonium sodium/potassium,then directly reacted with triphosgene to obtain crude products of N-carbonochloridoyl-N-[4-(trifluoromethoxy)phenyl]carbamate;finally,competing product was obtained by recrystallization.[Result]The intermediate N-chloroformyl-N-[4-(trifluoromethoxy)phenyl]carbamate was synthesized by the method.The content of products was higher than 98%.The yield of product reached above 96%(calculated by 4-trifluoromethoxy aniline).[Conclusion]The method used for the synthesis of intermediate N-chloroformyl-N-[4-(trifluoromethoxy)phenyl]methyl carbamate was simple,with less three wastes,higher safety and lower cost.
文摘We report a one-pot three-component synthesis of N-arylmethyl-4-(7-cyclohepta-1,3,5-trienyl)anilines by using various aromatic imines, tropylium tetrafluoroborate, and sodium tetrahydroborate in the presence of imidazole as activator.
文摘Objective To investigate the influence of captoprial and SNP on the release of ET -1 in cultured VSMC of rats. Methods Measurement of endothelin - 1 levels by radioimmljnoassay in various concentrations of captopril and/or sodium nitroprusside in cultured vascular smooth muscle cell (VSMC) of rats. Results Both captopril and SNP could reduce the high ET - 1 levels of VSMC which were caused by Ang Ⅱ. There was a linear relationship between Ang Ⅱlevels and ET -1 production ( r = 0. 760, P <0. 001 ) . Conclusion Endothelin - 1 may accelerate the formation and development of atherosclerosis through inhibiting endogenous NO production by VSMC. ACEI or NO inhibition of ET -1 release could reduce atherosclerosis formation.
基金financially supported by the National Natural Science Foundation of China (No.51234009)
文摘β-β″-Al2O3precursor powder was successfully prepared by a solid-phase sintering method with Li2CO3, Na2CO3 （as the sources of Li20 and Na20, respectively） and β″-Al2O3 powder as the raw materials. The precursor was characterized by X-ray diffraction （XRD） and scan- ning electron microscope （SEM）. The results indicate that the amount of Na20 in the raw materials has a great effect on the formation of β″-Al2O3 in the β-β″-Al2O3 precursor. When Na20 content is 10 wt%, the content of β″-Al2O3 phase reaches the maximum value of 86.24 wt% in the precursor. The β-β″-Al2O3 ceramic was prepared from β-β″-Al2O3 precursor powder by isostatic pressing and burying sintering process. The conductive property of the β-β″-Al2O3 ceramic was examined by electrochemical impedance spectroscopy （EIS） method, and the density was measured by the Archimedes method. The results reveal that when 10 wt% Na20 was added, the sample exhibits the best performance with the lowest resistivity of 4.51.cm and the highest density of 3.25 g.cm 3. A solid electrolyte battery of PtlSnQ, Na2SnO3113 β-β″-Al2O3 Na CrO2, Cr2lO3 Pt was assembled by the β-β″-Al2O3 electrolyte tube to measure the open potential of the resulting battery, and the formation free energy of sodium stannate was calculated In the temperature range of 1273-773 K, the relationship between formation free energy of sodiumstannate and temperature was generated as follows：△GNa2SnO3 0=-1040.83＋0.2221T±7.54.
