The effects of bispyribac sodium 10% SC and butachlor 50% SC on soil physico-chemical properties and microflora in transplanted kharifrice were investigated over two seasons (2010 and 2011 ) Effects of the herbicide...The effects of bispyribac sodium 10% SC and butachlor 50% SC on soil physico-chemical properties and microflora in transplanted kharifrice were investigated over two seasons (2010 and 2011 ) Effects of the herbicide on bulk density, water holding capacity, moisture content, soil pH, organic matter content, electrical conductivity, as well as total nitrogen, available phosphorus and available potassium contents were analyzed along with microflora population (total bacteria, actinomycetes and fungi). No significant changes in soil physico-chemical properties were observed. Herbicide treatments resulted in decreases in microbial counts initially. With the degradation of applied herbicides within a considerable time, the microflora populations even exceeded the initial count at 60 d after application of the herbicide.展开更多
The synthesis of sodium ferrite and its desulfurization performance in S2 -bearing sodium aluminate solutions were investigated. The thermodynamic analysis shows that the lowest temperature is about 810 K for synthesi...The synthesis of sodium ferrite and its desulfurization performance in S2 -bearing sodium aluminate solutions were investigated. The thermodynamic analysis shows that the lowest temperature is about 810 K for synthesizing sodium ferrite by roasting the mixture of ferric oxide and sodium carbonate. The results indicate that the formation process of sodium ferrite can be completed at 1173 K for 60 min, meanwhile raising temperature and reducing NazCO3 particle size are beneficial to accelerating the formation of sodium ferrite. Sodium ferrite is an efficient desulfurizer to remove the S2- in aluminate solution, and the desulfurization rate can reach approximately 70% at 373 K for 60 min with the molar ratio of iron to sulfur of 1:1-1.5:1. Furthermore, the desulfurization is achieved by NaFeS2·2H2O precipitation through the reaction of Fe(OH)4 and S^2- in aluminate solution, and the desulfurization efficiency relies on the Fe(OH)4^- generated by dissolving sodium ferrite.展开更多
This work investigated the separation of potassium from sodium in alkaline solution using substituted phenol-based extractants.Superior potassium extraction was achieved with 4-tert-butyl-2-(α-methylbenzyl)phenol(t-B...This work investigated the separation of potassium from sodium in alkaline solution using substituted phenol-based extractants.Superior potassium extraction was achieved with 4-tert-butyl-2-(α-methylbenzyl)phenol(t-BAMBP)than 4-sec-butyl-2-(α-methylbenzyl)phenol(BAMBP).The optimum conditions for the extraction were 1 mol/L t-BAMBP,3:1 volumetric phase ratio(O/A),and two extraction stages.After cross-current extraction,the extraction ratio of potassium reached 90.8%.After scrubbing with deionised water at phase ratio of 4:1 and scrubbing stage of 4,a sodium scrubbing efficiency of 88.2%was obtained.After stripping using 1 mol/L H_(2)SO_(4) at phase ratio of 3:1,the stripping efficiency of potassium reached 94.2%.The potassium/sodium(K/Na)concentration ratio increased 14.3 times from 0.15 in the feed solution to 2.3 in the stripping solution.The efficient separation of potassium from sodium in alkaline solution was achieved via solvent extraction with t-BAMBP.展开更多
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
Lactivicin,a novel inhibitor of bacterial cell wall synthesis,was isolated from the culture fil-trates of microorganism YK-258 and YK-422.It exhibits biological activities similar to those ofthe β-lactam antibiotics,...Lactivicin,a novel inhibitor of bacterial cell wall synthesis,was isolated from the culture fil-trates of microorganism YK-258 and YK-422.It exhibits biological activities similar to those ofthe β-lactam antibiotics,although it does not have a β-lactam ring in its molecule.Since the discovery of lactivicin,hundreds of its derivatives have been synthesized.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
以稗草和千金子为供试杂草,以南梗9108、南京11、K两优10号为供试水稻,通过室内整株生测法研究助剂GY-Tmax对双草醚、氰氟草酯防效和对水稻安全性的影响。结果表明,添加90 mL/667 m^2助剂GY-Tmax后,双草醚对3~4叶期稗草的ED90由3. 651 1...以稗草和千金子为供试杂草,以南梗9108、南京11、K两优10号为供试水稻,通过室内整株生测法研究助剂GY-Tmax对双草醚、氰氟草酯防效和对水稻安全性的影响。结果表明,添加90 mL/667 m^2助剂GY-Tmax后,双草醚对3~4叶期稗草的ED90由3. 651 1 g a. i./667 m^2降至0. 932 9 g a. i./667 m^2,这表明助剂GY-Tmax明显增加了双草醚对稗草的防效;双草醚对千金子的防效较差,且助剂GY-Tmax对双草醚防除千金子无明显增效作用。添加90 mL/667 m^2助剂GY-Tmax后,氰氟草酯对3~4叶期稗草和千金子的防效均有所提高,氰氟草酯对稗草的ED90由10. 903 5 g a. i./667 m^2降至5. 231 1 g a. i./667 m^2,对千金子的ED_(90)由6. 840 0 g a. i./667 m^2降至2. 873 6 g a. i./667 m^2。添加90 mL/667 m^2助剂GY-Tmax后,双草醚和氰氟草酯对南梗9108、南京11、K两优10号水稻的安全性与不添加助剂时相当。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
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
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
[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
基金supported by M/S Crystal Crop Protection Pvt.Ltd.,Corp.Office:G I/17,GT Karnal Road,Industrial Area,Azadpur(Near Azadpur Metro Station),Delhi 110033,India
文摘The effects of bispyribac sodium 10% SC and butachlor 50% SC on soil physico-chemical properties and microflora in transplanted kharifrice were investigated over two seasons (2010 and 2011 ) Effects of the herbicide on bulk density, water holding capacity, moisture content, soil pH, organic matter content, electrical conductivity, as well as total nitrogen, available phosphorus and available potassium contents were analyzed along with microflora population (total bacteria, actinomycetes and fungi). No significant changes in soil physico-chemical properties were observed. Herbicide treatments resulted in decreases in microbial counts initially. With the degradation of applied herbicides within a considerable time, the microflora populations even exceeded the initial count at 60 d after application of the herbicide.
基金Project(51374239)supported by the National Natural Science Foundation of China
文摘The synthesis of sodium ferrite and its desulfurization performance in S2 -bearing sodium aluminate solutions were investigated. The thermodynamic analysis shows that the lowest temperature is about 810 K for synthesizing sodium ferrite by roasting the mixture of ferric oxide and sodium carbonate. The results indicate that the formation process of sodium ferrite can be completed at 1173 K for 60 min, meanwhile raising temperature and reducing NazCO3 particle size are beneficial to accelerating the formation of sodium ferrite. Sodium ferrite is an efficient desulfurizer to remove the S2- in aluminate solution, and the desulfurization rate can reach approximately 70% at 373 K for 60 min with the molar ratio of iron to sulfur of 1:1-1.5:1. Furthermore, the desulfurization is achieved by NaFeS2·2H2O precipitation through the reaction of Fe(OH)4 and S^2- in aluminate solution, and the desulfurization efficiency relies on the Fe(OH)4^- generated by dissolving sodium ferrite.
基金Projects(52034002,U1802253)supported by the National Natural Science Foundation of ChinaProject(2019YFC1908401)supported by the National Technology Support Project of China。
文摘This work investigated the separation of potassium from sodium in alkaline solution using substituted phenol-based extractants.Superior potassium extraction was achieved with 4-tert-butyl-2-(α-methylbenzyl)phenol(t-BAMBP)than 4-sec-butyl-2-(α-methylbenzyl)phenol(BAMBP).The optimum conditions for the extraction were 1 mol/L t-BAMBP,3:1 volumetric phase ratio(O/A),and two extraction stages.After cross-current extraction,the extraction ratio of potassium reached 90.8%.After scrubbing with deionised water at phase ratio of 4:1 and scrubbing stage of 4,a sodium scrubbing efficiency of 88.2%was obtained.After stripping using 1 mol/L H_(2)SO_(4) at phase ratio of 3:1,the stripping efficiency of potassium reached 94.2%.The potassium/sodium(K/Na)concentration ratio increased 14.3 times from 0.15 in the feed solution to 2.3 in the stripping solution.The efficient separation of potassium from sodium in alkaline solution was achieved via solvent extraction with t-BAMBP.
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.
文摘Lactivicin,a novel inhibitor of bacterial cell wall synthesis,was isolated from the culture fil-trates of microorganism YK-258 and YK-422.It exhibits biological activities similar to those ofthe β-lactam antibiotics,although it does not have a β-lactam ring in its molecule.Since the discovery of lactivicin,hundreds of its derivatives have been synthesized.
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.
文摘以稗草和千金子为供试杂草,以南梗9108、南京11、K两优10号为供试水稻,通过室内整株生测法研究助剂GY-Tmax对双草醚、氰氟草酯防效和对水稻安全性的影响。结果表明,添加90 mL/667 m^2助剂GY-Tmax后,双草醚对3~4叶期稗草的ED90由3. 651 1 g a. i./667 m^2降至0. 932 9 g a. i./667 m^2,这表明助剂GY-Tmax明显增加了双草醚对稗草的防效;双草醚对千金子的防效较差,且助剂GY-Tmax对双草醚防除千金子无明显增效作用。添加90 mL/667 m^2助剂GY-Tmax后,氰氟草酯对3~4叶期稗草和千金子的防效均有所提高,氰氟草酯对稗草的ED90由10. 903 5 g a. i./667 m^2降至5. 231 1 g a. i./667 m^2,对千金子的ED_(90)由6. 840 0 g a. i./667 m^2降至2. 873 6 g a. i./667 m^2。添加90 mL/667 m^2助剂GY-Tmax后,双草醚和氰氟草酯对南梗9108、南京11、K两优10号水稻的安全性与不添加助剂时相当。
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[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.