Background The benefits of combining benzoic acid and essential oils(BAO)to mitigate intestinal impairment during the weaning process have been well established,while the detailed underlying mechanism has not been ful...Background The benefits of combining benzoic acid and essential oils(BAO)to mitigate intestinal impairment during the weaning process have been well established,while the detailed underlying mechanism has not been fully elucidated.Previous research has primarily focused on the reparative effects of BAO on intestinal injury,while neglecting its potential in enhancing intestinal stress resistance.Methods In this study,we investigated the pre-protective effect of BAO against LPS-induced stress using a modified experimental procedure.Piglets were pre-supplemented with BAO for 14 d,followed by a challenge with LPS or saline to collect blood and intestinal samples.Results Our findings demonstrated that BAO supplementation led to significant improvements in piglets’final weight,average daily gain,and feed intake/body gain ratio.Additionally,BAO supplementation positively influenced the composition of intestinal microbiota,increasing beneficial Actinobacteriota and Alloprevotella while reducing harmful Desulfobacterota,Prevotella and Oscillospira.Furthermore,BAO supplementation effectively mitigated oxidative disturbances and inflammatory responses induced by acute LPS challenge.This was evidenced by elevated levels of T-AOC,SOD,and GSH,as well as decreased levels of MDA,TNF-α,and IL-6 in the plasma.Moreover,piglets subjected to LPS challenge and pre-supplemented with BAO exhibited significant improvements in intestinal morphological structure and enhanced integrity,as indicated by restored expression levels of Occludin and Claudin-1 compared to the non-supplemented counterparts.Further analysis revealed that BAO supplementation enhanced the jejunal antioxidative capacity by increasing GSH-Px levels and decreasing MDA levels under the LPS challenge and stimulated the activation of the Nrf2 signaling pathway.Additionally,the reduction of TLR4/NF-κB/MAPK signaling pathways activation and proinflammatory factor were also observed in the jejunal of those piglets fed with BAO.Conclusions In summary,our study demonstrates that pre-supplementation of BAO enhances the anti-stress capacity of weaned piglets by improving intestinal microbiota composition,reinforcing the intestinal barrier,and enhancing antioxidative and anti-inflammatory capabilities.These effects are closely associated with the activation of Nrf2 and TLR4/NF-κB/MAPK signaling pathways.展开更多
Aim and Method Comparative molecular field analysis (CoMFA), a threedimensional quantitative structure-activity relationship (3D-QSAR) method was applied to a novelseries of C-3 substituted 4, 6-dichloioindole-2-carbo...Aim and Method Comparative molecular field analysis (CoMFA), a threedimensional quantitative structure-activity relationship (3D-QSAR) method was applied to a novelseries of C-3 substituted 4, 6-dichloioindole-2-carboxylic acids to study the relationship betweentheir structure and the affinity for the glycine site of the NMDA receptor. Result Hie coefficientsof cross-validation q^2 and non cross-validation r^2 for the model established by the study are0.744 and 0.993, respectively, the value of variance ratio F is 261.343, and standard error estimate(SE) is 0.039. Conclusion These values indicate that the CoMFA model may have a good prediction forthe activity of C-3 substituted 4, 6-dichloroin-dole-2-carboxylic acids. As a consequence, thepredicted activity values of new designed compounds supports our conclusion from the model.展开更多
A method for the conversion of α-acetamido-β-substituted phenyl acrylic acid (αtβSPAA)into substituted phenyl lactic acid(SPLA)is described and an improved Clemmensen reduction reagent is used.
The title compounds 2ac were synthesized and characterized for the first time. Their proton numbers are around 3.2±0.15 and are not in proportion with the valid acidity-basicity of the central phosphonic acids. ...The title compounds 2ac were synthesized and characterized for the first time. Their proton numbers are around 3.2±0.15 and are not in proportion with the valid acidity-basicity of the central phosphonic acids. The entirety of phosphonic acids 1a-c is as the coordinate center of heteropoly anions of 2ac.展开更多
Direct reduction of seven benzoic acids to alcohols via sodium borohydride-bromine (NaBH4-Br2) reagent was developed. The isolated yields for the seven acids to reduce reached 60.6-90.1%. This new synthesis route ha...Direct reduction of seven benzoic acids to alcohols via sodium borohydride-bromine (NaBH4-Br2) reagent was developed. The isolated yields for the seven acids to reduce reached 60.6-90.1%. This new synthesis route has the advantages of simple of application, low cost, mild nature, and satisfactory yields.展开更多
A one-pot synthesis of 2-(1-acyloxypcntyl) benzoic acids by trapping the carboxylatc/alkoxide dianion with acylating reagents following Grignard addition with n-BuMgBr to 2-formylbcnzoic acid was described. Compared...A one-pot synthesis of 2-(1-acyloxypcntyl) benzoic acids by trapping the carboxylatc/alkoxide dianion with acylating reagents following Grignard addition with n-BuMgBr to 2-formylbcnzoic acid was described. Compared with routine synthetic method, this novel procedure has the advantage of convenient operation and higher yields.展开更多
The properties of the modified surface of SnO2(110) with benzoic acid (Y-C6H4-COOH: Y is para position relative to -COOH group) derivatives were investigated using density functional theory. Zehner et al. mentioned th...The properties of the modified surface of SnO2(110) with benzoic acid (Y-C6H4-COOH: Y is para position relative to -COOH group) derivatives were investigated using density functional theory. Zehner et al. mentioned that the modification of surface dipole moment made it possible to tune the work function of the system. The experiment of Ganzorig et al. showed that there was a linear relationship between the dipole moment of the binding molecule and the work function change of the system using the modified surface of indium-tin oxide (ITO) with some benzoic acid derivatives. To elucidate the relation between the dipole moment of the molecule and the work function change, we investigated the modified surface of SnO2(110) using Sn7O14 cluster model which was embedded in the fixed point charges. On the modification of the surface, benzoic acid derivatives were bound to SnO2 surface. By changing the terminal group of benzoic acid with H, Cl, F, CF3 and CCl3, the work function changed and the dipole moment of the binding molecules of the modified SnO2(110) were evaluated. The results showed that there was a linear relationship between the dipole moment of the binding molecules and the work function changed. From this relation, the average value of the dipole moments of Sn-OOC linkage at the surface was also evaluated.展开更多
The efficacy of α mercapto β (2_furyl) acrylic acid (MFA), α mercapto β (5_sodiumsulfonate, 2_furyl) acrylic acid (MSFA) and α mercapto β (5_acetoxymethyl, 2_furyl) acrylic acid (MAFA) to mobilize intra...The efficacy of α mercapto β (2_furyl) acrylic acid (MFA), α mercapto β (5_sodiumsulfonate, 2_furyl) acrylic acid (MSFA) and α mercapto β (5_acetoxymethyl, 2_furyl) acrylic acid (MAFA) to mobilize intracellularly bound cadmium in liver and kidney was investigated in rats pre_exposed to cadmium. MFA was effective in reducing cadmium levels of hepatic and renal supernatant cytosolic fraction (SCF) while MSFA and MAFA were effective in lowering cadmium levels of renal SCF and hepatic SCF respectively. All the chelating agents also enhanced the excretion of cadmium more in feces than in urine. However, substitution on the furan ring lowered cadmium mobilizing efficacy of the parent compound, MFA. The treatment with MFA did not affect the status of endogenous zinc and copper while the treatment with MSFA and MAFA enhanced their excretion. MSFA increased hepatic and renal zinc and renal copper while MAFA increased their copper levels.展开更多
Invasive fungal infections have been gaining notoriety due to several factors, mainly their increasing incidence in immunocompromised patients. The aim of the present study was to evaluate the antifungal activity and ...Invasive fungal infections have been gaining notoriety due to several factors, mainly their increasing incidence in immunocompromised patients. The aim of the present study was to evaluate the antifungal activity and toxicity of the 3,4,5-trihydroxybenzoic acid (3,4,5-THB) and of its derivative, the 3,4,5-tris(acetyloxy)benzoic acid (3,4,5-TAB). The 3,4,5-THB was purchased and its derivative was obtained by purifying and characterizing performed using semisynthesis reactions (esterification), recrystallization, column chromatography and infrared analytical techniques and nuclear magnetic resonance. Minimum inhibitory concentration (MIC) and minimum lethal concentration (MLC) were determined in order to evaluate the antifungal activity of the compounds against four clinical isolates and four standard strains of Candida sp. and five clinical isolates of dermatophytes, following the Clinical and Laboratory Standards Institute protocols. The toxicity of the compounds was evaluated by determining the lethal dosis (LD50) using lethality assay of Artemia salina. The most sensitive yeasts to the 3,4,5-THB were C. albicans ATCC 10231 and C. krusei ATCC 6258, both presenting a MIC of 128 μg·mL-1. For Trichophyton sp. and Epidermophyton floccosum, the MIC was 32 μg·mL-1. The 3,4,5-TAB showed a lower inhibitory activity against Candida and dermatophyte species tested. The LD50 of 3,4,5-THB was 222.60 μg·mL-1 and the 3,4,5-TAB showed 481.69 μg·mL-1 of LD50. In conclusion, the 3,4,5-trihydroxybenzoic acid showed antifungal activity against species of medical importance, mainly dermatophytosis-causing fungi, and the 3,4,5-tris(acetyloxy)benzoic acid showed no increasing antifungal activity and toxicity in relation to the original compound.展开更多
Proceeding from natural amino acid L-asparagine and commercially available aldehydes a stereoselective synthesis was developed of (2S,4S)-2-alkyl(aryl)-3-(3-sulfanylpropanoyl)-6-oxohexahy- dropyrimidine-4-carboxylic a...Proceeding from natural amino acid L-asparagine and commercially available aldehydes a stereoselective synthesis was developed of (2S,4S)-2-alkyl(aryl)-3-(3-sulfanylpropanoyl)-6-oxohexahy- dropyrimidine-4-carboxylic acids, potential antihypertensive drugs, inhibitors of the angiotensin converting enzyme.展开更多
A new chemiluminescence flow system has been developed for sequential determina-tion of benzoic acid based on the reaction of the compound with copper carbonate entrapped in a solid-phase reactor. It was found that t...A new chemiluminescence flow system has been developed for sequential determina-tion of benzoic acid based on the reaction of the compound with copper carbonate entrapped in a solid-phase reactor. It was found that the unsaturated complex of Cu(II) and benzoic acid (1:1) has strong catalytic effect on the luminol-H2O2 chemiluminescence reaction. The calibration graph is linear over the range of 0.025 ~ 60 g/mL of benzoic acid, with a relative standard deviation of less than 3.0 %, and the detection limit is 0.01礸穖L-1. The proposed method was applied to the determination of benzoic acid content in different pharmaceutical formulations.展开更多
基金supported by the National Key Research and Development Program(2021YFD1300400)Natural Science Foundation of Guangdong Province(2021A1515010944)Science and Technology Projects in Guangzhou(202201011730).
文摘Background The benefits of combining benzoic acid and essential oils(BAO)to mitigate intestinal impairment during the weaning process have been well established,while the detailed underlying mechanism has not been fully elucidated.Previous research has primarily focused on the reparative effects of BAO on intestinal injury,while neglecting its potential in enhancing intestinal stress resistance.Methods In this study,we investigated the pre-protective effect of BAO against LPS-induced stress using a modified experimental procedure.Piglets were pre-supplemented with BAO for 14 d,followed by a challenge with LPS or saline to collect blood and intestinal samples.Results Our findings demonstrated that BAO supplementation led to significant improvements in piglets’final weight,average daily gain,and feed intake/body gain ratio.Additionally,BAO supplementation positively influenced the composition of intestinal microbiota,increasing beneficial Actinobacteriota and Alloprevotella while reducing harmful Desulfobacterota,Prevotella and Oscillospira.Furthermore,BAO supplementation effectively mitigated oxidative disturbances and inflammatory responses induced by acute LPS challenge.This was evidenced by elevated levels of T-AOC,SOD,and GSH,as well as decreased levels of MDA,TNF-α,and IL-6 in the plasma.Moreover,piglets subjected to LPS challenge and pre-supplemented with BAO exhibited significant improvements in intestinal morphological structure and enhanced integrity,as indicated by restored expression levels of Occludin and Claudin-1 compared to the non-supplemented counterparts.Further analysis revealed that BAO supplementation enhanced the jejunal antioxidative capacity by increasing GSH-Px levels and decreasing MDA levels under the LPS challenge and stimulated the activation of the Nrf2 signaling pathway.Additionally,the reduction of TLR4/NF-κB/MAPK signaling pathways activation and proinflammatory factor were also observed in the jejunal of those piglets fed with BAO.Conclusions In summary,our study demonstrates that pre-supplementation of BAO enhances the anti-stress capacity of weaned piglets by improving intestinal microbiota composition,reinforcing the intestinal barrier,and enhancing antioxidative and anti-inflammatory capabilities.These effects are closely associated with the activation of Nrf2 and TLR4/NF-κB/MAPK signaling pathways.
文摘Aim and Method Comparative molecular field analysis (CoMFA), a threedimensional quantitative structure-activity relationship (3D-QSAR) method was applied to a novelseries of C-3 substituted 4, 6-dichloioindole-2-carboxylic acids to study the relationship betweentheir structure and the affinity for the glycine site of the NMDA receptor. Result Hie coefficientsof cross-validation q^2 and non cross-validation r^2 for the model established by the study are0.744 and 0.993, respectively, the value of variance ratio F is 261.343, and standard error estimate(SE) is 0.039. Conclusion These values indicate that the CoMFA model may have a good prediction forthe activity of C-3 substituted 4, 6-dichloroin-dole-2-carboxylic acids. As a consequence, thepredicted activity values of new designed compounds supports our conclusion from the model.
文摘A method for the conversion of α-acetamido-β-substituted phenyl acrylic acid (αtβSPAA)into substituted phenyl lactic acid(SPLA)is described and an improved Clemmensen reduction reagent is used.
文摘The title compounds 2ac were synthesized and characterized for the first time. Their proton numbers are around 3.2±0.15 and are not in proportion with the valid acidity-basicity of the central phosphonic acids. The entirety of phosphonic acids 1a-c is as the coordinate center of heteropoly anions of 2ac.
文摘Direct reduction of seven benzoic acids to alcohols via sodium borohydride-bromine (NaBH4-Br2) reagent was developed. The isolated yields for the seven acids to reduce reached 60.6-90.1%. This new synthesis route has the advantages of simple of application, low cost, mild nature, and satisfactory yields.
文摘A one-pot synthesis of 2-(1-acyloxypcntyl) benzoic acids by trapping the carboxylatc/alkoxide dianion with acylating reagents following Grignard addition with n-BuMgBr to 2-formylbcnzoic acid was described. Compared with routine synthetic method, this novel procedure has the advantage of convenient operation and higher yields.
文摘The properties of the modified surface of SnO2(110) with benzoic acid (Y-C6H4-COOH: Y is para position relative to -COOH group) derivatives were investigated using density functional theory. Zehner et al. mentioned that the modification of surface dipole moment made it possible to tune the work function of the system. The experiment of Ganzorig et al. showed that there was a linear relationship between the dipole moment of the binding molecule and the work function change of the system using the modified surface of indium-tin oxide (ITO) with some benzoic acid derivatives. To elucidate the relation between the dipole moment of the molecule and the work function change, we investigated the modified surface of SnO2(110) using Sn7O14 cluster model which was embedded in the fixed point charges. On the modification of the surface, benzoic acid derivatives were bound to SnO2 surface. By changing the terminal group of benzoic acid with H, Cl, F, CF3 and CCl3, the work function changed and the dipole moment of the binding molecules of the modified SnO2(110) were evaluated. The results showed that there was a linear relationship between the dipole moment of the binding molecules and the work function changed. From this relation, the average value of the dipole moments of Sn-OOC linkage at the surface was also evaluated.
文摘The efficacy of α mercapto β (2_furyl) acrylic acid (MFA), α mercapto β (5_sodiumsulfonate, 2_furyl) acrylic acid (MSFA) and α mercapto β (5_acetoxymethyl, 2_furyl) acrylic acid (MAFA) to mobilize intracellularly bound cadmium in liver and kidney was investigated in rats pre_exposed to cadmium. MFA was effective in reducing cadmium levels of hepatic and renal supernatant cytosolic fraction (SCF) while MSFA and MAFA were effective in lowering cadmium levels of renal SCF and hepatic SCF respectively. All the chelating agents also enhanced the excretion of cadmium more in feces than in urine. However, substitution on the furan ring lowered cadmium mobilizing efficacy of the parent compound, MFA. The treatment with MFA did not affect the status of endogenous zinc and copper while the treatment with MSFA and MAFA enhanced their excretion. MSFA increased hepatic and renal zinc and renal copper while MAFA increased their copper levels.
文摘Invasive fungal infections have been gaining notoriety due to several factors, mainly their increasing incidence in immunocompromised patients. The aim of the present study was to evaluate the antifungal activity and toxicity of the 3,4,5-trihydroxybenzoic acid (3,4,5-THB) and of its derivative, the 3,4,5-tris(acetyloxy)benzoic acid (3,4,5-TAB). The 3,4,5-THB was purchased and its derivative was obtained by purifying and characterizing performed using semisynthesis reactions (esterification), recrystallization, column chromatography and infrared analytical techniques and nuclear magnetic resonance. Minimum inhibitory concentration (MIC) and minimum lethal concentration (MLC) were determined in order to evaluate the antifungal activity of the compounds against four clinical isolates and four standard strains of Candida sp. and five clinical isolates of dermatophytes, following the Clinical and Laboratory Standards Institute protocols. The toxicity of the compounds was evaluated by determining the lethal dosis (LD50) using lethality assay of Artemia salina. The most sensitive yeasts to the 3,4,5-THB were C. albicans ATCC 10231 and C. krusei ATCC 6258, both presenting a MIC of 128 μg·mL-1. For Trichophyton sp. and Epidermophyton floccosum, the MIC was 32 μg·mL-1. The 3,4,5-TAB showed a lower inhibitory activity against Candida and dermatophyte species tested. The LD50 of 3,4,5-THB was 222.60 μg·mL-1 and the 3,4,5-TAB showed 481.69 μg·mL-1 of LD50. In conclusion, the 3,4,5-trihydroxybenzoic acid showed antifungal activity against species of medical importance, mainly dermatophytosis-causing fungi, and the 3,4,5-tris(acetyloxy)benzoic acid showed no increasing antifungal activity and toxicity in relation to the original compound.
文摘Proceeding from natural amino acid L-asparagine and commercially available aldehydes a stereoselective synthesis was developed of (2S,4S)-2-alkyl(aryl)-3-(3-sulfanylpropanoyl)-6-oxohexahy- dropyrimidine-4-carboxylic acids, potential antihypertensive drugs, inhibitors of the angiotensin converting enzyme.
文摘A new chemiluminescence flow system has been developed for sequential determina-tion of benzoic acid based on the reaction of the compound with copper carbonate entrapped in a solid-phase reactor. It was found that the unsaturated complex of Cu(II) and benzoic acid (1:1) has strong catalytic effect on the luminol-H2O2 chemiluminescence reaction. The calibration graph is linear over the range of 0.025 ~ 60 g/mL of benzoic acid, with a relative standard deviation of less than 3.0 %, and the detection limit is 0.01礸穖L-1. The proposed method was applied to the determination of benzoic acid content in different pharmaceutical formulations.