OBJECTIVE The inhibitory effect of active ingredients of Tripterygium wilfordii Hook.F.(TWHF)(celastrol,triptolide,triptonide,wilforlide A,wilforgine and wilforine)on human carboxylester⁃ase 1(CES1)and CES2 was detect...OBJECTIVE The inhibitory effect of active ingredients of Tripterygium wilfordii Hook.F.(TWHF)(celastrol,triptolide,triptonide,wilforlide A,wilforgine and wilforine)on human carboxylester⁃ase 1(CES1)and CES2 was detected to investigate the herb-drug interactions(HDIs)of TWHF.METHODS Human liver microsomes catalysed hydrolysis of 2-(2-benzoyl-3-methoxyphenyl)benzothi⁃azole(BMBT)and fluorescein diacetate(FD)were used as the probe reaction to phenotype the activity of CES1 and CES2,respectively.The residual activities of CES1 and CES2 were detected by ultrahigh performance liquid chromatography(UPLC)after intervention with celastrol,triptolide,triptonide,wilforlide A,wilforgine and wilforine(100μmol·L^(-1)).Kinetics analysis,involving half inhibitory concentra⁃tion(IC_(50)),inhibition type and kinetic parameter(Ki),and in vitro-in vivo extrapolation(IVIVE),was carried out to predict the HDIs between these compounds and CES-metabolizing drugs.Molecular docking was performed to analyze the ligand-enzyme interaction.RESULTS Out of the six main con⁃stituents of TWHF,only celastrol exhibited strong inhibition towards both CES1 and CES2,with the inhibitory rates of 97.45%(P<0.05)and 95.62%(P<0.05),respectively.The IC_(50)was 9.95 and 4.02 mol·L^(-1),respectively,and the types of inhibition were all non-competitive inhibition.Based on the kinetics analysis,the Ki values were calculated to be 5.10 and 10.55μmol·L^(-1)for the inhibition of celastrol on CES1 and CES2,respectively.IVIVE indicated that celastrol might disturb the metabolic hydrolysis of clinical drugs in vivo by inhibiting CES1.Molecular docking results showed that hydrogen bonds and hydrophobic contacts contributed to the interaction of celastrol and CESs.CONCLUSION The inhibitory effect of celastrol on CES1 and CES2 might cause HDIs with clinical drugs hydrolysed by CESs.展开更多
This study aimed to understand the growing development and physiological characteristics of seeds harvested different days after pollination and the seedlings emerged from the seeds of yellow-seeded Brassica napus L.....This study aimed to understand the growing development and physiological characteristics of seeds harvested different days after pollination and the seedlings emerged from the seeds of yellow-seeded Brassica napus L..Two yellow-seeded cultivars‘Hongyuan 558’and‘Qinyou 806’were selected in this study,and 50 seeds were collected 30,35,and 40 d after pollination,respectively.The seeds were weighed and placed on filter paper for hydroponic experiments.The seed germination rate was determined 3-5 d later.The physiological indicators including superoxide dismutase(SOD),peroxidase(POD),and catalase(CAT)activities and malondialdehyde(MDA)content were measured for the seeds harvested different days after pollination and the 7-day-seedlings emerged from the seeds.The results showed that the seed dry weights and germination rates of both‘Qinyou 806’and‘Hongyuan 558’increased as the days after pollination increased,especially 30-35 d after pollination.The germination rate and dry and fresh weights of the seeds showed no significant differences between the two cultivars,and almost all the seeds germinated 40 d after pollination.As the days after pollination increased,the SOD activities in the seeds of both cultivars first increased and then decreased,reaching their peaks 35 d after pollination,which may be related to encountering adverse stress.The POD activity in the seeds of‘Qinyou 806’kept declining,and that of‘Hongyuan 558’first increased and then decreased,which may be related to the antioxidant mechanism and adaptive regulation.The CAT activities in the seeds of both cultivars first decreased and then increased.The MDA content in the seeds of‘Qinyou 806’first decreased and then increased,while that of‘Hongyuan 558’kept reducing and was the highest in the seeds 30 d after pollination,which indicated‘Hongyuan 558’was mildly affected by the environment and had strong resistance.The activities of SOD and POD in the seedlings of two cultivars that were emerged from the seeds 35-40 d after pollination became weakened,which may be related to their exposure to stress.The CAT activity in the seedlings of‘Hongyuan 558’was generally higher than that of‘Qinyou 806’,indicating that‘Hongyuan 558’had stronger stress resistance.The MDA content in the seedlings emerged from the seeds 35-40 d after pollination showed a decreasing trend,indicating that the seedlings emerged from the seeds harvested at this stage had mild cell membrane damage and enhanced stress resistance.In conclusion,‘Hongyuan 558’had strong environmental adaptability and stress resistance.展开更多
Pectinex XXL,a commercially prepared pectinase,was investigated for its potential application in the fruit juice industry.Polygalacturonic acid was used as the substrate for determining the enzymatic properties of Pec...Pectinex XXL,a commercially prepared pectinase,was investigated for its potential application in the fruit juice industry.Polygalacturonic acid was used as the substrate for determining the enzymatic properties of Pectinex XXL using the DNS method.According to the results,the optimal pH for Pectinex XXL activity was 4.5,and the enzyme was stable in the pH range of 3.0~4.5.The optimal pH and pH stability range are consistent with those of some tropical and subtropical fruits.The optimal temperature for Pectinex XXL activity was 60℃,and the enzyme remained stable after one hour in a water bath set at 40℃.Additionally,the enzymatic activity was not inhibited in the presence of 1 mmol/L of Na^(+),Mg^(2+),Ba^(2+),Co^(2+),Zn^(2+),and Fe^(2+),whereas it was slightly inhibited in the presence of 2 mmol/L of K^(+)and Fe^(2+)and partially inhibited in the presence of 1 and 2 mmol/L of Ca^(2+)and Mn^(2+),demonstrating its good stability in acids and excellent thermal catalytic performance.Based on the above experimental results,depectinization experiments were performed on plantain and cherry tomato juices using different amounts of Pectinex XXL.After one hour reaction with 16 U/mL of the enzyme,the yields of the plantain and cherry tomato juices were substantially increased by 119.03%and 15.97%,respectively,while their light transmittance was remarkably enhanced by 37.65%and 12.35%,respectively.Furthermore,the enzyme reduced the viscosity of the plantain and cherry tomato juices by 88.29%and 29.50%,respectively.The juice production experiments confirmed that this enzyme can significantly improve the yield and light transmittance of plantain juice,while effectively reducing its viscosity.These findings indicate the potential of Pectinex XXL in the industrial production of plantain juice.展开更多
文摘OBJECTIVE The inhibitory effect of active ingredients of Tripterygium wilfordii Hook.F.(TWHF)(celastrol,triptolide,triptonide,wilforlide A,wilforgine and wilforine)on human carboxylester⁃ase 1(CES1)and CES2 was detected to investigate the herb-drug interactions(HDIs)of TWHF.METHODS Human liver microsomes catalysed hydrolysis of 2-(2-benzoyl-3-methoxyphenyl)benzothi⁃azole(BMBT)and fluorescein diacetate(FD)were used as the probe reaction to phenotype the activity of CES1 and CES2,respectively.The residual activities of CES1 and CES2 were detected by ultrahigh performance liquid chromatography(UPLC)after intervention with celastrol,triptolide,triptonide,wilforlide A,wilforgine and wilforine(100μmol·L^(-1)).Kinetics analysis,involving half inhibitory concentra⁃tion(IC_(50)),inhibition type and kinetic parameter(Ki),and in vitro-in vivo extrapolation(IVIVE),was carried out to predict the HDIs between these compounds and CES-metabolizing drugs.Molecular docking was performed to analyze the ligand-enzyme interaction.RESULTS Out of the six main con⁃stituents of TWHF,only celastrol exhibited strong inhibition towards both CES1 and CES2,with the inhibitory rates of 97.45%(P<0.05)and 95.62%(P<0.05),respectively.The IC_(50)was 9.95 and 4.02 mol·L^(-1),respectively,and the types of inhibition were all non-competitive inhibition.Based on the kinetics analysis,the Ki values were calculated to be 5.10 and 10.55μmol·L^(-1)for the inhibition of celastrol on CES1 and CES2,respectively.IVIVE indicated that celastrol might disturb the metabolic hydrolysis of clinical drugs in vivo by inhibiting CES1.Molecular docking results showed that hydrogen bonds and hydrophobic contacts contributed to the interaction of celastrol and CESs.CONCLUSION The inhibitory effect of celastrol on CES1 and CES2 might cause HDIs with clinical drugs hydrolysed by CESs.
基金Supported by Major Project of Agricultural Biological Breeding(2023ZD0404205)Science and Technology Plan Project of Changsha City(kq2107016)。
文摘This study aimed to understand the growing development and physiological characteristics of seeds harvested different days after pollination and the seedlings emerged from the seeds of yellow-seeded Brassica napus L..Two yellow-seeded cultivars‘Hongyuan 558’and‘Qinyou 806’were selected in this study,and 50 seeds were collected 30,35,and 40 d after pollination,respectively.The seeds were weighed and placed on filter paper for hydroponic experiments.The seed germination rate was determined 3-5 d later.The physiological indicators including superoxide dismutase(SOD),peroxidase(POD),and catalase(CAT)activities and malondialdehyde(MDA)content were measured for the seeds harvested different days after pollination and the 7-day-seedlings emerged from the seeds.The results showed that the seed dry weights and germination rates of both‘Qinyou 806’and‘Hongyuan 558’increased as the days after pollination increased,especially 30-35 d after pollination.The germination rate and dry and fresh weights of the seeds showed no significant differences between the two cultivars,and almost all the seeds germinated 40 d after pollination.As the days after pollination increased,the SOD activities in the seeds of both cultivars first increased and then decreased,reaching their peaks 35 d after pollination,which may be related to encountering adverse stress.The POD activity in the seeds of‘Qinyou 806’kept declining,and that of‘Hongyuan 558’first increased and then decreased,which may be related to the antioxidant mechanism and adaptive regulation.The CAT activities in the seeds of both cultivars first decreased and then increased.The MDA content in the seeds of‘Qinyou 806’first decreased and then increased,while that of‘Hongyuan 558’kept reducing and was the highest in the seeds 30 d after pollination,which indicated‘Hongyuan 558’was mildly affected by the environment and had strong resistance.The activities of SOD and POD in the seedlings of two cultivars that were emerged from the seeds 35-40 d after pollination became weakened,which may be related to their exposure to stress.The CAT activity in the seedlings of‘Hongyuan 558’was generally higher than that of‘Qinyou 806’,indicating that‘Hongyuan 558’had stronger stress resistance.The MDA content in the seedlings emerged from the seeds 35-40 d after pollination showed a decreasing trend,indicating that the seedlings emerged from the seeds harvested at this stage had mild cell membrane damage and enhanced stress resistance.In conclusion,‘Hongyuan 558’had strong environmental adaptability and stress resistance.
文摘Pectinex XXL,a commercially prepared pectinase,was investigated for its potential application in the fruit juice industry.Polygalacturonic acid was used as the substrate for determining the enzymatic properties of Pectinex XXL using the DNS method.According to the results,the optimal pH for Pectinex XXL activity was 4.5,and the enzyme was stable in the pH range of 3.0~4.5.The optimal pH and pH stability range are consistent with those of some tropical and subtropical fruits.The optimal temperature for Pectinex XXL activity was 60℃,and the enzyme remained stable after one hour in a water bath set at 40℃.Additionally,the enzymatic activity was not inhibited in the presence of 1 mmol/L of Na^(+),Mg^(2+),Ba^(2+),Co^(2+),Zn^(2+),and Fe^(2+),whereas it was slightly inhibited in the presence of 2 mmol/L of K^(+)and Fe^(2+)and partially inhibited in the presence of 1 and 2 mmol/L of Ca^(2+)and Mn^(2+),demonstrating its good stability in acids and excellent thermal catalytic performance.Based on the above experimental results,depectinization experiments were performed on plantain and cherry tomato juices using different amounts of Pectinex XXL.After one hour reaction with 16 U/mL of the enzyme,the yields of the plantain and cherry tomato juices were substantially increased by 119.03%and 15.97%,respectively,while their light transmittance was remarkably enhanced by 37.65%and 12.35%,respectively.Furthermore,the enzyme reduced the viscosity of the plantain and cherry tomato juices by 88.29%and 29.50%,respectively.The juice production experiments confirmed that this enzyme can significantly improve the yield and light transmittance of plantain juice,while effectively reducing its viscosity.These findings indicate the potential of Pectinex XXL in the industrial production of plantain juice.
