Polychaete Neanthes japonica is a species geographically specific in China and Japan with important scientific implication and commercial value. In this study, the relations of body weight, salinity and temperature to...Polychaete Neanthes japonica is a species geographically specific in China and Japan with important scientific implication and commercial value. In this study, the relations of body weight, salinity and temperature to oxygen consumption and ammonia excretion of N. japonica were determined. Three different groups in body weight （large： 2.34±0.36 g, middle： 1.50±0.21 g and small： 0.62±0.12 g） were set for all experiments. Results show that the body weight is negatively related to the rates of oxygen consumption and ammonia excretion; and the relationship is significant. The oxygen consumption and ammonia excretion at 24℃ decreased at salinity from 5 to 30 and increased above 30, indicating that both lower and higher salinity are adverse and certain degree of salinity stress is necessary for enhancing the energy demand. At salinity 30, rising temperature from 18℃ to 30℃, the oxygen consumption increased before 27℃ and then decreased. However, the relation of ammonia excretion and temperature seems more complex. Two-way ANOVA shows that salinity, temperature and body weight all have a significant effect on the oxygen consumption and ammonia excretion of the worm. Moreover, interaction between salinity/temperature and body weight is also significant. O：N （oxygen/nitrogen） ratio varies greatly in this case from 5.97 to 463.22, indicating that N. japonica can regulate the type of metabolic substrate against environment changes.展开更多
Polychaetes provide an excellent food resource for fi sh and represent the dominant zoobenthos in marine ecosystems. Diel variation in the rates of metabolism and ammonia-N excretion of Marphysa sanguinea were studied...Polychaetes provide an excellent food resource for fi sh and represent the dominant zoobenthos in marine ecosystems. Diel variation in the rates of metabolism and ammonia-N excretion of Marphysa sanguinea were studied. The worms were grouped according to their wet body weight into small（S; 1.24±0.06 g）, medium（M; 4.00±0.30 g）, and large（L; 8.54±1.08 g） categories. Their weight-specifi c metabolic rates, based on aerobic respiration（ R）, were measured at 16℃（±0.2℃） and classed as either routine（ RR） or standard（ RS） rates. Both respiration types decreased with increasing body weight. Respiration was described by R = a W^b, where b was-0.400 9 and-0.532 0 for RR and RS, respectively. Diurnal changes in RS for each group was relatively flat, with a slightly increasing trend with time, but was relatively stable as a whole. RR of the diurnal variation of worms was higher than RS, but both had similar overall trends. The peak values of specifi c dynamic action（SDA）（ RSDA） in the S, M, and L groups were 2.704, 1.149, and 0.682 mg/（g·h）, respectively. The durations of SDA were 13, 6, and 6 h, respectively and the energy expenditures of SDA were 377.98, 117.34, and 74.94 J/g, respectively. These data indicate that the metabolic rates were higher in smaller individuals, which is advantageous for their rapid growth.展开更多
AIM: To investigate the tissue distribution, urinary and fecal excretions of 125I-lidamycin (125I-C-1027) in mice and its biliary excretion in rats. METHODS:The total radioactivity assay (RA method) and the radioactiv...AIM: To investigate the tissue distribution, urinary and fecal excretions of 125I-lidamycin (125I-C-1027) in mice and its biliary excretion in rats. METHODS:The total radioactivity assay (RA method) and the radioactivity assay after precipitation with 200 mL/L trichloroacetic add (TCA-RA method) were used to dete-rmine the tissue distribution,and the urinary and fecal excretions of 125I-C-1027 in mice and its biliary excretion in rats. RESULTS:Tissue concentrations reached the peak at the fifth minute after administration of 125I-C-1027 to mice. The highest concentration was in kidney, and the lowest in brain at all test-time points. The organs of the concentrations of 125I-C-1027 from high to low were kidney, lung, liver, stomach, spleen, uterus, ovary, intestine, muscle, heart, testis, fat, and brain in mice. The accumulative excretion amounts of 0-24 h, and 0-96 h after administration of 125I-C-1027 were 68.36 and 71.64% in urine, and 2.60 and 3.21% in feces of mice, respectively, and the accumulative excretion amount of 0-24 h was 3.57% in bile in rats. CONCLUSION: Our results reflect the characteristics of the tissue distribution, urinary and fecal excretions of 125I-C-1027 in mice and the biliary excretion of 125I-C-1027 and its metabolites in rats, and indicate that 125I-C-1027 and its metabolites are mainly distributed in kidney, and excreted in urine.展开更多
The effects of 60 day starvation on survival rate, condition index (CI), changes of nutrient composition of different tissues, respiration and excretion of scallop Chlamys farreri were studied in laboratory from Oct. ...The effects of 60 day starvation on survival rate, condition index (CI), changes of nutrient composition of different tissues, respiration and excretion of scallop Chlamys farreri were studied in laboratory from Oct. 17 to Dec. 15,1997. Two groups (control and starvation with 200 individuals each) were cultured in two 2 m 3 tanks, with 31 to 32 salinity water at 17℃. Starvation effects were measured after 10, 20, 40 and 60 days. There was no mass mortality of scallops of the two tanks and survival rates of the control and starvation groups were 93.5% and 92.0%, respectively. Starvation had strong effect on the meat condition of the scallops, especially after 10 days; when relative lipid percentage dropped sharply while relative protein percentage increased. The impact of starvation on the oxygen consumption rate (OCR) and the ammonia N excretion rate (AER) was obvious. The OCR increased rapidly after 10 days but decreased after 20 days. The AER increased after 10 days and 20 days, but decreased obviously from 20 to 40 days. The O:N ratios varied to different degrees, and minimized after 20 days. The low O:N ratios implied that the protein was the main material for the metabolism of C. farreri.展开更多
Objective To explore the anti-inflammatory phytoconstituents from various plant sources as tumour necrosis factor-α(TNF-α)-inhibitor,a mediator involved in the inflammatory disorder,by in silico molecular docking.Me...Objective To explore the anti-inflammatory phytoconstituents from various plant sources as tumour necrosis factor-α(TNF-α)-inhibitor,a mediator involved in the inflammatory disorder,by in silico molecular docking.Methods Based on previous findings,we performed the in silico assessment of anti-inflammatory phytoconstituents from different medicinal plants to understand their binding patterns against TNF-α(PDB ID:6OP0)using AutoDock Vina.Molecular docking was performed by setting a grid box(25×25×25)Åcentered at[-12.817×(-1.618)×19.009]A with 0.375A of grid spacing.Furthermore,Discovery Studio Client 2020 program was utilized to assess two-and three-dimensional(2D and 3D)hydrogen-bond interactions concerning an amino acid of target and ligand.Physicochemical properties were reported using the Lipinski’s rule and SwissADME database to support the in silico findings.Results From the selected medicinal plants,more than 200 phytocompounds were screened against TNF-α protein with binding scores in the range of -12.3 to -2.5 kcal/mol.Amongst them,emodin,aloe-emodin,pongamol,purpuritenin,semiglabrin,ellagic acid,imperatorin,α-tocopherol,and octanorcucurbitacin A showed good binding affinity as -10.6,-10.0,-10.5,-10.1,-11.2,-10.3,-10.1,-10.1,and -10.0 kcal/mol,respectively.Also,the absorption,distribution,metabolism,excretion,and toxicology(ADMET)profiles were well within acceptable limits.Conclusion Based on our preliminary findings,we conclude that the selected phytoconstituents have the potential to be good anti-inflammatory candidates by inhibiting the TNF-α target.These compounds can be further optimized and validated as new therapeutic components to develop more effective and safe anti-inflammatory drugs.展开更多
Drug discovery is a costly and time-consuming process, with very few novel molecular entities approved for clinical use today. With the advancement of computational chemistry, integrated X-ray crystallography and nucl...Drug discovery is a costly and time-consuming process, with very few novel molecular entities approved for clinical use today. With the advancement of computational chemistry, integrated X-ray crystallography and nuclear magnetic resonance spectroscopy technology, more and more potential therapeutic agents for the treatment of human diseases are discovered. Furthermore, multiple medicinal chemistry approaches have been developed in support of early drug discovery. However, there is still much can be done in the early phase of drug discovery to improve the chances of success of a drug candidate. This paper reviews the discovery and evaluation of new chemical entities in the early stages of drug development.展开更多
基金Supported by the National Natural Science Foundation of China (No. 30490233)the Three-Gorge Project and the Estuarine Environment (No. SX2004-018) from the Three Gorges Project Construction Committee
文摘Polychaete Neanthes japonica is a species geographically specific in China and Japan with important scientific implication and commercial value. In this study, the relations of body weight, salinity and temperature to oxygen consumption and ammonia excretion of N. japonica were determined. Three different groups in body weight （large： 2.34±0.36 g, middle： 1.50±0.21 g and small： 0.62±0.12 g） were set for all experiments. Results show that the body weight is negatively related to the rates of oxygen consumption and ammonia excretion; and the relationship is significant. The oxygen consumption and ammonia excretion at 24℃ decreased at salinity from 5 to 30 and increased above 30, indicating that both lower and higher salinity are adverse and certain degree of salinity stress is necessary for enhancing the energy demand. At salinity 30, rising temperature from 18℃ to 30℃, the oxygen consumption increased before 27℃ and then decreased. However, the relation of ammonia excretion and temperature seems more complex. Two-way ANOVA shows that salinity, temperature and body weight all have a significant effect on the oxygen consumption and ammonia excretion of the worm. Moreover, interaction between salinity/temperature and body weight is also significant. O：N （oxygen/nitrogen） ratio varies greatly in this case from 5.97 to 463.22, indicating that N. japonica can regulate the type of metabolic substrate against environment changes.
基金Supported by the National Natural Science Foundation of China(No.30901107)the National Marine Public Welfare Research Project(Nos.201305002,201305043)the Project of Marine Ecological Restoration Technology Research to the Penglai 19-3 Oil Spill Accident(No.19-3YJ09)
文摘Polychaetes provide an excellent food resource for fi sh and represent the dominant zoobenthos in marine ecosystems. Diel variation in the rates of metabolism and ammonia-N excretion of Marphysa sanguinea were studied. The worms were grouped according to their wet body weight into small（S; 1.24±0.06 g）, medium（M; 4.00±0.30 g）, and large（L; 8.54±1.08 g） categories. Their weight-specifi c metabolic rates, based on aerobic respiration（ R）, were measured at 16℃（±0.2℃） and classed as either routine（ RR） or standard（ RS） rates. Both respiration types decreased with increasing body weight. Respiration was described by R = a W^b, where b was-0.400 9 and-0.532 0 for RR and RS, respectively. Diurnal changes in RS for each group was relatively flat, with a slightly increasing trend with time, but was relatively stable as a whole. RR of the diurnal variation of worms was higher than RS, but both had similar overall trends. The peak values of specifi c dynamic action（SDA）（ RSDA） in the S, M, and L groups were 2.704, 1.149, and 0.682 mg/（g·h）, respectively. The durations of SDA were 13, 6, and 6 h, respectively and the energy expenditures of SDA were 377.98, 117.34, and 74.94 J/g, respectively. These data indicate that the metabolic rates were higher in smaller individuals, which is advantageous for their rapid growth.
基金Supported by the National High Technology Research and Development Program of China (863 Program), No. 2003AA2Z347D
文摘AIM: To investigate the tissue distribution, urinary and fecal excretions of 125I-lidamycin (125I-C-1027) in mice and its biliary excretion in rats. METHODS:The total radioactivity assay (RA method) and the radioactivity assay after precipitation with 200 mL/L trichloroacetic add (TCA-RA method) were used to dete-rmine the tissue distribution,and the urinary and fecal excretions of 125I-C-1027 in mice and its biliary excretion in rats. RESULTS:Tissue concentrations reached the peak at the fifth minute after administration of 125I-C-1027 to mice. The highest concentration was in kidney, and the lowest in brain at all test-time points. The organs of the concentrations of 125I-C-1027 from high to low were kidney, lung, liver, stomach, spleen, uterus, ovary, intestine, muscle, heart, testis, fat, and brain in mice. The accumulative excretion amounts of 0-24 h, and 0-96 h after administration of 125I-C-1027 were 68.36 and 71.64% in urine, and 2.60 and 3.21% in feces of mice, respectively, and the accumulative excretion amount of 0-24 h was 3.57% in bile in rats. CONCLUSION: Our results reflect the characteristics of the tissue distribution, urinary and fecal excretions of 125I-C-1027 in mice and the biliary excretion of 125I-C-1027 and its metabolites in rats, and indicate that 125I-C-1027 and its metabolites are mainly distributed in kidney, and excreted in urine.
文摘The effects of 60 day starvation on survival rate, condition index (CI), changes of nutrient composition of different tissues, respiration and excretion of scallop Chlamys farreri were studied in laboratory from Oct. 17 to Dec. 15,1997. Two groups (control and starvation with 200 individuals each) were cultured in two 2 m 3 tanks, with 31 to 32 salinity water at 17℃. Starvation effects were measured after 10, 20, 40 and 60 days. There was no mass mortality of scallops of the two tanks and survival rates of the control and starvation groups were 93.5% and 92.0%, respectively. Starvation had strong effect on the meat condition of the scallops, especially after 10 days; when relative lipid percentage dropped sharply while relative protein percentage increased. The impact of starvation on the oxygen consumption rate (OCR) and the ammonia N excretion rate (AER) was obvious. The OCR increased rapidly after 10 days but decreased after 20 days. The AER increased after 10 days and 20 days, but decreased obviously from 20 to 40 days. The O:N ratios varied to different degrees, and minimized after 20 days. The low O:N ratios implied that the protein was the main material for the metabolism of C. farreri.
文摘Objective To explore the anti-inflammatory phytoconstituents from various plant sources as tumour necrosis factor-α(TNF-α)-inhibitor,a mediator involved in the inflammatory disorder,by in silico molecular docking.Methods Based on previous findings,we performed the in silico assessment of anti-inflammatory phytoconstituents from different medicinal plants to understand their binding patterns against TNF-α(PDB ID:6OP0)using AutoDock Vina.Molecular docking was performed by setting a grid box(25×25×25)Åcentered at[-12.817×(-1.618)×19.009]A with 0.375A of grid spacing.Furthermore,Discovery Studio Client 2020 program was utilized to assess two-and three-dimensional(2D and 3D)hydrogen-bond interactions concerning an amino acid of target and ligand.Physicochemical properties were reported using the Lipinski’s rule and SwissADME database to support the in silico findings.Results From the selected medicinal plants,more than 200 phytocompounds were screened against TNF-α protein with binding scores in the range of -12.3 to -2.5 kcal/mol.Amongst them,emodin,aloe-emodin,pongamol,purpuritenin,semiglabrin,ellagic acid,imperatorin,α-tocopherol,and octanorcucurbitacin A showed good binding affinity as -10.6,-10.0,-10.5,-10.1,-11.2,-10.3,-10.1,-10.1,and -10.0 kcal/mol,respectively.Also,the absorption,distribution,metabolism,excretion,and toxicology(ADMET)profiles were well within acceptable limits.Conclusion Based on our preliminary findings,we conclude that the selected phytoconstituents have the potential to be good anti-inflammatory candidates by inhibiting the TNF-α target.These compounds can be further optimized and validated as new therapeutic components to develop more effective and safe anti-inflammatory drugs.
基金The Shanghai Committee of Science and Technology (Grant No.11DZ2260600)the Fundamental Research Funds for the Central Universities
文摘Drug discovery is a costly and time-consuming process, with very few novel molecular entities approved for clinical use today. With the advancement of computational chemistry, integrated X-ray crystallography and nuclear magnetic resonance spectroscopy technology, more and more potential therapeutic agents for the treatment of human diseases are discovered. Furthermore, multiple medicinal chemistry approaches have been developed in support of early drug discovery. However, there is still much can be done in the early phase of drug discovery to improve the chances of success of a drug candidate. This paper reviews the discovery and evaluation of new chemical entities in the early stages of drug development.
