Objective Lidamycin （LDM） can be dissociated to an apoprotein （LDP） and an active enediyne chromophore （AE）. The detached AE can reassemble with its LDP-containing fusion protein to endow the latter with potent ...Objective Lidamycin （LDM） can be dissociated to an apoprotein （LDP） and an active enediyne chromophore （AE）. The detached AE can reassemble with its LDP-containing fusion protein to endow the latter with potent antitumor activity. However, the reassembly of AE with LDP is affected by several factors. Our aim was to optimize the assembly efficiency of the AE with a LDP-containing fusion protein and investigate the influence of several factors on the assembly efficacy. Methods A method based on RP-HPLC was developed to analyze the assembly rate, and an orthogonal experimental design L9 （3^4） was used to investigate the effects of temperature, assembly time, pH and molecular ratio of LDP-containing fusion protein to AE on the assembly rate. Furthermore, the determined optimum conditions for the assembly rate of the LDP-containing fusion protein with AE were applied and evaluated. Results A calibration curve based on the LDM micromolar concentration against the peak-area of AE by HPLC was obtained. The order in which individual factors in the orthogonal experiment affected the assembly rate were temperature〉time〉pH〉molar ratio of AE to protein and all were statistically significant （P〈0.01）. The optimal assembly conditions were temperature at 10 ℃, time of 12 h, pH 7.0, and the molar ratio of AE： protein of 5：1. The assembly rate of AE with a LDP-containing fusion protein was improved by 23% after condition optimization. Conclusion The assembly rate of chromophore of lidamycin with its LDP-containing fusion protein was improved after condition optimization by orthogonal design, and the optimal conditions described herein should prove useful for the development of this type of LDP-containing fusion protein.展开更多
To improve antagonistic metabolites production of Bacillus subtilis strain BS501a, physical parameters of fermentation and metal inorganic salts in medium, namely initial pH value, culture temperature, fermentation ti...To improve antagonistic metabolites production of Bacillus subtilis strain BS501a, physical parameters of fermentation and metal inorganic salts in medium, namely initial pH value, culture temperature, fermentation time, concentrations of CaC12, FeSO4, ZnSO4, MnSO4 and MgSO4, were optimized using one-factor-at-a-time and orthogonal tests. The results show that the optimal physical parameters of fermentation are an initial pH of 7.0, a culture temperature of 30 ~C, and a fermentation time of 48 h. The optimal concentrations of metal inorganic salts in basal medium are 10.2 mmol/L CaCl2, 0.4 mmol/L FeSO4, 3.5 mmol/L ZnSO4, 0.6 mmol/L MnSO4 and 2.0 mmol/L MgSO4. Among the metal inorganic salts, MgSO4 and MnSO4 play important roles in the improvement of the antagonistic metabolites production of B. subtilis strain BS501a; especially, MgSO4 contributes a highly significant effect. The average diameter of inhibition zone of the BS501a filtered fermentation supernatant （FFS） cultured in the optimal fermentation conditions against Magnaporthe grisea DWBJ329 reaches 71.4 mm, and there is 2.4-fold increase in antifungal activity as compared with 21.2 mm under the pre-optimized conditions.展开更多
An attempt has been made to study the influence of wear parameters like applied load, sliding speed, sliding distance and percentage of reinforcement on the dry sliding wear of the metal matrix composites. A plan of e...An attempt has been made to study the influence of wear parameters like applied load, sliding speed, sliding distance and percentage of reinforcement on the dry sliding wear of the metal matrix composites. A plan of experiments, based on techniques of Taguchi, was performed to acquire data in controlled way. An orthogonal array and the analysis of variance were employed to investigate the influence of process parameters on the wear of composites. The objective is to establish a correlation between dry sliding wear of composites and wear parameters. These correlations were obtained by multiple regressions. Finally, confirmation tests were conducted to verify the experimental results foreseen from the mentioned correlations.展开更多
To estimate the direction-of-arrival （DOA） of wideband coherent signals, a new method by modifying the orthogonality of the projected suhspaces method is proposed. And it can deal with randomly position perturbed ar...To estimate the direction-of-arrival （DOA） of wideband coherent signals, a new method by modifying the orthogonality of the projected suhspaces method is proposed. And it can deal with randomly position perturbed arrays by using the Toeplitz method. This method needn＇t the primary information of DOA for focusing matrix and the sector dividing of interpolated method, which improving the precision of estimation and reducing the computational complexity. Simulations illustrate the effectiveness of this method.展开更多
Duloxetine hydrochloride enteric coated pellets were formulated using fluidized bed.Three separate layers,the drug layer,the barrier layer,and the enteric layer,were coated onto the inert core pellets.The pellets were...Duloxetine hydrochloride enteric coated pellets were formulated using fluidized bed.Three separate layers,the drug layer,the barrier layer,and the enteric layer,were coated onto the inert core pellets.The pellets were optimized with the acid resistance and drug release in simulated intestinal fluid as the process parameters,using the Taguchi L9 orthogonal array.Various other properties,such as surface morphology,bulk and tapped density,Hausner’s ratio,hardness,friability,yield of pellets,moisture content,and particle size distribution,were also studied in the optimized pellets.The concentration of the enteric polymer played a vital role in acid resistance,while the type of enteric polymer affected the drug release in simulated intestinal fluid.In both cases,it was determined that binder polymer concentration was not affected much.The comparisons between the optimized pellets and a market formulation yielded f1 and f2 values within a range of 4–5 and 60–65,respectively.Three month stability studies,conducted at accelerated conditions,showed the optimized pellets to be stable.Taguchi plays an important role in optimizing parameters,and optimization of duloxetine hydrochloride can be achieved with minimal trials.展开更多
基金supported by grants from "Significant new drug development" Science and Technology Major Projects of China (2009ZX09301-003 2009ZX09401-005 2010ZX09401-407)
文摘Objective Lidamycin （LDM） can be dissociated to an apoprotein （LDP） and an active enediyne chromophore （AE）. The detached AE can reassemble with its LDP-containing fusion protein to endow the latter with potent antitumor activity. However, the reassembly of AE with LDP is affected by several factors. Our aim was to optimize the assembly efficiency of the AE with a LDP-containing fusion protein and investigate the influence of several factors on the assembly efficacy. Methods A method based on RP-HPLC was developed to analyze the assembly rate, and an orthogonal experimental design L9 （3^4） was used to investigate the effects of temperature, assembly time, pH and molecular ratio of LDP-containing fusion protein to AE on the assembly rate. Furthermore, the determined optimum conditions for the assembly rate of the LDP-containing fusion protein with AE were applied and evaluated. Results A calibration curve based on the LDM micromolar concentration against the peak-area of AE by HPLC was obtained. The order in which individual factors in the orthogonal experiment affected the assembly rate were temperature〉time〉pH〉molar ratio of AE to protein and all were statistically significant （P〈0.01）. The optimal assembly conditions were temperature at 10 ℃, time of 12 h, pH 7.0, and the molar ratio of AE： protein of 5：1. The assembly rate of AE with a LDP-containing fusion protein was improved by 23% after condition optimization. Conclusion The assembly rate of chromophore of lidamycin with its LDP-containing fusion protein was improved after condition optimization by orthogonal design, and the optimal conditions described herein should prove useful for the development of this type of LDP-containing fusion protein.
基金Project(2010A210003) supported by Henan Province Natural Sciences Research PlanProject(0910SGYS34370-2) supported by Zhengzhou City Science and Technology Research PlanProject supported by the Youth Backbone Teacher of Universities in Henan Province Grants Plan
文摘To improve antagonistic metabolites production of Bacillus subtilis strain BS501a, physical parameters of fermentation and metal inorganic salts in medium, namely initial pH value, culture temperature, fermentation time, concentrations of CaC12, FeSO4, ZnSO4, MnSO4 and MgSO4, were optimized using one-factor-at-a-time and orthogonal tests. The results show that the optimal physical parameters of fermentation are an initial pH of 7.0, a culture temperature of 30 ~C, and a fermentation time of 48 h. The optimal concentrations of metal inorganic salts in basal medium are 10.2 mmol/L CaCl2, 0.4 mmol/L FeSO4, 3.5 mmol/L ZnSO4, 0.6 mmol/L MnSO4 and 2.0 mmol/L MgSO4. Among the metal inorganic salts, MgSO4 and MnSO4 play important roles in the improvement of the antagonistic metabolites production of B. subtilis strain BS501a; especially, MgSO4 contributes a highly significant effect. The average diameter of inhibition zone of the BS501a filtered fermentation supernatant （FFS） cultured in the optimal fermentation conditions against Magnaporthe grisea DWBJ329 reaches 71.4 mm, and there is 2.4-fold increase in antifungal activity as compared with 21.2 mm under the pre-optimized conditions.
文摘An attempt has been made to study the influence of wear parameters like applied load, sliding speed, sliding distance and percentage of reinforcement on the dry sliding wear of the metal matrix composites. A plan of experiments, based on techniques of Taguchi, was performed to acquire data in controlled way. An orthogonal array and the analysis of variance were employed to investigate the influence of process parameters on the wear of composites. The objective is to establish a correlation between dry sliding wear of composites and wear parameters. These correlations were obtained by multiple regressions. Finally, confirmation tests were conducted to verify the experimental results foreseen from the mentioned correlations.
文摘To estimate the direction-of-arrival （DOA） of wideband coherent signals, a new method by modifying the orthogonality of the projected suhspaces method is proposed. And it can deal with randomly position perturbed arrays by using the Toeplitz method. This method needn＇t the primary information of DOA for focusing matrix and the sector dividing of interpolated method, which improving the precision of estimation and reducing the computational complexity. Simulations illustrate the effectiveness of this method.
基金supported by the RA Chem Pharma Ltd.,Nacharam,Andhra Pradesh,India,and the G.Pulla Reddy College of Pharmacy,Hyderabad,India.
文摘Duloxetine hydrochloride enteric coated pellets were formulated using fluidized bed.Three separate layers,the drug layer,the barrier layer,and the enteric layer,were coated onto the inert core pellets.The pellets were optimized with the acid resistance and drug release in simulated intestinal fluid as the process parameters,using the Taguchi L9 orthogonal array.Various other properties,such as surface morphology,bulk and tapped density,Hausner’s ratio,hardness,friability,yield of pellets,moisture content,and particle size distribution,were also studied in the optimized pellets.The concentration of the enteric polymer played a vital role in acid resistance,while the type of enteric polymer affected the drug release in simulated intestinal fluid.In both cases,it was determined that binder polymer concentration was not affected much.The comparisons between the optimized pellets and a market formulation yielded f1 and f2 values within a range of 4–5 and 60–65,respectively.Three month stability studies,conducted at accelerated conditions,showed the optimized pellets to be stable.Taguchi plays an important role in optimizing parameters,and optimization of duloxetine hydrochloride can be achieved with minimal trials.
