The effefts of 6 α glucosyl β cyclodextrin(G β CD)on the thermostability and catalytic characteristics of horseradish peroxidase(HRP) were studied using the residual activity method.The results indicated that the m...The effefts of 6 α glucosyl β cyclodextrin(G β CD)on the thermostability and catalytic characteristics of horseradish peroxidase(HRP) were studied using the residual activity method.The results indicated that the mole ratio of [G β CD]/[HRP],pH and modification time were of the main factors.The optimum comprehensive results were achieved under the condition of [G β CD]/[HRP]=5,pH7.5,stirred 0.5h under 20℃ and then 2h under 10℃ continuously,which corresponding to that enzyme gained 89% of the native activity.The apparent constant of heat inactivation,k,drop to 67% of the original value under 75℃.G β CD showed nonspecific noncompetitive inhibition effect.The kinetic parameters calculated using experiment data indicated that K m was no change,and V max decreased to about 82% of the native enzyme.The apparent activation energy increased 11.15%.The pH range for higher activity got extended and optimum pH shifited toward alkaline range.展开更多
It is essential to develop new carriers for laryngeal drug delivery in light of the lack of therapy in laryngeal related diseases.When the inhalable micron-sized crystals ofγ-cyclodextrin metal-organic framework(CD-M...It is essential to develop new carriers for laryngeal drug delivery in light of the lack of therapy in laryngeal related diseases.When the inhalable micron-sized crystals ofγ-cyclodextrin metal-organic framework(CD-MOF)was utilized as dry powder inhalers(DPIs)carrier with high fine particle fraction(FPF),it was found in this research that the encapsulation of a glycoside compound,namely,scutellarin(SCU)in CD-MOF could significantly enhance its laryngeal deposition.Firstly,SCU loading into CD-MOF was optimized by incubation.Then,a series of characterizations were carried out to elucidate the mechanisms of drug loading.Finally,the laryngeal deposition rate of CD-MOF was 57.72±2.19%improved by SCU,about two times higher than that of CD-MOF,when it was determined by Next Generation Impactor(NGI)at 65 L/min.As a proof of concept,pharyngolaryngitis therapeutic agent dexamethasone(DEX)had improved laryngeal deposition after being co-encapsulated with SCU in CDMOF.The molecular simulation demonstrated the configuration of SCU in CD-MOF and its contribution to the free energy of the SCU@CD-MOF,which defined the enhanced laryngeal anchoring.In conclusion,the glycosides-like SCU could effectively enhance the anchoring of CD-MOF particles to the larynx to facilitate the treatment of laryngeal diseases.展开更多
文摘The effefts of 6 α glucosyl β cyclodextrin(G β CD)on the thermostability and catalytic characteristics of horseradish peroxidase(HRP) were studied using the residual activity method.The results indicated that the mole ratio of [G β CD]/[HRP],pH and modification time were of the main factors.The optimum comprehensive results were achieved under the condition of [G β CD]/[HRP]=5,pH7.5,stirred 0.5h under 20℃ and then 2h under 10℃ continuously,which corresponding to that enzyme gained 89% of the native activity.The apparent constant of heat inactivation,k,drop to 67% of the original value under 75℃.G β CD showed nonspecific noncompetitive inhibition effect.The kinetic parameters calculated using experiment data indicated that K m was no change,and V max decreased to about 82% of the native enzyme.The apparent activation energy increased 11.15%.The pH range for higher activity got extended and optimum pH shifited toward alkaline range.
基金supported by the Strategic Priority Research Program of the Chinese Academy of Sciences(No.XDA12050307,China)the ANR AntiTBnano project(ANR-14-CE08-0017,France)the National Research Council of Science and Technology Major Projects for“Major New Drugs Innovation and Development”(2018ZX09721002e009,China)
文摘It is essential to develop new carriers for laryngeal drug delivery in light of the lack of therapy in laryngeal related diseases.When the inhalable micron-sized crystals ofγ-cyclodextrin metal-organic framework(CD-MOF)was utilized as dry powder inhalers(DPIs)carrier with high fine particle fraction(FPF),it was found in this research that the encapsulation of a glycoside compound,namely,scutellarin(SCU)in CD-MOF could significantly enhance its laryngeal deposition.Firstly,SCU loading into CD-MOF was optimized by incubation.Then,a series of characterizations were carried out to elucidate the mechanisms of drug loading.Finally,the laryngeal deposition rate of CD-MOF was 57.72±2.19%improved by SCU,about two times higher than that of CD-MOF,when it was determined by Next Generation Impactor(NGI)at 65 L/min.As a proof of concept,pharyngolaryngitis therapeutic agent dexamethasone(DEX)had improved laryngeal deposition after being co-encapsulated with SCU in CDMOF.The molecular simulation demonstrated the configuration of SCU in CD-MOF and its contribution to the free energy of the SCU@CD-MOF,which defined the enhanced laryngeal anchoring.In conclusion,the glycosides-like SCU could effectively enhance the anchoring of CD-MOF particles to the larynx to facilitate the treatment of laryngeal diseases.
