A rapid and simple liquid chromatography method with on-line solid phase extraction was developed and validated for the quantitative determination of cyclophosphamide in rat plasma.The plasma sample was first extracte...A rapid and simple liquid chromatography method with on-line solid phase extraction was developed and validated for the quantitative determination of cyclophosphamide in rat plasma.The plasma sample was first extracted on an Acclaim？ Polar Advantage II C18 guard column（PA II C18,10 mm×4.6 mm,5 μm）,which was also the on-line Extraction Cartridge SPE column,by washing with 100% H2O for 1 min.The extracted sample was then eluted onto a PA II C18 column（150 mm×4.6 mm,5 μm） and separated by isocratic elution with acetonitrile-water（40：60,v/v）.The mobile phase was run at a flow rate of 1.0 mL/min,and the UV detector was set at 195 nm.Retention time of cyclophosphamide was 4.3 min and the total run-time was 6 min.The linear range of the standard curve was from 1.0 to 200 μg/mL（r2 = 0.9999）,and the limits of quantification and detection were 1.0 μg/mL（RSD10%,n = 5） and 0.3 μg/mL（RSD13%,n = 5）,respectively.Both intra-and inter-day variations were less than 5.6%.The developed method can be used for the therapeutic drug monitoring of cyclophosphamide in the clinic.展开更多
The binding pattern of Ethaselen to bovine serum albumin （BSA） was studied by fluorescence spectroscopic technique and Autodock 3.0.5 analysis. The result showed that the binding constant K of Ethaselen and BSA is 3...The binding pattern of Ethaselen to bovine serum albumin （BSA） was studied by fluorescence spectroscopic technique and Autodock 3.0.5 analysis. The result showed that the binding constant K of Ethaselen and BSA is 3.5×10^4L/mol and the number of binding sites n = 0.9. The binding between Ethaselen and BSA or human serum albumin （HSA） is mainly through hydrophobic interactions.展开更多
As a dendritic cell-specific C-type lectin receptor, DC-SIGN plays an important role in the early stages of many viral infections, including HIV and Ebola, making it an interesting therapeutic target. It has been foun...As a dendritic cell-specific C-type lectin receptor, DC-SIGN plays an important role in the early stages of many viral infections, including HIV and Ebola, making it an interesting therapeutic target. It has been found that DC-SIGN can recognize both highly mannosylated and branched fucosylated oligosaccharides. Herein, we synthesized a new series of homo-and Man-Fuc heteroglycoclusters with diverse structures. The binding properties of these compounds to tetrameric extracellular DC-SIGN were assessed by surface plasmon resonance(SPR). Heteroglycocluster 17 b showed high DC-SIGN-binding activity(K;= 2.6 μM). The structural determinants of this high affinity of 17 b were rationalized by docking and compared with its much less potent isomer 17 a. Therefore, 17 b might serve as a base for the development of potent inhibitors of DC-SIGN-dependent viral infection.展开更多
基金National Natural Science Foundation of China(Grant No.81072612)the Natural Science Foundation of Beijing(Grant No.7102107)+1 种基金the Open Foundation of State Key Laboratory of Natural and Biomimetic Drugs(Grant No.K20110109)Specialized Research Fund for the Doctoral Program of Higher Education(Grant No.20110001110021)
文摘A rapid and simple liquid chromatography method with on-line solid phase extraction was developed and validated for the quantitative determination of cyclophosphamide in rat plasma.The plasma sample was first extracted on an Acclaim？ Polar Advantage II C18 guard column（PA II C18,10 mm×4.6 mm,5 μm）,which was also the on-line Extraction Cartridge SPE column,by washing with 100% H2O for 1 min.The extracted sample was then eluted onto a PA II C18 column（150 mm×4.6 mm,5 μm） and separated by isocratic elution with acetonitrile-water（40：60,v/v）.The mobile phase was run at a flow rate of 1.0 mL/min,and the UV detector was set at 195 nm.Retention time of cyclophosphamide was 4.3 min and the total run-time was 6 min.The linear range of the standard curve was from 1.0 to 200 μg/mL（r2 = 0.9999）,and the limits of quantification and detection were 1.0 μg/mL（RSD10%,n = 5） and 0.3 μg/mL（RSD13%,n = 5）,respectively.Both intra-and inter-day variations were less than 5.6%.The developed method can be used for the therapeutic drug monitoring of cyclophosphamide in the clinic.
基金National Natural Science Foundation of China (Grant No. 30472036)Beijing Natural Science Foundation (Grant No. 7021001)
文摘The binding pattern of Ethaselen to bovine serum albumin （BSA） was studied by fluorescence spectroscopic technique and Autodock 3.0.5 analysis. The result showed that the binding constant K of Ethaselen and BSA is 3.5×10^4L/mol and the number of binding sites n = 0.9. The binding between Ethaselen and BSA or human serum albumin （HSA） is mainly through hydrophobic interactions.
基金National Natural Science Foundation of China(NSFC,Grant No.21172015)Wellcome Trust (UK,Grant No.097354/Z/11/Z)+1 种基金ML acknowledges the Research Project RVO61388963 of the Institute of Organic Chemistry and BiochemistryAcademy of Sciences of the Czech Republic,the Czech Science Foundation (Grant No.P20 8/12/G016)。
文摘As a dendritic cell-specific C-type lectin receptor, DC-SIGN plays an important role in the early stages of many viral infections, including HIV and Ebola, making it an interesting therapeutic target. It has been found that DC-SIGN can recognize both highly mannosylated and branched fucosylated oligosaccharides. Herein, we synthesized a new series of homo-and Man-Fuc heteroglycoclusters with diverse structures. The binding properties of these compounds to tetrameric extracellular DC-SIGN were assessed by surface plasmon resonance(SPR). Heteroglycocluster 17 b showed high DC-SIGN-binding activity(K;= 2.6 μM). The structural determinants of this high affinity of 17 b were rationalized by docking and compared with its much less potent isomer 17 a. Therefore, 17 b might serve as a base for the development of potent inhibitors of DC-SIGN-dependent viral infection.
