摘要
目的研究重组人血白蛋白与小分子药物的结合功能。方法在366nm下检测地西泮与人血白蛋白结合前后吸收值的变化,计算二者的结合常数;华法令与人血白蛋白结合后,用SephadexG-25HPLC柱进行分离,对游离华法令和二者结合产物分别积分,得到华法令与人血白蛋白的结合率。结果重组人血白蛋白与地西泮的结合常数为14·68mol Diaze-pam/mol rHSA,天然人血白蛋白与地西泮结合常数为12·82mol Diazepam/mol HSA。重组人血白蛋白中华法令的结合率为8·69%,而天然人血白蛋白中华法令的结合率为6·73%。结论重组人血白蛋白与天然人血白蛋白小分子药物结合功能基本一致。
Objective To study the binding function of recombinant human serum albumin（HSA） to small molecule drugs. Methods Determine the A366 values of Diazepam before and after binding to HSA and calculate the binding constant. Bind warfarin to HSA,and separate the conjugate and free warfarin by Sephadex G-2.5 HPLC,then integrate the peak areas of conjugate and free warfarin to calculate the binding rate. Results The binding constant of recombinant HSA to Diazepam was 14. 68 mol Diazepam/mol rHSA,and that of HSA to Diazepam was 12. 82 mel Diazepam/mol HSA. The binding rates of warfarin in rHSA and HSA were 8.69% and 6. 73% respectively. Conclusion The binding functions of recombinant and nature HSA to small molecule drugs were basically in agreement.
出处
《中国生物制品学杂志》
CAS
CSCD
2006年第5期499-501,共3页
Chinese Journal of Biologicals
基金
863计划资助项目(2002AA2Z345C)
关键词
人血白蛋白
小分子药物
结合功能
Human serum albumin
Small molecule drug
Binding function
