人血清白蛋白药物输运过程中的催化作用研究  

Catalytic Effects of Human Serum Albumin to the Bound Drugs during Plasma Transmission

作　　者：魏言春[1] 宋佳兴[1] 

机构地区：[1]华南师范大学生物光子学研究院激光生命科学研究所,暨激光生命科学教育部重点实验室,广东广州510631

出　　处：《激光生物学报》2013年第1期53-57,共5页Acta Laser Biology Sinica

基　　金：科技部国家重点基础研究973计划项目(2011CB910402;2010CB732602);教育部"长江学者与创新团队计划"创新团队项目(IRT0829);国家自然科学基金项目(81127004;11104087)资助

摘　　要：血清白蛋白(HSA)是人体中重要的药物结合蛋白。药物在体内和血清白蛋白可逆性地结合可以增强药物的生物兼容性、延长药物半衰期并达到缓释的效果。但是研究发现药物和白蛋白的结合有时也会形成负面的影响。本文以能和活性氧反应的化学发光试剂FCLA为分子探针,研究分析了HSA和药物的相互作用及产生的影响。实验发现,HSA能通过与FCLA分子的结合,对FCLA的氧化产生类似于酶催化效果,通过降低氧化反应所需的活化能加速了探针的氧化过程。研究结果表明,HSA和某些药物的结合能够引起药物抗氧化能力或抗药物交叉反应能力的改变,因此在利用HSA携带药物时,需要考虑结合所导致的药物稳定性的降低。该研究有助于揭示体内的药物动力学问题,指导合理用药,同时对于进行药物分子设计、开发新药也具有重要的指导意义。Human Serum Albumin （HSA） is a very important drugplasma protein. Many drugs can bind reversibly with HSA in plasma, resulting in an enhanced biocompatibility and delayed lifetime. However, for some drugs the bind ing can also induce some negative effects during their application. In our study, a chemiluminescence molecular reagent FCLA, which can react with reactive oxygen, was used as a probe to detect the interaction. The results indicate that FCLA can be bind to HSA. HSA provides a catalytic effect to accelerate the oxidation reaction, just as the enzymatic ac tion. The mechanism is deduced that may be due to the decreased reaction energy for the drugprotein binding. It means that as drugs bind to HSA, their antioxidative ability decreases or the interaction between different drugs is more easily aroused. This study will be helpful for the drug invention, designing and application.

关 键 词：血清白蛋白 催化 氧化 

分 类 号：Q505[生物学—生物化学]