Fc-Arg(NO2)-Gly-Asp(OMe)-OMe的合成及其与牛血清白蛋白的相互作用

以二茂铁，Gly，Asp和BOC-Arg(NO2)-OH为原料，采用液相合成法，以HBTU及HOBt为缩合剂合成了二茂铁-肽化合物Fc-Arg(NO2)-Gly-Asp(OMe)-OMe（5），其收率为38.7%，并对化合物5进行了表征。采用电化学、紫外-可见吸收光谱及荧光光谱等研究了近生理条件下其与牛血清白蛋白(BSA)的相互作用，讨论了其对BSA构象的影响。实验结果表明化合物5与BSA间相互作用为静态猝灭过程，反应结合位点数为0.856，结合常数为1.75×103 L•mol-1，并依据能量转移理论确定了其与BSA相互作用的最近距离为2.14 nm。

Synthesis of Fc-Arg(NO2)-Gly-Asp(OMe)-OMe and its Interaction with Bovine Serum Albumin

The ferrocene conjugate Fc-Arg(NO2)-Gly-Asp(OMe)-OMe (5) was synthesized from ferrocene, Gly,Asp and BOC-Arg(NO2)-OH by the method of solution synthesis with the yield of 38.7%. The compound 5 was characterized by 1H-NMR, IR and ESI-MS. Cyclic voltammetry, UV-visible absorption spectrum and fluorescence spectrum methods were used to investigate the interaction between compound 5 and bovine serum albumin (BSA). The interaction of BSA with compound 5 results in a conformational change of BSA. The experimental results indicated that the interaction involved a static quenching. The number of binding site n and equilibrium constant were 0.856 and 1.75×103 L•mol-1, respectively. Based on the energy tranfer theory, the binding distance between compound 5 and BSA was determinated to be 2.14 nm.Key words: ferrocene-peptide; bovine serum albumin; electrochemistry; UV-Visible absorption spectrum; fluorescence spectrum