通过荧光光谱法, 研究了在模拟生理条件下, 二茂铁-碳硼烷衍生物(FcSB1, FcSB2和FcSBCO)、 芳烃钌(Ⅱ)-碳硼烷衍生物(RuBFc和RuBCOOH)与牛血清白蛋白(BSA)之间的相互作用。 结果表明, 五种碳硼烷衍生物与BSA形成非荧光性复合物而猝灭了BSA的荧光。 二茂铁-碳硼烷衍生物FcSB1, FcSB2和FcSBCO显著地影响BSA的构象, 使BSA的三级结构变得更紧凑, 并显著使酪氨酸残基附近微环境的极性(位于ⅠA, ⅠB和ⅡA结构域)降低, 疏水性增强。 而芳烃钌(Ⅱ)-碳硼烷衍生物RuBFc和RuBCOOH对BSA构象的影响小于二茂铁-碳硼烷衍生物。 揭示了新型金属碳硼烷衍生物对蛋白结构和构象的影响, 为含碳硼烷、 二茂铁等多功能基团的新型药物的设计与筛选提供一定的实验依据。

The biointeractions between a series of new organometallic carborane derivatives and model protein bovine serum albumin (BSA) were investigated by means of fluorescence and synchronous spectroscopy. The observations demonstrate that the ferrocene-carborane conjugates (FcSB1, FcSB2 and FcSBCO) and the ruthenium(Ⅱ)-arene carborane complexes (RuBFc and RuBCOOH) can form a steady complex with BSA and statically quench its fluorescence. The ferrocene-carborane conjugates could remarkably affect the tertiary structure of BSA and induce the microenvironment changes of Trp and Tyr residues from hydrophilic to hydrophobic environment. But the effect of the ruthenium(Ⅱ)-arene carborane complexes on the tertiary structure of BSA is much less. This study would give meaningful insights into the evaluation of the promising biomedical applications of the new carborane derivatives and benefit the development of potential multifunctional metallodrugs.