【摘要】 采用毛细管区带电泳紫外检测方法,在pH8 0、浓度50mmol/L的磷酸盐缓冲溶液及运行电压15kV的条件下,测定了4种新合成的具有抗HIV 1活性的化合物(IG3,iso C3,C3,MC3)与牛血清白蛋白(BSA)相互作用的结合常数。在缓冲溶液中加入不同浓度的BSA,通过测定化合物迁移时间的变化,计算得到了上述4种化合物与BSA的结合常数分别为1 07×104,1 34×104,8 51×103和9 45×103L/mol。该方法简单、快捷,可用于研究结合比为1∶1的小分子与生物大分子的相互作用。更多还原

【Abstract】 The binding constants （K_b） of four novel anti-HIV-1 active compounds with bovine serum albumin （BSA） were determined by capillary zone electrophoresis （CZE） with UV detection under condition of phosphate buffer （pH 8.0, 50 mmol/L） at 15 kV running voltage. These molecules were synthesized by computer-simulated design with the property of inhibiting the binding of HIV-1 Tat protein to trans-activation response region （TAR） RNA required for HIV-1 transcription and blocking the HIV replication cycle. The results showed that with the addition of different concentrations of BSA into the buffer solution, the binding constants of four active compounds （IG₃,iso-C₃,C₃,MC₃） with BSA could be measured by the change of migration time. The experimental values of K_b were 1.07×10⁴, 1.34×10⁴, 8.51×10³ and （9.45×10³） （L/mol）, respectively. It is an easy and simple method to estimate the interaction of small molecules with biomacromolecules with 1∶1 molar binding ratio.更多还原