毛细管区带电泳法考察牛凝血酶、核酸适配体与丹参活性分子间的相互作用

发布时间：2018-10-08 20:36

【摘要】：采用毛细管区带电泳法(CZE)研究牛凝血酶(B-Thr)、凝血酶核酸适配体(Apt29)与丹参中3种活性物质(丹参素钠(SAS)、原儿茶酸(PA)、阿魏酸(FA))间的相互作用。电泳条件为:毛细管长度40 cm,紫外检测波长214 nm,分离电压15 kV,压力进样3.45 kPa,进样时间5 s。分别固定3种活性药物分子的浓度,改变B-Thr或Apt29的浓度,采用Scatchard方程和非特异性结合方程计算结合常数(K_b),表征药物分子和B-Thr或Apt29的相互作用大小。结果表明,PA与B-Thr结合能力最强,K_b为3.39×104L/mol,FA与B-Thr的K_b为1.05×104L/mol,SAS与B-Thr未表现出结合能力;在与Apt29的相互作用的研究中显示,SAS基本未与Apt29结合,FA与Apt29结合能力强于PA与Apt29的结合能力,FA、PA与Apt29的K_b分别为1.48×104L/mol和1.32×104L/mol。该研究报道了丹参活性分子与B-Thr、Apt29的相互作用结果,可为核酸适配体(蛋白质)与中药分子相互作用的探索提供新方法,适配体与中药分子相互作用亦可为中药分子的靶点发现、靶向转运提供借鉴。
[Abstract]:The interaction between bovine thrombin (B-Thr), thrombin nucleic acid aptamer (Apt29) and three active substances in Salvia miltiorrhiza (Salvia miltiorrhiza) (Danshensu sodium (SAS), protocatechuic acid (PA), ferulic acid (FA) was studied by capillary zone electrophoresis (CZE). The electrophoretic conditions were as follows: capillary length 40 cm, UV detection wavelength 214 nm, separation voltage 15 kV, pressure injection 3.45 kPa, injection time 5 s. The concentration of three active drug molecules was fixed, and the concentration of B-Thr or Apt29 was changed. The binding constant (Kapb) was calculated by Scatchard equation and non-specific binding equation to characterize the interaction between drug molecules and B-Thr or Apt29. The results showed that the binding ability of PA and B-Thr was the strongest, the KB of Kapa was 3.39 脳 10 ~ (4) L / mol ~ (-1) FA and B-Thr was 1.05 脳 10 ~ (4) L / mol ~ (-1) B-Thr. In the study of interaction with Apt29, it was found that the binding ability of FA and Apt29 was stronger than that of PA and Apt29. The Kb of FAPA and Apt29 were 1.48 脳 104L/mol and 1.32 脳 10 ~ 4 L / mol, respectively. This study reported the interaction between the active molecules of Salvia miltiorrhiza and B-Thrrnapt29, which could provide a new method for the interaction between aptamer (protein) and traditional Chinese medicine, and the interaction between aptamer and traditional Chinese medicine could also be the target of traditional Chinese medicine. Target transshipment provides reference.
【作者单位】：北京理工大学生命学院;
【基金】：国家自然科学基金项目(81573693,21675012,21375008)~~
【分类号】：R284;O658.9

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