超滤质谱法研究大黄蒽醌类化合物与人血清白蛋白的相互作用

Study on the Interactions between HSA and Rhubarb Anthraquinone Analogues by Ultrafiltration Mass Spectrometry

为研究药物小分子与靶蛋白的相互作用,建立了超滤技术和液相色谱电喷雾质谱联用方法(LC-ESI-MS),并用该法筛选了与人血清白蛋白(HSA)的作用的大黄蒽醌类物质(大黄酚、大黄酸、芦荟大黄素).通过比较大黄蒽醌类药物混合溶液与HSA结合前后的提取离子流图色谱峰,发现大黄酸与HSA结合能力最强,芦荟大黄素次之,大黄酚最弱.说明超滤质谱法是研究药物小分子和蛋白质相互作用的一种快速灵敏的分析方法.

To study the interactions between small drug molecules and the target protein, an ultrafiltration technology coupled with liquid chromatography-ESI-mass spectrometry （LC-ESI-MS） method was established and applied to screen the rhubarb anthraquinone analogues （chrysophanol, rhein and aloe-emodin ） that interacted with human serum albumin （HSA）. Comparing the extracted ion chromatography （EIC） of these drugs before and after the incubation with HSA, the sesults indicated that the binding affinity capacity of rhein was the strongest, followed by aloe-emodin, and chrysophanol was the weakest. This work demonstrated that ultrafiltration mass spectrometry is a fast and sensitive analytical method for the study of interactions of protein-ligand complexes.