In this paper,the noncovalent interactions between α1-acid glycoprotein（AAG） and the drugs,such as ketoprofen（KP） and anisodine hydrobromide（AN） were studied by using electrospray ion trap mass spectrometry met...In this paper,the noncovalent interactions between α1-acid glycoprotein（AAG） and the drugs,such as ketoprofen（KP） and anisodine hydrobromide（AN） were studied by using electrospray ion trap mass spectrometry method.The results show that both of the drugs had a strong coalescent interaction with AAG,the（dissociation） constants（Kd） and the apparent stoichiometric ratio of noncovalent complexes AN-AAG were（1.75×10-3 mol/L） and 1∶7,and those for KP-AAG complex were 4.95×10-4 mol/L and 1∶4,respectively.According to the thermodynamic parameters of the noncoralent complexes,the main sorts of binding force were static-electricity gravitation for KP-AAG and Van der Waals force for AN-AAG,respectively. The experiment proves that ESI-MS technology as a new method for studying the drug-protein noncoralent binding can offer some advantages in sensitivity,speed,accuracy and directness particularly in the determination of the stoichiormetry of the complex compared to other well-established methods such as circular dichroism and fluorescence spectroscopy,etc.展开更多
文摘目的分析tau蛋白、胶质纤维状酸性蛋白(glial fibrillary acidic protein,GFAP)以及抗β2糖蛋白1抗体(anti-β2 glycoprotein 1 antibody,aβ2-GP1)水平与高血压脑出血(hypertensive intracerebral hemorrhage,HICH)患者预后的相关性。方法将70例HICH患者纳入研究组,另将同时期进行健康体检的70例人员纳入对照组。比较两组tau蛋白、GFAP以及aβ2-GP1水平。比较不同预后HICH患者tau蛋白、GFAP、aβ2-GP1水平和美国国立卫生院卒中量表(National Institute of Health Stroke Scale,NIHSS)评分;并分析HICH患者相关指标与NIHSS评分的相关性。使用受试者工作特征(receiver operation characteristic,ROC)曲线分析相关指标预测HICH患者不良预后的临床价值。结果与对照组比较,观察组tau蛋白、GFAP以及aβ2-GP1水平均较高(P<0.05)。预后不良的HICH患者tau蛋白、GFAP、aβ2-GP1水平和NIHSS评分均较高(P<0.05);相关指标与NIHSS评分均呈正相关(均P<0.05)。相关指标预测HICH患者预后不良的最佳临界值:tau蛋白≥258.15ng/L、GFAP≥16.15ng/L、aβ2-GP1≥18.35 RU/mL,此时ROC曲线下面积(area under the curve,AUC)为0.908(95%CI:0.828~0.988,P<0.05)、0.871(95%CI:0.781~0.961,P<0.05)、0.839(95%CI:0.728~0.949,P<0.05),敏感度为77.27%、77.27%、72.73%,特异度为97.92%、85.42%、89.58%。结论HICH患者tau蛋白、GFAP以及aβ2-GP1水平较高,神经损伤较重、预后不良的HICH患者相关指标更高,监测HICH患者tau蛋白、GFAP以及aβ2-GP1水平可用于不良预后的评估。
文摘In this paper,the noncovalent interactions between α1-acid glycoprotein（AAG） and the drugs,such as ketoprofen（KP） and anisodine hydrobromide（AN） were studied by using electrospray ion trap mass spectrometry method.The results show that both of the drugs had a strong coalescent interaction with AAG,the（dissociation） constants（Kd） and the apparent stoichiometric ratio of noncovalent complexes AN-AAG were（1.75×10-3 mol/L） and 1∶7,and those for KP-AAG complex were 4.95×10-4 mol/L and 1∶4,respectively.According to the thermodynamic parameters of the noncoralent complexes,the main sorts of binding force were static-electricity gravitation for KP-AAG and Van der Waals force for AN-AAG,respectively. The experiment proves that ESI-MS technology as a new method for studying the drug-protein noncoralent binding can offer some advantages in sensitivity,speed,accuracy and directness particularly in the determination of the stoichiormetry of the complex compared to other well-established methods such as circular dichroism and fluorescence spectroscopy,etc.
