摘要
目的应用电喷雾离子阱质谱(ESI-MS)研究酮洛芬与人血清白蛋白、α1-酸性糖蛋白的非共价结合。方法应用ESI-MS分别测定酮洛芬、人血清白蛋白、α1-酸性糖蛋白以及酮洛芬与该两种蛋白形成的复合物的相对分子质量,通过结合前后的相对分子质量变化计算复合物化学计量比。考察了反应体系pH值以及质谱仪毛细管温度、锥孔电压等对药物与蛋白非共价结合的影响。结果酮洛芬(ketoprofen,KP)与人血清白蛋白(human serum albumin,HSA)和α1-酸性糖蛋白(α1-acid glycoprotein,AAG)形成非共价结合复合物的表观化学计量比分别为5∶1和4∶1。结论ESI-MS是研究药物与蛋白间非共价结合的一种新方法,具有灵敏、快速和准确的特点。
OBJECTIVE To study the noneovalent binding of ketoprofen with human serum albumin and α1-acid glyeoprotein by the electrospray ion trap mass spectrometry（ESI-MS） . METHODS The molecular weights of ketoprofen, human serum albumin, α1-acid glycoprotein and their complexes were measured by the electrospray ion trap mass spectrometry. The stoichiometric ratio was calculated. The influ- ences of pH values of injection solution, capillary temperatures and cone voltages on non calculated binding were studied. RESULTS The apparent stoichiometric ratios of noncovalent complexes KP-HSA and KP-AAG were 5 ： 1 and 4：1, respectively. CONCLUSION ESI-MS is a new method for studying the drug-protein noncovalent binding, and it offers some advantages in sensitivity, high-speed, accuracy.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2006年第6期460-462,共3页
Chinese Pharmaceutical Journal
