Aver'eva E V, Kivman G Ia, Markovich M N, Shraĭber N F, Pognoevskiĭ O T
Antibiot Khimioter. 1988 Jun;33(6):444-8.
Simultaneous binding of two drugs to human serum albumin (HSA) was studied by flow microcalorimetry. The following drug pairs were used: sulfadimethoxine and cefazolin. Sulfadimethoxine and dicloxacillin, sulfadimethoxine and chlortetracycline. A procedure for estimating the calorimetric titration curves in competing binding of the drugs to the HSA homogeneous active site is described. Comparison of the theoretical and experimental titration curves enabled detection of the ligand competition for the biopolymer binding site. It was shown that sulfadimethoxine displaced cefazolin in the HSA active site, the nature of the HSA association with dicloxacillin and sulfadimethoxine was independent and binding of doxycycline or chlortetracycline to HSA had no influence on sulfadimethoxine interaction with protein.
采用流动微量热法研究了两种药物与人血清白蛋白(HSA)的同时结合情况。使用了以下药物对:磺胺二甲氧嘧啶和头孢唑林、磺胺二甲氧嘧啶和双氯西林、磺胺二甲氧嘧啶和金霉素。描述了一种用于估算药物在与HSA均一活性位点竞争结合时的量热滴定曲线的方法。通过比较理论滴定曲线和实验滴定曲线,能够检测配体对生物聚合物结合位点的竞争情况。结果表明,磺胺二甲氧嘧啶在HSA活性位点取代了头孢唑林,HSA与双氯西林和磺胺二甲氧嘧啶的结合性质相互独立,强力霉素或金霉素与HSA的结合对磺胺二甲氧嘧啶与蛋白质的相互作用没有影响。