Ojha R P, Sanyal N K
Department of Physics, University of Gorakhpur.
Indian J Biochem Biophys. 1990 Aug;27(4):219-21.
The intercalative binding of the acridine antitumour drug 4'-(9-acridinylamino) methane-sulphonate-m-anisidine, a known inhibitor of nucleic acid synthesis, to native calf thymus DNA has been studied using optical titration method. Amsacrine (AMSA) exhibits positive cooperativity in their equilibrium binding to DNA as indicated by the positive slope in the initial region of the binding isotherms (Scatchard plots) under conditions simulating physiological ionic strengths. m-AMSA binds with a higher degree of cooperativity than o-AMSA. Although this correlates with the effectiveness of the drugs as antitumour agents, the exact relationship between the observation of cooperative binding and pharmacological activity is yet to be determined.
吖啶类抗肿瘤药物4'-（9-吖啶基氨基）甲磺酸盐间茴香胺是一种已知的核酸合成抑制剂，已采用光学滴定法研究了其与天然小牛胸腺DNA的嵌入结合。在模拟生理离子强度的条件下，安吖啶（AMSA）在与DNA的平衡结合中表现出正协同性，结合等温线（Scatchard图）初始区域的正斜率表明了这一点。间位-AMSA比邻位-AMSA具有更高程度的协同性。尽管这与药物作为抗肿瘤剂的有效性相关，但协同结合的观察结果与药理活性之间的确切关系尚待确定。
