Yesair D W, Callahan M, McComish M F, Taylor R F
Cancer Biochem Biophys. 1979;3(4):163-8.
The binding characteristics of the cancer chemotherapeutic Cain's quinolinium 6-amino-1-ethyl-4-[p-[[p-[(1-ethylpyridinium-4-yl) amino] phenyl] carbamoyl]-anilino]-quinolinium dibromide (NSC 113089) to lipid extracts from rat kidney, liver, heart and skeletal muscle has been studied. Such binding is saturable with an apparent KD congruent to 1.6 microM. Drug binding to the lipid extracts is displaceable by spermine, spermidine, calcium ions and protons. Spermine is the best displacing agent, achieving half drug displacement from the lipid extracts at approximately 6.3 microM regardless of tissue. The inability of the displacing agents to displace all the NSC 113089 bound to the lipid extracts as well as differences in the amount of agent bound to as compared to amount of drug displaced from the lipid extracts indicate that a number of drug binding sites may be present in the lipid extracts. The similarities of drug binding by rat tissue lipids to similar lipids extracted from normal animal and tumor tissues is discussed.
对癌症化疗药物卡因喹啉鎓盐6-氨基-1-乙基-4-[对-[[对-[(1-乙基吡啶鎓-4-基)氨基]苯基]氨基甲酰基]-苯胺基]-喹啉鎓二溴化物（NSC 113089）与大鼠肾脏、肝脏、心脏和骨骼肌脂质提取物的结合特性进行了研究。这种结合具有饱和性，表观解离常数（KD）约为1.6微摩尔。药物与脂质提取物的结合可被精胺、亚精胺、钙离子和质子取代。精胺是最佳的取代剂，无论何种组织，在约6.3微摩尔时可使脂质提取物中一半的药物被取代。取代剂无法取代与脂质提取物结合的所有NSC 113089，以及与从脂质提取物中取代的药物量相比结合的试剂数量存在差异，这表明脂质提取物中可能存在多个药物结合位点。讨论了大鼠组织脂质与从正常动物和肿瘤组织中提取的类似脂质的药物结合相似性。
