Studzian K, Tołwińska-Stańczyk Z, Wilmańska D, Palumbo M, Gniazdowski M
Department of General Chemistry, Institute of Physiology and Biochemistry, Medical University of Lódź, Poland.
Neoplasma. 1999;46(1):50-3.
The anticancer drug, nitracrine, a 1-nitro-9-aminoalkyl derivative of acridine exhibits potent cytotoxic effects which are due to its metabolic activation, followed by covalent binding to macromolecules--DNA being the target for the drug. The renaturable fraction of DNA from L-1210 cells pretreated with nitracrine is assayed by means of ethidium bromide fluorescence assay and chromatography on hydroxyapatite column. The effect of the drug was compared with furocoumarins of different DNA crosslinking potencies. The existence of crosslinks in DNA upon incubation of cells with nitracrine (1-4 microM) have been confirmed with two different methods under the conditions where 8-methoxypsoralen, a classic crosslinking agent induced the renaturation. The DNA preparation isolated from the drug pretreated cells exhibited decreased transcriptional template activity with E. coli DNA-dependent RNA polymerase.
抗癌药物硝吖啶，一种吖啶的1-硝基-9-氨基烷基衍生物，具有强大的细胞毒性作用，这是由于其代谢活化，随后与大分子共价结合——DNA是该药物的作用靶点。通过溴化乙锭荧光测定法和羟基磷灰石柱色谱法测定用硝吖啶预处理的L-1210细胞中可复性DNA的比例。将该药物的作用与具有不同DNA交联能力的呋喃香豆素进行了比较。在经典交联剂8-甲氧基补骨脂素诱导复性的条件下，用两种不同方法证实了细胞与硝吖啶（1-4 microM）孵育后DNA中存在交联。从药物预处理细胞中分离的DNA制剂对大肠杆菌DNA依赖性RNA聚合酶表现出降低的转录模板活性。
