Shah G H, Kataoka K, Ueno A, Ohtsuka Y, Mizushima T, Sekimizu K
Department of Microbiology, Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan.
Biol Pharm Bull. 1997 Dec;20(12):1233-4. doi: 10.1248/bpb.20.1233.
The activity of mammalian topoisomerase I is inhibited by acidic phospholipids. We investigated the effect of psychotropic drugs and local anesthetics on cardiolipin-inhibited calf thymus DNA topoisomerase I activity. Chlorpromazine, promethazine, and imipramine, which interact with phospholipids, suppressed the inhibitory effect of cardiolipin. The present results suggest that relaxation of DNA supercoiling is involved in the cytotoxic action of these drugs.
哺乳动物拓扑异构酶I的活性受到酸性磷脂的抑制。我们研究了精神药物和局部麻醉剂对心磷脂抑制的小牛胸腺DNA拓扑异构酶I活性的影响。与磷脂相互作用的氯丙嗪、异丙嗪和丙咪嗪抑制了心磷脂的抑制作用。目前的结果表明，DNA超螺旋的松弛参与了这些药物的细胞毒性作用。
