Rohde W, Mikelens P, Jackson J, Blackman J, Whitcher J, Levinson W
Antimicrob Agents Chemother. 1976 Aug;10(2):234-40. doi: 10.1128/AAC.10.2.234.
8-Hydroxyquinoline and several of its derivatives inactivate the transforming ability of Rous sarcoma virus and inhibit its ribonucleic acid-dependent deoxyribonucleic acid polymerase activity. The copper complex of these metal-binding ligands is as active as the free ligand. The activity of the 8-hydroxyquinolines is approximately 50-fold more effective than another group of metal-binding compounds that we have tested, the thiosemicarbazones. In contrast to the potency of the 8-hydroxyquinolines to inactivate Rous sarcoma virus, no intracellular inhibition of transformation could be demonstrated at a concentration that did not affect the growth and appearance of the cells. Cellular deoxyribonucleic acid synthesis was inhibited to a greater extent than was ribonucleic acid or protein synthesis. The phenomenon of "concentration quenching" was observed with high concentrations of drug, causing less inhibition of deoxyribonucleic acid synthesis than was observed with lower concentrations. Herpes simplex virus type 1 was inactivated also by the 8-hydroxyquinolines and their copper complexes. No intracellular inhibition of plaque formation was observed. Treatment with 8-hydroxyquinoline sulfate had no effect on the resolution of herpetic keratitis in rabbits. Some 8-hydroxyquinolines bind to deoxyribonucleic acid in the presence of copper, a phenomenon that may be important in their antiviral activity.
8-羟基喹啉及其几种衍生物可使劳氏肉瘤病毒的转化能力失活，并抑制其依赖核糖核酸的脱氧核糖核酸聚合酶活性。这些金属结合配体的铜络合物与游离配体具有相同的活性。8-羟基喹啉的活性比我们测试过的另一组金属结合化合物硫代氨基脲高约50倍。与8-羟基喹啉使劳氏肉瘤病毒失活的效力相反，在不影响细胞生长和外观的浓度下，未观察到对转化的细胞内抑制作用。细胞脱氧核糖核酸合成比核糖核酸或蛋白质合成受到更大程度的抑制。在高浓度药物下观察到“浓度猝灭”现象，与较低浓度相比，脱氧核糖核酸合成受到的抑制较少。1型单纯疱疹病毒也可被8-羟基喹啉及其铜络合物灭活。未观察到对空斑形成的细胞内抑制作用。用硫酸8-羟基喹啉治疗对兔疱疹性角膜炎的消退没有影响。一些8-羟基喹啉在有铜存在的情况下与脱氧核糖核酸结合，这一现象可能对其抗病毒活性很重要。
