Olive P L
Int J Radiat Oncol Biol Phys. 1982 Mar-Apr;8(3-4):687-91. doi: 10.1016/0360-3016(82)90713-1.
The fluorescence of three nitroheterocycles (AF-2, trans-5-amino-3-(2-(5-nitro-2furyl) vinyl)-1,2,4-oxadiazole and 4-NQO) was used to quantitate cellular uptake and binding using a fluorescence-activated cell sorter. Mean cellular fluorescence, proportional to the amount of bound drug, allowed accurate prediction of the amount of cell killing. At equitoxic concentrations, the same amount of drug was bound under either aerobic or hypoxic conditions. In addition, 5 mM glutathione was equally effective at inhibiting aerobic and hypoxic cell killing by AF-2. These results suggest that the mechanism for cell killing may be similar under aerobic and hypoxic conditions, and the presence of oxygen may influence the rate of drug uptake rather than the nature of the toxic species. The nitro anion radical, formed in the presence and absence of oxygen, seems a likely candidate for the "toxic species."
利用三种硝基杂环化合物（AF-2、反式-5-氨基-3-(2-(5-硝基-2-呋喃基)乙烯基)-1,2,4-恶二唑和4-硝基喹啉-1-氧化物）的荧光，通过荧光激活细胞分选仪对细胞摄取和结合进行定量分析。与结合药物量成正比的平均细胞荧光，能够准确预测细胞杀伤量。在等毒性浓度下，无论有氧还是缺氧条件，结合的药物量相同。此外，5 mM谷胱甘肽在抑制AF-2对有氧和缺氧细胞的杀伤作用方面同样有效。这些结果表明，有氧和缺氧条件下细胞杀伤机制可能相似，氧气的存在可能影响药物摄取速率而非有毒物质的性质。无论有无氧气存在时形成的硝基阴离子自由基似乎是“有毒物质”的一个可能候选者。
