Elferink J G, Deierkauf M
Biochim Biophys Acta. 1985 Sep 30;846(3):364-9. doi: 10.1016/0167-4889(85)90007-2.
Exposure of rabbit polymorphonuclear leukocytes to micromolar concentrations of quin2-AM results in high intracellular concentrations of quin2, which lead to inhibition of chemotaxis. The loading efficiency of polymorphonuclear leukocytes, being the percentage of quin2-AM which is taken up by the cells and transformed intracellularly into quin2, is very high, reaches a maximum after 30 min, is independent of the presence of extracellular Ca2+ and is fairly independent of cell concentration. As a consequence, inhibition of chemotaxis is strongly dependent on experimental conditions: with a low cell density (3 X 10(6)/ml) exposure to 20 microM quin2-AM results in complete inhibition of chemotaxis, whereas the same concentration of quin2-AM is nearly without effect when an 8-fold higher cell concentration is used. Inhibition by quin2 is dependent on extracellular Ca2+; inhibition is more pronounced in the absence of extracellular Ca2+ than in its presence. It is suggested that quin2 inhibits chemotaxis by interference with intracellular Ca2+.
将兔多形核白细胞暴露于微摩尔浓度的喹啉-2-乙酰甲酯(quin2-AM)会导致细胞内喹啉-2(quin2)浓度升高,进而抑制趋化性。多形核白细胞的负载效率,即被细胞摄取并在细胞内转化为quin2的quin2-AM的百分比,非常高,30分钟后达到最大值,与细胞外Ca2+的存在无关,且与细胞浓度相当无关。因此,趋化性的抑制强烈依赖于实验条件:在低细胞密度(3×10⁶/ml)下,暴露于20μM的quin2-AM会导致趋化性完全抑制,而当使用高8倍的细胞浓度时,相同浓度的quin2-AM几乎没有作用。quin2的抑制作用依赖于细胞外Ca2+;在没有细胞外Ca2+的情况下比在其存在时抑制作用更明显。有人提出,quin2通过干扰细胞内Ca2+来抑制趋化性。