Dougherty M A, Weimer G R, Nahrwold D L, Rose R C
Biochim Biophys Acta. 1979 Nov 2;557(2):486-93. doi: 10.1016/0005-2736(79)90345-6.
Absorption of the known chemical carcinogen, 2-acetylaminofluorene has been measured in the colon of guinea pigs. Unidirectional influx across the luminal cell membrane was determined in vitro, and transmural absorption across colonic mucosa was evaluated in vivo. The kinetics of unidirectional influx into colon in vitro do not indicate that absorption proceeds by simple diffusion. The observed saturable uptake is indicative of binding of 2-acetylaminofluorene to a cellular component. With 2-acetylaminofluorene present in the lumen in vivo at an initial concentration of 3.5 microM, the rate of absorption decreases over a 20 min period, which also indicates some form of specific interaction between 2-acetylaminofluorene and the intestinal mucosa. We have evaluated the hypothesis that surfactants and a bile salt act as cocarcinogens by increasing the rate of intestinal absorption of 2-acetylaminofluorene. The results lend no support to this possibility.
已在豚鼠结肠中测定了已知化学致癌物2-乙酰氨基芴的吸收情况。在体外测定了其跨腔细胞膜的单向流入,在体内评估了其跨结肠黏膜的透壁吸收。体外结肠单向流入的动力学并不表明吸收是通过简单扩散进行的。观察到的饱和摄取表明2-乙酰氨基芴与细胞成分发生了结合。当体内管腔中2-乙酰氨基芴的初始浓度为3.5微摩尔时,吸收速率在20分钟内下降,这也表明2-乙酰氨基芴与肠黏膜之间存在某种形式的特异性相互作用。我们评估了表面活性剂和一种胆盐通过增加2-乙酰氨基芴的肠道吸收速率而作为促癌剂的假说。结果不支持这种可能性。