Lasnitzki I, Bard D R, Franklin H R
Br J Cancer. 1975 Aug;32(2):219-29. doi: 10.1038/bjc.1975.152.
The uptake of 3-methycholanthrene and its metabolism to water-soluble derivatives were both determined in organ cultures of mouse and rat tissues, including prostate, skin, lung and skeletal muscle. All the tissues concentrated the carcinogen from the medium and metabolized part of it to water-soluble compounds. The uptake of tritiated 3-methylcholanthrene was highest in the absence of serum and declined with rising serum concentration. Except for skeletal muscle, it was consistently higher in the murine tissues. The uptake of the hydrocarbon by rat and mouse prostates rose rapidly with time, reaching a maximum after 18 h incubation; the amounts of carcinogen in the tissue then declined and remained at a lower level for the rest of the observation period. The major part of the radioactivity was released within 5 h of transferring the explants to medium without the tracer; 25-40% of the peak concentration of carcinogen, however, still remained in the tissue and further medium changes could not remove any more. Addition of unlabelled 3-methylcholanthrene to the initial incubation increased the radioactivity taken up and caused substantially larger quantities of the carcinogen to be retained after the medium had been changed. The explants converted between 15% and 30% of the 3-methylcholanthrene which they had incorporated to water-soluble derivatives within 48 h but there was no obvious relationship between the amounts of hydrocarbon taken up by the different tissues and the proportions metabolized. A considerable part of the 3-methylcholanthrene in the explants remained unconverted 24 h after its removal from the medium.
在小鼠和大鼠组织(包括前列腺、皮肤、肺和骨骼肌)的器官培养物中,测定了3-甲基胆蒽的摄取及其向水溶性衍生物的代谢情况。所有组织均从培养基中浓缩致癌物,并将其中一部分代谢为水溶性化合物。在无血清的情况下,氚标记的3-甲基胆蒽摄取量最高,且随血清浓度升高而下降。除骨骼肌外,其在小鼠组织中的摄取量始终较高。大鼠和小鼠前列腺对该烃类的摄取量随时间迅速增加,孵育18小时后达到最大值;之后组织中致癌物的量下降,并在观察期的剩余时间内维持在较低水平。将外植体转移至不含示踪剂的培养基后,大部分放射性在5小时内释放;然而,致癌物峰值浓度的25%-40%仍保留在组织中,进一步更换培养基也无法去除更多。在初始孵育中添加未标记的3-甲基胆蒽会增加摄取的放射性,并导致在更换培养基后有大量致癌物被保留。外植体在48小时内将其摄取的3-甲基胆蒽的15%-30%转化为水溶性衍生物,但不同组织摄取的烃类量与代谢比例之间没有明显关系。从培养基中取出24小时后,外植体中的相当一部分3-甲基胆蒽仍未转化。