Nagahara A, Kumagai S
Department of Biomedical Research on Food, National Institute of Health, Tokyo, Japan.
Food Chem Toxicol. 1991 Apr;29(4):243-7. doi: 10.1016/0278-6915(91)90021-x.
The excretion and distribution of 14C were studied in rats given by oral intubation 14C-labelled (-)-(1S,3S)-1-methyl-1,2,3,4-tetrahydro-beta-carboline-3-carboxylic acid and its stereoisomer, (-)-(1R,3S)-1-methyl-1,2,3,4-tetrahydro-beta-carboline-3-carboxylic acid (MTCAs), compounds that are known to become mutagenic on reaction with nitrite. For comparison, another group of rats was given by oral intubation products of the in vitro treatment of [14C]MTCAs with nitrite. When rats were given the untreated [14C]MTCAs, most of the 14C was excreted in the faeces within 24 hr and was noted only in the intestine on autoradiograms of rats killed 30 min and 6 hr after dosing. In contrast, when rats were given the nitrite-treated [14C]MTCAs, 14C was mainly excreted in the urine within 24 hr and was noted not only in the intestine but also in the liver and kidney on autoradiogram. These results suggest that the majority of MTCAs pass rapidly through the gastro-intestinal tract, while the bulk of the reaction products of MTCAs with nitrite are absorbed from the gastro-intestinal tract and excreted in the urine.
对经口插管给予14C标记的(-)-(1S,3S)-1-甲基-1,2,3,4-四氢-β-咔啉-3-羧酸及其立体异构体(-)-(1R,3S)-1-甲基-1,2,3,4-四氢-β-咔啉-3-羧酸(MTCAs)的大鼠进行了14C的排泄和分布研究,已知这些化合物与亚硝酸盐反应时会产生致突变性。作为对照,另一组大鼠经口插管给予用亚硝酸盐体外处理[14C]MTCAs的产物。当给大鼠未处理的[14C]MTCAs时,大部分14C在24小时内随粪便排出,给药后30分钟和6小时处死的大鼠的放射自显影片上仅在肠道中发现14C。相反,当给大鼠用亚硝酸盐处理的[14C]MTCAs时,14C在24小时内主要随尿液排出,放射自显影片上不仅在肠道中发现14C,在肝脏和肾脏中也有发现。这些结果表明,大多数MTCAs迅速通过胃肠道,而MTCAs与亚硝酸盐的大部分反应产物则从胃肠道吸收并随尿液排出。