~3H-萱草根素在小鼠体内吸收分布、排泄和代谢的初步观察

PRELIMINARY STUDY ON THE ABSORPTION, DISTRIBUTION, EXCRETION AND METABOLISM OF ^(3)H-HEMEROCALLIN IN MICE

本文应用放射性同位素示综技术,初步观察了~3H-萱草根素在小鼠体内吸收分布、排泄和代谢的全过程。~3H-萱草根素口服后0.5小时,小鼠血液中放射性即达到高峰,并以低浓度维持96小时以上;其随血液循环分布于各组织器官,以胃肠组织含量最高,其次是肝脏和脾脏。萱草根素有蓄积性;一次给药和以同等剂量分次(每天一次,三天)投药后的相同时间,各组织中~3H-萱草根素的含量差异不显著。主要排泄途径是粪便,其次是尿液。经有机溶剂处理后的尿液分为水、脂二相,其放射性测量和薄板层析放射自显影结果均表明:~3H-萱草根素在体内经过代谢后结构发生了变化,从尿液中排出的不是萱草根素原形,而是其代谢产物。

Hemerocallin ( phytotoxin of the Hemerocallis spp. ) causes poisoning in sheep and laboratory animals, but many toxicological aspects are still unknown.This research attempts to give a preliminary toxico-lological observation on the pattern of absorption, distribution, excretion and metabolism of 3H-labeled Hemerocallin in mice by means of tracing technique of radioisotope.The radioactivity in the blood reached its highest level at 30 minutes after 3H-Hemerocallin was adminste-red orally, and kept a low concentration over 96 hours. 3H-Hemero-callin was distributed in all tissues by blood circulation, its peak of concentration was in the tissues of alimentary tract and then in the liver. 3H-Hemerocallin concentration in different tissues varied with its affinity. When radioactivity of every tissue was determined at 96 hours after administration, the difference between single and divided dose ( 0.1 mg/20 g B.W. ) was not evident. The pathway of excretion was GI tract and kidney.By adding organic solvent, urine could be separated into two fraction ( water and lipid phase ) , and measured by thin-layer chromatographic radioautography and liquid scintillation counting.The results indicated that 3H-Hemerocallin was metabolized in the body of mice, and its structure was changed. Therefore, the 3H-Hemerocallin in urine was not the original form, but its metabolites.