Marandici A, Monder C
J Steroid Biochem. 1985 Apr;22(4):539-45. doi: 10.1016/0022-4731(85)90175-x.
The conversion of [4 14C]corticosterone[( 14C]B) and 11-deoxy-[1,2-3H]corticosterone [( 3H]DOC) to steroidal carboxylic acids was studied in the BALB/c mouse. There was rapid and preferential excretion of [3H]DOC metabolites into the gastrointestinal tract. Excretion of 14C through the kidney was higher than 3H excretion. Within minutes of intraperitoneal injection, levels of 3H and 14C in most organs reached their maximal levels and subsequently decreased in an exponential pattern. The majority of the organs took up 14C to a greater extent than 3H. Using tissue blood ratio of tracer (T/B) as criterion, it was found that liver, gall bladder, intestine, and kidney concentrated 3H and 14C-labeled steroid from blood. T/B for 3H exceeded that for 14C in the gastrointestinal tract. Abdominal fat preferentially took up [3H]DOC tracer, whereas [14C]B tracer was not taken up by this tissue. T/B was less than 1 for 3H and 14C in heart, thymus, spleen, brain, skeletal muscle and skin. In these organs uptake of B and its metabolites was greater than that of DOC and its metabolites. In liver, [14C]B and [3H]DOC were converted to carboxylic acid metabolites which accumulated in the intestine. The most abundant acid was 11 beta,20 alpha-dihydroxy-3-oxo-pregn-4-en-21-oic acid from B. The acid metabolites of DOC were not identified. For both steroids, acids were major metabolic end-products.
在BALB/c小鼠中研究了[4¹⁴C]皮质酮[¹⁴C]B和11-脱氧-[1,2-³H]皮质酮[³H]DOC向甾体羧酸的转化。[³H]DOC代谢产物迅速且优先排泄到胃肠道。¹⁴C通过肾脏的排泄高于³H的排泄。腹腔注射后几分钟内,大多数器官中的³H和¹⁴C水平达到最高水平,随后呈指数下降。大多数器官摄取¹⁴C的程度高于³H。以示踪剂的组织血药比(T/B)为标准,发现肝脏、胆囊、肠道和肾脏从血液中浓缩³H和¹⁴C标记的类固醇。胃肠道中³H的T/B超过¹⁴C的T/B。腹部脂肪优先摄取[³H]DOC示踪剂,而该组织不摄取[¹⁴C]B示踪剂。心脏、胸腺、脾脏、大脑、骨骼肌和皮肤中³H和¹⁴C的T/B小于1。在这些器官中,B及其代谢产物的摄取量大于DOC及其代谢产物。在肝脏中,[¹⁴C]B和[³H]DOC转化为积聚在肠道中的羧酸代谢产物。最丰富的酸是来自B的11β,20α-二羟基-3-氧代-孕-4-烯-21-酸。未鉴定出DOC的酸代谢产物。对于这两种类固醇,酸都是主要的代谢终产物。