Shattuck K E, Radominska-Pyrek A, Zimniak P, Adcock E W, Lester R, St Pyrek J
Hepatology. 1986 Sep-Oct;6(5):869-73. doi: 10.1002/hep.1840060511.
24-Norlithocholic (3 alpha-hydroxy-24-nor-5 beta-cholan-23-oic) acid is the lower homologue of lithocholic acid, a potent cholestatic agent. In order to characterize its cholestatic potential and metabolic fate, 3 beta-tritiated 24-norlithocholate was infused intravenously into adult male Sprague-Dawley rats prepared with an external biliary fistula. The results demonstrate that 24-norlithocholate does not induce cholestasis in rats when administered in doses in excess of those necessary for lithocholate to produce cholestasis. Hydroxyl- and carboxyl-linked glucuronides were identified as major metabolites secreted in the bile. Especially noteworthy is the identification of carboxyl-linked glucuronides of mono-, di- and trihydroxylated C23 bile acids. Their total amount (25% of recovered radioactive products) is comparable to that of the hydroxyl-linked glucuronide of 24-norlithocholic acid (41%). In this study, for the first time, a bile acid diglucuronide, substituted both at 3-hydroxyl and carboxyl groups, was detected (11%).
24-去甲石胆酸（3α-羟基-24-去甲-5β-胆烷-23-酸）是强效胆汁淤积剂石胆酸的低级同系物。为了表征其胆汁淤积潜力和代谢命运，将3β-氚标记的24-去甲石胆酸盐静脉注射到制备了体外胆瘘的成年雄性Sprague-Dawley大鼠体内。结果表明，当给予24-去甲石胆酸盐的剂量超过石胆酸盐产生胆汁淤积所需的剂量时，它不会在大鼠中诱导胆汁淤积。羟基连接和羧基连接的葡萄糖醛酸苷被鉴定为胆汁中分泌的主要代谢产物。特别值得注意的是鉴定出了单羟基、二羟基和三羟基化C23胆汁酸的羧基连接葡萄糖醛酸苷。它们的总量（占回收放射性产物的25%）与24-去甲石胆酸的羟基连接葡萄糖醛酸苷的总量（41%）相当。在本研究中，首次检测到一种在3-羟基和羧基均被取代的胆汁酸二葡萄糖醛酸苷（11%）。
