Kihira K, Okamoto A, Ikawa S, Mikami T, Yoshii M, Mosbach E H, Hoshita T
Institute of Pharmaceutical Sciences, Hiroshima University School of Medicine.
J Biochem. 1991 Jun;109(6):879-81. doi: 10.1093/oxfordjournals.jbchem.a123474.
Metabolism of sodium 3 alpha,7 alpha-dihydroxy-5 beta-cholane-24-sulfonate, the sulfonate derivative of chenodeoxycholic acid, was studied in hamsters. In bile fistula hamsters, the sulfonate analogue was efficiently absorbed from the ileum and secreted rapidly into the bile without any modification such as conjugation. However, absorption from the jejunum was smaller than that observed for the ileum. After oral administration, the sulfonate analogue of chenodeoxycholic acid was recovered quantitatively in the feces as the unchanged form in contrast to simultaneously administered chenodeoxycholic acid, which was entirely converted to lithocholic acid during its passage through the intestinal tract. These results demonstrate that the sulfonate analogue is absorbed mainly from the ileum by active transport, enters the enterohepatic circulation like the endogenous conjugated bile acids, and completely resists bacterial degradation.
在仓鼠中研究了鹅去氧胆酸的磺酸盐衍生物——3α,7α - 二羟基 - 5β - 胆烷 - 24 - 磺酸钠的代谢。在胆瘘仓鼠中,磺酸盐类似物能从回肠有效吸收,并迅速分泌到胆汁中,且没有任何如结合等修饰。然而,从空肠的吸收量小于回肠。口服给药后,与同时给药的鹅去氧胆酸不同,鹅去氧胆酸的磺酸盐类似物以未改变的形式定量地在粪便中回收,鹅去氧胆酸在通过肠道时完全转化为石胆酸。这些结果表明,磺酸盐类似物主要通过主动转运从回肠吸收,像内源性结合胆汁酸一样进入肠肝循环,并且完全抵抗细菌降解。