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豚鼠体内(24R和24S)-27-降-24-甲基-3α,7α-二羟基-5β-胆甾烷-26-酸及27-降-3α,7α-二羟基-5β-胆甾烷-26-酸的代谢

Metabolism of (24R and 24S)-27-nor-24-methyl-3alpha,7alpha-dihydroxy-5beta-cholestan-26-oic acids and 27-nor-3alpha,7alpha-dihydroxy-5beta-cholestan-26-oic acid in guinea pigs.

作者信息

Kihira K, Mosbach E H

出版信息

Steroids. 1978 Dec;32(5):659-67. doi: 10.1016/0039-128x(78)90076-4.

DOI:10.1016/0039-128x(78)90076-4
PMID:734700
Abstract

[7beta-3H]-(24R and 24S)-27-nor-24-methyl-3alpha,7alpha-dihydroxy-5beta-cholestan-26-oic acids and [7beta-3H]-27-nor-3alpha,7alpha-dihydroxy-5beta-cholestan-26-oic acid (C27 and C26 bile acids having the same nuclear configuration as cheno-deoxycholic acid and its precursor, 3alpha,7alpha-dihydroxy-5beta-cholestan-26-oic-acid) were synthesized and administered intraperitoneally to bile fistula guinea pigs. The biliary bile acids formed were hydrolyzed and analyzed by thin layer chromatography, and the metabolites were identified by the inverse isotope dilution method. The results showed that both (24R and 24S)-27-nor-24-methyl-3alpha,7alpha-dihydroxy-5beta-cholestan-26-oic acids were not metabolized by the liver and were excreted unchanged as their taurine and glycine conjugates whereas 27-nor-3alpha,7alpha-dihydroxy-5beta-cholestan-26-oic acid was converted to chenodeoxycholic acid.

摘要

[7β-³H]-(24R和24S)-27-降-24-甲基-3α,7α-二羟基-5β-胆甾烷-26-酸以及[7β-³H]-27-降-3α,7α-二羟基-5β-胆甾烷-26-酸(具有与鹅去氧胆酸及其前体3α,7α-二羟基-5β-胆甾烷-26-酸相同核构型的C27和C26胆汁酸)被合成并腹腔注射给胆瘘豚鼠。形成的胆汁胆汁酸经水解后用薄层色谱法分析,代谢产物通过反同位素稀释法鉴定。结果表明,(24R和24S)-27-降-24-甲基-3α,7α-二羟基-5β-胆甾烷-26-酸均未被肝脏代谢,而是以其牛磺酸和甘氨酸共轭物的形式原样排泄,而27-降-3α,7α-二羟基-5β-胆甾烷-26-酸则转化为鹅去氧胆酸。

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