Identification of four biliary metabolites of the diterpene sclareol in the laboratory rat.
Identification of four biliary metabolites of the diterpene sclareol in the laboratory rat.
复制标题
实验室大鼠中二萜香紫苏醇的四种胆汁代谢物的鉴定。
DOI：
10.3109/00498259309059400
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发表时间：
1993
期刊：
影响因子：
--
通讯作者：
L. Walker
中科院分区：
文献类型：
--
作者：
S. Kouzi;J. McChesney;L. Walker
1. Ag.l.c。建立了测定实验室大鼠微生物培养物和生物液中菌核醇(1)及其微生物代谢物：3-酮-菌核醇(2)、2 - α -羟基菌核醇(3)、3- α -羟基菌核醇(4)、3- β -羟基菌核醇(5)、18-羟基菌核醇(6)和2 - α， 18-二羟基菌核醇(7)的方法。2. 在实验大鼠体内研究了二萜(1)的代谢。这项体内研究的便利条件是，可获得的菌核醇微生物代谢物作为参比标准，以及生物体液中菌核醇及其代谢物的g.l.c.测定。3. 经静脉注射（100 mg/kg）后，(1)从大鼠血浆中迅速消失，呈双期消失。血浆中未检出巩膜醇的微生物代谢物。4. 静脉或口服给药后，大鼠尿液中均未检测到Sclareol(1)及其微生物代谢物；Unchanged(1)在48小时内以口服剂量的9%从大鼠粪便中排出。静脉注射后，0.02%的剂量在胆汁中恢复不变(1)。(1)（0.4%剂量）的四种胆道代谢物经glc -质谱分析鉴定为(2)和(4)-(6)。(1)的四种胆道代谢产物均被鉴定为(1)的微生物代谢产物。
1. Ag.l.c. method was developed to determine sclareol (1) and its microbial metabolites: 3-keto-sclareol (2), 2 alpha-hydroxysclareol (3), 3 alpha-hydroxysclareol (4), 3 beta-hydroxysclareol (5), 18-hydroxysclareol (6), and 2 alpha, 18-dihydroxysclareol (7) in both microbial cultures and biological fluids of the laboratory rat. 2. Metabolism of the diterpene (1) was studied in the laboratory rat. This in vivo study was facilitated by the availability of microbial metabolites of sclareol as reference standards, and the g.l.c. assay for sclareol and its metabolites in biological fluids. 3. Following i.v. treatment (100 mg/kg), the disappearance of (1) from rat plasma was rapid and biphasic. No microbial metabolites of sclareol were detectable in plasma. 4. Sclareol (1) and its microbial metabolites were not detected in rat urine following either i.v. or oral treatments; unchanged (1) was excreted in rat faeces to the extent of 9% of an oral dose in 48 h. 5. Following i.v. treatment, 0.02% dose was recovered in bile as unchanged (1). Four biliary metabolites of (1) (0.4% dose) were identified as (2), and (4)-(6) based on g.l.c.-mass spectrometry and comparisons with reference standards. All four biliary metabolites of (1) in rat have been identified as microbial metabolites of (1).