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Isolation and identification of metabolites of osthole in rats.
Lv, X; Wang, C-Y; Hou, J; Zhang, B-J; Deng, S; Tian, Y; Huang, S-S; Zhang, H-L; Shu, X-H; Zhen, Y-H; Liu, K-X; Yao, J-H; Ma, X-C.
Afiliación
  • Lv X; School of Pharmacy, Pharmacokinetic and Drug Transport Key Laboratory, Dalian Medical University, Dalian, China.
Xenobiotica ; 42(11): 1120-7, 2012 Nov.
Article en En | MEDLINE | ID: mdl-22630788
Osthole (Ost), one of the major components of Cnidium monnieri (L.) Cusson, is had the structure of an isopentenoxy-coumarin with a range of pharmacological activities. In the present study, the metabolism of Ost in male Sprague-Dawley rats was investigated by identifying Ost metabolites excreted in rat urine. Following an oral dose of 40 mg/kg Ost, 10 phase I and 3 phase II metabolites were isolated from the urine of rats, and their structures identified on the basis of a range of spectroscopic data, including 2D-NMR techniques. These metabolites were fully characterized as 5'-hydroxyl-osthole (M-1), osthenol (M-2), 4'-hydroxyl-osthole (M-3), 3, 5'-dihydroxyl-osthole (M-4), 5'-hydroxyl-osthenol (M-5), 4'-hydroxyl-2', 3'-dihydro-osthenol (M-6), 4'-hydroxyl-osthenol (M-7), 3, 4'-dihydroxyl-osthole (M-8), 2', 3'-dihydroxyl-osthole (M-9), 5'-hydroxyl-2', 3'-dihydroosthole (M-10), osthenol-7-O-ß-D-glucuronide (M-11), osthole-4'-O-ß-D-glucuronide (M-12) and osthole-5'-O-ß-D-glycuronate (M-13). This is the first identification of M-1, M-3 to M-13 in vivo. On the basis of the metabolites profile, a possible metabolic pathway for Ost metabolism in rats has been proposed. This is the first systematic study on the phases I and II metabolites of 8-isopentenoxy-coumarin derivative.
Asunto(s)

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Adyuvantes Inmunológicos / Cumarinas / Cnidium Tipo de estudio: Diagnostic_studies Límite: Animals Idioma: En Revista: Xenobiotica Año: 2012 Tipo del documento: Article País de afiliación: China Pais de publicación: Reino Unido

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Adyuvantes Inmunológicos / Cumarinas / Cnidium Tipo de estudio: Diagnostic_studies Límite: Animals Idioma: En Revista: Xenobiotica Año: 2012 Tipo del documento: Article País de afiliación: China Pais de publicación: Reino Unido