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用于分离和鉴定潜在细胞抑制药物奥拉西的代谢物的高效液相色谱分析

High-performance liquid chromatographic assay for the separation and characterization of metabolites of the potential cytostatic drug oracine.

作者信息

Wsól V, Kvasnicková E, Szotáková B, Hais I M

机构信息

Department of Biochemical Sciences, Faculty of Pharmacy, Charles University, Hradec Králové, Czech Republic.

出版信息

J Chromatogr B Biomed Appl. 1996 May 31;681(1):169-75. doi: 10.1016/0378-4347(96)00066-7.

DOI:10.1016/0378-4347(96)00066-7
PMID:8798926
Abstract

Oracine (I), a potential cytostatic drug, is enzymically converted to a number of metabolites whose formation has been studied in vitro and in vivo. The metabolites were separated by reversed-phase HPLC and characterized by UV spectra. Preparative TLC served for the isolation of the individual metabolites to allow their identification. Two metabolites were identified by Fourier transform NMR as 11-dihydrooracine (II) and a phenolic product (III). Two further metabolites (IV,V) were characterized. Some minor, presumably 11-dihydro metabolites and an 11-oxo metabolite produced in vitro and in vivo were revealed.

摘要

奥拉辛(I)是一种潜在的细胞生长抑制剂,可通过酶促反应转化为多种代谢产物,其生成过程已在体外和体内进行了研究。这些代谢产物通过反相高效液相色谱法进行分离,并通过紫外光谱进行表征。制备型薄层色谱用于分离各个代谢产物以进行鉴定。通过傅里叶变换核磁共振鉴定出两种代谢产物为11-二氢奥拉辛(II)和一种酚类产物(III)。另外两种代谢产物(IV,V)也得到了表征。还发现了一些在体外和体内产生的少量可能的11-二氢代谢产物和一种11-氧代代谢产物。

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