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无需样品制备即可同时对生物介质中的疏水性前药及其亲水性代谢物进行高效液相色谱分析。该方法在源自5-氟尿嘧啶的前核苷酸生物转化研究中的应用。

Simultaneous HPLC analysis of hydrophobic prodrugs and their hydrophilic metabolites in biological media without sample preparation. Application to the biotransformation studies of pronucleotides derived from 5-fluorouracil.

作者信息

Coussot G, Lefebvre-Tournier I, Hollecker L, Gosselin G, Imbach J L, Pompon A

机构信息

Laboratoire de Chimie Organique Biomoléculaire de Synthèse, UMR 5625 CNRS-UMII, Université Montpellier II, 34095 Montpellier, France.

出版信息

Nucleosides Nucleotides Nucleic Acids. 2001 Apr-Jul;20(4-7):855-8. doi: 10.1081/NCN-100002445.

Abstract

Improvements of an "on-line cleaning" HPLC method for analysis of biological samples are presented: (i) the use of cleaning precolumns filled with hydrophobic stationary phases instead of the hydrophilic ones previously used to eliminate the biological matrix: (ii) the combination in the mobile phase of anionic and cationic pairing reagents in order to retain on the precolumn all the metabolites, whatever their hydrophilicity and ionicity are. Such modifications allowed to study the biotransformation of prodrugs of 5-Fluorouracil, designed to act as antitumoral pronucleotides.

摘要

本文介绍了一种用于生物样品分析的“在线清洗”高效液相色谱(HPLC)方法的改进:(i)使用填充疏水固定相的清洗预柱,而非先前用于去除生物基质的亲水预柱;(ii)在流动相中组合使用阴离子和阳离子配对试剂,以便在预柱上保留所有代谢物,无论其亲水性和离子性如何。这些改进使得能够研究5-氟尿嘧啶前药的生物转化,这些前药被设计用作抗肿瘤前体核苷酸。

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