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高效液相色谱法测定小鼠血浆中的呫吨酮-4-乙酸

Determination of xanthenone-4-acetic acid in mouse plasma by high-performance liquid chromatography.

作者信息

Kestell P, McKeage M J, Baguley B C

机构信息

Cancer Research Laboratory, University of Auckland Medical School, New Zealand.

出版信息

J Chromatogr. 1991 Mar 8;564(1):315-21. doi: 10.1016/0378-4347(91)80097-v.

Abstract

Xanthenone-4-acetic acid (XAA) was synthesised during a search for improved analogues of flavone-8-acetic acid, an antitumour agent with a unique mechanism of action but with a number of pharmacological disadvantages. We describe a simple, selective high-performance liquid chromatographic assay suitable for the detection of XAA in mouse plasma. After addition of an internal standard (3-methyl-XAA), plasma was acidified with trichloroacetic acid and extracted with toluene. After evaporation of solvent, samples were chromatographed on a C18 4-microns Novapak cartridge (mobile phase: water-acetonitrile-acetic acid, 65:35:2, v/v) using fluorescence detection. At the maximum tolerated dose of XAA (725 mumol/kg), nonlinear pharmacokinetics were observed.

摘要

在寻找黄酮 -8- 乙酸的改良类似物过程中合成了呫吨酮 -4- 乙酸(XAA),黄酮 -8- 乙酸是一种具有独特作用机制但存在许多药理学缺点的抗肿瘤药物。我们描述了一种适用于检测小鼠血浆中 XAA 的简单、选择性高效液相色谱法。加入内标(3-甲基 -XAA)后,用三氯乙酸将血浆酸化,并用甲苯萃取。溶剂蒸发后,样品在 C18 4 微米的诺瓦帕克柱(流动相:水 - 乙腈 - 乙酸,65:35:2,v/v)上进行色谱分析,采用荧光检测。在 XAA 的最大耐受剂量(725 μmol/kg)下,观察到非线性药代动力学。

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