Department of Pharmaceutical Chemistry, Institute of Pharmaceutical Sciences, Karl-Franzens University Graz, Graz, Austria.
J Sep Sci. 2013 Feb;36(4):670-6. doi: 10.1002/jssc.201200768.
5-Hydroxymethylfurfural (5-HMF) is a natural occurring substance taken up by everyday food. In former studies it was shown that 5-HMF is completely decomposed in the body after oral or intravenous application resulting in three main metabolites named 5-hydroxymethylfuroic acid, 2,5-furandicarboxylic acid, and N-(hydroxymethyl)furoyl glycine, and possibly a forth metabolic substance, termed 5-sulphoxymethylfurfural, is formed. Determination is possible via HPLC using a hydrophilic interaction chromatography (HILIC) column with an appropriate gradient system (ACN/ammonium formate 100 mM, pH 2.35). Urine samples were purified by use of an SPE method beforehand working with ScreenA cartridges. This cleaning procedure was validated based on ICH guidelines in terms of linearity, quantification, and detection limit, as well as precision, repeatability, and accuracy. Analysis of real-life samples coming from two healthy probands and one cancer patient, who all received 240 mg 5-hydroxymethylfurfural orally once a day, showed dicarboxylic acid and the glycine conjugate in their urine samples. Recovery of the initial compound in form of transformed metabolites was up to 90% within 48 h. Potentially toxic 5-sulphoxymethylfurfural could not be found.
5-羟甲基糠醛（5-HMF）是一种天然存在于日常食品中的物质。在以前的研究中表明，5-HMF 在口服或静脉应用后会在体内完全分解，生成三种主要代谢产物，分别为 5-羟甲基糠酸、2,5-呋喃二甲酸和 N-（羟甲基）糠酰甘氨酸，并且可能形成第四种代谢产物，称为 5-磺基甲基糠醛。通过使用亲水相互作用色谱（HILIC）柱和适当的梯度系统（ACN/100mM 甲酸铵，pH2.35），可以通过 HPLC 进行测定。尿液样品在使用 ScreenA 小柱进行 SPE 方法纯化之前进行预处理。该清洗程序是根据 ICH 指南进行验证的，包括线性、定量和检测限，以及精密度、重复性和准确性。对来自两个健康志愿者和一个癌症患者的实际样本进行分析，这些患者每天口服 240mg 5-羟甲基糠醛，结果显示在尿液样本中存在二羧酸和甘氨酸结合物。在 48 小时内，初始化合物以转化代谢产物的形式回收了高达 90%。未发现潜在有毒的 5-磺基甲基糠醛。
