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黄酮类化合物3',4',5'-三甲氧基黄酮醇的合成及其在小鼠血浆和组织中的高效液相色谱荧光检测法测定

Synthesis of the flavonoid 3',4',5'-trimethoxyflavonol and its determination in plasma and tissues of mice by HPLC with fluorescence detection.

作者信息

Britton Robert G, Fong Isabel, Saad Shaban, Brown Karen, Steward William P, Gescher Andreas, Sale Stewart

机构信息

Department of Cancer Studies and Molecular Medicine, RKCSB, Leicester Royal Infirmary, University of Leicester, Leicester, LE2 7LX, UK.

出版信息

J Chromatogr B Analyt Technol Biomed Life Sci. 2009 Apr 1;877(10):939-42. doi: 10.1016/j.jchromb.2009.02.043. Epub 2009 Feb 24.

DOI:10.1016/j.jchromb.2009.02.043
PMID:19282252
Abstract

3',4',5'-Trimethoxyflavonol (TMFol) was synthesized as a potential colorectal cancer chemopreventive agent. An HPLC method for determination for TMFol in murine plasma and tissues was developed and validated using human plasma. Analyte was separated (C(18) column; fluorescence detection 330nm excitation, 440nm emission) using 69% methanol and 0.1M ammonium acetate buffer (pH 5.1) as mobile phase. The method was linear for 50-2500ng/ml plasma and 0.05-10microg/g tissue (r>0.99). TMFol was recovered from plasma or tissues using solid phase columns or organic solvent protein precipitation, respectively. Recovery at low, medium and high concentrations was 97.6-107.3%, with inter- and intra-day coefficients of variation of <10%. The lower limit of quantitation for plasma was 50ng/ml. The method was applied to measure steady-state TMFol plasma and tissue levels in mice which received dietary TMFol (0.2%).

摘要

3',4',5'-三甲氧基黄酮醇(TMFol)作为一种潜在的结直肠癌化学预防剂被合成出来。开发了一种用于测定小鼠血浆和组织中TMFol的高效液相色谱法,并使用人血浆进行了验证。以69%甲醇和0.1M醋酸铵缓冲液(pH 5.1)作为流动相,在C(18)柱上分离分析物(荧光检测,激发波长330nm,发射波长440nm)。该方法在血浆浓度为50 - 2500ng/ml和组织浓度为0.05 - 10μg/g时呈线性(r>0.99)。分别使用固相柱或有机溶剂蛋白沉淀法从血浆或组织中回收TMFol。低、中、高浓度下的回收率为97.6 - 107.3%,日内和日间变异系数<10%。血浆的定量下限为50ng/ml。该方法用于测量接受含0.2%TMFol饮食的小鼠血浆和组织中的稳态TMFol水平。

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引用本文的文献

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Preclinical colorectal cancer chemopreventive efficacy and p53-modulating activity of 3',4',5'-trimethoxyflavonol, a quercetin analogue.3',4',5'-三甲氧基黄酮醇,一种槲皮素类似物,在临床前结直肠癌化学预防功效和 p53 调节活性。
Cancer Prev Res (Phila). 2010 Aug;3(8):929-39. doi: 10.1158/1940-6207.CAPR-09-0236. Epub 2010 Jul 13.