Key Laboratory of Environment and Genes Related to Diseases, Ministry of Education, China.
J Pharm Biomed Anal. 2010 Apr 6;51(5):1032-6. doi: 10.1016/j.jpba.2009.11.007. Epub 2009 Nov 13.
We have developed an online analytical method that combines alpha(1A)-adrenoceptor (alpha(1A)AR) cell membrane chromatography (alpha(1A)AR-CMC) with high performance liquid chromatography and mass spectrometry (HPLC/MS) for the identification of active components from Radix Caulophylli acting on the human alpha(1A)AR. Fractions retained by the alpha(1A)AR-CMC column were captured into a loop and the components were directly analyzed by combining an 8 port column switcher with an HPLC/MS system for separation and preliminary identification. Using methoxamine as a positive control drug, magnoflorine and caulophine from Radix Caulophylli were identified as the active molecules acting on the alpha(1A)AR. This new alpha(1A)AR-CMC-online-HPLC/MS method can be applied for screening active components acting on alpha(1A)AR from traditional Chinese medicines exemplified by Radix Caulophylli. This method will be of great utility in drug discovery using natural medicinal herbs as a source of novel compounds.
我们开发了一种在线分析方法，将 α1A-肾上腺素能受体（α1AAR）细胞膜色谱（α1AAR-CMC）与高效液相色谱和质谱（HPLC/MS）相结合，用于鉴定来自八角枫作用于人类 α1AAR 的活性成分。用 α1AAR-CMC 柱保留的馏分被捕获到一个环中，并通过将 8 端口柱切换器与 HPLC/MS 系统结合，直接对成分进行分析，以进行分离和初步鉴定。使用甲氧胺作为阳性对照药物，从八角枫中鉴定出小檗碱和八角枫碱是作用于 α1AAR 的活性分子。这种新的 α1AAR-CMC-在线-HPLC/MS 方法可用于从八角枫等中药中筛选作用于 α1AAR 的活性成分。该方法将在利用天然草药作为新型化合物来源的药物发现中具有很大的应用价值。
