Mervai Zsolt, Sólyomváry Anna, Tóth Gergő, Noszál Béla, Molnár-Perl Ibolya, Baghy Kornélia, Kovalszky Ilona, Boldizsár Imre
1st Department of Pathology and Experimental Cancer Research, Semmelweis University, Üllői út 26, Budapest 1085, Hungary.
Department of Plant Anatomy, Institute of Biology, Eötvös Loránd University, Pázmány Péter sétány 1/C, Budapest 1117, Hungary.
Fitoterapia. 2015 Jan;100:19-26. doi: 10.1016/j.fitote.2014.10.017. Epub 2014 Nov 11.
The molecular constituents of Cirsium brachycephalum fruits were identified, quantified and isolated for the first time. The lignan glycoside tracheloside was the main compound, which was transformed quantitatively into its aglycone trachelogenin by endogenous enzymatic treatment of the fruit. Following this transformation by high performance liquid chromatography (HPLC) hyphenated with UV and mass spectrometry (MS) detections on a quantitative basis, the enzyme-hydrolyzed fruit was found to be the richest raw material containing trachelogenin (17.2mg/g) reported to date. Thus, the enzyme-hydrolyzed fruit was used to isolate trachelogenin using preparative HPLC in order to (1) unambiguously confirm its identity by gas chromatography-MS, nuclear magnetic resonance spectroscopy and optical rotation, and (2) investigate its in vitro antiproliferative activities against the SW480 colon adenocarcinoma cell line. Trachelogenin significantly affected the phosphorylation of key proteins such as β-Catenin, c-Myc and GSK3 in the β-Catenin signaling pathway in a concentration-dependent manner. These changes account for the antiproliferative effects of trachelogenin.
首次对短头蓟果实的分子成分进行了鉴定、定量和分离。木脂素糖苷络石苷是主要化合物，通过对果实进行内源性酶处理，它被定量转化为其苷元络石苷元。在通过高效液相色谱（HPLC）与紫外和质谱（MS）检测联用对这种转化进行定量分析后，发现经酶水解的果实是迄今为止报道的含络石苷元最丰富的原料（17.2mg/g）。因此，使用制备型HPLC从经酶水解的果实中分离络石苷元以（1）通过气相色谱 - 质谱、核磁共振光谱和旋光性明确确认其身份；（2）研究其对SW480结肠腺癌细胞系的体外抗增殖活性。络石苷元以浓度依赖的方式显著影响β-连环蛋白信号通路中关键蛋白如β-连环蛋白、c-Myc和GSK3的磷酸化。这些变化解释了络石苷元的抗增殖作用。
