Post-Graduate Program in Pharmaceutical Sciences, State University of Maringá, Av. Colombo, 5790, BR-87020-900, Maringá, PR, Brazil.
Molecules. 2012 Feb 14;17(2):1852-9. doi: 10.3390/molecules17021852.
Arctium lappa L. (Asteraceae) is used in folk medicine around the World, and shows several kinds of biological activity, particularly in vitro antitumor activity in different cell lines. This study evaluated the antiproliferative activity of the crude extract, semipurified fractions, and isolated compounds from the leaves of A. lappa, through bioassay-guided testing in Caco-2 cells. The crude extract was obtained with a 50% hydroethanolic extract and then partitioned with hexane, ethyl acetate, and n-butanol. The ethyl-acetate fraction (EAF) showed antiproliferative activity. This fraction was subjected to sequential column chromatography over silica gel to afford onopordopicrin (1), mixtures of 1 with dehydromelitensin-8-(4'-hydroxymethacrylate) (2), a mixture of 2 with dehydromelitensin (3), mixture of 1 with melitensin (4), dehydrovomifoliol (5), and loliolide (6). The compounds were identified by spectroscopic methods (NMR, MS) and comparison with literature data. This is the first description of compounds 2-5 from this species. The compounds tested in Caco-2 cells showed the following CC(50) (µg/mL) values: 1: 19.7 ± 3.4, 1 with 2: 24.6 ± 1.5, 2 with 3: 27 ± 11.7, 1 with 4: 42 ± 13.1, 6 30 ± 6.2; compound 5 showed no activity.
牛蒡（菊科）在世界各地的民间医学中被使用，并显示出多种生物活性，特别是在不同细胞系中的体外抗肿瘤活性。本研究通过在 Caco-2 细胞中的生物测定指导测试，评估了牛蒡叶的粗提取物、半纯化馏分和分离化合物的抗增殖活性。粗提取物用 50%的水-乙醇提取物获得，然后用正己烷、乙酸乙酯和正丁醇进行分配。乙酸乙酯馏分（EAF）显示出抗增殖活性。该馏分通过硅胶柱色谱进行连续层析，得到牛蒡内酯（1）、1 与脱水米利定-8-（4'-羟甲基丙烯酸盐）（2）的混合物、2 与脱水米利定（3）的混合物、1 与米利定（4）的混合物、脱氢沃霉醇（5）和洛利奥内酯（6）。通过光谱方法（NMR、MS）和与文献数据的比较鉴定了这些化合物。这是该物种中化合物 2-5 的首次描述。在 Caco-2 细胞中测试的化合物显示出以下 CC（50）（µg/mL）值：1：19.7 ± 3.4，1 与 2：24.6 ± 1.5，2 与 3：27 ± 11.7，1 与 4：42 ± 13.1，6 30 ± 6.2；化合物 5 没有活性。
