Evaluation of the Antiproliferative Activity of the Leaves from Arctium lappa by a Bioassay-Guided Fractionation

Molecules

Fabio Bahls Machado¹  Rafael Eidi Yamamoto¹  Karine Zanoli¹  Samara Requena Nocchi¹  Cláudio Roberto Novello¹  Ivânia Teresinha Albrecht Schuquel¹  Cássia Mônica Sakuragui¹  Heinrich Luftmann¹  Tânia Ueda-Nakamura¹  Celso Vataru Nakamura¹ 

[1] ¹Post-Graduate Program in Pharmaceutical Sciences, State University of Maringá, Av. Colombo, 5790, BR-87020-900, Maringá, PR, Brazil

关键词: Asteraceae;    Arctium lappa;    antiproliferative activity;    sesquiterpene lactones;   

DOI  :  10.3390/molecules17021852

来源: mdpi

【 摘 要 】

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 CC₅₀ (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.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.