title: Cytotoxic and DNA topoisomerases I and II inhibitory constituents from the roots of Aralia cordata.
abstract: Bioactivity-guided fractionation, based on the DNA topoisomerase inhibitory activity, lead to the isolation of five compounds (1-5) from the methylene chloride extract of the roots of Aralia cordata Thunb. (Araliaceae). These compounds were identified as ent-pimara-8(14), 15-dien-19-oic acid (1), ent-pimara-8(14), 15-dien-18-oic acid (2), 16alpha-hydrogen-17-isovaleryloxy-ent-kauran-19-oic acid (3), 16alpha-hydroxy-17-isovaleryloxy-ent-kauran-19-oic acid (4) and dehydrofalcarindiol-8-acetate (5) from their spectral data. Compound 3 was isolated for the first time from this plant, and also showed the strongest inhibition of both DNA topoisomerase I and II activities, with 53 and 96% inhibitions, respectively, at a concentration of 20 microM. However, all the compounds exhibited either weak or no cytotoxicities against the human colon carcinoma cell line (HT-29), the human breast carcinoma cell line (MCF-7) and human hepato blastoma cell line (HepG-2).
authors: College of Pharmacy, Yeungnam University, Gyongsan 712-749, Korea.
authors: Chang-Seob
authors: CS
authors: Seo
authors: Gao
authors: G
authors: Li
authors: Chul-Ho
authors: CH
authors: Kim
authors: Chong-Soon
authors: CS
authors: Lee
authors: Yurngdong
authors: Y
authors: Jahng
authors: Hyun-Wook
authors: HW
authors: Chang
authors: Jong-Keun
authors: JK
authors: Son
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000302:isolation & purification* / Q000494:pharmacology; D027983:Aralia / Q000737:chemistry*; D004791:Enzyme Inhibitors / Q000302:isolation & purification* / Q000494:pharmacology; D018517:Plant Roots / Q000737:chemistry*; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D004791:Enzyme Inhibitors; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors