title: Two new benzofurans from Gastrodia elata and their DNA topoisomerases I and II inhibitory activities.
abstract: Two new benzofurans, 1-furan-2-yl-2-(4-hydroxyphenyl)-ethanone (1) and 5-(4-hydroxybenzyloxymethyl)-furan-2-carbaldehyde (2), together with five known compounds, 4-hydroxybenzyl methyl ether (3), 5-(hydroxymethyl)-furfural (4), gastrodin (5), beta-sitosterol (6) and beta-sitosterol glucoside (7) were isolated from the rhizome of Gastrodia elata Blume. In DNA topoisomerase I and II inhibition assays in vitro at a concentration of 20 microM, 1 showed potent inhibitory activity, 66% and 71% inhibition, respectively, compared to the positive control compounds, camptothecin and etoposide, 71% and 22% inhibition, respectively. All of these compounds exhibited weak or no cytotoxicities against human colon carcinoma cell line (HT-29), human breast carcinoma cell line (MCF-7) and human hepatocellular carcinoma cell line (HepG-2).
authors.affiliation: College of Pharmacy, Yeungnam University, Gyongsan, Republic of Korea.
authors.forename: Yeun-Kyung
authors.initials: YK
authors.lastname: Lee
authors.forename: Mi-Hee
authors.initials: MH
authors.lastname: Woo
authors.forename: Chul-Ho
authors.initials: CH
authors.lastname: Kim
authors.forename: Youngsoo
authors.initials: Y
authors.lastname: Kim
authors.forename: Sung-Ho
authors.initials: SH
authors.lastname: Lee
authors.forename: Byeong-Seon
authors.initials: BS
authors.lastname: Jeong
authors.forename: Hyun-Wook
authors.initials: HW
authors.lastname: Chang
authors.forename: Jong-Keun
authors.initials: JK
authors.lastname: Son
mesh_terms: D000970:Antineoplastic Agents / Q000302:isolation & purification / Q000494:pharmacology; D001572:Benzofurans / Q000302:isolation & purification / Q000494:pharmacology*; D045744:Cell Line, Tumor; D031668:Gastrodia / Q000737:chemistry*; D006801:Humans; D010946:Plants, Medicinal / Q000737:chemistry; D027343:Rhizome / Q000737:chemistry; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors
chemical_list: D000970:Antineoplastic Agents; D001572:Benzofurans; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors