Two new benzofurans from Gastrodia elata and their DNA topoisomerases I and II inhibitory activities.
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).
Lee
Yeun-Kyung
YK
College of Pharmacy, Yeungnam University, Gyongsan, Republic of Korea.
Woo
Mi-Hee
MH
Kim
Chul-Ho
CH
Kim
Youngsoo
Y
Lee
Sung-Ho
SH
Jeong
Byeong-Seon
BS
Chang
Hyun-Wook
HW
Son
Jong-Keun
JK
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
D000970:Antineoplastic Agents; D001572:Benzofurans; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors