Sesquiterpene lactones, inhibitors of farnesyl protein transferase, isolated from the flower of Artemisia sylvatica

被引:38
作者
Lee, SH
Kang, HM
Song, HC
Lee, H
Lee, UC
Son, KH
Kim, SH
Kwon, BM
机构
[1] Korea Res Inst Biosci & Biotechnol, Taejon 305600, South Korea
[2] Chungbuk Natl Univ, Coll Pharm, Chongju 360763, South Korea
[3] Korea Res Inst Ginseng & Tobacco, Taejon 305, South Korea
[4] Kyunghee Univ, Grad Sch East West Med Sci, Seoul 130, South Korea
关键词
sesquiterpene lactones; Artemisia sylvatica; farnesyl protein;
D O I
10.1016/S0040-4020(00)00394-X
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Five sesquiterpene lactones, 8-acetylarteminolide (1), artanomaloide (2), arteminones (3 and 4), and dehydromatricarin (5), were isolated from the methanolic extract of the flower of Artemisia sylvatica and characterized on the basis of their spectral data. New sesquiterpene lactone 1 was identified as a configurational isomer of artanomaloide (2), and the new arteminones 3 and 4 are determined as stereoisomers. 8-Acetylarteminolide (1) strongly inhibited FPTase with an IC50 of 1.8 mu M, however, the other sesquiterpene lactones mildly inhibited the transferase with an IC50 of 22-300 mu M. (C) 2000 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:4711 / 4715
页数:5
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