Harbinatic acid, a novel and potent DNA polymerase β inhibitor from Hardwickia binata

被引:23
作者
Deng, JZ
Starck, SR
Hecht, SM
Ijames, CF
Hemling, ME
机构
[1] Univ Virginia, Dept Chem, Charlottesville, VA 22901 USA
[2] Univ Virginia, Dept Biol, Charlottesville, VA 22901 USA
[3] SmithKline Beecham Pharmaceut, Dept Phys & Struct Chem, King Of Prussia, PA 19406 USA
来源
JOURNAL OF NATURAL PRODUCTS | 1999年 / 62卷 / 07期
关键词
D O I
10.1021/np990099r
中图分类号
Q94 [植物学];
学科分类号
071001 ;
摘要
Bioassay-guided fractionation of an active methyl ethyl ketone extract of Hardwickia binata, using an assay sensitive to DNA polymerase beta inhibition, resulted in the isolation of a potent inhibitor. This proved to be a novel diterpenoid, which has been named harbinatic acid (1). The structure of 1 was established as 3 alpha-O-trans-p-coumaroyl-7-labden-15-oic acid from spectroscopic analysis and by comparison with the published data for a structurally related compound. Compound 1 strongly inhibited calf thymus PNA polymerase beta, with an IC50 value of 2.9 mu M.
引用
收藏
页码:1000 / 1002
页数:3
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