Harbinatic acid, a novel and potent DNA polymerase β inhibitor from Hardwickia binata
被引:23
作者:
Deng, JZ
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机构:Univ Virginia, Dept Chem, Charlottesville, VA 22901 USA
Deng, JZ
Starck, SR
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机构:Univ Virginia, Dept Chem, Charlottesville, VA 22901 USA
Starck, SR
Hecht, SM
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机构:Univ Virginia, Dept Chem, Charlottesville, VA 22901 USA
Hecht, SM
Ijames, CF
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机构:Univ Virginia, Dept Chem, Charlottesville, VA 22901 USA
Ijames, CF
Hemling, ME
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机构:Univ Virginia, Dept Chem, Charlottesville, VA 22901 USA
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.