Harbinatic acid, a novel and potent DNA polymerase β inhibitor from Hardwickia binata
Harbinatic acid, a novel and potent DNA polymerase β inhibitor from Hardwickia binata
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DOI：
10.1021/np990099r
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发表时间：
1999-07-01
影响因子：
5.1
通讯作者：
Hemling, ME
中科院分区：
文献类型：
--
作者：
Deng, JZ;Starck, SR;Hemling, ME
利用对DNA聚合酶β抑制敏感的测定方法，生物测定引导分离了一种活性甲基乙基酮提取物，分离出一种有效的抑制剂。这被证明是一种新的二萜，已被命名为哈宾酸(1)。通过光谱分析和与已发表的结构相关化合物的数据比较，确定了1的结构为3 α -o -反式-对香豆醇-7-负载-15-酸。化合物1对犊牛胸腺PNA聚合酶β有较强的抑制作用，IC50值为2.9 μ M。
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.