The cyanogenic glucoside, prunasin (D-mandelonitrile-beta-D-glucoside), is a novel inhibitor of DNA polymerase beta.
The cyanogenic glucoside, prunasin (D-mandelonitrile-beta-D-glucoside), is a novel inhibitor of DNA polymerase beta.
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氰基葡萄糖苷 prunasin（D-扁桃腈-β-D-葡萄糖苷）是一种新型 DNA 聚合酶 β 抑制剂。
DOI：
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发表时间：
1999
期刊：
影响因子：
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通讯作者：
K. Sakaguchi
中科院分区：
文献类型：
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作者：
Y. Mizushina;N. Takahashi;A. Ogawa;K. Tsurugaya;H. Koshino;M. Takemura;S. Yoshida;A. Matsukage;F. Sugawara;K. Sakaguchi
一种DNA聚合酶β（pol. beta）抑制剂已经独立地从两种生物体中分离出来;红紫苏（Perilla frutescens）和艾蒿（Artemisia vulgaris）。这些分子通过光谱分析确定为生氰葡糖苷、D-扁桃腈-β-D-葡糖苷、prunasin。该化合物在150 μ M时抑制大鼠pol. β的活性，但不影响小牛DNA聚合酶α和植物DNA聚合酶、人免疫缺陷病毒1型逆转录酶、小牛末端脱氧核苷酸转移酶或任何原核DNA聚合酶或检测的DNA和RNA代谢酶的活性。该化合物剂量依赖性地抑制pol. β活性，IC（50）值为98 μ M，其中聚dA/寡聚dT（12-18）和dTTP分别作为DNA模板和底物。该化合物对pol. β的抑制作用与底物dTTP具有竞争性。在脂肪酸存在下抑制增强，IC（50）值降低至约40 μ M。在C（10）-癸酸存在下，底物dTTP的K（i）值降低了28倍，表明脂肪酸使化合物更容易进入底物结合位点。
A DNA polymerase beta (pol. beta) inhibitor has been isolated independently from two organisms; a red perilla, Perilla frutescens, and a mugwort, Artemisia vulgaris. These molecules were determined by spectroscopic analyses to be the cyanogenic glucoside, D-mandelonitrile-beta-D-glucoside, prunasin. The compound inhibited the activity of rat pol. beta at 150 microM, but did not influence the activities of calf DNA polymerase alpha and plant DNA polymerases, human immunodefficiency virus type 1 reverse transcriptase, calf terminal deoxynucleotidyl transferase, or any prokaryotic DNA polymerases, or DNA and RNA metabolic enzymes examined. The compound dose-dependently inhibited pol. beta activity, the IC(50) value being 98 microM with poly dA/oligo dT(12-18) and dTTP as the DNA template and substrate, respectively. Inhibition of pol. beta by the compound was competitive with the substrate, dTTP. The inhibition was enhanced in the presence of fatty acid, and the IC(50) value decreased to approximately 40 microM. In the presence of C(10)-decanoic acid, the K(i) value for substrate dTTP decreased by 28-fold, suggesting that the fatty acid allowed easier access of the compound to the substrate-binding site.
影响因子：
56.9
作者：
Johnson, RE;Prakash, S;Prakash, L
通讯作者：
Prakash, L