DIFFERENTIAL INHIBITORY EFFECTS OF SOME CATECHIN DERIVATIVES ON THE ACTIVITIES OF HUMAN-IMMUNODEFICIENCY-VIRUS REVERSE-TRANSCRIPTASE AND CELLULAR DEOXYRIBONUCLEIC AND RIBONUCLEIC-ACID POLYMERASES
DIFFERENTIAL INHIBITORY EFFECTS OF SOME CATECHIN DERIVATIVES ON THE ACTIVITIES OF HUMAN-IMMUNODEFICIENCY-VIRUS REVERSE-TRANSCRIPTASE AND CELLULAR DEOXYRIBONUCLEIC AND RIBONUCLEIC-ACID POLYMERASES
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DOI：
10.1021/bi00463a029
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发表时间：
1990-03-20
期刊：
影响因子：
2.9
通讯作者：
ONO, K
中科院分区：
文献类型：
--
作者：
NAKANE, H;ONO, K
茶树的两种成分[即，发现（-）-表儿茶素没食子酸酯和（-）-表没食子儿茶素没食子酸酯]对逆转录酶和细胞DNA和RNA聚合酶的活性有不同的抑制作用。在针对每种酶物种优化的测定条件下，观察到逆转录酶对这些化合物的最强抑制。50%抑制人免疫缺陷病毒（HIV）逆转录酶活性所需的（-）-表儿茶素没食子酸酯和（-）-表没食子儿茶素没食子酸酯的浓度在0.01-0.02 μ g/mL的范围内。另一方面，（-）-表儿茶素、（-）-表没食子儿茶素和没食子酸，（-）-表儿茶素没食子酸酯和（-）-表没食子儿茶素没食子酸酯的成分，在浓度高达1 μ g/mL时都不抑制HIV逆转录酶的活性。这些化合物抑制逆转录酶和其他DNA聚合酶的模式相对于模板引物是竞争性的，而抑制RNA聚合酶的模式相对于核苷酸底物是竞争性的。HIV逆转录酶对（-）-表儿茶素没食子酸酯和（-）-表没食子儿茶素没食子酸酯的Ki值分别测定为7.2和2.8 nM，比这些化合物的其他DNA和RNA聚合酶的Ki值小1-2个数量级。
The two componetns of Camellia sinensis (tea plant) [i.e., (-)-epicatechin gallate and (-)-epigallocatechin gallate] were found to differentially inhibit the activities of reverse transcriptase and cellular DNA and RNA polymerases. Under the assay conditions optimized for each enzyme species, the strongest inhibition by these compounds was observed with reverse transcriptase. The concentrations of (-)-epicatechin gallate and (-)-epigallocatechin gallate required for 50% inhibition of the activity of human immunodeficiency virus (HIV) reverse transcriptase were in the range of 0.01-0.02 .mu.g/mL. On the other hand, neither (-)-epicatechin, (-)-epigallocatechin, nor gallic acid, the constituents of (-)-epicatechin gallate and (-)-epigallocatechin gallate, was inhibitory to the activity of HIV reverse transcriptase at concentrations up to 1 .mu.g/mL. The mode of inhibition of reverse transcriptase and other DNA polymerases by these compounds was competitive with respect to the template-primer, whereas the mode of inhibition of RNA polymerase was competitive with respect to the nucleotide substrate. The Ki values of HIV reverse transcriptase for (-)-epicatechin gallate and (-)-epigallocatechin gallate were determined to be 7.2 and 2.8 nM, respectively, which are smaller by 1-2 orders of magnitude than the Ki''s of other DNA and RNA polymerases for these compounds.