Loya S, Tal R, Kashman Y, Hizi A
Department of Cell Biology and Histology, Sackler School of Medicine, Tel Aviv, Israel.
Antimicrob Agents Chemother. 1990 Oct;34(10):2009-12. doi: 10.1128/AAC.34.10.2009.
We studied the effect of the natural marine substance illimaquinone on the catalytic activities of reverse transcriptase from human immunodeficiency virus type 1. Illimaquinone inhibited the RNase H activity of the enzyme at concentrations of 5 to 10 microgram/ml, whereas RNA-dependent DNA polymerase and DNA-dependent DNA polymerase activities were considerably less susceptible to this inhibition. Two synthetic derivatives of illimaquinone, in which the 6'-hydroxyl group at the ortho position to one of carbonyl groups of the quinone ring was modified, proved ineffective in inhibiting the human immunodeficiency virus type 1 reverse transcriptase RNase H function, suggesting involvement of the 6'-hydroxyl group in blocking the enzymatic activity.
我们研究了天然海洋物质伊利马醌对1型人类免疫缺陷病毒逆转录酶催化活性的影响。伊利马醌在浓度为5至10微克/毫升时可抑制该酶的核糖核酸酶H活性，而依赖RNA的DNA聚合酶和依赖DNA的DNA聚合酶活性对此抑制作用的敏感性则低得多。对伊利马醌的两种合成衍生物进行了研究，其中醌环羰基之一邻位的6'-羟基被修饰，结果证明它们对抑制1型人类免疫缺陷病毒逆转录酶的核糖核酸酶H功能无效，这表明6'-羟基参与了对酶活性的阻断。
