Chang C W, Lin M T, Lee S S, Liu K C, Hsu F L, Lin J Y
Institute of Biochemistry, College of Medicine, National Taiwan University, Taiwan.
Antiviral Res. 1995 Aug;27(4):367-74. doi: 10.1016/0166-3542(95)00020-m.
Two lignans, phyllamycin B and retrojusticidin B isolated from Phyllanthus myrtifolius Moon have been demonstrated to have a strong inhibitory effect on human immunodeficiency virus-1 reverse transcriptase activity (HIV-1 RT), but much less inhibitory effect on human DNA polymerase-alpha (HDNAP-alpha) activity. Fifty percent inhibitory concentrations of phyllamycin B and retrojusticidin B were determined to be 3.5 and 5.5 microM for HIV-1 RT, and 289 and 989 microM for HDNAP-alpha, respectively. The mode of inhibition was found to be non-competitive inhibition with respect to template-primer and triphosphate substrate. Several tannins such as caffeoylquinates (CQs) isolated from Lonicera japonica Thunb, galloylquinates (GQs) and galloylshikimates (GSs) purified from Castanopsis hystrix were shown to have a much less selective inhibitory effect on HIV-1 RT.
从桃金娘叶叶下珠中分离得到的两种木脂素，叶下珠霉素B和去氢异叶下珠素B，已被证明对人类免疫缺陷病毒1型逆转录酶活性（HIV-1 RT）具有强烈的抑制作用，但对人类DNA聚合酶α（HDNAP-α）活性的抑制作用则小得多。叶下珠霉素B和去氢异叶下珠素B对HIV-1 RT的50%抑制浓度分别确定为3.5和5.5微摩尔，对HDNAP-α的抑制浓度分别为289和989微摩尔。发现抑制模式相对于模板引物和三磷酸底物为非竞争性抑制。从忍冬中分离得到的几种单宁，如咖啡酰奎宁酸（CQs），以及从红锥中纯化得到的没食子酰奎宁酸（GQs）和没食子酰莽草酸（GSs），对HIV-1 RT的选择性抑制作用要小得多。
