DIFFERENTIAL INHIBITION OF REVERSE-TRANSCRIPTASE AND CELLULAR DNA POLYMERASE-ALPHA ACTIVITIES BY LIGNANS ISOLATED FROM CHINESE HERBS, PHYLLANTHUS-MYRTIFOLIUS MOON, AND TANNINS FROM LONICERA-JAPONICA THUNB AND CASTANOPSIS-HYSTRIX
DIFFERENTIAL INHIBITION OF REVERSE-TRANSCRIPTASE AND CELLULAR DNA POLYMERASE-ALPHA ACTIVITIES BY LIGNANS ISOLATED FROM CHINESE HERBS, PHYLLANTHUS-MYRTIFOLIUS MOON, AND TANNINS FROM LONICERA-JAPONICA THUNB AND CASTANOPSIS-HYSTRIX
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DOI：
10.1016/0166-3542(95)00020-m
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发表时间：
1995-08-01
影响因子：
7.6
通讯作者：
LIN, JY
中科院分区：
文献类型：
--
作者：
CHANG, CW;LIN, MT;LIN, JY
从叶下珠（Phyllanthus myrtifolius Moon）中分离的两种木脂素，叶下霉素（phyllamycin）B和杀逆菌素（retrojusticidin）B已被证明对人类免疫缺陷病毒-1逆转录酶（HIV-1 RT）活性具有强抑制作用，但对人类DNA聚合酶-α（HDNAP-α）活性的抑制作用小得多。叶拉霉素B和杀逆菌素B的50%抑制浓度被确定为对HIV-1 RT分别为3.5和5.5 μ M，对HDNAP-α分别为289和989 μ M。抑制模式被认为是非竞争性抑制相对于模板引物和三磷酸底物。从红锥中提取的没食子酰奎尼酸酯（GQs）和没食子酰莽草酸酯（GSs）对HIV-1 RT的抑制作用较强。
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 mu M for HIV-1 RT, and 289 and 989 mu M 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.