ANTI-AIDS AGENTS .2. INHIBITORY EFFECTS OF TANNINS ON HIV REVERSE-TRANSCRIPTASE AND HIV REPLICATION IN H9 LYMPHOCYTE-CELLS
ANTI-AIDS AGENTS .2. INHIBITORY EFFECTS OF TANNINS ON HIV REVERSE-TRANSCRIPTASE AND HIV REPLICATION IN H9 LYMPHOCYTE-CELLS
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DOI：
10.1021/np50069a008
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发表时间：
1990-05-01
影响因子：
5.1
通讯作者：
LEE, KH
中科院分区：
文献类型：
--
作者：
NONAKA, G;NISHIOKA, I;LEE, KH
九单宁，包括没食子单宁和鞣花单宁被评估为潜在的HIV复制抑制剂。1，3，4-三-O-没食子酰奎宁酸、3，5-二-O-没食子酰莽草酸、3，4，5，-三-O-没食子酰莽草酸、安石榴苷和安石榴苷在感染的H9淋巴细胞中抑制HIV复制，细胞毒性很小。两种化合物石榴苷和石榴皮素C分别以8和5 μ M的ID 50抑制纯化的HIV逆转录酶。用H9淋巴细胞的进一步研究表明，诃子酸和石榴苷不直接灭活病毒。然而，在这些条件下，1，3，4-三-O-没食子酰奎宁酸和3，5-二-O-没食子酰莽草酸是更有效的抑制剂。所有单宁似乎都能抑制病毒与细胞的相互作用。因此，尽管单宁具有抗RT活性，但其抑制HIV的机制可能与这种酶无关。
Nine tannins, including gallo-and ellagitannins were evaluated as potential inhibitors of HIV replication. 1,3,4-Tri-O-galloylquinic acid, 3,5-di-O-galloylshikimic acid, 3,4,5,-tri-O-galloylshikimic acid, punicalin, and punicalagin inhibited HIV replication in infected H9 lymphocytes with little cytotoxicity. Two compounds, punicalin and punicacoretin C, inhibited purified HIV reverse transcriptase with ID50 of 8 and 5 .mu.M, respectively. Further studies with H9 lymphocytes indicated that chebulagic acid and punicalin did not inactivate virus directly. However, 1,3,4-tri-O-galloylquinic acid and 3,5-di-O-galloylshikimic acid were more effective inhibitors under those conditions. All tannins appear to inhibit virus-cell interactions. Thus in spite of their anti-RT activity, the mechanism by which tannins inhibit HIV may not be associated with this enzyme.