Harzianoic acids A and B, new natural scaffolds with inhibitory effects against hepatitis C virus
Harzianoic acids A and B, new natural scaffolds with inhibitory effects against hepatitis C virus
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哈茨酸A和B，具有抑制丙型肝炎病毒作用的新型天然支架
DOI：
10.1016/j.bmc.2018.12.038
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发表时间：
2019-02-01
影响因子：
3.5
通讯作者：
Lin, Wenhan
中科院分区：
文献类型：
--
作者：
Li, Bo;Li, Li;Lin, Wenhan
从海绵相关真菌哈茨木霉中分离出两种新的倍半萜类似物，即哈茨酸 A (1) 和 B (2)。它们的结构是根据与配置分配的 ECD 数据相关的广泛光谱分析确定的。哈齐酸 A 和 B 的结构特征是具有环丁烷核的倍半萜烯和去甲倍半萜烯，这在自然界中并不常见。两种化合物均表现出降低 HCV RNA 水平的抑制活性，且细胞毒性较低。作用方式的初步研究表明，该化合物阻断了HCV生命周期的进入步骤，而病毒E1/E2和宿主细胞CD81是潜在的靶蛋白。
Two new sesquiterpene-based analogues, namely harzianoic acids A (1) and B (2), were isolated from a sponge-associated fungus Trichoderma harzianum. Their structures were determined on the basis of the extensive spectroscopic analyses in association with the ECD data for the configurational assignment. Harzianoic acids A and B were structurally characterized as a sesquiterpene and a norsesquiterpene with a cyclobutane nucleus, which is uncommonly found from nature. Both compounds exhibited the inhibitory activity to reduce the HCV RNA levels with low cytotoxicity. The preliminary investigation of the mode of action revealed that the compounds blocked the entry step in the HCV life cycle, while the viral E1/E2 and the host cell CD81 were the potential target proteins.