Daphneodorins A-C, Anti-HIV Gnidimacrin Related Macrocyclic Daphnane Orthoesters from Daphne odora
Daphneodorins A-C, Anti-HIV Gnidimacrin Related Macrocyclic Daphnane Orthoesters from Daphne odora
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DOI：
10.1021/acs.orglett.9b03539
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发表时间：
2020-01-03
期刊：
影响因子：
5.2
通讯作者：
Koike, Kazuo
中科院分区：
文献类型：
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作者：
Otsuki, Kouharu;Li, Wei;Koike, Kazuo
从瑞香（Daphne odora Thunb.）中分离出三种新的与格尼迪木春相关的大环瑞香烷（GMDs），即瑞香奥多林A - C（2 - 4），以及格尼迪木春（1）。它们的结构通过大量的物理化学和光谱分析得以确定。化合物2和3在亚纳摩尔浓度下就能有效抑制HIV - 1复制（半数有效浓度分别为0.16和0.25 nM）。化合物2 - 4代表了一种新型的大环上高度氧化的GMDs，这表明通过进一步的化学修饰，其在抗HIV药物开发方面具有良好的潜力。
Three novel gnidimacrin related macrocyclic daphnanes (GMDs), daphneodorins A-C (2-4), were isolated from Daphne odora Thunb., together with gnidimacrin (1). Their structures were established by extensive physicochemicai and spectroscopic analyses. Compounds 2 and 3 potently inhibited HIV-1 replication at subnanomolar concentrations (EC50 0.16 and 0.25 nM, respectively). Compounds 2-4 represent a novel type of GMDs that are highly oxygenated on the macrocyclic ring, suggesting good potential for anti-HIV drug development by further chemical modification.