Thorectidiol A Isolated from the Marine Sponge Dactylospongia elegans Disrupts Interactions of the SARS-CoV-2 Spike Receptor Binding Domain with the Host ACE2 Receptor.
Thorectidiol A Isolated from the Marine Sponge Dactylospongia elegans Disrupts Interactions of the SARS-CoV-2 Spike Receptor Binding Domain with the Host ACE2 Receptor.
复制标题
从海洋海绵 Dactylospongia elegans 中分离出来的 Thorectidiol A 可破坏 SARS-CoV-2 刺突受体结合域与宿主 ACE2 受体的相互作用。
DOI：
10.1021/acs.jnatprod.2c01030
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发表时间：
2023
影响因子：
5.1
通讯作者：
Andersen,RaymondJ
中科院分区：
文献类型：
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作者：
Williams,DavidE;Cassel,Joel;Zhu,Jin-Lin;Yang,Jian-Xiong;deVoogd,NicoleJ;Matainaho,Teatulohi;Salvino,JosephM;Wang,YanAlexander;Montaner,LuisJ;Tietjen,Ian;Andersen,RaymondJ
从采集于巴布亚新几内亚的海洋海绵Dacacortidae spongia elegans（Thorectidae科，网角藻目）中分离的Thorectidiols是一类对称和不对称的二聚联苯部分萜类立体异构体，推测是共存外消旋单体Thorectidol（3）的氧化苯酚偶联产物。该家族的一个成员thorectidiol A（1）已以其天然形式分离出来，其结构已通过NMR、MS和ECD数据分析阐明。海绵提取物的乙酰化促进了额外的thorecitidol二乙酸酯立体异构体的分离和外消旋单体thorecitidol乙酸酯的分离（6）。外消旋thorectidiol A（1）显示出选择性抑制SARS-CoV-2刺突受体结合域（RBD）与宿主ACE 2受体的相互作用，IC 50 = 1.0 ± 0.7 μM。
Thorectidiols isolated from the marine spongeDactylospongia elegans(family Thorectidae, order Dictyoceratida) collected in Papua New Guinea are a family of symmetrical and unsymmetrical dimeric biphenyl meroterpenoid stereoisomers presumed to be products of oxidative phenol coupling of a co-occurring racemic monomer, thorectidol (3). One member of the family, thorectidiol A (1), has been isolated in its natural form, and its structure has been elucidated by analysis of NMR, MS, and ECD data. Acetylation of the sponge extract facilitated isolation of additional thorectidiol diacetate stereoisomers and the isolation of the racemic monomer thorectidol acetate (6). Racemic thorectidiol A (1) showed selective inhibition of the SARS-CoV-2 spike receptor binding domain (RBD) interaction with the host ACE2 receptor with an IC50= 1.0 ± 0.7 μM.