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Discovery and biological evaluation of dispirocyclic and polycyclic ent-clerodane dimers from Isodon scoparius as novel inhibitors of Toll-like receptor signaling
Organic Chemistry Frontiers ( IF 4.6 ) Pub Date : 2022-06-14 , DOI: 10.1039/d2qo00723a
Xing-Ren Li 1 , Li Chen 2, 3 , Kun Hu 1 , Bing-Chao Yan 1 , Xue Du 1 , Xiao-Nian Li 1 , Han-Dong Sun 1 , Shi-Jun He 2, 3 , Pema-Tenzin Puno 1
Affiliation  

Scoparicacids A–C (1–3), three novel ent-clerodane dimers with unprecedented dispirocyclic 6/6/5/6/6 and hexacyclic 6/6/5/6/5/6 ring systems, were isolated from Isodon scoparius. A biomimetic synthesis of 3 was achieved using a double aldol reaction to construct a 5/6/5 ring system in one step. 2 and 3 exhibited significant immunosuppression on the proliferation of B lymphocytes evoked by TLR signaling stimulation in a dose-dependent manner and significantly abrogated the downstream pathway of TLR7 signaling in B cells.

中文翻译:

发现和生物学评估来自 Isodon scoparius 的双螺环和多环 ent-clerodane 二聚体作为 Toll 样受体信号传导的新型抑制剂

从Isodon scoparius中分离出具有前所未有的双螺环 6/6/5/6/6 和六环 6/6/5/6/5/6 环系统的三种新的内环戊二烯二聚体Scoparicacids A-C ( 1-3 ) 。使用双醛醇反应一步构建5/6/5环系统,实现了3的仿生合成。图23对TLR信号刺激诱发的B淋巴细胞增殖表现出显着的免疫抑制作用,呈剂量依赖性,并显着消除B细胞中TLR7信号传导的下游通路。
更新日期:2022-06-14
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