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

当前位置： X-MOL 学术 › Org. Chem. Front. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

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2和3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

点击分享查看原文

点击收藏

阅读更多本刊最新论文本刊介绍/投稿指南11