称取整数 A 和 B，具有抑制 NLRP3 炎性体激活作用的来自 的三环[4.4.0.0]十四烷 clerodane 二萜。
Callintegers A and B, Unusual Tricyclo[4.4.0.0]tetradecane Clerodane Diterpenoids from with Inhibitory Effects on NLRP3 Inflammasome Activation.
机构信息
Key Laboratory of Medicinal Chemistry for Natural Resource of Ministry of Education, Yunnan Characteristic Plant Extraction Laboratory, Yunnan Research & Development Center for Natural Products, School of Chemical Science and Technology and School of Medicine, Yunnan University, Kunming 650500, People's Republic of China.
State Key Laboratory for Conservation and Utilization of Bio-Resources in Yunnan, Yunnan University, Kunming 650091, People's Republic of China.
出版信息
J Nat Prod. 2022 Nov 25;85(11):2675-2681. doi: 10.1021/acs.jnatprod.2c00568. Epub 2022 Oct 26.
Callintegers A () and B (), unprecedented clerodane norditerpenoids based on a novel carbon skeleton, were isolated from . Compounds and possess a novel 6/6/6-fused tricyclic ring system. Their structures and absolute configurations were determined by quantum chemical calculations, spectroscopic analysis, and single-crystal X-ray diffraction methods. Biological evaluation showed that compound inhibited IL-1β secretion in a dose-dependent manner with an IC value of 5.5 ± 3.2 μM. Caspase-1 maturation and IL-1β secretion were also reduced, indicating that compound impaired NLRP3 inflammasome activation.
从 Calliergon 中分离得到两个新型倍半萜化合物（）和（），它们分别是基于 novel carbon skeleton 的 clerodane norditerpenoids。化合物 和 均具有 novel 6/6/6-fused tricyclic ring system。通过量子化学计算、光谱分析和单晶 X 射线衍射方法确定了它们的结构和绝对构型。生物活性评价表明，化合物 呈剂量依赖性抑制 IL-1β 分泌，IC 值为 5.5 ± 3.2 μM。半胱天冬酶-1 成熟和 IL-1β 分泌也减少，表明化合物 可损害 NLRP3 炎症小体激活。
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