当前位置: X-MOL 学术Bioorgan. Chem. › 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.)
Water-soluble matrine-type alkaloids with potential anti-neuroinflammatory activities from the seeds of Sophora alopecuroides
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2021-09-08 , DOI: 10.1016/j.bioorg.2021.105337
Ding Luo 1 , Qiang Lin 1 , Jin-Lin Tan 1 , Hai-Yue Zhao 1 , Xiao Feng 2 , Neng-Hua Chen 1 , Zhong-Nan Wu 1 , Chun-Lin Fan 1 , Yao-Lan Li 1 , Wei-Long Ding 3 , Fei Xiao 2 , Guo-Cai Wang 1 , Yu-Bo Zhang 4
Affiliation  

A phytochemical investigation on the alkaloids from water-soluble part of Sophora alopecuroides led to obtain forty matrine-type alkaloids (140) including eighteen new ones (118), which covers almost all positions of the oxygen substitution in matrine-type structure. Notably, eight compounds (18) belong to rare bis-amide matrine-type alkaloid. The new structures were determined based on extensive spectroscopic data, electronic circular dichroism (ECD) calculations, and six instances, verified by X-ray crystallography. Most of isolates showed anti-neuroinflammatory activities based on the expression of tumor necrosis factor (TNF)-α and interleukin (IL)-6 in BV2 microglia cells. Especially, compound 39 can suppress those two mediator secretions in a dose-dependent manner with IC50 values of 21.6 ± 0.5 and 16.7 ± 0.8 μM, respectively. Further mechanistic study revealed that 39 suppressed the phosphorylation of IκBα and p65 subunit to regulate the NF-κB signaling pathway.



中文翻译:

苦参种子中具有潜在抗神经炎症活性的水溶性苦参碱型生物碱

苦参水溶性部分生物碱的植物化学研究,获得苦参型生物碱40种(140),其中新的18种118),几乎涵盖了苦参型氧取代的所有位置。结构体。值得注意的是,8种化合物(1 - 8)属于稀有双酰胺苦参碱型生物碱。新结构是基于广泛的光谱数据、电子圆二色性 (ECD) 计算和 X 射线晶体学验证的六个实例确定的。大多数分离株显示出基于肿瘤坏死因子 (TNF) 的表达的抗神经炎症活性BV2 小胶质细胞中的白细胞介素 (IL)-6。特别是,化合物39可以以剂量依赖性方式抑制这两种介质的分泌,IC 50值分别为 21.6 ± 0.5 和 16.7 ± 0.8 μM。此外机理研究揭示,39抑制I的磷酸化κα和p65亚单位,以调节NF- κ乙信号传导途径。

更新日期:2021-09-12
down
wechat
bug