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Lindenane sesquiterpenoid dimers from Chloranthus holostegius with anti-neuroinflammatory activities in BV-2 microglia
Phytochemistry ( IF 3.2 ) Pub Date : 2023-09-12 , DOI: 10.1016/j.phytochem.2023.113859
Zhao-Chun Zhan 1 , Yi-Ping Xia 1 , Qing Tang 1 , Hui-Hui Zhu 1 , Jing-Yi Du 1 , Jun-Xing Cai 1 , Yan-Jun Chen 2 , Zhong-Nan Wu 1 , Yao-Lan Li 1 , Neng-Hua Chen 3 , Guo-Cai Wang 1 , Yu-Bo Zhang 2
Affiliation  

Fifteen undescribed lindenane-type sesquiterpenoid dimers, designated chloranholides F−T (115), together with twenty-five known analogs (1640), were isolated from the whole plants of Chloranthus holostegius. The isolate structures were elucidated by analysis of spectroscopic data and chemical methods, and their absolute configurations were determined by X-ray crystallography and electronic circular dichroism spectra. In anti-neuroinflammatory assays, all isolates were evaluated by examination of their inhibitory effect on nitric oxide (NO) in LPS-stimulated BV-2 cells, and the results showed that 2124, 26, 30, 32 and 36 significantly inhibited the production of the inflammatory mediator NO, with IC50 values ranging from 3.18 to 11.46 μM, which was better than that of quercetin. Structure-activity relationship analysis revealed that two essential functional groups played an indispensable role in the anti-inflammatory effects. Moreover, 22 and 24 inhibited the LPS-induced upregulation of iNOS and COX-2 enzymes in BV-2 microglia at the protein level.



中文翻译:

来自金粟兰的林烯倍半萜二聚体在 BV-2 小胶质细胞中具有抗神经炎症活性

从金粟兰(Chloranthus holostegius)的整株植物中分离出15 种未描述的茚烷型倍半萜二聚体,命名为金雀花素 F−T ( 115 ),以及 25 种已知类似物 ( 1640 ) 通过光谱数据分析和化学方法阐明了分离物的结构,并通过X射线晶体学和电子圆二色光谱确定了它们的绝对构型。在抗神经炎症测定中,通过检查其对 LPS 刺激的 BV-2 细胞中一氧化氮 (NO) 的抑制作用来评估所有分离株,结果表明212426303236显着抑制炎症介质NO的产生,IC 50值范围为3.18至11.46 μM,优于槲皮素。构效关系分析表明,两个重要的官能团在抗炎作用中发挥着不可或缺的作用。此外,2224在蛋白质水平上抑制BV-2小胶质细胞中LPS诱导的iNOS和COX-2酶的上调。

更新日期:2023-09-16
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