Bioorganic Chemistry ( IF 5.1 ) Pub Date : 2021-08-30 , DOI: 10.1016/j.bioorg.2021.105312 Mei-Li Guo 1 , Hong-Tao Xu 1 , Jun-Jie Yang 1 , Gui-Xin Chou 2
Trolliusditerpenosides A-Q (1–17), seventeen new labdane-diterpenoid glycosides, were isolated from the dried flowers of Trollius chinensis Bunge, a plant that has been commonly used as both an anti-inflammatory folk medicine and a healthcare tea for its therapeutic and anti-viral and antibacterial properties. Their structures were corroborated via comprehensive spectroscopic analysis, ECD calculations, and single-crystal X-ray diffraction analysis. Furthermore, the inhibitory activities on lipopolysaccharide (LPS)-induced NO production in RAW 264.7 macrophages of all compounds (1–17) were evaluated in vitro. Compounds 3, 6, 7, and 11 displayed significant inhibitory activities against NO production, with IC50 values ranging from 1.6 ± 0.1 to 14.4 ± 0.2 μM. In addition, compounds 3, 6, 7, and 11 all down-regulated the mRNA expression of iNOS, COX-2, and IL-1β in RAW 264.7 cells mediated by LPS. These findings not only support the chemical context of genus Trollius but also the exploration of new chemical entities with pharmacological significance from this genus.
中文翻译:
金莲花花中的二萜苷及其抑制一氧化氮的活性
Trolliusditerpenosides AQ(1 - 17),17新半日花烷-二萜糖苷,购自的干燥花中分离金莲花邦吉,已被普遍用作既抗炎民间医药和保健茶其治疗和抗植物- 病毒和抗菌特性。它们的结构通过综合光谱分析、ECD 计算和单晶 X 射线衍射分析得到证实。此外,在脂多糖(LPS)诱导的NO产生的抑制活性在RAW所有化合物(264.7巨噬细胞中1 - 17)在体外评价。化合物3 , 6 , 7和11显示出对 NO 产生的显着抑制活性,IC 50值范围为 1.6 ± 0.1 至 14.4 ± 0.2 μM。此外,化合物3,6,7,和11都下调iNOS的mRNA的表达,COX-2和IL-1 β由LPS介导的RAW 264.7细胞。这些发现不仅支持金莲花属的化学背景,而且支持对该属具有药理意义的新化学实体的探索。