Kuo Li-Ming Yang, Tseng Pei-Yi, Lin Yu-Chi, Liaw Chia-Ching, Zhang Li-Jie, Tsai Keng-Chang, Lin Zhi-Hu, Ho Hsiu-O, Kuo Yao-Haur
School of Pharmacy, Taipei Medical University, Taipei, Taiwan, Republic of China.
Department of Life Sciences and Institute of Genome Sciences, National Yang Ming University, Taipei, Taiwan, Republic of China.
Planta Med. 2018 Dec;84(18):1348-1354. doi: 10.1055/a-0647-1901. Epub 2018 Jul 9.
Phytochemical investigation of ethanol extracts from two Taiwanese collections of resulted in the isolation of eighteen hirsutinolide-type sesquiterpenoids, including seven new ones designated as vernolides E - K (1: -7: ). All structures were determined by a combination of detailed spectroscopic analyses (NMR and MS) and comparison with reported data. In an anti-inflammatory assay, compounds 3, 7, 9, 11: , and 14: exhibited strong inhibitory activities toward NO production by LPS-induced RAW264.7 macrophages, with IC values of 1.18, 0.85, 0.66, 0.71 and 0.45 µM, respectively, without affecting cellular viability at 40 µM. Preliminary structure-activity relationships indicate that the ester groups at C-8 and C-13 may enhance inhibition of NO production.
对来自台湾两个采集样本的乙醇提取物进行植物化学研究，结果分离出18种海紫苏内酯型倍半萜类化合物，其中包括7种新的化合物，命名为春黄菊内酯E-K（1：-7： ）。所有结构均通过详细的光谱分析（核磁共振和质谱）以及与已报道数据的比较来确定。在抗炎试验中，化合物3、7、9、11： 和14： 对脂多糖诱导的RAW264.7巨噬细胞产生NO表现出强烈的抑制活性，IC值分别为1.18、0.85、0.66、0.71和0.45μM，在40μM时不影响细胞活力。初步的构效关系表明，C-8和C-13位的酯基可能增强对NO产生的抑制作用。
