School of Pharmacy, Xinxiang Medical University, Xinxiang 453003, PR China.
School of Pharmacy, Xinxiang Medical University, Xinxiang 453003, PR China.
Fitoterapia. 2019 Nov;139:104372. doi: 10.1016/j.fitote.2019.104372. Epub 2019 Oct 25.
Four new sesquiterpene lactones, named artemargyinolides A-D (1-4), and seven known sesquiterpenoids (5-11) were isolated from Artemisia argyi. Their structures were elucidated based on the extensive analysis of spectroscopic data. The absolute configuration of 1 was assigned by X-ray crystallographic analysis. Compound 1 is an unprecedented sesquiterpene dimer-monoterpene lactone. The cyclooxygenases (COX-1 and COX-2) inhibitory activities of all isolated compounds were evaluated. Compounds 1, 2, 4, and 6-11 showed inhibitory activity against COX-2 with IC values ranging from 35.78 ± 0.39 to 256.07 ± 0.38 μM. However, compounds 7, 9, and 10 exhibited weak inhibitory activity against COX-1 with IC values of 465.70 ± 1.53, 281.43 ± 3.56, and 490.45 ± 6.07 μM, respectively. Other compounds are inactive against COX-1. Therefore, compounds 1, 2, 4, 6, 8, and 11 displayed selective COX-2 inhibitory activity.
从艾草中分离得到了 4 种新的倍半萜内酯，分别命名为 artemargyinolides A-D（1-4）和 7 种已知的倍半萜类化合物（5-11）。根据光谱数据分析，确定了它们的结构。通过 X 射线晶体学分析确定了 1 的绝对构型。化合物 1 是一种前所未有的倍半萜二聚体-单萜内酯。评价了所有分离得到的化合物对环氧化酶（COX-1 和 COX-2）的抑制活性。化合物 1、2、4 和 6-11 对 COX-2 具有抑制活性，IC 值范围为 35.78 ± 0.39 至 256.07 ± 0.38 μM。然而，化合物 7、9 和 10 对 COX-1 表现出较弱的抑制活性，IC 值分别为 465.70 ± 1.53、281.43 ± 3.56 和 490.45 ± 6.07 μM。其他化合物对 COX-1 无活性。因此，化合物 1、2、4、6、8 和 11 对 COX-2 表现出选择性抑制活性。
