环氧合酶
体外
化学
立体化学
弹性蛋白酶
风湿病
消炎药
IC50型
药理学
医学
生物化学
内科学
酶
作者
Haodong Yang,Bao-Long Hou,Yayun Yang,Zhishu Tang,Hongbo Xu
出处
期刊:Fitoterapia
[Elsevier]
日期:2024-07-01
卷期号:176: 106021-106021
被引量:1
标识
DOI:10.1016/j.fitote.2024.106021
摘要
Acanthopanacis Cortex (A.-C) with a long history of >1000 years, has been used to treat rheumatism effectively. Nineteen diterpenoids have been isolated from A.-C, including six new compounds (1–6). Among them, compounds 7, 9–11, 13, and 17 were discovered from A.-C for the first time. The structures of 1–6 were determined by analyzing their NMR data and comparing their experimental and calculated electronic circular dichroism spectra. Moreover, the single-crystal X-ray diffraction data of 1, 2, 8, and 14 were provided. The anti-inflammatory activity of 1–5 and 7–18 on neutrophil elastase, cyclooxygenase-1 (COX-1), and cyclooxygenase-2 (COX-2) has been studied in vitro, and the results showed that 15 had almost no inhibitory effects on COX-1 at 200 μM but a significant activity against COX-2 with an IC50 of 0.73 ± 0.006 μΜ. It indicated that compound 15 can provide valuable information for the design of selective COX-2 inhibitors.
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