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从艾蒿中提取的内酯环开裂型倍半萜类化合物通过酯键连接的杂二聚体,对一氧化氮没有抑制活性。

Lactone ring-opening seco-guaianolide involved heterodimers linked via an ester bond from Artemisia argyi with NO inhibitory activity.

机构信息

Jiangsu Key Laboratory of Bioactive Natural Product Research and State Key Laboratory of Natural Medicines, School of Traditional Chinese Pharmacy, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, People's Republic of China.

Jiangsu Key Laboratory of Bioactive Natural Product Research and State Key Laboratory of Natural Medicines, School of Traditional Chinese Pharmacy, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, People's Republic of China.

出版信息

Fitoterapia. 2019 Jan;132:94-100. doi: 10.1016/j.fitote.2018.12.004. Epub 2018 Dec 4.

DOI:10.1016/j.fitote.2018.12.004
PMID:30529065
Abstract

Investigation into the chemical diversity of Artemisia argyi led to the discovery of four new (1-4) and one known (5) guaianolide sesquitenpenoid dimers linked via ester bond, and five other known mono-sesquiterpenoids (6-10). Their structures were determined via extensive spectroscopic data, and the absolute configurations of these compounds were elucidated by calculated ECD analysis and chemical method. The dimeric sesquiterpenoids exhibited NO production inhibitory activity with IC values ranging from 7.02 to 32.1 μM. The studies further suggested that compound 2 inhibited inflammatory responses via suppression of the expression of iNOS, resulting from activation of nuclear factor-kappaB (NF-κB) and phosphorylation of MAPKs (ERK and p38).

摘要

对艾草的化学成分研究发现了四个新的(1-4)和一个已知的(5)通过酯键连接的愈创木烷型倍半萜二聚体,以及另外五个已知的单倍半萜(6-10)。通过广泛的光谱数据分析确定了它们的结构,并通过计算ECD 分析和化学方法阐明了这些化合物的绝对构型。二聚倍半萜具有抑制 NO 产生的活性,IC 值范围为 7.02 至 32.1 μM。研究进一步表明,化合物 2 通过抑制 iNOS 的表达来抑制炎症反应,这是由于核因子-κB(NF-κB)的激活和 MAPKs(ERK 和 p38)的磷酸化。

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