Synthesis and anti-inflammatory activity of three series of coumarin-based derivatives
10.11665/j.issn.1000-5048.2024072101
- VernacularTitle:三类基于香豆素母核衍生物的合成及其抗炎活性
- Author:
Xiujuan ZHAO
1
;
Hengli YANG
;
Jinye WU
;
Xiaoqi ZHENG
;
Yaoping ZHANG
;
Yuping LIN
;
Chunyan HU
Author Information
1. 云南中医药大学中药学院, 昆明 650500
- Publication Type:Journal Article
- Keywords:
coumarin derivatives;
synthesis;
anti-inflammatory activity
- From:
Journal of China Pharmaceutical University
2025;56(1):40-48
- CountryChina
- Language:Chinese
-
Abstract:
In this work, starting from 4-hydroxycoumarin, three series of 22 coumarin derivatives, among which 8 have not been reported in the literature, were synthesized and their in vitro anti-inflammatory activities and mechanisms of action were preliminarily investigated using mouse macrophage model. The results showed that most of the derivatives could significantly inhibit the production of pro-inflammatory factor NO, with compounds 2e, 2f, 2g, 2h, 2i, 2j, 4e, and 4f showing better anti-inflammatory activity than the positive control drug dexamethasone. Further experiments showed that compounds 2h and 4f significantly inhibited the production of pro-inflammatory factors IL-6, TNF-α and IL-1β in RAW264.7 macrophages, and could, therefore, be used as lead compounds for further studies.
