Synthesis and anti-inflammatory activity of ursolic acid derivative-chalcone conjugates
10.16438/j.0513-4870.2015-1162
- VernacularTitle:熊果酸衍生物与查耳酮缀合物的合成及抗炎活性
- Author:
Juan TAN
1
;
Wei HUANG
1
;
Shan-long CHEN
2
;
Yuan YUE
3
Author Information
1. Department of Medicine, Wuhan Third Hospital, Wuhan 430060, China
2. Department of Medicine, Hainan General Hospital, Haikou 570311, China
3. School of Pharmaceutical Sciences, Wuhan University, Wuhan 430071, China
- Publication Type:ORIGINAL ARTICLES
- Keywords:
ursolic acid derivative-chalcone conjugate;
derivative;
anti-inflammatory
- From:
Acta Pharmaceutica Sinica
2016;51(6):938-
- CountryChina
- Language:Chinese
-
Abstract:
A series of novel conjugates with ursolic acid core and different chalcone ligands were synthesized via ursolic acid, 4-hydroxyacetophenone and aromatic aldehydes. All of the conjugates were confirmed by the application of IR, 1H NMR, 13C NMR and HR-MS. The anti-inflammatory effect was observed for the target compounds in xylene-induced mouse ear edema and carrageenan-induced paw edema in rats. The preliminary bioassay test demonstrated that these compounds had potent anti-inflammatory activities, and their activities were better than that of the parent ursolic acid. Among them, 1-en-3-oxoursolic acid-chalcone conjugates (6a-6g) exhibited higher activities than analogues 5a-5g and 7a-7g.
