Synthesis and biological evaluation of moscatilin analogs as anti-inflammatory agents
10.11665/j.issn.1000-5048.20210205
- VernacularTitle:杓唇石斛素类似物的合成及其抗炎活性
- Author:
GUAN Li
1
;
WANG Chunyang
;
ZHAO Huiru
;
LI Weize
;
FENG Feng
Author Information
1. 西安医学院药学院
- Publication Type:Journal Article
- Keywords:
moscatilin;
bibenzyl;
synthesis;
anti-inflammatory activity
- From:
Journal of China Pharmaceutical University
2021;52(2):171-176
- CountryChina
- Language:Fijian
-
Abstract:
Using syringaldehyde as raw material, the phosphine ylide intermediate was efficiently synthesized through acetylated hydroxyl protection, aldehyde group reduction, chlorination and reaction with triphenylphosphine. On this basis, moscatilin (MST) and its 12 analogs (MST-1-MST-12) were synthesized by wittig reaction, deacetylation and double bond reduction. All the structures were confirmed by 1H NMR, 13C NMR and ESI-MS. Bacterial lipopolysaccharide-induced mouse macrophage RAW264.7 inflammation model was used to conduct preliminary anti-inflammatory activity tests in vitro for the target compounds. Results showed that all compounds could inhibit the production of inflammatory factor NO, and that MST-5 exhibited the strongest anti-inflammatory activity (IC50= 0.428 μmol/L).Further exploration is expected for the study of the anti-inflammatory mechanism of MST-5.
