Synthesis of N-Substituted sinomenine derivatives and its inhibitory effect against NF-κB transcriptional activity
10.3724/SP.J.1008.2015.00413
- Author:
Fan YANG
1
Author Information
1. Department of Medicinal Chemistry, School of Pharmacy, Yantai University
- Publication Type:Journal Article
- Keywords:
Anti-inflammatory agents;
Modification;
NF-κB;
Sinomenine
- From:
Academic Journal of Second Military Medical University
2014;36(4):413-417
- CountryChina
- Language:Chinese
-
Abstract:
Objective To design and synthesize a series of sinomenine derivatives and to investigate their anti-inflammation activities in vitro. Methods Nine sinomenine derivatives were synthesized via demethylate of N atom, nucleophilic substitution and classical Click Reaction using sinomenine as the starting material.The target compounds were evaluated for their influence on NF-κB transcriptional activity in vitro. Results All the synthesized compounds were reported for the first time, and they were confirmed by 1HNMR and LC-MS. Biological studies showed that all the synthetic derivatives exhibited certain inhibitory effect against NF-κB transfection in vitro, but was weaker than that of sinomenine. Conclusion Replacing N-methyl with large group or long side chain on nitrogen atom may weaken the anti-inflammatory activity of sinomenine.
