Synthesis of novel matrine derivatives and their in vitro anti-inflammatory activity
10.3724/SP.J.1008.2011.01223
- Author:
Jun-Xiang GUO
1
Author Information
1. Department of Organic Chemistry
- Publication Type:Journal Article
- Keywords:
Derivatives;
Matrine;
NF-κB;
Tumor necrosis factor-α
- From:
Academic Journal of Second Military Medical University
2011;32(11):1223-1226
- CountryChina
- Language:Chinese
-
Abstract:
Objective To design and synthesize a series of novel matrine derivatives and to investigate their in vitro ant-inflammation activities. Methods Ten novel matrine analogues were synthesized via thiosulfate reaction and classical Michael addition using sophocarprne as the staring material. The effects of all the analogues on TNF-α production and NF-κB transcriptional activity were evaluated in vitro. Results The synthesied compounds were confirmed correct by 1HNMR and ESI-MS. Biological studies showed that the synthetic derivatives had inhibitory effects against TNF-α production and NF-κB transcriptional activity. Compound If had the strongest inhibitory effect against TNF-α production, with an IC50 value of 9. 4 μmol/L. Conclucion Introduction of finer small substitutes at the 13-potion of matrine can enhance its ant-inflammatory activity.
