Synthesis of novel matrine derivatives and their in vitro anti-inflammatory activity / 第二军医大学学报

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.