Structural Modification Of Rheumatoid Arthritis Drug Sinomenine

Rheumatoid arthritis (RA) is symmetric multi-joint synovitis characteristic of autoimmune diseases, characterized by joint bone destruction and loss of function or disability, is a serious threat to human health. Caulis sinomenii as the traditional Chinese medicine pharmacy treatment of arthritis drug main ingredient, after several years of clinical tests, it can improve joint symptoms and side effects. SINOMENINE (Sinomenine SN) is an alkaloid, isolated from Caulis sinomenii. Previous studies have shown that SN posseses anti-inflammatory, analgesic, anti-rheumatism, immunosuppression pharmacological effects. The half-life of the main components of caulis sinomenii is short. Its release of histamine can lead to other side effects such as skin rash, and instability to light or heat. There is a need to modify the structure so as to improve its function. We have modified A ring and C ring of SN by halogen substitution and Grignard reaction and synthesized two sinomenine derivatives.