Sinomenine is a clinically available drug for the treatment of rheumatoid arthritis（RA）.In a continuous research aiming at discovery of sinomenine derivates with better bioactivity,a cross-coupling reaction of sinom...Sinomenine is a clinically available drug for the treatment of rheumatoid arthritis（RA）.In a continuous research aiming at discovery of sinomenine derivates with better bioactivity,a cross-coupling reaction of sinomenine and 1,2-dihydroxybenzene catalyzed by a fungus Coriolus unicolor afforded an unique C-C cross-coupled compound 2,together with（S）-disinomenine and （R）-disinomenine.The structure of 2 was elucidated by MS and NMR spectroscopy.Compound 2 was further assayed for the inhibitory activity on IL-6 overproduction in SW982 cells and exhibited a much more potent activity on IL-6（96%inhibition） compared with those of（S）-disinomenine and sinomenine（17%and 12%inhibition,respectively）.展开更多
基金supported by National Natural Science Foundation of China(Nos20872060,20936002 and 31100080)the Fundamental Research Funds for Central University(No1082020502)
文摘Sinomenine is a clinically available drug for the treatment of rheumatoid arthritis（RA）.In a continuous research aiming at discovery of sinomenine derivates with better bioactivity,a cross-coupling reaction of sinomenine and 1,2-dihydroxybenzene catalyzed by a fungus Coriolus unicolor afforded an unique C-C cross-coupled compound 2,together with（S）-disinomenine and （R）-disinomenine.The structure of 2 was elucidated by MS and NMR spectroscopy.Compound 2 was further assayed for the inhibitory activity on IL-6 overproduction in SW982 cells and exhibited a much more potent activity on IL-6（96%inhibition） compared with those of（S）-disinomenine and sinomenine（17%and 12%inhibition,respectively）.
