Abstract: Rutaecarpine was one of the main bioactive ingredients isolated from Chinese herbs 'Wu-Chu-Yu' ,and has been shown to have various biological effects such as cardiovascular protection,neuroprotection,gastric mucosal protection，and anti-inflammatory effects.Studies on multiple disease models showed rutaecarpine has a superior ability to bind various proteins,such as TRPV1，COX-2，NADPH and AChE,which prevents the progress of disease through multi-targets.This review summarize的 the recent advances on the biological activity of rutaecarpine and focuse的 on pharmacological targets,aiming to provide more evidence supporting its use as a lead compound to design more multi-target drugs.

Key words: rutaecarpine, multi-targets, TRPV1, NADPH, COX-2