Jatrorrhizine has neuroprotective, antioxidative, anti-inflammatory, antihypercholesterolemic, and anti-hyperglycemia effects.Jatrorrhizine is expected to be developed as a new gastric prokinetic drug, it is metabolized by human CYP1A2 and multiple UGT1A isoforms. It has inhibitory activities against the expression of inducible NO syntase (iNOS) and cyclooxygenase-2 (COX-2), and can improve the utilization and excretion of cholesterol by up-regulating the mRNA and protein expression of LDLR and CYP7A1.