Leonurus japonicus Houtt,a Chinese traditional herbal medicine,has been widely used to cure gynecological diseases,such as incomplete abortion and menoxenia.Leonurine,a major active alkaloid compound only be found in Leonurus japonicus Houtt,has been successfully extracted and purified.Recent evidence has shown that leonurine can regulate a variety of pathologic processes including oxidative stress,inflammation,fibrosis,apoptosis,and multiple metabolic disorders.Here,we have reviewed the pharmacological actions and biological functions of leonurine,with a focus on the role of leonurine in the amelioration of various pathological processes.Insights into the related signaling pathways and molecular mechanisms have strengthened our understanding on the function of leonurine in the alleviation of multiple pathological states.Our summary of the existing researches should help direct future research into the basic science and clinical applications in related diseases.