Lycorine is the major active component from the amaryllidaceae family plant Lycoris radiate, a represent traditional Chinese medicinal herb, and is one of the typical alkaloids with pyrrolophenanthridine nucleus core. Lycorine has drawn great interest in medicinal field due to its divergent chemical structures and multiple biological functions, as well as pharmacological effects on various diseases. Accumulated evidence shows that lycorine not only possesses strong pharmacological effects on many diseases, including anti-leukemia, anti-tumor, anti-angiogenesis, anti-virus, anti-bacteria, anti-inflammation, and antimalaria, but also exerts many other biological functions, such as inhibition of acetylcholinesterase and topoisomerase, suppression of ascorbic acid biosynthesis, and control of circadian period length. Notably, lycorine exhibits its numerous pharmacological effects on various diseases with very low toxicity and mild side effects. The divergent chemical structures, multiple biological functions, and very low toxicity of lycorine imply that the agent is a potential drug candidate that warrants for further preclinical and clinic investigation.