Amentoflavone is initially derived from extracts of Selaginella tamariscina. In recent years, amentoflavone has been discovered to be a natural polyphenolic compound with a variety of biologically activities, including anti-inflammatory,anti-microbial,anti-tumor,anti-oxidative and neuroprotective effects,and so on. For example,amentoflavone inhibits ability of NF-κB-mediated inducible nitric oxide synthase( iNOS) and reduces nitric oxide( NO) generation; thereby it prevents the inflammatory responses to NO. These effects of amentoflavone have attracted attention of researchers in various countries. In this article,we reviewed the progress in studies on the biological activities and pharmacological effects of amentoflavone to provide references for its research and development.