Matrine is a quinolizidine alkaloid isolated from the roots of Sophora flavescens (Kushen),
Sophora tonkinensis, and Sophora alopecuroides (Kudouzi). Matrine and its derivatives have displayed
a broad scope of biological properties such as anticancer activity, anti-inflammatory activity,
antiviral activity, analgesic effect, anti-fibrotic activity, insecticidal activity, antimicrobial activity,
etc. The present review has summarized the biological activities and structural modifications of matrine
and its derivatives focused on their N-1 position and lactam ring from 2010 to 2015. In addition,
the mechanism of action and structure-activity relationships of matrine and its derivatives are discussed.