Andrographolide is one of the major natural active constituents in Andrographis panniculata of Acanthaceae family. Andrographolide and its derivatives are proved to posses a wide range of biological activities, such as anti-inflammatory, antiviral, anti-tumor, anti-human immunodeficiency virus(HIV), hepatoprotective and α-glucosidase inhibition activity. In this paper, the development of synthesis of rographolide derivatives and their related pharmacological activities were reviewed.