Tryptanthrin is a natural indolequinazoline alkaloid,is one of the bioactive components of many traditional Chinese herbal medicines,such as Indigo Naturalis,Isatidis Folium and Isatidis Radix.The antibacterial and anti-inflammatory effects of tryptanthrin have been reported for a long time.Recently,some studies have found that it also has anti-tumor,anti-virus,anti-angiogenesis,anti-parasitic and other pharmacological activities.Coupled with the characteristics of stable structure,low toxic and side effects,and easy absorption by the intestinal tract,it has become a current research hotspot.This review focused on the pharmacological activities of tryptanthrin,and at the same time summarized its natural sources,synthetic methods,as well as absorption,distribution,metabolism and toxicity in vivo.It is expected to provide a more comprehensive literature information support for the further research,development and utilization of tryptanthrin.