Benzophenanthridine alkaloids belong to the benzyl isoquinoline family of alkaloids, which are mainly found in Papaveraceae and Rutaceae. To date, over.100 compounds have been isolated from natural herbal medicines which display a variety of pharmacological functions. In this paper, we have summarized the work since 1980 and our own research on benzophenanthridine alkaloids in terms of their chemical structures and distribution, biosynthesis, biotransformation and metabolism, spectral characteristics, pharmacological activities and toxicity. This review lays the foundation for further research into benzophenanthridine alkaloids and their potential applications.