Liriodenine, an oxoaporphine-type alkaloid, widely exists in various forest plants as a non-food bioactive natural product. It showed a great diversity of biological effects, such as anticancer, antimicrobial, antiparasitic, insecticidal activities as well as inhibitory effects on topoisomerase and cholinesterase. Additionally, liriodenine possesses a delicate molecular backbone containing planar hydrophobic conjugated system. Thus, it is extremely promising to be developed in pharmaceutical and agrochemical industries. In this review, we systematically summarized its sources, chemistry, and bioactivities. Furthermore, some expectations for the future research and development were prospectively proposed based on the related publications of this field up to May in 2022. © 2022 Elsevier B.V.