Amaryllidaceae plants are currently appreciated as a plentiful source of unique bioactive alkaloids. Among them, lycorine is one of the major pyrrolophenanthridine alkaloids commonly isolated from different species of this family. Over the past years, lycorine has attracted great research interest owing to its superlative biological potential and pharmacological actions, including antitumor, antiangiogenic, antiviral, antibacterial, antimalarial, anti-parasite, antioxidant, hepatoprotective, analgesic, anti-inflammatory activities, and inhibition of ascorbic acid synthesis, among many others. Therefore, this review was undertaken to highlight the chemical, chromatographic, spectral, and biological aspects of this promising Amaryllidaceae alkaloid, together with a future perspective for its potential application in the pharmaceutical field.