The amaryllidaceae family consists of about 75 genera and 1100 species that are wide-spread in the tropics and warm temperate regions of the world. Since the first isolation of lycorine, more than 500 amaryllidaceae alkaloids have been isolated over the past three decades. The enormous numbers of diverse amaryllidaceae alkaloids are classified into different groups mainly according to their structural features. The representative alkaloids are norbelladine, lycorine, hippeastrine, narwedine, haemanthamine, pancratistatin, pretazettine, montanine, galanthindole, cherylline and ismine. Recently, more extensive studies have revealed that amaryllidaceae alkaloids exhibit a wide range of bioactivities, such as antitumor, antiviral, antibacterial, antifungal, antimalarial and analgesic. Acetylcholinesterase (AChE) inhibitory and cytotoxic activities have also been reported. The aim of the present review is to discuss the recent developments on the biological and pharmacological activities of amaryllidaceae alkaloids with IC 50 or EC 50 values since 2005, supporting the potential therapeutic possibilities for the use of these compounds.