Artabotrys is a genus of small trees in the family Annonaceae. This genus contained over 100 perennial medicinal plants available in the old world tropics. Artabotrys plants have a lengthy history of use in medicine for malaria, diarrhea, backache, and scrofula treatments, as well as some of which were used as tea-like beverages. About 90 reports were reviewed from inception to now, in which the decoctions of about 9 species were used in traditional folk medicines. With 234 isolated compounds, Artabotrys metabolites can be classified as alkaloids, terpenoids, sterols, flavonoids, polyoxygenated cyclohexenes, fatty acids, acetogenins, etc. Significantly, alkaloidal aporphines were separated and identified as the main isolates. Artabotrys plants are also rich in the essential oils. Especially, A. hexapetalus exerted a great role in perfumery industry. Artabotrys constituents possessed various pharmacological values, such as antioxidative, antidiabetic, hepatoprotective, and mosquito repellency, but cytotoxic and antimicrobial activities are the most striking features. In conclusion, Artabotrys plant extracts and their metabolites are of great socio-economic importance, thereby more and more phytochemical and pharmacological investigations are expected.