Medicinal plants have been known as a rich source of natural products (NPs). Due to their diverse chemical structures and remarkable pharmacological activities, NPs are regarded as important repertoires for drug discovery and development.Biebersteiniaplant species belong to the Biebersteiniaceae family, and have been used in folk medicines in China and Iran for ages. However, the chemical properties, bioactivities and modes of action of the NPs produced by medicinalBiebersteiniaspecies are poorly understood despite the fact that there are only four knownBiebersteiniaspecies worldwide. Here, we reviewed the chemical classifications and diversity of the various NPs found in the four knownBiebersteiniaspecies. We found that the major chemical categories in these plants include flavonoids, alkaloids, phenylpropanoids, terpenoids, essential oils and fatty acids. We also discussed the anti-inflammatory, analgesic, antibacterial, antioxidant, antihypertensive and hypoglycemic effects of the fourBiebersteiniaspecies. We believe that the present review will facilitate the exploration of traditional uses and pharmacological properties ofBiebersteiniaspecies, extraction of the NPs and elucidation of their molecular mechanisms, as well as the development of novel drugs based on the reported properties and mode-of-action.