There are approximately 260 known species in the genus
Millettia
, many of which are used in traditional medicine to treat human and other animal ailments in various parts of the world. Being in the Leguminosae (Fabaceae) family,
Millettia
species are rich sources of isoflavonoids. In the past three decades alone, several isoflavonoids originating from
Millettia
have been isolated, and their pharmacological activities have been evaluated against major diseases, such as cancer, inflammation, and diabetes. Despite such extensive research, no recent and comprehensive review of the phytochemistry and pharmacology of
Millettia
isoflavonoids is available. Furthermore, the structural diversity of isoflavonoids in
Millettia
species has rarely been reported. In this review, we comprehensively summarized the structural diversity of
Millettia
isoflavonoids, the methods used for their extraction and isolation protocols, and their pharmacological properties. According to the literature, 154 structurally diverse isoflavonoids were isolated and reported from the various tissues of nine well-known
Millettia
species. Prenylated isoflavonoids and rotenoids were the most dominant subclasses of isoflavonoids reported. Other subclasses of reported isoflavonoids include isoflavans, aglycone isoflavones, glycosylated isoflavones, geranylated isoflavonoids, phenylcoumarins, pterocarpans and coumaronochromenes. Although some isolated molecules showed promising pharmacological properties, such as anticancer, anti-inflammatory, estrogenic, and antibacterial activities, others remained untested. In general, this review highlights the potential of
Millettia
isoflavonoids and could improve their utilization in drug discovery and medicinal use processes.
Supplementary Information
The online version contains supplementary material available at 10.1007/s11101-022-09845-w.