Vernonia amygdalina Delile, which is in the Asteraceae family, is used as food and medicine all over the world, especially in Africa and Asia. This review reports the phytochemical, ethnopharmacological, phyto-cosmeceutical, and toxicological potentials of the plant. Recent scientific exploration of the plant has mainly focused on both its nutritional potential and ethnopharmacological properties. The antioxidant, anti-inflammatory, antidiabetic, hepatoprotective, hematological, anti-plasmodial, antimicrobial, anticancer, neurological, cosmeceutical, and other pharmacological values of V. amygdalina continue to be extensively explored. Many empirical studies of the therapeutic potential of the plant have attributed the ethnomedicinal properties of the plant to its phytochemical constituents, which include glycosides, saponins, tannins, terpenoids, etc. Compounds obtained from the leaves, root, stem, and flowers, which include vemoniosides, vernoamyosides, vernoniamyosides, vernoniosides, vernolide, vernodalol, vernodalin, vernomenin, vernomygdin, vernodalinol, epivernodalol, vernolepin, coumarins, luteolin, edotides, etc. have been identified as bioactive constituents responsible for numerous pharmacological activities of the plant. In addition, the toxicological evaluation of the plant revealed that it is safe for consumption at relatively high concentrations.