Adansonia digitataL. fruit, also known as baobab, has been used traditionally throughout the world for its medicinal properties. Ethnopharmacological uses of various plant parts have been reported for hydration, antipyretic, antiparasitic, antitussive, and sudorific properties and also in the treatment of diarrhea and dysentery in many African countries. Several studies have revealed that in addition to these applications, baobab has antioxidant, anti-inflammatory, analgesic, and antimicrobial activities. The health benefits of baobab have been attributed to its bioactive compounds, namely phenols, flavonoids, proanthocyanins, tannins, catechins, and carotenoids. Baobab fruit is also an important source of vitamin C and micronutrients, including zinc, potassium, magnesium, iron, calcium, and protein, which may reduce nutritional deficiencies. Despite scientific studies revealing that this fruit has a wide diversity of bioactive compounds with beneficial effects on health, there is a gap in the review of information about their mechanisms of action and critical analysis of clinical trials exploring, in particular, their effect on glycemia regulation. This work aims to present a current overview of the bioactive compounds, biological activities, and effects ofA. digitatafruit on blood glucose, highlighting their potential mechanisms of action and effects on glycemia regulation, evaluated in recent animal and human trials.