Acanthospermum hispidum DC is a medicinal plant present in America, Africa, Australia, India, Hawaii, and Brazil. In Brazil, the species is used in the treatment of gastrointestinal, respiratory disorders and has expectorant action. In the literature, there are studies on the chemical composition of the species, with reports of the presence of alkaloids, flavonoids, hydrolyzable tannins, terpenes, and steroids. In addition, several studies have reported in vitro and in vivo studies that prove the biological properties of extracts and compounds isolated from different organs of the A. hispidum plant, including hepatoprotectors, antioxidants, antimicrobials and antiparasitic. The objective of this review is to update the knowledge about the phytochemical, pharmacological and toxicity aspects of A. hispidum, and to contribute to the recognition of the species and direct new studies. An extensive bibliographic search was conducted in different scientific databases. The presence of different chemical constituents in A. hispidum has been identified, among these constituents are flavonoids, tannins, terpenes, and steroids. Additionally, antimicrobial and antiparasitic activities were mainly attributed to the species, and other activities not previously described were presented, such as anticholinesterase, antioxidant, hepatoprotective, and hypoglycemic, all based on results of in vitro and in vivo studies. Finally, no reports of toxic effects were found in the in vitro and in vivo tests. After analyzing the articles, it was evidenced that other experiments with different models using animals are essential to evaluate the possible mechanisms of action of the extracts and compounds isolated of A. hispidum. Therefore, this review may contribute to the recognition of the importance of A. hispidum and its potential as a medicinal plant and may also guide the conduct of future research regarding the constituents, biological activities, and toxicity of the species.
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