Amazonian Camu camu fruit (Myrciaria dubia (Kunth) McVaugh) has been called a “superfruit” due to its high levels of bioactive and antioxidant compounds such as polyphenols, carotenoids, and vitamin C. The biofunctional properties of camu camu fruit (including pulp, peel, and seeds) have been well established through several in vitro and in vivo studies. Several reports confirmed the nutritious and biofunctional value of camu camu extracts or its food-derived products, exhibiting antioxidant, antihyperglycemic, antihypertensive, and antiobesity activity, contributing to quality life improvement. Other studies showed antimicrobial, anti-inflammatory, antiproliferative, antihepatotoxic, antihemolytic, antimutagenic, and cell rejuvenation bioactivities. This Review summarizes the bioactive profile of camu camu fruit through the understanding of some physiological modulation processes and its contribution to the Amazon bioeconomy under the development of biofunctional food ingredients exhibiting health benefits.

Malic acid derivatives from camu-camu (Myrciaria dubia) fruit exhibited a strong in vitro inhibitory activity toward pancreatic α-amylase and α-glucosidase enzymes. During a bioguided chromatographic fractionation process of the whole fruit (pulp and peelings) polar extract, isomers (S)-4-butoxy-2-hydroxy-4-oxobutanoic acid (1) and (S)-4-butoxy-3-hydroxy-4-oxobutanoic acid (2) (84:16) were isolated and identified as a potent inhibitor of α-amylase (IC50= 11.69 ± 1.75 μg/mL) and α-glucosidase (IC50 = 102.69 ± 4.16 μg/mL). The chemical structures were confirmed by HPLC-ESIMS and 1H and 13C NMR (one- and two-dimensional) analyses. The structure-based virtual screening demonstrated that the aliphatic moiety plays a significant role in the binding mode of the test alkyl malate esters. Compound 1 exhibited the best interaction profile to bind both enzymes, having key structural features to form relevant contacts by involving adequate enzyme–ligand complex stabilization and compactness over time.