Pereskia aculeata Mill., a species of the family Cactaceae, is considered a non-conventional leafy vegetable. This species has been consumed mainly for its protein and mineral (iron and calcium) content, and represents a strategy for improving the nutritional value of diets in rural communities. P. aculeata protein is of high quality (with an abundance of the essential amino acids lysine and tryptophan) and high digestibility. Additionally, P. aculeata seems to be a promising thickening ingredient as it is rich in a mucilage, which has potential to serve as a functional food ingredient that contributes to favorable sensory properties and to dietary soluble fiber requirements. Further, P. aculeata leaves are an abundant source of vitamin C, the provitamin A carotenoids α- and β-carotene, and several xanthophylls, including lutein and violaxanthin. Additionally, the P. aculeata essential oil contains several terpenes and terpenoids commonly found in herbs and spices used as culinary seasonings and in traditional medicinal practices. The objective of this chapter was to gather information on the active compounds present in P. aculeata leaves that can demonstrate beneficial health effects.