Leaves of Spinacia oleracea have been widely used as vegetable foods. Some studies on the chemical composition of spinach shown that, it contains an elevated amount of micronutrients (vitamins and minerals), also has an important economic value and some agronomic advantages. S. oleracea in traditional medicine is reported to cure more than one health problem.This review focuses on the ethnopharmacological uses and pharmacological and phytochemical studies of Spinacia oleracea.Information on S. oleracea was obtained via electronic search of scientific databases such as Scopus, PubMed, Google Scholar, Scirus, Science Direct, Scielo, Web of Science, Medline, Springerlink, BioMed Central (BMC), and SciFinder for publications on this plant. In addition, books on medicinal herbs were also consulted.Approximately 100 chemical compounds were isolated and characterized from S. oleracea. The major active components of the plant are flavones, flavanols, methylenedioxyflavonol glucuronides, glucuronides, and carotenoids, which were extensively investigated. This review revealed potential pharmacological properties of these isolated compounds such as anti-obesity, anti-α-amylase, bile-acid binding capacity, anti-mutagenic, anti-oxidant, anticancer, anti-inflammatory, cognitive and mood effect, hypoglycemic, and anti-hypertriglyceridemia.S. oleracea is an important edible plant also used for ethnomedical therapy of obesity, inflammation of lungs, lumbago, flatulence, and treatment of urinary calculi. Pharmacological and phytochemical studies of this plant including bioactives, which have been adequately studied, support its uses in the traditional medicines. Additionally, prospects and future trends of this plant are proposed.