Over the past decades, there has been increasing attention on polyphenol-rich foods including fruits and vegetables on human health. Polyphenols have been shown to possess some potential beneficial effects on human health and they are widely found in foods consumed by populations worldwide. Capparis spinosa (C. spinosa) is an important source of different secondary metabolites of interest to humankind. The traditional therapeutic applications of C. spinosa have been reported in Ancient Romans. Numerous bioactive phytochemical constituents have been isolated and identified from different parts (aerial parts, roots and seeds) of C. spinosa which are responsible alone or in combination for its various pharmacological activities. Therefore, this paper is a review of publications on the phytochemical and pharmacological properties of C. spinosa. There is insufficient evidence to suggest that C. spinosa or its extracts are able to improve the biomarkers of cardiovascular disease and diabetes. However, these studies used different parts of C. spinosa plant, methods of preparation and types of solvents, which cause the evaluation of activity of C. spinosa difficult and involve quite heterogeneous data. There is also evidence, although limited, to suggest benefits of C. spinosa in improving human health. Therefore, the relationship between C. spinosa and improved human health outcomes requires further study.