Phytonutrients are plant foods that contain many natural bioactive compounds, called phytochemicals, which show specific biological activities. These phytonutrients and their phytochemicals may play an important role in health care maintaining normal organism functions (as preventives) and fighting against diseases (as therapeutics). Phytonutrients’ components are the primary metabolites (i.e., proteins, carbohydrates, and lipids) and phytochemicals or secondary metabolites (i.e., phenolics, alkaloids, organosulfides, and terpenes). For years, several phytonutrients and their phytochemicals have demonstrated specific pharmacological and therapeutic effects in human health such as anticancer, antioxidant, antiviral, anti-inflammatory, antibacterial, antifungal, and immune response. This review summarizes the effects of the most studied or the most popular phytonutrients (i.e., turmeric, garlic, cinnamon, graviola, and oregano) and any reported contraindications. This article also presents the calculated physicochemical properties of the main phytochemicals in the selected phytonutrients using Lipinski’s, Veber’s, and Ghose’s rules. Based on our revisions for this article, all these phytonutrients have consistently shown great potential as preventives and therapeutics on many diseases in vitro, in vivo, and clinical studies.