The prevention of pathologies by diet management is an important public health challenge. The Mediterranean diet (Med diet) is considered one of the healthiest dietary patterns. According to current scientific research, this dietary pattern is linked to a decreased prevalence and incidence of various chronic diseases, including cardiovascular disease, diabetes, cancer, and age-related cognitive decline, as well as a lower overall mortality rate. In the Mediterranean diet, a high consumption of Virgin Olive Oil (VOO), fruit, nuts, vegetables, and grains is linked to a decreased incidence of many diseases and a longer life expectancy. According to numerous studies, VOO is the major food responsible for the health and nutritional benefits of the Mediterranean diet. VOO chemical compounds have been shown in vitro and in vivo investigations to have potentially favorable health benefits as a result of their biological activities. VOO composition has been linked to a variety of biological activities, including antioxidant, anti-inflammatory, anti-diabetic, anti-cancer, and antiviral characteristics. As a result, increasing attention is being paid to the composition of VOO and the identification of its biologically active components. Because of their antioxidant, anti-inflammatory, and anti-thrombotic properties, phytochemicals, particularly phenolic compounds, have health-promoting effects, especially on cardiovascular and metabolic illnesses. These characteristics are even more important in light of the COVID-19 severe illness's heightened inflammatory and pro-thrombotic consequences. This overview collects and discusses the scattered data available in the literature concerning VOO compounds of biological interest and highlights their possible mechanisms of action and effects on human health. In vitro studies and in vivo intervention trials were selected and included in the study after conducting literature searches through "PubMed" and "Web of Science." In the majority of investigations, the ability of VOO phytochemicals to prevent the oxidation process at both the initiation and promotion/progression phases of several pathologies has been verified. The health benefits discussed in this article support the prospective health benefits acquired from VOO as a possible candidate in developing pharmaceutical preparations and nutraceutical or functional foods for a variety of pathological disorders. This idea could pave the way for future in vivo research and, eventually, clinical trials. In addition, greater research into the mechanisms of action and efficacy is needed to clarify the real biological potential of VOO phytochemicals on humans by performing intervention studies on populations at high disorder risk.