Bioactive compounds of plant origin are used all over the world because of their positive impact on human and animal health and because of their beneficial, specific properties. The most popular bioactive compounds beneficial to health have been identified and defined earlier. Others are yet to be discovered. In particular, the most common biological activities of these compounds were indicated, such as antiallergic, antidepressant, antidiabetic, anti-inflammatory, antimicrobial, antioxidant, antitumor, antiviral, antithyroid, anxiolytic, to cardioprotective, hepatoprotective, and flatulence-inhibiting effects. The beneficial properties of bioactive compounds may be associated with substances like alcohols, terpenoids, phenolic antioxidants, and rosmarinic acid, which are present in several medicinal plants. The updated review considers the physiological, botanical, phytochemical, and medical aspects of herbal bioactive compounds as well as their therapeutic properties, with a focus on their health benefits and the potential use of nutraceuticals.