This review focuses on the bioactive and functional properties of mulberry (Morus spp., Moraceae) leaves and shoot extracts, highlighting their potential as a rich source of health-promoting compounds. Traditionally valued for feeding Bombyx mori silkworms, mulberry leaves and shoots exhibit significant medicinal potential due to their diverse bioactive composition, including flavonoids, phenolics, anthocyanins, alkaloids, vitamins, and minerals. These compounds contribute to various pharmacological activities such as antioxidant, antidiabetic, antihyperlipidemic, anti-inflammatory, antimicrobial, immune-modulating, and anticancer effects. Some of these effects are linked to mechanisms like α-glucosidase and α-amylase inhibition, reduced foam cell and fat formation, NF-κB signaling suppression, apoptosis promotion, and modulation of oxidative stress and inflammation. Recent studies highlighted the efficacity of key bioactive components like oxyresveratrol or 1-deoxynojirimycin from young mulberry leaves and shoots in preventing and managing metabolic, cardiovascular, skin, and cancer-related conditions, as well as in supporting immune system health. These findings underscore the therapeutic relevance of these phytochemicals in modern preventive and complementary medicine. Bioactive compound extraction commonly involves the use of methanol, acetone, vinegar, or glycerin, resulting in diverse formulations such as tinctures, extracts, tonics, and elixirs. Maceration in hydroalcoholic solutions is particularly effective for preserving the bioavailability of active constituents, with the alcohol-to-water ratio being crucial for extraction efficiency. In pharmaceutical applications, mulberry extracts are valuable in dietary supplements, dermatological formulations, and preventive therapies against degenerative diseases. Moreover, their inclusion in combination therapies may enhance the efficacy of conventional treatments. The promotion of these products can positively impact the valorization of local natural resources, offering an opportunity for sustainable and innovative pharmaceutical development. The novelty of this review lies in its comprehensive approach to mulberry leaf and shoot extracts, highlighting not only their well-documented antioxidant and metabolic health benefits, but also drawing attention to their less-explored properties, supporting future research and applications in health-related fields.