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Mulberry plants belonging to the Moraceae family have been grown for the purpose of being the nutrient source for silk worm and raw materials for the preparation of jams, marmalades, vinegars, juices, wines, and cosmetics. <i>Morus nigra</i> L. (black mulberry) is native to Southwestern Asia, and it has been used as a traditional herbal medicine for animals and humans. In this article, recent research progress on various biological and pharmacological properties of extracts, fractions, and isolated active constituents from different parts of <i>M. nigra</i> are reviewed. <i>M. nigra</i> exhibited a wide-spectrum of biological and pharmacological therapeutic effects including antinociceptive, anti-inflammatory, antimicrobial, anti-melanogenic, antidiabetic, anti-obesity, anti-hyperlipidemic, and anticancer activities. <i>M. nigra</i> also showed protective effects against various human organs and systems, mainly based on its antioxidant capacity. These findings strongly suggest that <i>M. nigra</i> can be used as a promising nutraceutical resource to control and prevent various chronic diseases.