Medicinal plants of the Moraceae family have been well-known traditionally for their versatile applications in various fields including cosmetic, agriculture, food as well as pharmaceutical industries. The phytochemicals and pharmacology of the various parts of the Morus alba tree bestow its current and traditional uses as cosmetics, fodder, food, and medicine. It is commonly known as mulberry, which is one of the popular and ancient plants valued for its broad variety of therapeutic and nutritional values and is mostly planted in Asia. M. alba leaves are mainly used by silkworms as their food and used as fodder for cattle in many parts of the world. Generally, Mulberry fruits are used as fresh fruits, juices, and jams. They are beneficial for health due to the presence of biologically active phytochemicals having potential pharmacological activities. Depending on the maturity stages and cultivars, in mulberry fruit, a large number of nutritive compounds like amino acids, fatty acids, minerals, vitamins, and bioactive compounds such as polysaccharides, chlorogenic acid, anthocyanins, quercetin, and rutin have been reported. The mulberry root bark contains stilbenoids, alkaloids, and flavonoids, and has antihyperlipidemic, antimicrobial, anti-inflammatory, cytotoxic, and skin-whitening properties. The medicinal and biomedical importance of M. alba is reflected in its wide range of pharmacological activities for the treatment of various infectious diseases like inflammation, cancer, and gastrointestinal disorders. This chapter summarizes bioactive compounds, ethnobotany, phytochemistry, and nutraceutical and pharmacological potential of M. alba. Phytochemical screening of Morus alba has shown the presence of a large number of pharmacologically phytochemicals and secondary metabolites like alkaloids, glycosides, steroids, saponins, and phenolic compounds. The phenolic compounds include flavonoids, anthocyanins, terpenoids, and tannins which have remarkable antidiabetic, antioxidative, antistress, antimicrobial, anticancer, nephroprotective, antimutagenic, hepatoprotective, immune-modulatory, anxiolytic, cholesterol-lowering and anthelmintic effects. Generally, M. alba plant is multi-functional and has favorable pharmacological and medicinal properties. On the basis of the literature review of Morus species and their phytomedicinal effects, we reached the conclusion and anticipate that herbal products of M. alba hold excellent potential for future research. © 2023 Elsevier Inc. All rights reserved.