| Summary: | Deoxynojirimycin (DNJ), the first isolated iminosugar, is a natural alkaloid acting as a potent inhibitor of α-glucosidase with high nutritional value. It naturally occurs in plants (especially <i>Morus</i> spp.), microbes, and insects or can be synthesized. Diverse biological activities, such as antihyperglycemic, lipid-lowering, antitumor, antiviral, and anti-inflammatory, have been recognized for this compound. However, DNJ has not been approved as a food supplement until now. Several studies, also in clinics, are carried out on <i>Morus</i> spp. containing DNJ. Among <i>Morus</i> spp., <i>Morus alba</i> L. (white mulberry), <i>Morus nigra</i> L. (black mulberry), and <i>Morus rubra</i> L. (red mulberry) are the three main species that grow all over the world. Some spurious studies have been conducted on Reducose<sup>®</sup> and Glubloc™, two products that contain DNJ and <i>Morus alba</i>, respectively. However, mulberry allergy, including respiratory allergy, airborne contact urticaria, anaphylaxis, oral allergy syndrome, and food induced urticaria, may be observed. This review aims to explore a crucial and timely question: how DNJ exerts its biological effects and what role it may play in therapeutic applications. We provide a comprehensive summary of the current understanding of DNJ’s pharmacological potential and the methods used for its production. We also report recent developments in clinical studies on <i>Morus alba</i>, Reducose<sup>®</sup> and Glubloc™.
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