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For centuries, based on empiric knowledge, macrofungi or mushrooms have been used for pharmaceutical purposes in several cultures, including Asian countries. In this context, numerous scientists worldwide have been investigating the diverse chemical groups isolated from mushrooms, including polysaccharides, proteins, lipids, terpenoids, and polyphenols. Beyond their nutritional potential, these macromolecules have been associated with several medicinal properties, including anticancer, immunomodulatory, anti-inflammatory, antioxidant, antidiabetic, cholesterol-lowering, antibacterial, antiviral, hepatoprotective, and neuroprotective effects, among others. Most of these research studies have focused on the functional and biological potential of mushroom extracts. Furthermore, several other studies have indicated possible beneficial synergistic effects between the different bioactive molecules present in mushrooms. Therefore, nowadays, beyond diet, macrofungal species can be consumed as functional foods, nutraceuticals, and pharmaceutical products to treat or prevent human disorders. This chapter describes the main bio-functional macromolecules obtained from edible mushrooms and their associated human health benefits. Further, additional research studies focusing on nutraceutical and functional applications of mushroom macromolecules should be performed to validate their efficacy and safety, which will be of utmost importance for developing innovative food products and biomedical innovations.

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