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Mushrooms have been consumed as food since earliest history, and they are part of human culture due to their sensory characteristics and attractive culinary attributes. Over the last few decades, studies into the pharmacological and therapeutic properties of mushrooms have become a matter of great interest to the scientific community, as they contain diverse bioactive compounds with health-promoting benefits. This chapter discusses recent advances and trends in mushroom utilization as functional health promoters. Special attention is given to the most important biological properties that have been widely reported for mushroom extracts and their related metabolites, including antioxidant, anti-inflammatory, neuroinflammatory, antimicrobial, immunomodulatory, cytotoxic, cardioprotective, antidiabetic, anti-aging, and hepatoprotective properties. Despite the promising potential of mushrooms as nutritional adjuvants with profound therapeutic properties, studies analysing their mechanism of action and validating their clinical effectiveness remain lacking.

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