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Apposite energy is required for body activity. Energy is derived from the oxidation of various biomolecules like carbohydrates, lipids, and proteins. These bio-molecules in the proper amount are essential for the structural and functional activities of any living being. Certain vitamins and enzymes are also needed for the maintenance of biochemical processes. Our daily food is the major source of these biomolecules. From the last few decades, researchers have placed giant effort into searching for a food material that can provide nearly all the essential components required to maintain the energy need and consequently, balancing the body’s homeostasis. Mushrooms have the potential to address the above-raised issues. Besides their pleasant flavor and culinary value, mushrooms are an important source of biomolecules that include large macromolecules (protein, carbohydrate, lipid, and nucleic acid) as well as small molecules (primary metabolites, secondary metabolites, and natural products). This chapter discusses the bioactive compounds in edible mushroom and their activities.