Chemical constituents of mushrooms provide a wide range of therapeutic effects, enabling them to act as immunomodulatory, anticarcinogenic, antiviral, antioxidant, and anti-inflammatory agents. The accumulated secondary metabolites in medicinal mushrooms are widely accepted as sources of safe and effective nutraceuticals, cosmeceuticals, and pharmaceuticals. These compounds, working individually or synergistically, underscore mushrooms’ vast potential as powerhouses of health-benefiting molecules. The cardioprotective effects of mushrooms are attributed to their rich composition of polysaccharides, sterols, antioxidants, and anti-inflammatory compounds alongside triterpenes, unique amino acids like ergothioneine, and fibrinolytic enzymes. This diverse array of bioactive works synergistically to improve lipid profiles, regulate blood pressure, and maintain vascular integrity. As such, mushrooms represent a powerful functional food with significant potential for inclusion in preventive dietary strategies aimed at reducing the global burden of cardiovascular disease. While the preclinical data are compelling, the path forward requires a continued commitment to rigorous scientific validation. This chapter delves into the goodness of mushroom nutraceuticals on human health from a holistic perspective. Immunomodulation, anti-inflammatory, and anticancer action are explained based on research findings. Besides, cognitive enhancement and neuroprotection as well as cardiovascular effects from mushrooms are detailed. Additionally, the metabolic and endocrine effects on the human body are described in detail. It also aims to provide researchers and food industrialists with more pathways in mushroom research, perhaps in functional food products involving mushrooms as their bioactive components.