Edible mushrooms have long been valued as functional foods and traditional remedies, yet a significant developmental gap hinders their transition from nutraceuticals to standardized pharmaceutical ingredients. This narrative review provides a comprehensive and integrative analysis of edible mushroom-derived bioactive compounds as emerging candidates for pharmaceutical development. It examines major chemical classes, including polysaccharides (e.g., β-glucans), proteins (e.g., lectins, FIPs), triterpenoids (e.g., ganoderic acids), nucleosides (e.g., adenosine and cordycepin), and phenolic compounds, which underpin immunomodulatory, anticancer, antioxidant, anti-inflammatory, and metabolic activities. Beyond bioactivity, the review critically examines the downstream processing pipeline required for translation into pharmaceutical ingredients, encompassing controlled biomass production, pre-extraction processing, extraction technologies, isolation and purification strategies, and structural elucidation techniques. Key bottlenecks are identified, including bioavailability limitations of β-glucans (2–5%), lack of standardization, limited human clinical evidence, and regulatory constraints, explaining why robust preclinical evidence has not consistently translated into clinical success. Emerging solutions are also highlighted, including application of multi-omics tools, nano-encapsulation strategies, and synthetic biology approaches to improve scalability and reproducibility. By synthesizing research on natural product chemistry, biotechnology, and pharmacology, this study maps the journey of edible mushrooms from traditional dietary components to pharmaceutical-grade ingredients, providing a focused resource for researchers and industry stakeholders aiming to navigate mushroom-based drug development.
Adesida et al. (Sat,) studied this question.