[Original Russian text published in Uspekhi Sovremennoi Biologii, 2026, Vol. 146, No. 1, pp. 43–55] This review summarizes current scientific data on the molecular mechanisms of action of lichen compounds: depsidones, depsidiones, anthraquinones, and dibenzofurans. The antimicrobial, antioxidant, anti-inflammatory, and cytotoxic effects identified in experimental models in vitro and partially confirmed in vivo are analyzed. The efficacy, environmental friendliness, and limitations of current methods for extracting biologically active compounds from lichens are assessed: ultrasound (UAE), microwave (MAE), supercritical fluid extraction (SFE), and enzymatic extraction (EAE). Prospects for the development of pharmaceuticals, topical antimicrobial agents based on usnic acid, and dietary supplements with antioxidant properties are discussed. Particular attention is paid to critical barriers: ensuring a sustainable raw material base, the economic aspects of lichen biomass production, methods for purifying total biomass, the need for strict standardization of extracts, and the requirements for a comprehensive toxicological safety assessment in accordance with international regulatory standards. Keywords: lichens, secondary metabolites, biological activity, standardization, immunomodulators, toxicological safety.