Marine metabolites and sea-based biomaterials derived from diverse oceanic organisms have emerged as a rich source of bioactive compounds with significant therapeutic potential for human diseases. This review explores their applications in cardiovascular disorders, cancer therapy, neurodegenerative diseases, and metabolic syndromes, emphasizing their unique molecular architectures and underlying mechanisms of action. Importantly, several value-added marine-derived products are obtained from waste generated by fishing and aquaculture industries, reinforcing their relevance within a sustainable and circular bioeconomy framework. Representative case studies, including ziconotide for pain management and trabectedin for cancer treatment, highlight the successful translation of marine metabolites from discovery to clinical use. Despite their promise, challenges such as regulatory constraints, limited natural availability, and batch-to-batch variability associated with isolation-based production remain significant barriers. In this context, the integration of alternative synthetic and semi-synthetic approaches, alongside advances in biotechnology and chemical synthesis, offers viable strategies to enhance reproducibility, quality control, and scalability. Furthermore, emerging applications of marine-derived biomolecules in regenerative medicine and tissue engineering underscore their expanding therapeutic relevance. Looking ahead, the impact of climate change on marine biodiversity poses additional challenges to the availability and compositional consistency of marine resources, necessitating adaptive and sustainable sourcing strategies. Overall, this review underscores the critical importance of continued and responsible exploration of marine biodiversity to support innovative and effective therapeutic solutions for human health.
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