Nature continues to be an invaluable source for discovering bioactive molecules, significantly influencing modern pharmaceutical development. Bioactive peptides, short amino acid sequences with inherent biological actions, have recently gained attention within drug discovery due to their diverse pharmacological potentials. These peptides, abundantly present in marine organisms, fungi, plants, and microorganisms, exhibit various bioactivities including antimicrobial, anticancer, immunomodulatory, neuroprotective, and anti-inflammatory effects. Despite substantial progress in identifying clinically relevant peptides through traditional screening techniques, a vast array of natural resources remains understudied, leaving considerable therapeutic potential yet to be realized. Moreover, bioactive peptides face crucial limitations such as poor stability, reduced bioavailability, and susceptibility to enzymatic degradation, significantly hindering their clinical translation. Advancements in metabolomics, proteomics, computational drug discovery, and peptide engineering are essential to overcome these barriers, thereby enabling rapid identification, characterization, and optimization of innovative peptide-based drugs.

This Research Topic aims to comprehensively examine recent advancements and future perspectives in the discovery, optimization, and formulation of bioactive peptides derived from natural sources. Specifically, the primary goals are to explore underutilized natural resources for novel peptide discovery, employ advanced analytical techniques and computational approaches for peptide design, and address major pharmaceutical challenges via peptide modification and innovative drug delivery systems.

To gather further insights in bioactive peptides and their therapeutic applications, we welcome articles addressing, but not limited to, the following themes:

• Discovery and bioprospecting of novel bioactive peptides from various natural origins.
• High-throughput and innovative screening methodologies for identifying therapeutic peptides.
• Strategies enhancing peptide stability, bioavailability, and pharmacokinetic profiles.
• AI-driven computational modeling and structure-activity relationship (SAR) analysis for optimized bioactivity.
• Advanced nanotechnology-based formulations and novel delivery systems promoting peptide efficacy and targeted action.

To be eligible for peer review, all manuscripts submitted to the Ethnopharmacology specialty section must comply with The Four Pillars of Ethnopharmacology. You can freely download the full version here. Please be aware that any submissions to Frontiers in Pharmacology that involve plant extracts or preparations must meet these four pillars as the minimum standard for sample characterization. Please also evaluate your manuscript using the ConPhyMP tool and ensure compliance with the standards outlined in the ConPhyMP statement (Front. Pharmacol. 13:953205).

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