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REVIEW ARTICLE

Pharmacological and toxicological perspectives of bioactive peptides

Adel Ghorani-Azam1,2 ,  Sina Karimipour3 ,  Samaneh Sepahi2,4*
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1 Department of Forensic Medicine and Toxicology, School of Medicine, Urmia University of Medical Sciences, Urmia, Iran
2 Food and Drug Research Center, Food and Drug Administration, Ministry of Health and Medical Education, Tehran, Iran
3 Laser Applications in Medical Sciences Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran
4 Food and Beverages Safety Research Center, Urmia University of Medical Sciences, Urmia, Iran
Global Translational Medicine, 025510094 https://doi.org/10.36922/GTM025510094
Received: 16 December 2025 | Revised: 23 March 2026 | Accepted: 23 April 2026 | Published online: 12 May 2026
© 2026 by the Author(s). This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution 4.0 International License ( https://creativecommons.org/licenses/by/4.0/ )
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Abstract

Bioactive peptides, from dietary and environmental sources, represent a promising front line for developing pharmaceuticals, functional foods, and a new generation of antibiotics. However, their therapeutic application necessitates a comprehensive understanding of their mechanisms of action and toxicological profile. Peptides exhibit effective mechanisms in combating bacterial infections and cancer therapy. However, findings reveal significant toxicological concerns, hemolytic activity, immunogenic reactions, and instability in the cellular environment that can lead to unpredictable metabolic byproducts. Furthermore, the dose and source of peptides are critical determinants of their safety and efficacy. Accordingly, the dual nature of bioactive peptides necessitates a balanced approach to enhance their efficacy while minimizing their potential harm. For these purposes, peptide-specific toxicological screening is essential for translating these natural compounds into safe and effective therapeutic agents. The purpose of this article is to comprehensively review the potential applications of bioactive peptides, their pharmacological mechanisms, and toxicological profiles to elucidate their efficacy and safety for use in food and medicine.

Keywords
Natural peptides
Toxicology
Pharmacology
Food-derived peptides
Peptide drugs
Bioactive peptides
Funding
None.
Conflict of interest
The authors declare that they have no competing interests.
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