Glucosinolate Derivatives: Emerging Anti-Inflammatory Agents

Glucosinolates are sulfur-containing secondary metabolites predominantly found in Brassicaceae plants, which, upon enzymatic hydrolysis, generate bioactive compounds with potent anti-inflammatory properties. These derivatives modulate key inflammatory pathways by inhibiting NF-κB nuclear translocation, reducing pro-inflammatory cytokine production, including TNF-α, IL-6, and IL-1β, and suppressing iNOS and COX-2 expressions. They also activate NRF2-dependent antioxidant defenses, upregulating enzymes such as HO-1 and NQO1, and regulate MMPs, contributing to tissue protection during chronic inflammation. Evidence from in vitro and in vivo studies consistently demonstrates their ability to attenuate inflammation and oxidative stress. Although approximately 137 glucosinolates have been identified, only about twelve have been investigated in detail regarding the anti-inflammatory activity of their derivatives, highlighting a significant gap in current knowledge and considerable potential for the discovery of new therapeutic compounds. In this context, a systematic survey was conducted of plant species reported in scientific literature as sources of glucosinolates, with particular emphasis on studies evaluating their extracts and fractions for anti-inflammatory potential in in vitro and in vivo experimental models. Additionally, this review also aims to highlight the anti-inflammatory and antioxidant potential of glucosinolate-derived compounds, focusing on their modulation of the NF-κB and NRF2 signaling pathways and their ability to regulate matrix metalloproteinases. It also emphasizes that, despite the broad diversity of glucosinolates identified to date, only a limited number have been functionally investigated. By addressing this gap, and based on the systematic survey performed, this review underscores the need for further research to fully explore their therapeutic potential.

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Publication Details

Journal
Pharmaceuticals
Published
2026-04-22
DOI
https://doi.org/10.3390/ph19050658
Primary Topic
Genomics, phytochemicals, and oxidative stress
Type
article
Field-Weighted Citation Impact
0.00

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article

Glucosinolate Derivatives: Emerging Anti-Inflammatory Agents

Maria Teresa Cruz, Sónia Pinho, Artur Figueirinha, Sandrine Ressurreição et al.
Pharmaceuticals
Genomics, phytochemicals, and oxidative stress
article

Glucosinolate Derivatives: Emerging Anti-Inflammatory Agents

Maria Teresa Cruz, Sónia Pinho, Artur Figueirinha, Sandrine Ressurreição, Lígia Salgueiro
article en

Abstract

Glucosinolates are sulfur-containing secondary metabolites predominantly found in Brassicaceae plants, which, upon enzymatic hydrolysis, generate bioactive compounds with potent anti-inflammatory properties. These derivatives modulate key inflammatory pathways by inhibiting NF-κB nuclear translocation, reducing pro-inflammatory cytokine production, including TNF-α, IL-6, and IL-1β, and suppressing iNOS and COX-2 expressions. They also activate NRF2-dependent antioxidant defenses, upregulating enzymes such as HO-1 and NQO1, and regulate MMPs, contributing to tissue protection during chronic inflammation. Evidence from in vitro and in vivo studies consistently demonstrates their ability to attenuate inflammation and oxidative stress. Although approximately 137 glucosinolates have been identified, only about twelve have been investigated in detail regarding the anti-inflammatory activity of their derivatives, highlighting a significant gap in current knowledge and considerable potential for the discovery of new therapeutic compounds. In this context, a systematic survey was conducted of plant species reported in scientific literature as sources of glucosinolates, with particular emphasis on studies evaluating their extracts and fractions for anti-inflammatory potential in in vitro and in vivo experimental models. Additionally, this review also aims to highlight the anti-inflammatory and antioxidant potential of glucosinolate-derived compounds, focusing on their modulation of the NF-κB and NRF2 signaling pathways and their ability to regulate matrix metalloproteinases. It also emphasizes that, despite the broad diversity of glucosinolates identified to date, only a limited number have been functionally investigated. By addressing this gap, and based on the systematic survey performed, this review underscores the need for further research to fully explore their therapeutic potential.

PharmaceuticalsVol. 19(5)
Polytechnic Institute of Coimbra (PT), Rede de Química e Tecnologia (PT), University of Coimbra (PT)
European Commission, Ministério da Ciência, Tecnologia e Ensino Superior, Fundação para a Ciência e a Tecnologia
Openalex Percentile: Top 13%
Genomics, phytochemicals, and oxidative stress
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