Cited by 129Inflammatory mediators and NSAID effectsNatural Compounds in Disease TreatmentBioactive natural compounds

Targeting COX-2 expression by natural compounds: A promising alternative strategy to synthetic COX-2 inhibitors for cancer chemoprevention and therapy

Cerella, Claudia, Sobolewski, Cyril, Dicato, Mario, Diederich, Marc·2010·Biochemical Pharmacology

Abstract

Cyclooxygenase (COX)-2 is a pro-inflammatory immediate early response protein, chronically up-regulated in many pathological conditions. In autoimmune diseases, it is responsible for degenerative effects whereas in cancer, it correlates with poor prognosis. A constitutive expression of COX-2 is triggered since the earliest steps of carcinogenesis. Consequently, strategies aimed at inhibiting COX-2 enzymatic activity have been clinically applied for the treatment of autoimmune disorders; in addition, the same approaches are currently investigated for anti-cancer purposes. However, COX-2 protein inhibitors (i.e., NSAIDs and COXIBs) are not amenable to prolonged administration since they may cause severe side effects, and efforts are underway to identify alternative approaches for chemoprevention/therapy. COX-2 expression is a multi-step process, highly regulated at transcriptional and post-transcriptional levels. Defects in the modulation of one or both of these steps may be found in pathological conditions. Targeting COX-2 expression may therefore represent a promising strategy, by which the same preventive and therapeutic benefits may be gained while avoiding the severe side effects of COX-2 enzymatic inhibition. Naturally occurring compounds derived from plants/organisms represent a huge source of biologically active molecules, that remains largely unexplored. Derived from plants/organisms used in traditional forms of medicine or as dietary supplements, these compounds have been experimentally investigated for their anti-inflammatory and anti-cancer potential. In this review, we will analyze how natural compounds may modulate the multistep regulation of COX-2 gene expression and discuss their potential as a new generation of COX-2 targeting agents alternative to the synthetic COX-2 inhibitors.

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Crossref · 10.1016/j.bcp.2010.06.050

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Authors
Cerella, C., Sobolewski, C., Dicato, M., & Diederich, M.
Affiliations
Hôpital Kirchberg (LU)
Corresponding author
Diederich, Marc
Venue
Biochemical Pharmacology
Publisher
Elsevier BV
Published
2010-12
Volume
80
Issue
12
Pages
1801-1815
ISSN
0006-2952 (ISSN-L)
OpenAlex
W2064546820
Cited by
129
References
154
Citations by year
2026: 3 · 2025: 6 · 2024: 5 · 2023: 6 · 2022: 5 · 2021: 17 · 2020: 4 · 2019: 4 · 2018: 8 · 2017: 7 · 2016: 8 · 2015: 11 · 2014: 14 · 2013: 7 · 2012: 10
FWCI
1.08
Type
journal article
Language
en
Open access
closed
Locations
  • Biochemical Pharmacology (publishedVersion)
  • PubMed (publishedVersion)
Funders
  • Fondation Recherche Cancer et Sang
  • Action LIONS Vaincre le Cancer
  • Een Häerz fir kriibskrank Kanner
  • Recherches Scientifiques Luxembourg
Topics
  • Health Sciences › Medicine › Pharmacology › Inflammatory mediators and NSAID effects
  • Health Sciences › Medicine › Complementary and alternative medicine › Natural Compounds in Disease Treatment
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Bioactive natural compounds
Keywords
cyclooxygenase-2, natural compounds, phytochemicals, chemoprevention, anticancer agents, COX-2 inhibitors, nonsteroidal anti-inflammatory drugs, transcriptional regulation, post-transcriptional regulation, anti-inflammatory activity, carcinogenesis, traditional medicine, dietary supplements
MeSH terms
Animals, Antineoplastic Agents, Biological Products, Humans, Neoplasms, Protein Processing, Post-Translational, RNA, Messenger, Transcription, Genetic, Gene Expression Regulation, Enzymologic, Anticarcinogenic Agents, RNA Stability, MicroRNAs, Cyclooxygenase 2, Cyclooxygenase 2 Inhibitors, Molecular Targeted Therapy

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