Carvacrol, a component of thyme oil, activates PPARα and γ and suppresses COX-2 expression
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Cyclooxygenase-2 (COX-2), the rate-limiting enzyme in prostaglandin biosynthesis, plays a key role in inflammation and circulatory homeostasis. Peroxisome proliferator-activated receptors (PPARs) are ligand-dependent transcription factors belonging to the nuclear receptor superfamily and are involved in the control of COX-2 expression, and vice versa. Here, we show that COX-2 promoter activity was suppressed by essential oils derived from thyme, clove, rose, eucalyptus, fennel, and bergamot in cell-based transfection assays using bovine arterial endothelial cells. Moreover, from thyme oil, we identified carvacrol as a major component of the suppressor of COX-2 expression and an activator of PPARalpha and gamma. PPARgamma-dependent suppression of COX-2 promoter activity was observed in response to carvacrol treatment. In human macrophage-like U937 cells, carvacrol suppressed lipopolysaccharide-induced COX-2 mRNA and protein expression, suggesting that carvacrol regulates COX-2 expression through its agonistic effect on PPARgamma. These results may be important in understanding the antiinflammatory and antilifestyle-related disease properties of carvacrol.
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PPARs are ligand-activated transcription factors comprising PPARα, PPARβ/δ, and PPARγ, which play roles in lipid and carbohydrate metabolism, cell proliferation and differentiation, and inflammation.
“Peroxisome Proliferator-Activated Receptor (PPARs) are ligand-activated transcription factors that belong to the superfamily of nuclear hormone receptors, which also includes receptors for vitamin D, vitamin A, thyroid hormone, bile acids, and steroid hormones. The PPAR subfamily comprises three isotypes, PPARα, PPARβ/δ, and PPARγ, which play various roles in lipid and carbohydrate metabolism,”
From Antioxidant and Anti-Inflammatory Activities of Essential Oils: A Short Review (2010) · cites this paper as [132]
Carvacrol suppresses LPS-induced COX-2 mRNA and protein expression in human U937 cells, suggesting that carvacrol regulates COX-2 expression through its agonistic effect on PPARγ.
“In human macrophage-like U937 cells, carvacrol suppressed LPS-induced COX-2 mRNA and protein expression, suggesting that carvacrol regulates COX-2 expression through its agonistic effect on PPARγ [132].”
From Antioxidant and Anti-Inflammatory Activities of Essential Oils: A Short Review (2010) · cites this paper as [132]
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Antioxidant and Anti-Inflammatory Activities of Essential Oils: A Short Review
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- Authors
- Hotta, M., Nakata, R., Katsukawa, M., Hori, K., Takahashi, S., & Inoue, H.
- Affiliations
- Nara Women's University (JP)
- Akita Research Institute for Food and Brewing (JP)
- Corresponding author
- Inoue, Hiroyasu
- Venue
- Journal of Lipid Research
- Publisher
- Elsevier BV
- Published
- 2010-01
- Volume
- 51
- Issue
- 1
- Pages
- 132-139
- ISSN
- 0022-2275 (ISSN-L)
- PMC
- PMC2789773
- OpenAlex
- W2169478020
- Cited by
- 260
- References
- 41
- Citations by year
- 2026: 11 · 2025: 13 · 2024: 13 · 2023: 21 · 2022: 19 · 2021: 22 · 2020: 25 · 2019: 10 · 2018: 12 · 2017: 11 · 2016: 8 · 2015: 17 · 2014: 24 · 2013: 14 · 2012: 24
- FWCI
- 5.37
- Type
- journal article
- Language
- en
- Open access
- hybrid
- doi.org
- Licence
- Locations
- Journal of Lipid Research (publishedVersion, cc-by)
- Europe PMC (PubMed Central) (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Peroxisome Proliferator-Activated Receptors
- Health Sciences › Medicine › Pharmacology › Inflammatory mediators and NSAID effects
- Health Sciences › Nursing › Nutrition and Dietetics › Fatty Acid Research and Health
- Keywords
- carvacrol, thyme essential oil, PPARα, PPARγ, cyclooxygenase-2, essential oils, anti-inflammatory activity, lipopolysaccharide, macrophages, endothelial cells, prostaglandin synthesis, nuclear receptors
- MeSH terms
- Cymenes, Anti-Inflammatory Agents, Non-Steroidal, Humans, Lipopolysaccharides, Gas Chromatography-Mass Spectrometry, Oils, Volatile, Plant Oils, Promoter Regions, Genetic, Monoterpenes, Cell Line, Tumor, Thymus Plant, PPAR alpha, PPAR gamma, Cyclooxygenase 2
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