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Eur J Pharmacol. 2015 Mar 5;750:141-50. doi: 10.1016/j.ejphar.2015.01.018. Epub 2015 Jan 23.

Evaluation of the anti-inflammatory, anti-catabolic and pro-anabolic effects of E-caryophyllene, myrcene and limonene in a cell model of osteoarthritis.

Author information

1
Centre for Neuroscience and Cell Biology, University of Coimbra, Coimbra, Portugal; Faculty of Pharmacy, University of Coimbra, Coimbra, Portugal. Electronic address: ana.t.rufino@gmail.com.
2
Centre for Neuroscience and Cell Biology, University of Coimbra, Coimbra, Portugal; Faculty of Pharmacy, University of Coimbra, Coimbra, Portugal. Electronic address: madalena_ribeiro8@hotmail.com.
3
Centre for Neuroscience and Cell Biology, University of Coimbra, Coimbra, Portugal; Faculty of Pharmacy, University of Coimbra, Coimbra, Portugal. Electronic address: catota_coura@hotmail.com.
4
Orthopedics Department and Bone Bank, University and Hospital Center of Coimbra, Coimbra, Portugal; Faculty of Medicine, University of Coimbra, Coimbra, Portugal. Electronic address: fernandojudas@gmail.com.
5
Centre for Neuroscience and Cell Biology, University of Coimbra, Coimbra, Portugal; Centro de Estudos Farmacêuticos, Faculty of Pharmacy, University of Coimbra, Coimbra, Portugal. Electronic address: ligia@ff.uc.pt.
6
Centre for Neuroscience and Cell Biology, University of Coimbra, Coimbra, Portugal; Centro de Estudos Farmacêuticos, Faculty of Pharmacy, University of Coimbra, Coimbra, Portugal. Electronic address: Cavaleir@ff.uc.pt.
7
Centre for Neuroscience and Cell Biology, University of Coimbra, Coimbra, Portugal; Faculty of Pharmacy, University of Coimbra, Coimbra, Portugal. Electronic address: afmendes@ff.uc.pt.

Abstract

Osteoarthritis is a progressive joint disease and a major cause of disability for which no curative therapies are yet available. To identify compounds with potential anti-osteoarthritic properties, in this study, we screened one sesquiterpene, E-caryophyllene, and two monoterpenes, myrcene and limonene, hydrocarbon compounds for anti-inflammatory, anti-catabolic and pro-anabolic activities in human chondrocytes. At non-cytotoxic concentrations, myrcene and limonene inhibited IL-1β-induced nitric oxide production (IC50=37.3μg/ml and 85.3µg/ml, respectively), but E-caryophyllene was inactive. Myrcene, and limonene to a lesser extent, also decreased IL-1β-induced NF-κB, JNK and p38 activation and the expression of inflammatory (iNOS) and catabolic (MMP-1 and MMP-13) genes, while increasing the expression of anti-catabolic genes (TIMP-1 and -3 by myrcene and TIMP-1 by limonene). Limonene increased ERK1/2 activation by 30%, while myrcene decreased it by 26%, relative to IL-1β-treated cells. None of the compounds tested was able to increase the expression of cartilage matrix-specific genes (collagen II and aggrecan), but both compounds prevented the increased expression of the non-cartilage specific, collagen I, induced by IL-1β. These data show that myrcene has significant anti-inflammatory and anti-catabolic effects in human chondrocytes and, thus, its ability to halt or, at least, slow down cartilage destruction and osteoarthritis progression warrants further investigation.

KEYWORDS:

Chronic inflammation; MAPK; NF-κB; Natural products; Osteoarthritis

PMID:
25622554
DOI:
10.1016/j.ejphar.2015.01.018
[Indexed for MEDLINE]

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