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Open AccessArticle

Anti-Inflammatory and Chondroprotective Effects of Vanillic Acid and Epimedin C in Human Osteoarthritic Chondrocytes

1
AO Research Institute Davos, 7270 Davos Platz, Switzerland
2
Department of Biomedical Engineering, University of Basel, 4123 Allschwil, Switzerland
3
Department of Biomedicine, University Hospital Basel, University of Basel, 4001 Basel, Switzerland
4
Translational Medicine R&D Center, Shenzhen Institutes of Advanced Technology, Chinese Academy of Sciences, Shenzhen 518057, China
5
Department of Orthopaedics & Traumatology, The Chinese University of Hong Kong, Hong Kong SAR, China
6
Department of Health Sciences and Technology, ETH Zürich, 8092 Zürich, Switzerland
*
Author to whom correspondence should be addressed.
Biomolecules 2020, 10(6), 932; https://doi.org/10.3390/biom10060932
Received: 13 May 2020 / Revised: 15 June 2020 / Accepted: 17 June 2020 / Published: 19 June 2020
(This article belongs to the Section Natural and Bio-inspired Molecules)
In osteoarthritis (OA), inhibition of excessively expressed pro-inflammatory cytokines in the OA joint and increasing the anabolism for cartilage regeneration are necessary. In this ex-vivo study, we used an inflammatory model of human OA chondrocytes microtissues, consisting of treatment with cytokines (interleukin 1β (IL-1β)/tumor necrosis factor α (TNF-α)) with or without supplementation of six herbal compounds with previously identified chondroprotective effect. The compounds were assessed for their capacity to modulate the key catabolic and anabolic factors using several molecular analyses. We selectively investigated the mechanism of action of the two most potent compounds Vanillic acid (VA) and Epimedin C (Epi C). After identification of the anti-inflammatory and anabolic properties of VA and Epi C, the Ingenuity Pathway Analysis showed that in both treatment groups, osteoarthritic signaling pathways were inhibited. In the treatment group with VA, nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) signaling was inhibited by attenuation of the nuclear factor of kappa light polypeptide gene enhancer in B-cells inhibitor alpha (IκBα) phosphorylation. Epi C showed a significant anabolic effect by increasing the expression of collagenous and non-collagenous matrix proteins. In conclusion, VA, through inhibition of phosphorylation in NF-κB signaling pathway and Epi C, by increasing the expression of extracellular matrix components, showed significant anti-inflammatory and anabolic properties and might be potentially used in combination to treat or prevent joint OA. View Full-Text
Keywords: osteoarthritis; vanillic acid; Epimedin C; anti-inflammatory effects; NF-κB signaling pathway; anabolic; anti-catabolic osteoarthritis; vanillic acid; Epimedin C; anti-inflammatory effects; NF-κB signaling pathway; anabolic; anti-catabolic
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Ziadlou, R.; Barbero, A.; Martin, I.; Wang, X.; Qin, L.; Alini, M.; Grad, S. Anti-Inflammatory and Chondroprotective Effects of Vanillic Acid and Epimedin C in Human Osteoarthritic Chondrocytes. Biomolecules 2020, 10, 932.

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