Anti-inflammatory and pro-anabolic effects of 5-aminosalicylic acid on human inflammatory osteoarthritis models
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Published on: May 20, 2020
Kaihu Li1,2, Yong Zhu1, Penghui Zhang2,3
1Department of Orthopaedics, Xiangya Hospital of Central South University, Changsha, China.
Background:
Osteoarthritis (OA) is the most common degenerative joint disease, mainly affecting the elderly worldwide, for which the drug treatment remains a major challenge. Low-grade inflammation plays a pivotal role in OA onset and progression. Exploration of notable anti-inflammatory and disease-modifying drugs on human samples could facilitate the evaluation of therapeutic strategies for OA.
Methods:
The anti-inflammatory drug 5-aminosalicylic acid (5-ASA) is a first-line drug for ulcerative colitis (UC), however no study has explored the effects of 5-ASA on articular chondrocytes. In this work, both in vitro (chondrocyte pellets) and ex vivo (osteochondral explants) human inflammatory OA models were applied to evaluate the effects of 5-ASA.
Results:
In the inflammatory pellet model, 5-ASA remarkably downregulated the gene expression of interleukin-6 (IL-6), and cyclooxygenase-2 (COX-2) while upregulating proteoglycan 4 (PRG4) and cartilage oligomeric matrix protein (COMP) gene expression. Total glycosaminoglycan (GAG) synthesis by pellets was markedly increased in 5-ASA-treated groups compared with the inflammatory group. In conditioned medium, inflammatory mediators (IL-8, nitric oxide) were markedly inhibited upon 5-ASA treatment. Moreover, histological staining showed 5-ASA retained proteoglycan content and inhibited degradation of extracellular matrix (ECM) core components, aggrecan (ACAN) and collagen type II (COL2). In the inflammatory explant model, 5-ASA mitigated signs of OA development by reducing inflammatory mediators and GAG loss.
Conclusions:
These findings suggest that 5-ASA has anti-inflammatory and pro-anabolic effects on human chondrocyte pellet and osteochondral explant inflammatory OA models.
The Translational Potential Of This Article:
Disease-modifying OA drugs are an unmet clinical need for the treatment of OA. Our study explored and demonstrated the anti-inflammatory and protective effects of 5-ASA on in vitro and ex vivo human inflammatory OA models, showing its translational potential for OA treatment.
Insights
5-aminosalicylic acid (5-ASA) demonstrates anti-inflammatory and cartilage-protective effects in human osteoarthritis models. This suggests its potential as a disease-modifying osteoarthritis drug (DMOAD) for treating this common degenerative joint disease.
Area of Science:
- Biomedical research
- Drug discovery
- Osteoarthritis research
Background:
- Osteoarthritis (OA) is a prevalent degenerative joint disease with limited drug treatment options.
- Low-grade inflammation is a key factor in OA initiation and progression.
- Developing disease-modifying drugs for OA requires evaluation on human samples.
Purpose of the Study:
- To investigate the effects of 5-aminosalicylic acid (5-ASA) on human articular chondrocytes.
- To evaluate 5-ASA's therapeutic potential for osteoarthritis (OA).
Main Methods:
- Utilized in vitro (chondrocyte pellets) and ex vivo (osteochondral explants) human inflammatory OA models.
- Assessed gene expression (IL-6, COX-2, PRG4, COMP, ACAN, COL2) and matrix synthesis (GAG).
- Measured inflammatory mediators in conditioned medium and explant cultures.
Main Results:
- 5-ASA reduced pro-inflammatory gene expression (IL-6, COX-2) and increased cartilage matrix gene expression (PRG4, COMP).
- 5-ASA enhanced glycosaminoglycan (GAG) synthesis and preserved proteoglycan content.
- 5-ASA inhibited inflammatory mediators (IL-8, nitric oxide) and mitigated GAG loss in explant models.
Conclusions:
- 5-ASA exhibits significant anti-inflammatory and pro-anabolic effects in human OA models.
- These findings highlight 5-ASA's potential as a disease-modifying osteoarthritis drug (DMOAD).
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