Abstract
In this study, 34 Traditional Chinese Medicine (TCM) compounds were screened for potential anabolic and anti-inflammatory properties on human osteoarthritic (OA) chondrocytes. The anabolic effects were assessed by measuring the glycosaminoglycan (GAG) relative to the DNA content using a 3D pellet culture model. The most chondrogenic compounds were tested in an inflammatory model consisting of 3 days of treatment with cytokines (IL-1β/TNF-α) with or without supplementation of TCM compounds. The anti-inflammatory effects were assessed transcriptionally, biochemically and histologically. From the 34 compounds, Vanilic acid (VA), Epimedin A (Epi A) and C (Epi C), 2′′-O-rhamnosylicariside II (2-O-rhs II), Icariin, Psoralidin (PS), Protocatechuicaldehyde (PCA), 4-Hydroxybenzoic acid (4-HBA) and 5-Hydroxymethylfurfural (5-HMF) showed the most profound anabolic effects. After induction of inflammation, pro-inflammatory and catabolic genes were upregulated, and GAG/DNA was decreased. VA, Epi C, PS, PCA, 4-HBA and 5-HMF exhibited anti-catabolic and anti-inflammatory effects and prevented the up-regulation of pro-inflammatory markers including metalloproteinases and cyclooxygenase 2. After two weeks of treatment with TCM compounds, the GAG/DNA ratio was restored compared with the negative control group. Immunohistochemistry and Safranin-O staining confirmed superior amounts of cartilaginous matrix in treated pellets. In conclusion, VA, Epi C, PS, PCA, 4-HBA and 5-HMF showed promising anabolic and anti-inflammatory effects.
Highlights
Occurrence of age-related musculoskeletal disorders is increasing, with osteoarthritis (OA) being the most prevalent joint disorder
Cytotoxicity assay of monolayer cultures showed that after 48 h of treatment with Traditional Chinese Medicine (TCM) compounds (1 μM, 10 μM, 25 μM, 50 μM), more than 75% of the cells were viable in all treatment groups
It is necessary to inhibit pro-inflammatory cytokines that are excessively abundant in osteoarthritic joints [18]
Summary
Occurrence of age-related musculoskeletal disorders is increasing, with osteoarthritis (OA) being the most prevalent joint disorder. The avascular nature of cartilage, combined with low cell density and slow matrix turnover rate, results in a lack of effective methods to prevent or treat OA [7]. If conventional treatment such as physical therapy or weight reduction fails to alleviate symptoms, simple analgesics are initially recommended (e.g., acetaminophen). Non-steroidal anti-inflammatory drugs (NSAIDs), including specific or non-specific cyclooxygenase 2 (COX-2) inhibitors, are used frequently [10,11,12] These systemic treatments are often insufficient and bear the risks of gastrointestinal, renal or cardiovascular side effects [13,14,15].
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
