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Effects of prodelphinidins isolated from Ribes nigrum on chondrocyte metabolism and COX activity
Nancy Garbacki1, Luc Angenot, Corinne Bassleer
1Laboratoire de Physiologie humaine, Institut Léon Frédéricq, Université de Liège, Belgium. N.Garbacki@ulg.ac.be
Abstract:
Articular diseases, such as osteoarthritis, is the clinical expression of the loss of cartilage function. COX inhibitors are widely used in the treatment of such pathologies for their beneficial effects on inflammation but often produce a negative activity on cartilage synthesis. In this study, we determined the effect of different prodelphinidins, the major compounds isolated from Ribes nigrum leaves, on the proteoglycans (PGs), type II collagen (coll. II) and prostaglandin E(2) (PGE(2)) production by differentiated human chondrocytes cultivated in long term (12 days) and in clusters as well as their inhibition potential on COX-1 and COX-2 in vitro. Gallocatechin trimer (GC-GC-GC) showed the higher stimulation of PGs and coll. II production (1 microg ml(-1)) and the synthesis of PGE(2) was significantly reduced by gallocatechin dimer (GC-GC), gallocatechin-epigallocatechin (GC-EGC) and GC-GC-GC at 10 and 100 microg ml(-1). The inhibition of PGE(2) synthesis was confirmed by the in vitro test on purified COX enzymes, showing the selectivity of prodelphinidins on COX-2. However, the prodelphinidins had no effects on COX activity in the whole blood assay. Our studies suggest that the prodelphinidins fractions from R. nigrum may be useful as an additive agent in the prevention of osteoarthritis.
Insights
Prodelphinidins from Ribes nigrum leaves show potential for osteoarthritis prevention by stimulating cartilage components and inhibiting prostaglandin E(2) synthesis. These compounds may offer a novel therapeutic approach for articular diseases.
Area of Science:
- Biochemistry
- Pharmacology
- Rheumatology
Background:
- Articular diseases like osteoarthritis involve cartilage dysfunction.
- Common treatments (COX inhibitors) reduce inflammation but can harm cartilage synthesis.
- Prodelphinidins from Ribes nigrum leaves are investigated for their chondroprotective effects.
Purpose of the Study:
- To evaluate the impact of prodelphinidins on proteoglycans (PGs), type II collagen (coll. II), and prostaglandin E(2) (PGE(2)) production in human chondrocytes.
- To assess the in vitro inhibition potential of prodelphinidins on cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) enzymes.
Main Methods:
- Differentiated human chondrocytes were cultured long-term (12 days) in clusters.
- Effects of prodelphinidins on PGs, coll. II, and PGE(2) production were measured.
- In vitro assays were performed using purified COX enzymes and a whole blood assay.
Main Results:
- Gallocatechin trimer (GC-GC-GC) significantly stimulated PGs and coll. II production.
- Gallocatechin dimer (GC-GC), GC-EGC, and GC-GC-GC reduced PGE(2) synthesis.
- Prodelphinidins selectively inhibited COX-2 in vitro but showed no effect in whole blood assays.
Conclusions:
- Prodelphinidins from Ribes nigrum leaves demonstrate chondroprotective and anti-inflammatory properties.
- These compounds may serve as beneficial additives for preventing osteoarthritis progression.
- Further research is warranted to explore their therapeutic potential in articular diseases.