Biochemical basis of the effect of chondroitin sulphate on osteoarthritis articular tissues

Abstract

Osteoarthritis is a chronic disease characterised by irreversible damage to joint structures, including loss of articular cartilage, osteophyte formation, alterations in the subchondral bone and synovial inflammation. Pain, functional disability and impairment of health-related quality of life are major complaints in patients with osteoarthritis. Several compounds have been investigated for their positive effects on the relief of clinical symptoms and improvement of structural changes in osteoarthritis. It has been shown that chondroitin sulphate interferes with the progression of structural changes in joint tissues and is used in the management of patients with osteoarthritis. This review summarises data from relevant reports describing the mechanisms of action of chondroitin sulphate involved in the beneficial effects of the drug.

Pharmacoproteomic Study of Three Different Chondroitin Sulfate Compounds on Intracellular and Extracellular Human Chondrocyte Proteomes

“…Use of CS for in Vitro Studies-Although the oral bioavailability of CS is acceptable (15-24%), ϳ90% is depolymerized or degraded either in plasma or the joints (7,30). Many in vitro studies have used high and variable concentrations of CS, ranging from 12.5 to 2000 g/ml but generally 200 g/ml or lower.…”

“…This is particularly evident because, in general, only CS has been investigated for effects in vitro, and virtually no information is available on the mixture of depolymerized or degradation products that are known to exist in inflamed joints (31). Nevertheless, these in vitro investigations (principally using chondrocytes or cartilage explants of bovine or human origin) have provided insight into the likely actions of CS (7,24,30,(32)(33)(34)(35)(36), including increased synthesis of proteoglycan, hyaluronic acid, and aggregan, blockade of proteoglycan degradation by interleukin-1 and other pro-inflammatory cytokines and metalloproteinases, prevention of oxyradical formation, modulation of chondrocyte signaling pathways, control of apoptosis, and stress-or aging-related changes in regeneration or repair (36). Thus, it can be summarized that CS has inhibitory effects on multiple cartilage catabolic reactions while also enhancing anabolic processes.…”

“…CS is a glycosaminoglycan and a major component of the extracellular matrix of many connective tissues, including cartilage. Although its mechanisms of action remain unclear, in vitro experiments suggest that CS stimulates the production of proteoglycans by chondrocytes (6,7) and synoviocytes (6) and inhibits the expression of IL-1-induced metalloproteinases and prostaglandin E2 (7)(8)(9), thus preventing cartilage damage. At the same time, CS has shown to have a positive effect on some of the OA-related pathological processes involving the synovial tissue and subchondral bone (7).…”

Chondroprotectors in the treatment of osteoarthoris

“…[35]. Подавляет преждевременную гибель (апоптоз) хондроцитов [36], а также подавляет биосинтез ИЛ 1β и дру-гих медиаторов воспаления [37][38][39]. Улучшает микроцир-куляцию в субхондральной кости и синовиальной ткани.…”

Chondroitin sulfate in the treatment of osteoarthritis: from in vitro studies to clinical recommendations

“…What is more, considering the slow acting effect of the drug in humans, the in vitro and in vivo systems were used for quite short durations. Different authors have suggested that the high concentration used in vitro was used to compensate these concerns [Tat et al 2010;Monfort et al 2008b]. Differences in the purity and properties of CS could be responsible for the disparity of the effects.…”