Glucosamine Sulfate: Functions

The following physiological processes are influenced by glucosamine sulfateStimulation of anabolic, cartilage-protective effects (= chondroprotectants/cartilage-protective substances):

  • Main substrate for collagen synthesis and for the formation of glycosaminoglycans and proteoglycans, respectively, in the extracellular matrix (extracellular matrix, intercellular substance, ECM, ECM) of cartilage tissue.
  • Increase the incorporation of proline and sulfate in the cartilage matrix.
  • Increase proteoglycan synthesis in human chondrocytes – cells of cartilage tissue.
  • Increase in adhesion (attachment) of chondrocytes to fibronectin, a glycoprotein involved in many different physiological processes, such as tissue repair.
  • Stimulation of synoviocytes (cells of the synovial fluid) and thus increase the synovial viscosity (flow properties of the synovial fluid).

Inhibition of catabolic processes:

  • Inhibition of proteolytic – protein degrading – enzymes, for example, stromelysin – an endopeptidase that dissolves peptide bonds within a molecule, such as from proteoglycan, fibronectin and some types of collagen.
  • Inhibition of collagenase and phospholipase A2 activity, preventing cartilage degradation.
  • Inhibition of the production of cytokines-cells that influence inflammation-in particular, interleukin-1 and tumor necrosis factor (TNF)-alpha-induced nitride oxide (NO) release in cultures of human chondrocytes
  • Inhibition of peroxide formation and activity of lysosomal enzymes that cleave macromolecules, such as proteins, polysaccharides, lipids and nucleic acids.

Anti-inflammatory processes:

  • Inhibition of proinflammatory (pro-inflammatory) mediators without affecting prostaglandin synthesis.

Glucosamine sulfate and osteoarthritis

Glucosamine sulfate, like chondroitin sulfate, is classified as a chondroprotectant, which is used in degenerative joint disease. They also belong to the SYSADOA (English Symptomatic Slow Acting Drugs in Osteoarthritis) class and are characterized by a lack of direct analgesic effect (pain-relieving effect). In more than 30 clinical studies – controlled, double-blind, randomized – with approximately 8,000 patients with gonarthrosis (osteoarthritis of the knee joint), the clinical relevance of glucosamine sulfate could be confirmed. According to the latest findings, glucosamine sulfate has, on the one hand, decongestant and analgesic properties for joint problems. On the other hand, this substance can restore already damaged cartilage and tendon tissue and thus lead to an improvement in the function of the affected joints. According to the GAIT study, joint pain in gonarthrosis patients was reduced by 65.7% after 24 weeks of glucosamine (1,500 mg/day). In a long-term clinical study over 3 years, glucosamine sulfate was also found to reduce the symptoms of gonarthrosis – stiffness, pain, loss of function – and prevent structural changes in the knee joint, slowing the progression of gonarthrosis. Regarding the joint space situation, no joint space narrowing could be measured in the glucosamine sulfate supplemented group. Glucosamine sulfate finally qualifies as a disease modifying substance and belongs to the group of DMOAD – disease modifying osteoarthritis drugs. A recent placebo and NSAID-controlled study with 329 gonarthrosis patients over 3 months of treatment and 2 additional months of follow-up also showed a longer-lasting efficacy or pain relief and very good tolerability of glucosamine sulfate compared to common analgesics (non-steroidal anti-inflammatory drugs (NSAID), NSAID). After cessation of therapy, the symptom-modifying efficacy of glucosamine sulfate persists for at least 2 months. In contrast, the benefit of NSAIDs diminishes rapidly after treatment is discontinued. A side effect of glucosamine use is a slightly reduced risk of disease and death from a cardiovascular event:

  • The hazard ratio for a cardiovascular event was 0.85 (95% confidence interval 0.80 to 0.90)
  • Cardiovascular death was 12% less likely to occur among glucosamine users (hazard ratio 0.78; 0.70 to 0.87)
  • Coronary heart disease occurred 18% (hazard ratio 0.82; 0.76 to 0.88) and stroke 9% (hazard ratio 0.91; 0.83 to 1.00) less frequently.