Table 2

Principal characteristics of the in vitro studies testing glucosamine





Glucosamine sulfate

Human OA chondrocytes

5-500 μM

Inhibition of PLA2 and collagenase in a lesser extent through PKC inhibition


Human OA chondrocytes stimulated with IL-1β

10-1,000 mg/L

Inhibition of NF-κB activation

Inhibition of COX-2 expression and synthesis and PGE2 release


Human chondrocytes stimulated with IL-1β

10 mM

Influence of the proteomic profile


Human OA cartilage explants

5 mM

Inhibition of catabolic and anabolic gene expression

Superiority over glucosamine hydrochloride in the same conditions


Human OA osteoblasts

200 μg/ml

Inhibition of pro-resorptive agents


Glucosamine hydrochloride

Transfected cell lines

10 mM

Inhibition of ADAMTS-5 expression and activity


Human OA synovium explants

0.5-5 mM

Induction of HA production

No effect of N-acetylglucosamine



Rat chondrosarcoma cell line and

2-16 mM

Inhibition of aggrecanase-dependent cleavage


bovine cartilage explants

Rat chondrocytes stimulated with IL-1β g/L


Reversion of IL-1β deleterious effect on PG anabolism


Rat chondrocytes stimulated with IL-1β

4.5 g/L

Inhibition of NF-κB


Rat chondrocytes stimulated with IL-1β

20 mM

Inhibition of inflammatory cytokines, chemokines and growth factors

Inhibition of MMPs and aggrecanase-1


Human synovial cells and chondrocytes

0.1-1.0 mM

Stimulation of HA and GAG production

Stimulation of HA synthase activity

No effect of N-acetylglucosamine



Human chondrocytes stimulated with IL-1β

10 mM

Inhibition of iNOS, COX-2 and IL-6 expression


Human chondrocytes

5-20 mM

Increased synthesis of GAG and HA due to acceleration of facilitated glucose uptake

Superiority over native glucosamine


Human chondrocytes (normal and OA) stimulated with IL-1β

2 mM

Prevention of the cytokine-induced demethylation of CpG site in the IL-1β promoter resulting in decreased expression of IL-1β


ADAMTS-5, a disintegrin and metalloproteinase with thrombospondin motifs 5; COX-2, cyclooxygenase-2; GAG, glycosaminoglycan; HA, hyaluronic acid; iNOS, inducible nitric oxide synthase; MMP, matrix metalloproteinase; OA, osteoarthritis; PG, proteoglycan; PKC, protein kinase C; PGE2, prostaglandin E2; PLA2, phospholipase A2.

Henrotin et al. Arthritis Research & Therapy 2012 14:201   doi:10.1186/ar3657