Table 2

Principal characteristics of the in vitro studies testing glucosamine

Model

Concentration

Results

Reference

Glucosamine sulfate

Human OA chondrocytes

5-500 μM

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

[12]

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

[17]

Human chondrocytes stimulated with IL-1β

10 mM

Influence of the proteomic profile

[20]

Human OA cartilage explants

5 mM

Inhibition of catabolic and anabolic gene expression

Superiority over glucosamine hydrochloride in the same conditions

[25]

Human OA osteoblasts

200 μg/ml

Inhibition of pro-resorptive agents

[24]

Glucosamine hydrochloride

Transfected cell lines

10 mM

Inhibition of ADAMTS-5 expression and activity

[13]

Human OA synovium explants

0.5-5 mM

Induction of HA production

No effect of N-acetylglucosamine

[22]

D(+)-Glucosamine

Rat chondrosarcoma cell line and

2-16 mM

Inhibition of aggrecanase-dependent cleavage

[11]

bovine cartilage explants

Rat chondrocytes stimulated with IL-1β g/L

1-4.5

Reversion of IL-1β deleterious effect on PG anabolism

[14]

Rat chondrocytes stimulated with IL-1β

4.5 g/L

Inhibition of NF-κB

[16]

Rat chondrocytes stimulated with IL-1β

20 mM

Inhibition of inflammatory cytokines, chemokines and growth factors

Inhibition of MMPs and aggrecanase-1

[15]

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

[21]

N-acetylglucosamine

Human chondrocytes stimulated with IL-1β

10 mM

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

[18]

Human chondrocytes

5-20 mM

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

Superiority over native glucosamine

[26]

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

[19]

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