Experimental Pharmacology of Glucosamine Sulfate

Chiusaroli, Riccardo; Piepoli, Tiziana; Zanelli, Tiziano; Ballanti, P.; Lanza, Marika; Rovati, Lucio C.; Caselli, Gianfranco

doi:10.1155/2011/939265

Cited by 43 publications

(47 citation statements)

References 29 publications

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“…Minimal effective concentrations of glucosamine ranged between 1 µM and 10 µM for inflammatory factors and cytokines such as COX-2, inducible nitric oxide synthase (iNOS), tumor necrosis factor-alpha, IL-6 or IL-1 itself, and between 0.1 µM and 1 µM for matrix degradation factors, such as stromelysin-1 and A Disintegrin And Metalloproteinase with Thrombospondin motif (ADAM-TS5) (aggrecanase 2). Interestingly, the gene expression of NF-kB subunits and JunB was inhibited at even lower concentrations, between 1 nM and 0.1 µM [Chiusaroli et al 2011]. Therefore, while glucosamine modulation of OA-relevant gene expression triggered by IL-1 is probably initiated by a decrease in NF-kB nuclear translocation [Letari et al 2003], the effect on transcription might be sustained afterwards by the inhibition of NF-kB subunit expression [Chiusaroli et al 2011].…”

Section: 21)mentioning

confidence: 99%

Crystalline glucosamine sulfate in the management of knee osteoarthritis: efficacy, safety, and pharmacokinetic properties

Rovati¹,

Girolami²,

Persiani³

2012

Therapeutic Advances in Musculoskeletal

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Abstract:Glucosamine is an amino monosaccharide and a natural constituent of glycosaminoglycans in articular cartilage. When administered exogenously, it is used for the treatment of osteoarthritis as a prescription drug or a dietary supplement. The latter use is mainly supported by its perception as a cartilage building block, but it actually exerts specific pharmacologic effects, mainly decreasing interleukin 1-induced gene expression by inhibiting the cytokine intracellular signaling cascade in general and nuclear factor-kappa B (NF-kB) activation in particular. As a whole, the use of glucosamine in the management of osteoarthritis is supported by the clinical trials performed with the original prescription product, that is, crystalline glucosamine sulfate. This is the stabilized form of glucosamine sulfate, while other formulations or different glucosamine salts (e.g. hydrochloride) have never been shown to be effective. In particular, long-term pivotal trials of crystalline glucosamine sulfate 1500 mg once daily have shown significant and clinically relevant improvement of pain and function limitation (symptom-modifying effect) in knee osteoarthritis. Continuous administration for up to 3 years resulted in significant reduction in the progression of joint structure changes compared with placebo as assessed by measuring radiologic joint space narrowing (structure-modifying effect). The two effects combined may suggest a disease-modifying effect that was postulated based on an observed decrease in the risk of undergoing total joint replacement in the follow up of patients receiving the product for at least 12 months in the pivotal trials. The safety of the drug was good in clinical trials and in the postmarketing surveillance. Crystalline glucosamine sulfate 1500 mg once daily is therefore recommended in the majority of clinical practice guidelines and was found to be cost effective in pharmacoeconomic analyses. Compared with other glucosamine formulations, salts, or dosage forms, the prescription product achieves higher plasma and synovial fluid concentrations that are above the threshold for a pharmacologically relevant effect, and may therefore justify its distinct therapeutic characteristics.

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Section: 21)mentioning

confidence: 99%

Crystalline glucosamine sulfate in the management of knee osteoarthritis: efficacy, safety, and pharmacokinetic properties

Rovati¹,

Girolami²,

Persiani³

2012

Therapeutic Advances in Musculoskeletal

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“…This was probably because two different meta-analyses3 11 had already produced identical and favourable results of such studies, mirroring the conclusions from the Cochrane Review 2. It was felt perhaps inappropriate then, to pool the outcomes of such trials with those of ineffective products that have not been characterised in the same way in terms of quality,4 pharmacokinetics12 and correspondence of human biological fluid levels with mechanistic data,13 irrespective of any possible secondary subgroup analysis. Thus, while data sharing from clinical trials should be encouraged, sponsor should also be reassured about the use of such data, especially when completely different products are considered in meta-analyses.…”

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confidence: 99%

Different glucosamine sulfate products generate different outcomes on osteoarthritis symptoms

2017

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“…For example, Imagawa et al found that O-GlcNAc could prevent cytokine-induced demethylation of a specific CpG site in the IL-1β promoter and this was associated with decreased expression of IL-1β [58]. Other investigators have generated in vitro evidence that GlcN.S attenuates NF-κB activation at concentrations comparable to those seen in patients following oral supplemental ingestion [59]. …”

Section: Discussionmentioning

confidence: 99%

Physiological effects of oral glucosamine on joint health: current status and consensus on future research priorities

et al. 2013

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The aim of this paper was to provide an overview of the current knowledge and understanding of the potential beneficial physiological effects of glucosamine (GlcN) on joint health. The objective was to reach a consensus on four critical questions and to provide recommendations for future research priorities. To this end, nine scientists from Europe and the United States were selected according to their expertise in this particular field and were invited to participate in the Hohenheim conference held in August 2011. Each expert was asked to address a question that had previously been posed by the chairman of the conference. Based on a systematic review of the literature and the collection of recent data, the experts documented the effects of GlcN on cartilage ageing, metabolic/kinetic and maintenance of joint health as well as reduction of risk of OA development. After extensive debate and discussion the expert panel addressed each question and a general consensus statement was developed, agreeing on the current state-of-the-art and future areas for basic and clinical studies. This paper summarizes the available evidence for beneficial effects of GlcN on joint health and proposes new insight into the design of future clinical trials aimed at identifying beneficial physiological effect of GlcN on joint tissues.

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Experimental Pharmacology of Glucosamine Sulfate

Cited by 43 publications

References 29 publications

Crystalline glucosamine sulfate in the management of knee osteoarthritis: efficacy, safety, and pharmacokinetic properties

Crystalline glucosamine sulfate in the management of knee osteoarthritis: efficacy, safety, and pharmacokinetic properties

Different glucosamine sulfate products generate different outcomes on osteoarthritis symptoms

Physiological effects of oral glucosamine on joint health: current status and consensus on future research priorities

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