What is the Mechanism of action of Green Lipped Mussel Extract (GLME)?

The therapeutic effect results from the complementary effects of the unique combination of biologically active compounds found in the green-lipped mussel as follows:

Glycosaminoglycans (GAG) Synthesis

GLM Extract contains Glucosamine, Chondroitin sulphate, Hyaluronic acid and Dermantan Sulphate. GLM Extract is a natural source of glucosamine - not free glucosamine - a component of joint cartilage and of synovial fluid that has been shown to slow the structural damage within arthritic joints. Chondroitin sulphate makes up the basic ground substance of both, the bone and cartilage and may inhibit catabolic cytokine initiated degradation of the cartilage. Hyaluronic acid is a nonsulphated GAG found in the proteoglycans structure and it also contributes to the viscosity of the synovial fluid.

Inhibition of Cytokine Function

Cytokines are chemical messengers produced by cells in response to a variety of stimuli. Catabolic cytokines present in arthritic joints perform a number of detrimental functions, which result in an accelerated breakdown of cartilage and enhanced inflammation. The catabolic cytokines, Interleukin-1 (IL-1), Interleukin-2 (IL-2) and Tumor Necrosis Factor - alpha (TNF-) are the ones mainly associated with destructive function in the arthritic joint due to their influence on neutrophils infiltration, matrix metalloproteinase and proinflammatory prostaglandin production. Studies using arthritic rats have demonstrated the inhibitory effect of GLM Extract on neutrophils activity and pro-inflammatory prostaglandin synthesis along with the inhibition of catabolic cytokine activity at the cellular level.

Selective COX-2 Inhibition

GLM Extract is a selective inhibitor of cyclo-oxygenase type 2. Inhibiting the activity of cycloxygenase enzymes, which convert cell membrane phospholipids into pro-inflammatory prostaglandins, is an important anti-inflammatory mechanism. However, there are two isozyme of cycloxygenase, designated as COX-1 and COX-2. The COX-1 isozyme is a constitutional enzyme that has an important role in maintaining the health and integrity of the digestive system, kidney function and platelet aggregation whereas, COX-2 isozyme is induced in response to an inflammatory stimulus. The fact that GLM Extract is able to inhibit COX-2 selectivity without inhibiting COX-1 activity means that the product does not have any damaging effects on the stomach and does not adversely affect kidney function or platelet aggregation.

5-Lipoxygenase Inhibition

In addition to cyclo-oxygenase inhibitory activity, GLM Extract has been shown to inhibit 5-Lipoxygenase activity in stimulated human polymorphonuclear leukocytes in vitro. 5-Lipoxygenase activity is similar to cycloxygenase enzymic activity involving the conversion of endogenous arachidonic acid to proinflammatory and broncho-constrictive leukotrienes. These leukotrienes are adversely indicated in arthritic and asthmatic disorders and inhibition of their function is important for the control of these disorders.

Apoptosis Reduction

Apoptosis is a term used to describe programmed cell death. This is a normal physiological function but can become uncontrolled in some disease states. In arthritis, an elevated level of apoptosis can occur in the body′s white blood cells (T-lymphocytes). T-lymphocytes have been shown to be important mediators in the tissue destruction seen in rheumatoid arthritis. Animal studies have shown that GLM Extract inhibits the accumulation of T-lymphocytes at inflammatory sites. However, this is still to be proven in the case of human lymphocytes.

Inhibition of Histamine Production

Histamine production is normally associated with allergy reactions. However, it is also a component of the acute phase of inflammation and its control is therefore influential in the symptomatic relief of inflammatory disorders such as arthritis. Japanese researchers discovered that GLM Extract naturally contains an active anti-histamine component in the form of Phospholipid Lysolecithin. Although anti-histamine preparations are not a standard part of treatment of arthritic diseases, their complementary function in inhibiting the acute-mediator driven phase of inflammation is beneficial.

Micronutrients

GLM Extract is prepared from marine mussels, which have naturally assimilated micronutrients from their sea environment, in a manner, which retains all the components in a stable and functional state. Some minerals such as boron, manganese and copper have influence as anti-inflammatory agents either directly or synergistically with other mediators. Fat-soluble vitamins such as A, D, E and K are not in excess in GLM Extract and there is no danger of hypervitaminosis or biosynthesis of excess calcium.

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