Evergreen - Glucosamine

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Glucosamine: ingredient of Evergreen

Osteoarthritis (OA) is the most common form of joint disor-
der afflicting the world’s population, changing significantly the quality of life. It has been noted recently, an increase of attention to the use of chondroprotective methods for the treatment of OA. To better understand the function of these substances, it’s necessary to know the structure of cartilage.

The cartilage: particular form of a ligament in good health

In a normal condition of healthy, the articulation of the bones are covered by cartilage and surrounded by synovial fluid. In a healthy joint, the cartilage is smooth and the synovial fluid provides a proper lubrication.
Normally the cartilage is composed of 2% of cells, called chondrocytes, 20 - 40% from the extracellular matrix and from 60 - 80% of water. The chondrocytes form and retain the matrix which, in turn, plays a habitat conducive to the development of these cells.

The extracellular matrix is composed to 60% of collagen (predominantly type II collagen) and from 40% of proteoglycans which in turn are composed of glycosaminoglycans (or mucopolysaccharides) linked to a protein chain. The most significant glycosaminoglycans are chondroitin-6 sulfate, chondroitin sulfate-4, Keratan Sulfate and Dermatan Sulfate. In the matrix the proteoglycans are connected to molecules of hyaluronic acid so as to make particular aggregates in the form of feather. These aggregates are very hydrophilic, this illustrates the considerable volume of water present in the matrix. The proteoglycans are connected in parallel to the collagen fibrils, with the task to circumscribe the water in excess that can totally alter the physical characteristics of the cartilage.

Structure of cartilage

Like all other connective tissues of the human body, also the articular cartilage is a living substance that is dynamic and continually worn and replaced.
In healthy individuals, applies a proportion between the breakup of the old fabric (through the synthesis of organic substances by the chondrocytes) and the recomposition of a new one.

Glucosamine: ingredient of Evergreen

Structure of cartilage (continued ...)

The Osteoarthritis, on the contrary, develops if the cartilage is damaged more quickly compared to the period used by the body to avvicendarla. At this juncture, there is a lower production of glycosaminoglycans, which determines a reduction of the bonds between collagen and proteoglycans. The consequence is a greater demand for water within the matrix, which results in a lower resistance of cartilage, limiting its regular job and support. This course develops inevitably snervando the joint damage and ensuring that, over the years, could become incurable.

Only the 2-3% of cases osteoarthritis arise from accidents or injuries to joints, by innate disability or additional diseases under these circumstances is called secondary osteoarthritis. The percentage more remarkable is delineated by primary osteoarthritis (localized or diffuse), arising apparently without compelling reasons but only with the advance of years. The primary ostoartriti are found most likely over 50 years. Some studies report that after 65 years, 75% of peo-
ple are afflicted with osteoarthritis more or less important.

Treatment of Osteoarthritis

The two possibilities that for specialists should have a method of treatment to cure osteoarthritis are:

  • Reduce the symptoms of the disorder
  • Prevent disease progression

With the traditional treatment methods we are accustomed to act through surgery, the change of habits of life of patients or medication.
The surgery is certainly very useful but it is recommended only in the most dire of circumstances.
The effort to change certain attitudes in the wrong way of life is quite difficult. It is well known that a drop in body weight,a healthier nutrition and light and a physical activity targeted are reasons which would produce benefits but are often painfully feasible in daily life.
The use of treatment with non-steroidal and anti-inflammatory drugs (aspirin, ibuprofen, etc.) And corticosteroids, has a timely result on inflammatory states that are the result of chance of pain but most often are the cause of concomitant effects not marginal as the ’onset of necrosis renal, gastric ulcers, decreased immune activity and also does not stop the osteoarthritis and not have regenerative effects or regenerating.

Glucosamine: ingredient of Evergreen

Chondoprotective Agents: chondrocytes

In recent times, scientific research has focused its attention on the examination of active ingredients that restrict the development of the osteoarthritis and stimulate repair of damaged cartilage: these substances are chondroprotective agents. The distinctive elements that should possess are:

  • Encouraging the chondrocytes to produce collagen and proteoglycans
  • Prevent cartilage degradation (for example by inhibition of protein compounds)

The compounds that have shown to be equipped with such qualities are those existing in nature in cartilage, among which the most significant ones are the hyaluronic acid, the glucosamine and the chondroitin sulphate.

Chondoprotective agents: Hyaluronic Acid

It is produced by chains of glucuronic acid and N-acetylglucosamine. It has the function of lubricator in the synovial fluid. When used orally, the absorption level enteric is limited: for this reason is often used in the case of intra-articular injections.

Chondoprotective Agents: Glucosamine

It is an amino-mono-saccharide that chondrocytes synthesize from glucose and who plays the role of precursor for the glycosa-
minoglycans. In situations of osteoarthritis, an additi-
onal contribution of gluco-
samine gives to the chondrocytes much raw material, will balance the gap between cartilage degradation and restructuring, promoting faster recovery.

Some research has provided tests of a certain result anti-inflammatory presumably due to an arrest of free radicals. Consequently to assimilation orally, the entity of glucosami-
ne available to the body is equal to approximately 45% of the ingested: the expulsion occurs mainly in the urine. It has been documented that the intake of salts of glucosamine (glucosamine hydrochloride and glucosamine sulfate) may provide beneficial results for the treatment of osteoarthritis. In addition, there isn’t evidence of any harm, nor collateral consequences.


Glucosamine: ingredient of Evergreen

Chondoprotective Agents: Chondroitin Sulphate

As already indicated, is the glycosaminoglycan that is active in a quantity more relevant to the interior of the cartilages. It is a polymer of glucuronic acid and N-acetylgalactosamine sulfate which can is reveal in multiple tissues, among which there are the tendons, intervertebral discs, the bones, the cornea and the heart valves.

Its major job in relation with the cartilage is to give shape to the links with the collagen fibrils. It was also substantiated an inhibitor result in respect of enzymes (collagenase and elastase) active in the synovial fluid and that has caused regression of the cartilage.
Over the years the production of chondroitin sulfate by chondrocytes decreases, with the consequence of having a cartilage increasingly weakened.

Assume chondroitin sulfate in the case of osteoarthritis can facilitate the increase of the glycosaminoglycans concentration in cartilage and limiting its excessive degradation.
The dose absorbed following oral intake was quantified to be approximately 20% of the total. Even in this circumstance, was not seen no harm or harmful side outcomes.

Many studies recently disclosed have reported that after oral administration of this drug, patients have noticed a decrease in pain (mild anti-inflammatory activity), with a consequent decrease in ’use of anti-inflammatory drugs or other analgesics.

Synergistic effect

Both the glucosamine that the chondroitin sulphate, evaluated separately, do not enjoy all three peculiarities of a condoprotettore, while this is found if their effects are additi-
ve. In summary:

  • Glucosamine: stimulates the metabolism of chondrocytes and proteoglycans
  • Chondroitin sulfate: it inhibits enzymes that break down cartilage

Since the Glucosamine promotes the formation of new cartilage and the chondroitin sulfate slows the degradation, the result that follows after a combined administration for periods during the gradual disability, will be the limitation of the osteoarthritis development.


Glucosamine: ingredient of Evergreen

Synergic function of Glucosamine and Chondroi-
tin Sulfate

Do not underestimate that we can find a synergy between the two active ingredients, going to strengthen individual performance. In the United States are implementing clinical trials coordinated by the NIH (National Institute of Health), which is expected to last three years and will involve more than 3000 individuals with the task of comparing the results of this combination of substances with that of other anti-inflammatory drugs.

Results

In recent times, it has received significant interest from researchers in respect of chondroprotective agents (chondroitin sulfate, hyaluronic acid, glucosamine) as active ingredients for the treatment of osteoarthritis. Although additional studies are needed definitive, it is already clear that the intra-articular hyaluronic acid is very useful for the lubrication of the joints, while also reducing inflammation and swelling.

A particular interest has been directed to the use of glucosamine and chondroitin sulphate which, introduced in dietary formulations who are assimilated orally, appear to play a synergistic role in order to limit the development of osteoarthritis. The ease of use and the total absence of contraindications can promote a new approach for the treatment of osteoarthritis disease the whose path was considered almost uncontrollable until a few years ago.

The glucosamine is a substance that the human body has the ability to synthesize. It participates in the production of glycosaminoglycans, which are essential for the health of the cartilage. In the same way as other useful parts, with the attrition, the amount of glucosamine generated by the body is reduced and the cartilages of course deteriorate. A research (such as the one that appeared in the scientific journal “Lancet”), has documented that supplementation with glucosamine may stop the osteoarthritis in 85% of cases. No negative consequence worthy of note was recorded while taking glucosamine orally.

Further analysis revealed that the positive effect of glucosamine is enhanced if it is associated to the chondroitin, a substance that attracts and holds water that is useful to sustain and lubricate the joints.
For preventive use, the recommended dosage (for people between 54 and 90 kg body weight) is 750 mg. per day of glucosamine and 600 mg. chondroitin, usually divided into three doses. Under conditions of arthritis already at an advanced stage, such doses may be duplicates.

The drugs usually recommended are anti-inflammatory drugs (NSAIDs), which can certainly control the painful symptoms but are by now well known gastrointestinal side effects, associated with prolonged intake. The studies and researches are never interrupted and have followed various curative methods comprising, for example, the opportunity to intervene on the origin of the problem of the joint disorder. This could be the case of glucosamine sulfate.

Glucosamine: ingredient of Evergreen

Results (continued ...)

Some time ago, this substance had provoked attention and enthusiasm for successes achieved because not only has improved the symptoms but also limited the pathological aggravation. It is a molecule usually generated by the human body and is derived from glucosamine, a glucide monoaminosaccharide that participates in the composition of the extracellular matrix of cartilage.

It was found that glucosamine, given externally at pharmacological doses acting on osteoarthritis of the knee presumably for the interdiction of a nuclear element and therefore particle chromosomal governing mediators causing the synovial inflammation and the cartilage destruction.

The research has proving that with the intake of glucosamine for a long period (three years) could limit the development of osteoarthritis and this was demonstrated by the conservative factor of the spaces between the joints detected with an X-ray. It also obtained an advancement of the clinical picture that was transformed and also in a better control of symptoms.

The results in the short term

The researchers from Spain and Portugal in particular have insisted later on the form analgesic and anti-inflammatory but limited in time. These scholars have tried to understand how to use the glucosamine to heal the patient’s symptoms and stop feeling pain and consequently of being able to move.
To assess the favorable change was chosen Lequesne index, a test that ascertains the degree of pain and disorder and the possibility of ambulation and activities in daily behaviors. About 300 patients were distributed doses of glucosamine sulphate (1500 mg. Per day), paracetamol (1000 mg. Three times per day) or a drug inert according to a model randomized and double blind.
The preference of paracetamol as an analgesic for comparison is not occasional, as it is the Eular, the European League against Rheumatism (European league against rheumatism) that specifies how primary pharmacological intervention in opposition to pain.Were any terms of comparison and complementary effectiveness, including the effectiveness on patients who responded well to treatment (responders).

The dosage is fundamental

A first finding was made after six months of treatment with obvious comparisons of appreciation of the two active ingredients. In comparison against placebo have achieved good effects but those obtained with glucosamine was more advantageous than those than those achieved by paracetamol, with the benefit of not have harmful side outcomes. Paracetamol has virtually no gastrointestinal effects but the long-term work on the biochemistry of the liver can increasing the transaminases

The framers of the analysis defined “Guides” (Glucosamine Unum In Die Efficacy) and previewed at a meeting in Milan have highlighted the importance of dose and of the form (phosphate) in which the active ingredient is given. Glucosamine, in fact, being a natural substance, is proposed in the United States as a dietary supplement without the limits of dosage, while in Europe, while being of free sale, is allowed a limited dose (one sixth of the drug), significantly different from the one announced by the treaty referred to as therapeutic method.