What Are the Benefits of Chondroitin?

Chondroitin generally refers to chondroitin sulfate, alias Kantling, a white or light yellow amorphous powder chemical. The molecular formula is C ₁₃ H ₂₁ NO ₁₆ S and the molecular weight is 479.36800.

Chinese name: Chondroitin sulfate
Foreign name: Chondroitin Sulfate

CAS number: 9007-28-7
Molecular formula: C13H21NO16S
Molecular weight: 479.36800

Chondroitin compounds

Chondroitin Basic Information

Chinese name: chondroitin sulfate

Chinese alias: shark chondroitin; sulfate sulfate;

English name: (5) -2- (Carboxyamino) -2-deoxy-3-O--D-glucopyranuronosyl-4-O-sulf o--L-arabino-hexopyranose

English alias: chondroitin-4-sulfate; Cholyltaurine; 2-[(R) -4-((3R, 5S, 7R, 8R, 9S, 10S, 12S, 13R, 14S, 17R) -3,7,12-trihydroxy -10,13-dimethyl-hexadecahydrocyclopenta [a] phenanthren-17-yl) pentanoylamino] ethanesulfonic acid; [14C] -Taurocholic acid; chonodroitinsufuric acid;

CAS number: 9007-28-7

Molecular formula: C ₁₃ H ₂₁ NO ₁₆ S

Chemical structure:

Molecular weight: 479.36800

Exact mass: 479.05800

PSA: 287.45000 ^[1]

Chondroitin physical and chemical properties

Appearance and properties: white or light yellow amorphous powder

Storage conditions: Store at RT. ^[1]

Chondroitin uses

It is mainly used in arthritis, eye drops, etc. It has analgesic effect and promotes cartilage regeneration. It has certain effects on improving elderly degenerative arthritis and rheumatoid arthritis and can improve joint problems ^[1] .

Basic overview of chondroitin drugs

[Source] It is an acidic mucopolysaccharide extracted and extracted from cartilage tissues such as laryngeal bone, nasal bone and trachea of pigs. This product contains aminohexose based on glucosamine (C ₆ H13O ₅ N), which shall not be less than 24.0% of the indicated amount of chondroitin sulfate ^[2] .

[Character] This product is white or off-white powder; odorless; hygroscopic. The aqueous solution of this product is viscous and does not condense when heated. This product is soluble in water and insoluble in ethanol, acetone or glacial acetic acid. ^[3]

[Consumption and Consumption] China is the world's largest producer and exporter of chondroitin sulfate, and more than 4/5 of the world's output is provided by China ^[4] . Shandong and Hebei are the largest distribution centers in China. Well-known companies include Jiaxing Hengjie Biological, Hebei Sanxin Group, Yantai Dongcheng Biochemical, Qingdao Green Extract Bio, Qingdao Jiulong Biological, Sinochem (Qingdao) Industry and other companies.

Chondroitin mechanism of action

1. Provide cushioning effect, alleviate impact and friction during action

The role of chondroitin is like a "liquid magnet", which can absorb water into the proteoglycan molecules, make the cartilage thick and sponge-like, and increase the amount of synovial fluid in the joints. In this way, it can provide a "padding" effect to enhance the joint's shock absorption ability and ease the impact and friction when walking or jumping.

2. Deliver important oxygen and nutrients to the joints to help remove waste from the joints

One of the important functions of chondroitin is to serve as a pipeline to transport important oxygen supplies and nutrients to cartilage, while eliminating carbon dioxide and waste. Since articular cartilage has no blood supply, all the oxygenation, nourishing and lubricating effects come from synovial fluid. The loss of chondroitin due to aging, injury or disease will cause the loss of synovial fluid, resulting in cartilage malnutrition, dryness, thinning and fragility. In addition, if cartilage lacks proper nutrition, cartilage damage due to injury or daily wear will be more difficult to regenerate or heal.

Chondroitin is also very important when taking glucosamine, because chondroitin can promote the process of glucosamine penetration into the joints. Numerous studies have shown that, including one published in the New England Journal of Medicine, that combined intake of glucosamine and chondroitin can more effectively protect, reverse damage and promote repair of articular cartilage.

3. Other effects of chondroitin:

Inhibits cartilage-damaging enzymes (such as collagenase, elastase, and cathepsin) to prevent cartilage from being broken down or dissolved.

Can start at the root of the problem and inhibit the activity of COX-2 to stop joint inflammation.

Chondroitin clinical study

[Indications] Hypolipidemic drugs. It is mainly used to treat hyperlipidemia. Its clinical applications include:

1. Chondroitin sulfate as a health food or health drug has long been used in the prevention and treatment of coronary heart disease, angina pectoris, myocardial infarction, coronary atherosclerosis, myocardial ischemia and other diseases. It has no obvious side effects and can significantly reduce the incidence of patients with coronary heart disease And mortality. Long-term clinical application has found that lipids such as fat deposited on the walls of arteries and veins can be effectively removed or reduced, which can significantly reduce plasma cholesterol, thereby preventing the formation of atherosclerosis.

2. Chondroitin sulfate is used to treat neuralgia, neuromigraine, arthralgia, arthritis, scapular joint pain, and pain after abdominal surgery. ^[5]

3. Prevention and treatment of hearing disorders caused by streptomycin and hearing difficulties caused by various noises, tinnitus, etc., have significant effects.

4. It has adjuvant treatment for chronic nephritis, chronic hepatitis, keratitis and corneal ulcer.

5. It was reported in 2010 that chondroitin in shark cartilage has antitumor effect.

6. In addition, chondroitin sulfate is also used in eye drops, cosmetics, and wound healing agents. ^[6]

[Chemical composition] It is an acidic mucopolysaccharide extracted and extracted from cartilage tissues such as laryngeal bone, nasal bone and trachea of pigs. This product contains aminohexose based on glucosamine (C6H13O5N), which should not be less than 24.0% of the indicated amount of chondroitin sulfate. ^[6]

[Pharmacological action] Chondroitin sulfate is widely present in human and animal cartilage tissue. Its medicinal preparation mainly contains two isomers of chondroitin sulfate A and chondroitin sulfate C. The content of chondroitin sulfate in the cartilage of animals of different breeds and ages is different. Its pharmacological effects are:

1. Chondroitin sulfate can remove lipids and lipoproteins from blood in the body, remove cholesterol from blood vessels around the heart, prevent atherosclerosis, and increase the conversion rate of lipids and fatty acids in cells. ^[6]

2. Chondroitin sulfate can effectively prevent coronary heart disease. It has anti-atherosclerosis and anti-atherogenic plaque formation effects on experimental atherosclerosis models; it can increase coronary artery division or collateral circulation of atherosclerosis, and can accelerate the effects of experimental coronary atherosclerosis or embolism. Healing, regeneration and repair of myocardial necrosis or degeneration. ^[6]

3. It can increase the biosynthesis of messenger ribonucleic acid (mRNA) and deoxyribonucleic acid (DNA) in cells and promote cell metabolism. ^[6]

4. Low anticoagulant activity. Chondroitin sulfate has a mild anticoagulant effect. Chondroitin sulfate A per lmg is equivalent to the anticoagulant activity of 0.45U heparin. This anticoagulant activity does not depend on antithrombin III to function, it can exert anticoagulant activity through the fibrinogen system. ^[6]

5. Chondroitin sulfate also has anti-inflammatory, accelerated wound healing and anti-tumor effects. ^[6]

[Adverse reactions] Individuals have chest tightness, nausea, and slight bleeding from the gums. ^[6]

Chondroitin mechanism of action

Chondroitin has been proven to supplement the joint soft tissue structure through oral administration. Chondroitin can be used clinically to effectively relieve the pain and inflammation of arthritis, and it can also delay joint aging.

Human clinical trials have shown that oral chondroitin can increase the secretion of synovial fluid and the concentration of hyaluronic acid, an inter-articular lubricant, while reducing the activity of chondroitin-degrading enzymes and delaying the degeneration of bones and joints. Injecting hyaluronic acid directly into joints to delay the deterioration of degenerative arthritis, taking chondroitin to increase the concentration of hyaluronic acid between joints is similar to the principle of the effect expected from this medical behavior.

According to the evaluation of multiple human clinical studies on oral chondroitin sulfide in recent years, compared with the group taking nonsteroidal analgesic and anti-inflammatory drugs (NSAIDs), taking chondroitin improves the clinical symptoms of arthritis by about 5%. X. In the overall medical evaluation, compared with the group without chondroitin or glucosamine (see the introduction of glucosamine), the treatment effect is at least 25% higher, and the arthritis group with chondroitin and glucosamine alone The clinical symptom improvement effect is quite similar (39-40%), but the group using chondroitin alone has a slightly higher trend of 1%, and the combined treatment using chondroitin and glucosamine is significantly better than using any one ingredient alone. The clinical effect is about 7-20% higher.

There are also some clinical research reports on the prevention and treatment of arteriosclerosis in chondroitin. The experimental results show that the proportion of patients with coronary arteriosclerosis who take 2000 mg of chondroitin sulphide per day is only 1.7% (1/60), compared with the control In the group with arteriosclerosis who did not take chondroitin, the incidence of acute coronary heart disease was about 27% (16/60). As for the role of chondroitin in the prevention and treatment of cardiovascular disease, there are no clear results, but studies show that For those who have been taking chondroitin sulfide for a long time on a high-fat diet, the rate of increase in blood fat seems to be lower than that of the group without chondroitin sulfide, and at the same time it has the effect of reducing thrombosis.

In addition, chondroitin is also one of the components of the blood vessel wall. Does chondroitin also repair blood vessels due to blood fat deposition and damage the tube wall, and reduce the thrombus aggregation reaction caused by the uneven surface of the tube wall? All may be the reason why chondroitin reduces the acute attack rate of coronary heart disease, but the biochemical medical community still needs further research to confirm the true effect of chondroitin in the prevention of cardiovascular disease.

Chondroitin suitable population

Chondroitin can increase the production of bone and joint fluid and prevent the wear of chondrocytes, so it is the best nutritional supplement for patients with degenerative arthritis. In addition, for some athletes, dancers with heavy joint movements, or ethnic groups who are overweight due to overweight, taking chondroitin as a prevention of joint degradation is necessary.

In addition, it is widely used in the treatment of degenerative arthritis, which is also the main component of joint connective buffer tissue glucosamine, but combined with chondroitin supplementation can greatly improve the clinical symptoms of arthritis.

Chondroitin taking method

Most clinical studies on arthritis have found that taking 1200 mg of chondroitin per day can effectively improve the pain and inflammation of arthritis. Chondroitin is not a relieving analgesic and anti-inflammatory component. When diagnosed with degenerative arthritis or arthritis caused by overloaded joints, chondroitin must be taken continuously for at least six months until the conditions that cause joint burden are lifted So far, if you are a patient with degenerative arthritis over 50 years of age, you need to continuously supplement joint fluid nutrients such as chondroitin and glucosamine.

Chondroitin Pharmacopeia related

[Identification]

(1) In the chromatogram recorded under the content determination, the retention times of the three main peaks of the test solution should be compared with the retention of the chondroitin sulfate A peak, the chondroitin sulfate B peak, and the chondroitin sulfate C peak of the reference solution, respectively. Time is consistent. ^[3]

(2) The infrared light absorption spectrum of this product should be consistent with that of the chondroitin sulfate reference product (Appendix WC). ^[3]

(3) Identification of significant sodium salt in aqueous solution of this product (1) Reaction (Appendix m). ^[3]

[Check] Nitrogen content is taken from this product and measured according to the nitrogen determination method (Appendix WD second method). Based on the dry product, the nitrogen content should be 2.5% -3.5%.

Take 0.5g of this product for acidity, dissolve it in 10ml of water, and measure it according to law (Appendix VI H). The pH value should be 6.0-7.0. Take 0.1g of this product and check it according to law (Appendix WA). Compared with the control solution made from 5ml of standard sodium chloride solution, it must not be more concentrated (0.5%). Take 0.1g of this sulfate and check it according to law (Appendix MB). Compared with the control solution made of 2.4ml of standard potassium sulfate solution, it must not be more concentrated (0.24%). Take this product for weight loss and dry it at 105 ° C for 4 hours. The weight loss should not exceed 10.0% (Appendix 1 L). Take 1.0g of this product and check it according to law (Appendix WN). According to the dry product calculation, the remaining residue should be 20.0% ~ 30.0%. The heavy metal shall be taken as the residue left under the burning residue, and shall be inspected in accordance with the law (Appendix 1 H second method). The content of heavy metal shall not exceed 20 parts per million. ^[3]

[Determination of content] Determined according to effective liquid chromatography (Appendix VD). Chromatographic conditions and system suitability tests use strong anion-exchange silica gel as a filler (such as a Hypersil SAX column, 250mmX 4.6mm, 5mm), and water (adjust the pH to 3.5 with dilute hydrochloric acid) as the mobile phase A; 2mol / L chlorine Sodium chloride solution (pH adjusted to 3.5 with dilute hydrochloric acid) was mobile phase B; the flow rate was 1.0 ml per minute; the detection wavelength was 232 nm. Perform a linear gradient elution according to the table below. Take the reference solution and inject it into the liquid chromatograph. The components elute in the order of chondroitin sulfate B, chondroitin sulfate C and chondroitin sulfate A, chondroitin sulfate B peak, chondroitin sulfate C peak and chondroitin sulfate A peak. The resolution should meet the requirements. ^[3]

Weigh about 0.1g of this product by measuring method, accurately weigh it, place it in a 10ml measuring flask, add water to dissolve and dilute to the mark, shake the hook, filter through a 0.45fxm filter, accurately measure 100 ^ 1, and place it in a test tube with a stopper Add trimethylolaminomethane buffer solution (take 6.06g of trimethylolaminomethane and 8.17g of sodium acetate trihydrate, dissolve in 900ml of water, adjust the pH to 8.0 with dilute hydrochloric acid, and dilute to 1000ml with water) 80 (Vl , Mix thoroughly, add human chondroitin sulfate ABC enzyme solution (take an appropriate amount of chondroitin sulfate ABC enzyme, and dilute with the above buffer to a solution containing 0.1 units per 100fJ according to the indicated unit) 100fxl, shake and place at 37 ° C The reaction was performed in a water bath for 1 hour, taken out, heated at 100 ° C for 5 minutes, and cooled with cold water. Centrifuge at 10,000 rpm for 20 minutes, take the supernatant, filter through a 0.45Fm filter membrane, and use it as a test solution. Precision amount 20pl was injected into the liquid chromatograph, and the chromatogram was recorded. Another appropriate amount of chondroitin sulfate reference was accurately weighed and measured in the same way. Chondroitin sulfate A, chondroitin sulfate B and chondroitin sulfate C were measured according to the external standard method. Calculate the sum of the peak areas of ^[3]