effi-science/e-sciences

Chondroitin

1. Chondroitin: what is it?

Chondroitin is a molecule used in the treatment of osteoarthritis. Like glucosamine, it belongs to the class of "slow-acting symptomatic treatments", molecules that have a deep effect on osteoarthritis.

 

A. Chondroitin is naturally present in the body

Within the joint, chondrocytes are the cells responsible for the formation of cartilage and the destruction of worn cartilage, as well as the synthesis of glucosamine and chondroitin.

It is the chondrocytes that will form the chondroitin, it is assembled as a chain from smaller elements. Then, these chains of chondroitin will be assembled into larger elements, the proteoglycans, and then these will also be assembled. These proteoglycans will attract and fix the water molecules and ensure that the joint is well lubricated and can absorb shocks.

 

 

B. Chondroitin supplements

Chondroitin is used as a dietary supplement for joint relief. As it is a rather large molecule, the body has to split it before it can be absorbed, which is why its absorption is generally not very high (10-20%) [1]. It is then transported in the blood and concentrates in the synovial fluid and cartilage. The chondroitin used by E-sciences comes from the trachea of cattle. For a long time chondroitin was extracted from sharks and rays, but the methods of harvesting it are not very environmentally friendly: the fins are cut off and the sharks are thrown back into the sea alive.

 

The provenance of the cattle is very well controlled, and the cartilage is recovered during the slaughter process for the meat.

 

It is important to take chondroitin in sufficient dosage: 1200 mg / day. It is also important to take the right amount every day, so that there is a constant dose in the body. Also, chondroitin is a slow-acting drug, so the effects can only be assessed after 3 to 6 months.

2. Osteoarthritis and chondroitin: how does it work?

Chondroitin will act on both aspects of osteoarthritis: the wear and tear of the cartilage and the inflammatory cascade [2].

Chondroitin molecules do not enter the cells of the joint (chondrocytes, osteoblasts etc) but their effects are via receptors on the membranes of these cells [1]. These effects can be divided into two broad categories:

A. Effects on cartilage 

B. Effects on the inflammatory cascade

 

A. Effects on cartilage

Chondroitin has three distinct effects that maintain healthy cartilage: 

- anti-apoptosis effect 

- allow chondrocytes to create more proteoglycans 

- prevent metalloproteases from degrading them.

1. Anti-apoptosis effect

The poor renewal of cartilage is partly the result of too much death of the cells that make cartilage, the chondrocytes.

When a cell is worn out, it is eliminated in a programmed way: this process is called apoptosis (if the death of the cell does not take place in a programmed way, it is called lysis or necrosis). In osteoarthritis the apoptosis process is deregulated, the enzymes responsible for cell death are overactivated. Chondroitin regulates these enzymes and therefore prevents cell death.

 

2. Increases proteoglycan synthesis

A chondroitin supplement "delivers" bricks with which the body can build up new proteoglycans, essential components of cartilage.

 

3. Reduction of metalloproteinases

Metalloproteases are the enzymes that destroy elements of the cartilage and the joint matrix. Indeed, the body must be able to get rid of worn-out components. However, in osteoarthritis, these enzymes are present in excessive quantities. The inflammatory cytokines stimulate the cartilage cells to produce more proteases, so the destruction of the components is increased. Metalloproteinases are contained by inhibitors, the TIMPs. Chondroitin will signal the cell to increase the number of TIMPS, which will prevent the metalloproteinases from doing any harm.

 

B. Effects on the inflammatory cascade

The inflammatory cascade is a complex phenomenon where many molecules will induce others, set in motion complex systems, create disturbances, etc.

A major culprit in osteoarthritis problems is the pro-inflammatory cytokine interleukin-1-beta (or IL-1β).

Chondroitin

IL-1β is therefore responsible for several effects, at different levels: 

- increased chondrocyte death 

- activation of COX-2 enzymes and thus production of prostaglandins responsible for the sensation of pain (more info here ) 

- increased synthesis of metalloproteinases 

- decreased proteoglycan synthesis

 

In addition, IL-1β triggers other cytokines such as NO (nitric oxide) and TNF-α (tumor necrosis factor alpha), which will reinforce its effects.

 

We have already seen that chondroitin will act at the level of cartilage, but in addition to that it will also prevent the production of NO and inhibit the activation of COX-2

 

3. Effects of chondroitin

Cartilamine Chondro

Cartilamine Chondro is recommended in cases of more severe joint discomfort than described for Cartilamine 1500. It is suitable for severe cartilage damage.  

From €21.90

[1] Du Souich, Patrick. 2014. "Absorption, Distribution and Mechanism of Action of SYSADOAS." Pharmacology & Therapeutics 142 (3) (June): 362-74. 

[2] Henrotin, Yves, Mariane Mathy, Christelle Sanchez, and Cecile Lambert. 2010. "Chondroitin Sulfate in the Treatment of Osteoarthritis: From in Vitro Studies to Clinical Recommendations." Therapeutic Advances in Musculoskeletal Disease 2 (6) (December): 335-48.

[3] ZEGELS B, et al. 2013. "Equivalence of a Single Dose (1200 Mg) Compared to a Three-Time a Day Dose (400 Mg) of Chondroitin 4&6 Sulfate in Patients with Knee Osteoarthritis. Results of a Randomized Double Blind Placebo Controlled Study." Osteoarthritis and Cartilage / OARS, Osteoarthritis Research Society 21 (1) (January): 22-7.

[4] WILDI L.M., et al. 2011. "Chondroitin Sulphate Reduces Both Cartilage Volume Loss and Bone Marrow Lesions in Knee Osteoarthritis Patients Starting as Early as 6 Months after Initiation of Therapy: A Randomised, Double-Blind, Placebo-Controlled Pilot Study Using MRI." Annals of the Rheumatic Diseases 70 (6) (June): 982-9.

[5] RAILHAC J-J, et al. 2012. "Effect of 12 Months Treatment with Chondroitin Sulfate on Cartilage Volume in Knee Osteoarthritis Patients: A Randomized, Double-Blind, Placebo-Controlled Pilot Study Using MRI." Clinical Rheumatology 31 (9) (September): 1347-57.

[6] UEBELHART D, et al. 2004. "Intermittent Treatment of Knee Osteoarthritis with Oral Chondroitin Sulfate: A One-Year, Randomized, Double-Blind, Multicenter Study versus Placebo." Osteoarthritis and Cartilage / OARS, Osteoarthritis Research Society 12 (4) (April): 269-76.