Dietary Supplements for Maintaining Normal Joint and Cartilage Function

Human biomechanics is at the core of modern approaches to health maintenance, prevention, and treatment of diseases, particularly those related to the musculoskeletal system. Modern kinesitherapy and physical therapy focus on studying the effect of the central nervous system on the entire locomotor apparatus. Besides the muscular and skeletal systems, connective tissue, and particularly joints, are common causes of reduced mobility, diminished quality of life, and inability to realize one’s potential in life, including in sports careers. Athletes, along with physically active individuals and the elderly, are the most affected groups of patients with joint pain. Athletes are exposed to joint injuries mainly due to intense mechanical loads and imbalances between inflammatory processes and recovery. For most other patients, the causes of biological pathological changes in the joints are congenital genetic patterns, autoimmune processes, and primary non-infectious chronic inflammatory diseases such as obesity. While measures for preserving the skeletal system are relatively well-known and often emphasized in general preventive actions, it seems that discussions about joints and connective tissue begin only when chronic or acute health issues and diseases arise. The initial symptoms of joint damage or disease include redness, swelling, and tenderness of the joints, warm (heated) joints, stiffness and weakness in the joints, or their “clicking.” Ultimately, there may be a loss of range of motion and limping. The most significant groups of patients with chronic joint diseases are those diagnosed with arthritis, osteoarthritis, and rheumatoid arthritis. Due to the side effects of nonsteroidal anti-inflammatory drugs, most of these patients seek additional interventions and safe dietary supplements during disease treatment—likely the most widespread form of self-care in modern times.

Joint Diseases

Arthralgia (joint pain) is a signal of inflammatory processes in the joints and connective tissue. It can be caused by mechanical stimuli and load or by intrinsic pathological processes affecting the ligaments, bursae, and tendons surrounding the joints. Injury can also affect the connective tissue within the joint itself. Arthritis encompasses over 100 different pathological conditions (e.g., degenerative and inflammatory arthritis) that affect the joints and other parts of the body. Ultimately, arthritis is a cause of disability and a significant factor in limited mobility for more than 19 million people. Osteoarthritis (Arthrosis) is a slowly progressive joint disease and the most common type, which can occur in any joint cartilage. However, it is most notably present in the joints of the hands, spine, hips, knees, and feet. It results in stiffness, swelling of the joints, pain, and restricted movement. This disease is one of the most common causes of chronic work incapacity. Rheumatoid Arthritis is the most common inflammatory autoimmune joint disease, often manifested by pain and symmetrical swelling of the small joints of the hands and feet, as well as other synovial structures. Other symptoms may include weight loss, fatigue, and general weakness. Sometimes, vasculitis can also occur. Unfortunately, this disease is often progressive, affecting other joints with destructive processes that lead to irreversible bone erosion and structurally damaged and deformed joints, resulting in long-term pain and reduced mobility.

Non-Steroidal Anti-Inflammatory Drugs (NSAIDs)

The most commonly used drugs and the first-line therapy for joint diseases are non-steroidal anti-inflammatory drugs, such as COX-2 inhibitors. However, the side effects of continuous use of these drugs are well-known, including increased intestinal permeability and the erosive effect of some drugs on the gastrointestinal mucosa. Considering their range of action, patients and pharmacists are often inclined to recommend dietary supplements with controlled origins and known mechanisms of action and limited potential side effects.

Dietary Supplements

In the extensive range of pharmaceutical dietary supplements, there are products that exhibit certain seasonality for various reasons. Before summer, patients focus on aesthetics and are more conscious of reducing excess body weight, while in winter, the most sought-after supplements are those for modulating immune response and for respiratory health. While the reasons for this specific popularity are more or less justified, dietary supplements whose popularity is not dictated by the season but by objective conditions throughout the year certainly include those that benefit joint and cartilage health.

Source of Raw Materials

Many patients, upon visiting a pharmacy, insist on information regarding the origin of the ingredients or raw materials used in a product formulation, whether for objective or subjective reasons. Patients do not necessarily have to be vegans; rather, an increasing number of patients who are flexible in their dietary choices still emphasize controlled sourcing of the food and dietary supplements they consume. As a result, modern dietary supplement formulations increasingly focus on the origin of raw materials, while ensuring a well-formulated product with active ingredients that have a clearly known mechanism of action.

Standardization of Extracts for Active Ingredients

In the not-so-distant past, dietary supplements available in our market often contained various plant and other substances without known standardized potentially active components. Regardless of the application and reason for use, pharmacists today, and increasingly patients, demand nutraceuticals and phytopharmaceuticals with clearly identified active substances in standardized concentrations.

Overview of Some Plant Species and Ingredients Used in the Formulation of Dietary Supplements for Joints and Cartilage

The range of dietary supplements that have beneficial effects on joints could be categorized into three fundamental and crucial mechanisms for joint health. – Pain Mediation: they participate in mediating pain – Repair Processes: They contribute to the repair processes of structural damage. – Inflammatory Modulation: They play a role in modulating inflammatory processes.  Extract of Indian Frankincense Resin (Boswellia serrata)

Early studies from the mid-1980s highlighted the potential of the extract from the resin of Indian frankincense, a plant species perhaps better known by its original name, Boswellia serrata. The primary active compounds are boswellic acids, a group of organic acids that inhibit the transcription factor NF-kappaB, 5-lipoxygenase, and leukotriene production. Among the boswellic acids, 3-acetyl-11-keto-beta-boswellic acid (AKBA) is the most pharmacologically active. AKBA affects the enzymatic activity of cyclooxygenase-1 (COX-1) and can therefore mediate the reduction of inflammation. Studies have shown that boswellic acids have relatively poor pharmacological bioavailability, suggesting that it would be prudent to use synergistic substances, known as biocatalysts, in dietary supplement formulations and future studies, or to employ alternative approaches. In animal models with experimentally induced arthritis, boswellic acid showed an inhibitory effect on leukocytes, significantly reduced concentrations of inflammatory mediators (IL-1β, IL-6, TNF-α, IFN-γ, and PGE2), and increased concentrations of IL-10. Initial clinical studies suggested effectiveness in autoimmune diseases such as rheumatoid arthritis. More recent clinical studies have demonstrated that a combination of Boswellia serrata and Curcuma longa extracts, administered twice daily at 500 mg each to 54 participants, was more effective than the selective COX-2 inhibitor celecoxib at 100 mg twice daily, with no observed toxicity. Glucosamine Sulfate

Glucosamine sulfate is considered one of the most commonly used dietary supplements for the treatment of osteoarthritis. In vitro studies suggest that glucosamine may stimulate synovial production of hyaluronic acid and exhibit antioxidant effects on chondrocytes through gene expression effects on inducible nitric oxide synthase. The beneficial effects of glucosamine on joint health are due to its multifaceted mechanism of action. One of these mechanisms includes its favorable impact on capillary permeability (K trans) in patients with patellar degeneration, observed after 6 months of use. Methylsulfonylmethane (MSM)

This organosulfur molecule is naturally present in the human body in cerebrospinal fluid and plasma. It is a significant donor of biologically available sulfur in many biochemical reactions, particularly in the formation of new tissues, joint ligaments, and muscles. MSM is believed to have chemopreventive properties, anti-inflammatory effects, neutralizing action on reactive oxygen species, anti-atherosclerotic effects, and inhibitory action on the synthesis of prostacyclin 2 (PGI2).
Some clinical studies have used a model with 120 participants, where the experimental group received 5 grams of MSM, along with either 7.2 mg of boswellic acid or 1500 mg of glucosamine sulfate. The combination of MSM and boswellic acid proved to be more effective compared to the traditional approach of using glucosamine sulfate alone. Vitamins, Herbal, and Other Active Ingredients in Supplementation Strategy

Uncontrolled inflammatory processes are the underlying cause of joint pain and chronic joint diseases. However, inflammation itself is a normal physiological response and should not be suppressed entirely. The problem lies in excessive inflammation and the imbalance between inflammation and anti-inflammation. This is important to note because, in the U.S. dietary supplement market, there have been supplements advertised as ones that stop inflammation. The American FDA has taken a stance, which has been accepted by responsible dietary supplement manufacturers. Therefore, the essence of using dietary supplements that benefit joint health is not in their ability to stop immune-inflammatory processes but rather in their modulatory effects on such processes. Omega-3 Fatty Acids

Often popularly referred to as vitamin F, these long-chain fatty acids are among the most significant and potent anti-inflammatory agents in food, particularly in concentrated dietary supplements. A review of scientific literature conducted in 2012 concluded that EPA and DHA, long-chain polyunsaturated omega-3 fatty acids from fish oil and marine sources, are moderately beneficial in alleviating symptoms of rheumatoid arthritis. Participants in many studies included in this review reported experiencing shorter periods of morning stiffness, reduced joint swelling and pain, and a decreased need for anti-inflammatory medications during the intake of omega-3 fatty acids. Curcumin (Curcuma longa)

The rhizome of turmeric has traditionally been used in Indian and traditional medicine to reduce inflammatory processes. Curcumin, a well-known biologically active compound, modulates key molecular sites that regulate inflammation, including COX-2, 5-LOX, transcription factors, cytokines, receptors, and adhesion molecules on cell surfaces. Some studies have shown that curcumin can improve walking performance and overall inflammatory status, as measured by the CRP (C-reactive protein) parameter. A randomized, double-blind, placebo-controlled study published in 2014 involved 40 participants diagnosed with knee osteoarthritis, in which a dose of 1,500 mg of patented curcumin was administered in three divided doses over 6 weeks. Piperine was used in this combination as a synergistic biocatalyst for curcuminoid kinetics. The study group of 19 volunteers with mild to moderate knee osteoarthritic changes showed significant improvement, measurable through the standardized WOMAC, VAS, and LPFI scales, compared to the 21 participants in the placebo group. Proline is a non-essential amino acid that, along with vitamin C, participates in the process of hydroxylation of proline, a biochemical process essential for collagen. It is rarely added directly in dietary supplement formulations but is often a component of amino acid premixes in sports supplements.

Conclusion

It appears that an effective approach to self-care and treatment of joint health disorders does not involve the previously common strategy of using a single biologically active component, but rather a combination of biologically active substances with different mechanisms of action. When implementing such strategies and interventions through supplementation, it is crucial to ensure anti-inflammatory effects, modulation of inflammatory mediators, as well as support for the regeneration of structurally damaged tissue.

Sources:

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