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Preserving Corporal Infrastructure
Helping customers boost general well-being to fortify defenses against pathogens

by Kyle Bradley

Baby Boomers have several things to consider as retirement approaches. Getting that beach house in Florida or that rustic cabin in Montana may be high on the list. But so, too, may be dealing with the increasing pain and limited mobility of arthritis, osteoporosis or both. “Arthritis and joint pain are a near universal consequence of aging,” said Jeremy Appleton N.D., CNS, owner of Praxis Natural. “As health-conscious individuals find themselves on the other side of 40, it is not difficult to motivate them to take their joint health seriously.”

The reality, however, is not everyone is health conscious. Marci Clow, MS, RD, senior director, technical services, Rainbow Light Nutritional Systems, noted, “Many consumers choose not to take action until they have a potential issue.” Many manufacturers are emphasizing the importance of prevent ion, and communicating this to consumers should be on the minds of retailers.

Roger V. Kendall, Ph.D., vice president, Food Science of Vermont, agreed that prevention is hard to sell. Nevertheless, “supplementation is an important part of maintaining good health,” he said. “Somebody who is health conscious and committed to living long and well will be looking at all elements of bone and joint health.” Fortunately, numerous products are available in the marketplace as manufacturers address demand for effective bone and joint health therapy without the possible harmful side effects of prescription (Rx) and over-the-counter (OTC) medications.

The Problems

The Centers for Disease Control and Prevention (CDC) estimated in 2006 that 21.6 percent of the adult U.S. population (46.4 million persons) had doctor-diagnosed arthritis, and 8.3 percent (17.4 million) had arthritis-attributable activity limitations. CDC further expects arthritis will affect 67 million adults in the United States by 2030. It is not surprising, then, that the National Institutes of Health (NIH) has 147 studies on general or localized arthritis in the recruiting stages, which indicates how much more ground scientists aim to cover before the big flux.

The Arthritis Foundation recognizes more than 100 different types of arthritis and related conditions; but, two general, well-known types are rheumatoid arthritis (RA) and osteoarthritis (OA). RA and OA have different origins, but similar unpleasant symptoms. RA is the autoimmune variety of arthritis, meaning the human immune system mistakenly attacks the body’s own tissues. OA is the wear-and-tear variety of arthritis, in which the surface layer of cartilage at the joint breaks down and wears away, allowing bones under the cartilage to rub together, causing pain, swelling and loss of motion of the joint.

A previously overlooked factor contributing to arthritis is obesity, as sedentary lifestyles and bad diets have more to do with arthritis than many consumers realize. “For every ten pounds of extra weight, an additional 30 pounds of pressure is added to the joints of the hips, knees and ankles,” said Dean Mosca, president, Proprietary Nutritionals. Because the detriments of OA can take years to manifest, joint degradation from excess body weight may not be apparent until long after significant damage is done. By that time, the exercise necessary to lose weight is difficult to perform, and the lack of physical activity has weakened bones.

In fact, bone health is integrally connected to joint function, and osteoporosis is another problem for the aging population, particularly for women. The condition is characterized by low bone mass and structural deterioration of bone tissue, leading to bone fragility and an increased susceptibility to fractures, especially of the hip, spine and wrist. The National Osteoporosis Foundation estimates roughly 10 million Americans have osteoporosis, and some 44 million Americans are at significant risk because of low bone mass.

“When it comes to osteoporosis, prevention is worth of ton of cure,” Kendall noted. “You have to get the bone density mass early, particularly with women because of hormonal changes at menopause. Young women who exercise and keep their weight under control can build a good foundation for bone structure.”

Today, nutritional compounds offer a world of hope for both arthritis and osteoporosis sufferers.

Collagen Support

Obviously, arthritis isn’t a new phenomenon, and increased demand means more joint care products have come to market in step with scientific advances. “Because there are so many entries in the category, the joint health market could be described as competitive, saturated and overwhelming to the consumer,” Clow said. “Innovation, research and product quality are driving the market and, because of this, new entries need to of fer something compelling and differentiated from the masses of products available in this category.”

However, this saturation has also demonstrated to consumers benefits of the old reliables of joint supplements. “Almost everyone I have talked to knows what glucosamine, chondroitin and MSM are,” Appleton said. These three compounds are staples of dietary supplements addressing joint health, and studies testing the efficacy of these compounds have found they work best when combined.

“Combination products work in synergy to bring about relief of symptoms, give better range of motion and better rebuilding of tissue,” Kendall said. “The more ingredients with research on them the better, particularly when you talk about glucosamine and chondroitin.”

Glucosamineis an amino sugar the body naturally produces and distributes in chondrocytes and synoviocytes of cartilage and other connective tissue; it’s primarily responsible for the promotion and maintenance of the structure and function of cartilage in joints, pain relief and anti-inflammatory proper ties. Chondroitin is a long, branching sulfated disaccharide predominant in articular cartilage, where it is thought to promote water retention and elasticity, and inhibit enzymes responsible for breaking down car tilage and deteriorating the joint. When combined, the synergistic effect of glucosamine and chondroitin helps produce more hyaluronic acid, which increases synovial fluid viscosity.1

A 2007 study found glucosamine sulfate at the oral oncedaily dosage of 1,500 mg was more effective than placebo in treating knee OA symptoms.2 Glucosamine treatment also produced noticeable improvements in RA symptoms.3 A Canadian population sample fur ther concluded some consumers are using glucosamine to manage pain and symptoms of arthritis and back pain, while others use it as a preventive measure to maintain health.4

One of the most significant recent studies on glucosamine for joint heal th was the NIH- sponsored Glucosamine/chondroitin Arthritis Intervention Trial (GAIT), which involved more than 1,500 OA patients and indicated a glucosamine/chondroitin combination was significantly more effective at reducing moderate to severe knee pain than placebo.5 In a preventive role, glucosamine sulfate was found to delay joint failure by down- regulating the expressions of enzymes causing destruction of articular cartilage in the early stages of OA. Further, the glucosaminechondroitin sulfate combination reduced moderate to severe pain in patients with OA symptoms. A subsequent risk trial using the observed safe level (OSL) or highest observed intake (HOI) assessment method supported safe intake up to 2,000 mg/d for glucosamine, and 1,200 mg/d for chondroitin sulfate.6

Despite study results in favor of supplementation with glucosamine, chondroitin or both, reviewers have been cautious, stating evidence to this point is suggestive and has “so far failed to prove convincingly that [glucosamine] works, how it might work, or whether it is safe to take long-term.”7 Other reviewers said “recommending glucosamine sulfate (GS), glucosamine hydrochloride (GH), and chondroitin sulfate (CS) for the treatment of mild knee pain from OA is ineffective,” and that further research is needed to “identify specific characteristics in patients that results in a positive response.”8

That hasn’ t impacted innovation in the field, as glucosamine and chondroitin are often seen in combination formulas, particularly with methylsulfonylmethane (MSM). MSM is an organic sulfur-containing compound that occurs naturally in fruits, vegetables and grains. It helps with maintaining healthy cell membranes and building strong connective tissues as well as provides pain relief associated with arthritis. On its own, sulfur supports collagen and connective tissue and enzymes, hormones and immunoglobulins. MSM appears to play a role in cartilage preservation, cell wall stabilization and support of healthy muscles, nerve tissue, vital organs and the brain.

One recent study found MSM (as OptiMSM®, from Bergstrom Nutrition) significantly improved knee joint function in adults who took 3,000 mg twice daily for 12 weeks.9 Statistically significant reductions in serum homocysteine (a risk factor for cardiovascular disease) and urinary malondialdehyde (a marker of oxidative stress) were also observed, with no significant adverse events reported. Subsequent toxicity tests in rats showed a single oral dose of 500 mg of MSM was rapidly absorbed, well distributed, and completely excreted from the body.10

Collagen itself is a popular ingredient in joint health formulations. “Type II collagen administered orally works with the immune system by a process called oral tolerization,” said Evelyn Scalora, product manager, InterHealth Nutraceuticals, suppl ier of UC-II ® undenatured Type II collagen. “In the case of UC-II, small amounts taken orally have been shown to turn off the immune response targeted at the type II collagen present in bone joint cartilage.” A study presented in March 2006 found giving UC-II to osteoarthritic dogs decreased overall pain by 62 percent, and when combined with glucosamine and chondroitin, reduced pain by 57 percent.

The human body also produces hyaluronic acid (HA) naturally, and supplemental HA is a newer ingredient on the shelf. The mucopolysaccharide is part of the glycosaminoglycan (GAG) group in which chondroitin sul fate appear s. When not bound to other molecules, HA binds with water to form a stiff yet viscous gel, which is why it functions well in joint formulations for increasing lubrication in cartilage between bones. Supplementation with HA, hyaluronan or hylan in patients with knee OA helped with pain reduction and physical function improvement in adults, with low risk of harm.11 A separate study supported the use of the HA products in the treatment of knee OA, with few adverse events repor ted in the hyaluronan/hylan trials.12 HA base hydrogel can also be used for cell and growth factor carriers for tissue regeneration.13

Supporting Players

Mineral complexes are popular in many joint health products, as minerals are essential for enzymatic reactions and general wellness. Trace Minerals, for example, uses its ConcenTrace® mineral complex in its liquid coral calcium to increase bioavailability. Another complex derived from naturally-occurring volcanic mineral deposits, and included in OrthoSil® (from Maximum International), includes 65 macro and trace minerals from igneous rocks of mountains in Canada. An unpublished pilot study showed the complex (as SierraSil™, from Sierra Mountain Minerals Inc.) was effective in alleviating symptoms of patients diagnosed with OA.14 A separate in vitro study, conducted at Case Western Reserve University School of Medicine in Cleveland, Ohio, found the complex significantly reduced the breakdown of cartilage structural integrity, caused by the pro-inflammatory cytokine IL-1Beta Interleukin, by 68 to 73 percent. Also included in Orthosil are bromelain, a natural protein-digesting enzyme from pineapple, and an extract of Polygonum cuspidatum (as Protykin®, from InterHealth), which pair to inhibit proinflammatory substances in white blood cells, according to Bill Downs, president, Allied Nutraceutical Ingredients.

Fatty acids also play a role in joint function. “Fish oil is a wonderful anti-inflammatory,” noted Jacob Teitelbaum, M.D. After three years of intervention with a combination therapy including fish oil for RA symptoms, 75 percent of participants in one study continued supplementation, while only 21 percent continued using nonsteroidal anti-inflammatory drugs (NSAIDs).15 A recent meta-analysis quantified var ying outcomes related to omega-3 polyunsaturated fatty acids’ effects on joint pain.16 After three to four months of supplementation, patients reported reductions in joint pain intensity, minutes of morning stif fness, number of painful and/or tender joints and NSAID consumption. Another study, involving 250 patients with nonsurgical neck or back pain, reported consumption of 1,200 mg/d of omega-3 EFAs (eicosapentaenoic acid and docosahexaenoic acid) significantly reduced arthritic pain;  88 percent of participants indicated they’d continue taking fish oil after the study concluded.17

Cetylated fatty acid esters are a newer player in this category, seen as Celadrin®, from Proprietary Nutritionals. “Celadrin is a unique fatty acid that is stable in the presence of oxygen,” Mosca said. “Celadrin focuses on the immune system by stopping inflammation and relubricating the joint capsule.” A published study on a one-month intervention with Celadrin topical cream reported it was effective for reducing pain and improving functional performance in individuals with knee OA.18 Patients saw significant improvements in stair-climbing ability (12 percent), balance and strength (16.5 percent), and range of motion (3.5 percent). Pain was also significantly reduced. A recent double blind, placebo-controlled study commissioned by Proprietary Nutritionals, which has been submitted for publication, found consuming Celadrin for eight weeks increased walking distance ability in patients with knee discomfort by 45 percent. Participants further claimed a 35 percent decrease in knee pain over a period of 60 days.

Botanical compounds also offer support in joint formulas, particularly in impacting pain and inflammation. Teitelbaum said willow bark, the original source of aspirin, blocks the release of prostaglandins, compounds associated with pain and inflammation generated by the cyclooxygenase (COX) pathway. Willow bark has been shown to provide short-term improvements in patients with chronic lower back pain.19Cherry fruit extract—a traditional anti-gout remedy—supports healthy uric acid levels, while potentially modulating inflammatory pathways through healthy C-reactive protein (CRP).20Capsaicin, a natural component of chili peppers, works as a topical analgesic by isolating the TRPV1 protein responsible for relaying pain from nerve cells; it is considered to be safe and effective as an external analgesic, and was shown in recent study to enhance the penetration of an anti-inflammatory agent through human skin.21

More exotic botanicals for joint health include boswellia, yucca and devil’s claw. The extract of the Indian herb Boswellia serrata has natural anti-inflammatory activity, working to switch off pro-inflammatory cytokines and mediators.22Yucca was reported in a research review to have established anti-arthritic and antiinflammatory effects.23 And devil’s claw appears to be effective in reducing the main clinical symptom of OA pain,24 as well as an effective anti-inflammatory and analgesic preparation in the treatment of acute and subacute inflammation from degenerative joint diseases.25

The Bones of Bones

The best known players in the bone health field are calcium and vitamin D. “The most abundant mineral in the body, calcium supports bone health, nerve health and healthy heart function,” Teitelbaum said. Many consumers probably associate calcium with bones, but knowledge of which form of calcium salt is appropriate and how to maximize absorption are not common knowledge. Also, as Teitelbaum noted, drinking a glass of milk may not do the trick for getting sufficient calcium. “Supplemental calcium may have superior benefits for the support of healthy bone than the traditional dietary sources,” he said.

Appleton agreed consumers may have little idea of the interplay between calcium and other vitamins and minerals. “People are generally pretty savvy about the need for calcium,” he said. But, “they seldom realize they need magnesium as well, and that calcium supplements should always be accompanied by vitamin D.”

Another critical vitamin for bone health is vitamin K. One recent report supported intervention with adequate amounts of vitamin K in the prevention and primary management of osteoporosis.26

Another study found vitamin K may reduce fracture risk by increasing bone mineral density as well as improving bone microarchitecture.27 Several chronic diseases associated with abnormal calcification, affecting many elderly, indicate vitamin K supplementation may reduce overall bone loss.28

The form of vitamin K appears to impact efficacy. Recent research from Maastricht University, the Netherlands, demonstrated vitamin K2 as menaquinone (or MK-7) was superior to vitamin K1 for absorption, bioavailability and efficacy.29 MK-7 more effectively promoted and activated markers of bone building than K1. “This is the first human study using natural vitamin K2 as a dietary supplement,” said lead researcher Leon Schurgers, Ph.D. “It shows vitamin K2 as MK-7 is clearly the most beneficial and potent K-vitamin one can take.”

Beyond just vitamins and supplements, women can take action to prevent osteoporosis. Kendall has formulated bone health products containing ipriflavone, a soy derivative. “Studies show this soy derivative, in the level of 600 mg, allows rebuilding of bone structure over a six month period,” said Kendall. “So, along with the key minerals [for bone health] calcium, boron, zinc, copper and folic acid, you’re getting the restorative effect.” Ipriflavone may influence bone metabolism by regulating the functional balance between osteoblasts and osteoclasts.30 Animal research suggests daily ipriflavone intake in conjunction with a bone regeneration procedure may improve the quality of newly generated bone.31

Bone regeneration is also the mechanism of a new ingredient from hops (Humulus lupulus L.). The active ingredients in Pharmachem’s Perluxan are alpha acids from hops—humulone, cohumulone and adhumulome. At low doses, the compounds inhibit bone resorption by reducing the transition of osteoblasts to osteoclasts; at high doses they also reduce inflammation and the associated pain by isolating the actions of inflammatory enzymes such as prostaglandin E2. “An important distinction about hops for bone health, as opposed to genistein, daidzein or ipriflavone, is that hops offer a non-estrogenic solution to bone loss or bone resorption,” said Gregory Bonfilio, business development manager, Pharmachem. “Given the proven anti-inflammatory effects of hops, the extract offers both anti-bone resorptive activity plus pain relief.” A second fraction of hops extract available from Pharmachem is xanthohumol, which has been effective in countering bone resorption because of a small amount of an estrogenic substance contained therein.

Down to Business

With any crowded market, profitable products must stand out from the competition. Chris Meletis, N.D., director of training, Trace Minerals, urged retailers to select products based on their quality and bioavailability. Teitelbaum added: “There are a variety of price points for products in bone and joint health, and it is critical consumers be able to understand the different advantages. Merchandise products so people can see: good, better, best.” While retailers can help guide consumers to appropriate products to meet their individual needs, informed consumers are likely already reading up on ingredients and looking to get value for their dollar. “Consumers are always comparing price and value, so they need to understand how they get more as they pay more,” Teitelbaum said.

In addition, Mosca advised retailers to sell the customer the appropriate product, but not over promise results. Dietary supplements aren’t able to make disease-related claims—such as “curing” arthritis, so retailers must watch their marketing. “We can talk about structure-function claims—about maintaining the appropriate structure and function of a body system, whether it’s a bone or a joint, or the digestive tract,” Kendall said.

Something else important for consumers to understand is dietary supplements for bone and joint health may take longer to work than conventional options. “Most products take a long time to work,” said Downs. Because results aren’t always immediate, it can be easy for consumers to abandon effective treatment with dietary supplements that are slowly rebuilding cartilage and restoring proper function of effected joints and bones. “People need to know that when you’re taking natural things to heal joints, it takes six weeks because it is actually rebuilding the system and healing it, as opposed to [prescription] meds that poison the system,” Teitelbaum added.

Ultimately, knowledge is the bottom line for both retailers and consumers. “It comes down to educating yourself,” Kendall said. “We try to encourage the consumer to become Internet savvy and connect with retailers who are well-educated in all these [health] areas.” The abundant products on the market mean more considerations for consumers, and an honest retailer can help them navigate the maze of marketing claims.

“Manufacturers share the challenge of helping the public distinguish between sound science and the misinformation, speculation and folklore surrounding the use and safety of supplements,” Clow explained. Kendall agreed, noting: “Rather than giving them an eight- to ten-page technical review, you’ve got to break things down into little bullet points.”

At the end of the day, despite the technicality of mechanisms in bone and joint products, straightforwardness is best. Said Teitelbaum, “Make it simple for the consumer to understand what you offer.”

To view the references for this story, click here.


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