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CoQ10 at the Heart of the Matter

Coenzyme Q10 (CoQ10) promotes a healthy heart—and so much more

Heather Granato

References

Coenzyme Q10 (CoQ10) is found in every living organism, giving rise to its scientific name ubiquinone (from its ubiquitous positioning). It's also increasingly taking over shelf space in retail stores and finding itself the subject of Web sites, mainstream media articles and the key compound in products from smoothies to skin cream.

"In the natural products market, I have seen an increase in consumer awareness and demand for dietary supplements such as CoQ10," said Hank Cheatham, director, sales and marketing, American Health Formulations (AHF). "Even among mass market consumers, there is increasing demand for natural products, such as CoQ10, with scientifically demonstrated efficacy but no evidence of unwanted side effects."

Driving that interest is greater media attention, noted Linda Miles L.Ac., D.O.M., vice president, derma e®. She observed, "The vast amounts of research being conducted on CoQ10 and the media's frequent dissemination of information on this ingredient and its benefits have contributed to its popularity."

Neil E. Levin, CCN, DANLA, nutrition education manager, NOW Foods, noted, "There is actually a fair amount of consistently positive press on CoQ10, with a significant part of that because of this antioxidant nutrient's role in cardiovascular and heart health. … I would go so far as to suggest CoQ10 has picked up some of the wide popularity as a heart nutrient that vitamin E had several years ago, but lost due to consumer confusion caused by unwarranted negative publicity. The fact that CoQ10 is so obviously safe, versatile and useful has propelled it to a high place on the list of cardiovascular nutrients."

Indeed, heart health remains the hottest area for CoQ10 promotion. "Consumers are very aware of the benefits of CoQ10 for heart health, as it has been a common topic in news and magazine articles," said Paula Hanek, brand manager, Enzymatic Therapy. "Some M.D.'s are recommending that people taking statin drugs for cholesterol issues take a CoQ10 supplement. The aging of the Boomer population has had a big impact on supplements; since CoQ10 supports healthy aging, it's a definite item of interest."

Cheatham agreed, noting the heart health product category in general is growing in direct correlation with the aging population. "Seniors and Baby Boomers understandably become more concerned with heart issues as they age and are the driving force behind the increasing interest in CoQ10," he said. "CoQ10 offers solutions for many of these consumers who are suffering from hypertension, elevated cholesterol, atherosclerosis and similar maladies."

Steve Holtby, president and CEO, Soft Gel Technologies Inc. (SGTI), added: "The majority of consumers using CoQ10 are still mostly heart patients, as research repeatedly demonstrates its safety and efficacy in preserving heart health, slowing or reversing disease progression, and minimizing side effects of other medications, such as statin drugs. However, CoQ10 is now being touted for many other applications, such as Parkinson's disease, diabetes and energy, since it supports the body through a number of metabolic pathways, including antioxidant protection, membrane stabilization and energy production. Evidence is accumulating for CoQ10's role in the treatment of mitochondrial disorders and neurodegenerative disease. With more research showing there is a decrease in plasma and tissue concentrations of CoQ10 associated with aging, it is being touted as a critically important nutrient that should be considered for optimum health. Word of it is reaching the masses because it is an effective supplement in replenishing diminished CoQ10 levels to protect against oxidative stress and age-related diseases."

In fact, market research firm Mintel noted ongoing research supports the use of CoQ10 beyond its traditional cardiac and energy benefits into eye care, obesity and even fertility. The company added a combination of items including the aging population and rising health care costs are likely to continue to drive consumers to opt for functional foods and dietary supplements with CoQ10.

Gene Bruno, M.S., M.H.S., consultant to Jarrow Formulas, agreed there is great potential for CoQ10 for a broad range of consumers. "CoQ10 is one of those encompassing dietary supplements with both general health benefits (e.g., anti-aging, antioxidant) as well as specific health applications (e.g., cardiovascular issues, diabetes, etc.)," he said. "Consequently, it has broad appeal to a great number of individuals."

That broad appeal and awareness is continuing to grow. "At the beginning of the decade, it was estimated less than 1 million consumers were taking CoQ10," observed Scott Steinford, president, ZMC-USA. "As a result of strong scientific studies as well as medical community endorsement, CoQ10 has now become one of the top three non-letter-vitamin supplements recommended by physicians or their staff. Also, at the beginning of the decade, the average dosage was under 30 mg. The average dosage of CoQ10 supplement users is expected to reach 100 mg within the next five years."

Ultimately, it's the range of health effects that position CoQ10 as a nutrient positioned for market growth. "The multiple roles of CoQ10 in the human body make it uniquely useful in protecting cells and energizing essential processes such as heart action and immunity," Levin said. "Energy supports the constant pumping of the heart muscle, but also supports immune functions and antioxidant activity. Lack of energy is a common complaint heart by doctors, and active people need good sources of energy, so nutrients that promise to improve the energetics of the body are always in demand."

In fact, energy production is the cornerstone of CoQ10's benefits to the body. CoQ10, most commonly referring to ubiquinone, is a lipid-soluble enzymatic cofactor that plays a key role in cellular energy production; its reduced form, ubiquinol, is a potent lipophilic antioxidant that can both protect against oxidative damage and help regenerate other antioxidants.

From the time of its discovery in the late 1950s, scientists looked into its role in cellular energy, longevity and the health of such organs as the heart, kidneys and liver. In fact, CoQ10 is responsible for 95 percent of energy expenditure in some areas of cells. At the metabolic level, CoQ10 plays an important role in the production of adenosine triphosphate (ATP), the form of energy used by the cells, from carbohydrates and fats. Information from the Linus Pauling Institute (LPI) at Oregon State University noted CoQ10 works as part of the mitochondrial electron transport chain, shuttling fatty acids, glucose molecules and protons across the mitochondrial membrane to release energy to produce ATP. In addition, CoQ10 as ubiquinol is an important cellular antioxidant. LPI's team stated ubiquinol may inhibit lipid peroxidation, neutralize free radicals and regenerate alpha-tocopherol.

Stephen T. Sinatra, M.D., a board-certified cardiologist, certified bioenergetic psychotherapist, and anti-aging specialist, is an outspoken advocate for the use of CoQ10 and a proponent of "metabolic cardiology"—using integrated nutritional support to enhance well-being of patients with heart issues. He spoke recently on a Webinar for Natural Products INSIDER (the sister publication to Natural Products Marketplace), and noted there are many causes of CoQ10 deficiency, including impaired CoQ10 synthesis, related to nutritional deficiency, genetic or acquired defect in CoQ10 synthesis, as well as interference from pharmaceutical drugs. As far as its health benefits, he said, "CoQ10 has an unusual ability to enhance fatty acid oxidation in cells while removing excess harmful substances such as acyl groups and free radicals from basement membranes. CoQ10 acts like the spark plug to ignite the energy process in the mitochondria to form ATP, the energy of life."

As the heart is the greatest energy consuming organ in the body, it is not surprising one of the most active areas of research for CoQ10 is in the area of heart health, with scientists documenting its critical role as far back as the 1960s. Because CoQ10 works to prevent oxidation of cholesterol, particularly LDL cholesterol, it may help prevent the onset of atherosclerosis. Indian researchers noted administration of 3 mg/d of CoQ10 (Q-Gel®, from Tishcon) in rabbits with high trans fat levels helped limit oxidative damage and atherosclerosis development.⁽¹⁾ Supplementing with a combination of CoQ10 and alpha-tocopherol has been shown to increase plasma levels of vitamin E and beneficial high-density lipoprotein (HDL) cholesterol,⁽²⁾ and reduce atherosclerosis at the aortic root and descending thoracic aorta.⁽³⁾ Research also supports its therapeutic use as an adjunct to treatment for congestive heart failure.⁽⁴⁾

In addition, CoQ10 may help lower systolic and diastolic blood pressure in hypertension.⁽⁵⁾ The Natural Standard Patient Monograph on CoQ10 noted there is good scientific evidence for the use of CoQ10 for lowering blood pressure, and that low blood levels of CoQ10 are found in people with hypertension.

Interestingly, with all CoQ10's heart health benefits, patients being treated with pharmaceuticals for high cholesterol may find themselves in a worse position. The enzyme hydroxymethylglutaryl (HMG)-CoA reductase plays an important role in regulating cholesterol synthesis; inhibiting this activity is the goal of the statin class of cholesterol-reducing pharmaceuticals. Unfortunately, the same HMG-CoA reductase pathway also regulates CoQ10 synthesis. Italian researchers noted statin treatment generally results in lower plasma levels of CoQ10, possibly related to the fact that the drugs lower levels of LDL, the primary transport molecule for LDL; however, there is also a decrease of CoQ10 seen in the platelets and lymphocytes, suggesting CoQ10 synthesis itself may be inhibited.⁽⁶⁾ Interestingly, new studies suggest statin treatment may also lead to type II diabetes as it reduces the body's stores of CoQ10.⁽⁷⁾

Intervention studies with statins have examined the impact of the drugs on CoQ10 levels. Japanese researchers found treatment with pitavastatin reduced CoQ10 levels in patients with hypercholesterolemia by 7.7 percent; atorvastatin reduced those levels by 26.1 percent.⁽⁸⁾ Similarly, Italian researchers reported three months of statin therapy dose dependently reduced total cholesterol, as well as levels of ubiquinol and ubiquinone in plasma.⁽⁹⁾ The researchers concluded: "The concomitant administration of ubiquinone with statins, leading to its increase in plasma, lymphocytes and liver may cooperate in counteracting the adverse effects of statins."

CoQ10 may also be an important neuroprotective agent. Because CoQ10 levels decline with age,⁽¹⁰) accelerating precursors of beta-amyloid deposition, CoQ10 supplementation may be preventive against Alzheimer's disease (AD), Parkinson's disease (PD) and other neurodegenerative disorders.⁽¹¹⁾ In one study, CoQ10 therapy attenuated amyloid beta-peptide toxicity in brain mitochondria isolated from elderly rats.⁽¹²⁾ Hong Kong researchers similarly found in a group of 48 mice (four genotypes), those treated with CoQ10 (1,200 mg/d) after ischemic injury for 28 days had amyloid precursor protein (APP) mutations and smaller infarct volumes, while the volumes of hemisphere and hippocampus on the infarcted side were larger than those treated with placebo, suggesting CoQ10 could protect the brain from ischemic-related atrophy in aged and susceptible transgenic mice.⁽¹³⁾ A follow-up study by the team using 112 aged mice found 2,400 mg/d of CoQ10 exerted a neuroprotective effect against age related neurodegeneration, possibly suggesting application for the nutrient in preventing mild cognitive impairment and AD.⁽¹⁴⁾

A study out of Weill Medical College of Cornell University, New York, found administration of CoQ10 via the diet could protect against the loss of dopamine, exerting neuroprotective effects in a model of PD.⁽¹⁵⁾ Japanese researchers also found a link between oxidized CoQ10 levels in cerebrospinal fluid of patients with amyotrophic lateral sclerosis (ALS), suggesting mitochondrial oxidative damage may play a role in pathogenesis of ALS.⁽¹⁶⁾

Researchers are also examining CoQ10's effects on energy production and athletic performance. "CoQ10 is being increasingly recognized to provide benefits for sustained endurance athletic activities such as running or cycling, as opposed to the more usually recognized benefits associated with weight lifting and muscle mass," Steinford noted. Japanese researchers have reported oral supplementation with CoQ10 (300 mg/d) can improve physical performance in a workload trial,⁽¹⁷⁾ and reduce exercise-induced muscle injury.⁽¹⁸⁾ Similarly, Chinese researchers report CoQ10 supplementation could not only attenuate strain-induced muscle damage, but enhance regeneration.⁽¹⁹⁾ And a trial in 22 aerobically trained and 19 untrained male and female adults who received a placebo or fast-melt CoQ10 supplement for 14 days reported supplementation increased muscle CoQ10 concentration and lowered serum superoxide dismutase (SOD) oxidative stress, while also increasing plasma CoQ10 concentrations and time to exercise exhaustion.⁽²⁰⁾ Finally, CoQ10 also appears to assist in fat oxidation, as supplementation with CoQ10 augments autonomic nervous activity during exercise.⁽²¹⁾

With all these health benefits, it's no wonder consumers are increasingly interested in CoQ10. At the same time, companies are working to deliver quality ingredients and more bioavailable formulations. Holtby noted one of the major talking points in the industry is the difference between ubiquinone and ubiquinol. "The dominant form of CoQ10 in human blood and the liver is ubiquinol, although the common supplement form is the fully oxidized ubiquinone form," he said. "Those who are young and healthy can easily convert CoQ10 to ubiquinol. But as we age, our ability to convert CoQ10 into ubiquinol diminishes, especially for those with chronic disease states."

To serve the broad range of consumers looking to take CoQ10, many companies offer both ubiquinone (standard CoQ10) as well as the reduced form ubiquinol, allowing shoppers to select the product at the price point that works for their health issues. For example, Levin noted NOW offers a wide range of CoQ10 products. "Most are in the very well-researched form of ubiquinone and others are in the newer form of ubiquinol," he said.

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The issue of pricing has been a sensitive one in the CoQ10 area. "The factor of economics has played an important role in making CoQ10 more affordable," Steinford observed. "As late as 2005, the wholesale bulk price of CoQ10 was over $1,200/kg. Now, because of a more diversified group of suppliers, the price of raw material has come down to less than a third of that price. This has allowed the average daily consumption to increase without increased shelf price. This more economical bulk pricing of CoQ10 has also allowed for advanced technology of delivery components, which supports the many higher bio-available products on the market to be affordable. Overall, the profitability and economy of CoQ10 continue to allow it to be a preferred ingredient for both the retailer and the consumer."

Many companies are using innovative technology to increase the bioavailability of CoQ10 in dietary supplements. "Bioavailability of a supplement can be significantly impacted by the delivery system utilized," Holtby said. "Various ingredients have differing characteristics such as solubility in lipids or water, small or large particle size, and granular or crystalline form. Different delivery systems such as tablets, two-piece hard shell capsules, and soft gel capsules have characteristics that lend themselves to optimizing the delivery and absorption of various ingredients. CoQ10, being a highly lipophilic and crystalline material, presents specific challenges that require an innovative approach. … In general, the effect of dosage form on bioavailability depends on the rapidity with which the particular form releases the nutrient into the biological fluids, or how rapidly the nutrient may permeate a cell membrane. Not surprisingly, absorption is most rapid from solutions and decreases in the order: solutions, suspensions, capsules, compressed tablets, coated tablets."

To address those concerns, SGTI developed its CoQsol® and CoQsol-CF™ formulations, using a lipid-based soft gel delivery system, to increase absorption. "A soft gel delivery system plays a key role in enhancing the effectiveness of CoQ10 getting into the bloodstream," Holtby noted. Additionally, SGTI developed the CoQH-CF™ product, soft gels with a liquid inner fill of solubilized Kaneka QH™ ubiquinol plus alpha-lipoic acid, d-limonene and capric and caprylic acid to protect the CoQ10 from oxidation. "This unique soft gel delivery system allows individuals who are unable to process CoQ10 effectively on their own to increase plasma levels of CoQ10 in its reduced form."

AHF is also taking advantage of new technology to increase bioavailability of CoQ10. "The Self Emulsified Drug Delivery System (SEDDS) technology works by converting poor water-soluble CoQ10 into nano-sized particles," Cheatham explained. "This process results in a product with three-to-five times higher bioavailability and absorption into the body's vital organs." An unpublished study compared the bioavailability of Summit Vitamins SEDDS CoQ10 to another brand, and found its softgel had a 287 percent increase in absorption comparatively.

Enzymatic Therapy offers CoQ10 in two different formulations. Smart Q10™ is a unique chewable delivery system featuring Vitaline brand CoQ10; the chews include a natural form of ubiquinone and are available in a variety of flavors. Hanek noted the company's other product, ActiveLife Q10™ features reduced ubiquinol. "Because the conversion rate of CoQ10 to [ubiquinol] tends to decline with age and some people have a tough time converting CoQ10 to its active, reduced form, supplementing with reduced CoQ10 can more easily support cellular energy and overall health," she said. "It is designed for those who cannot properly process CoQ10 or those experiencing a natural decline in CoQ10 production associated with aging."

Bruno said Jarrow Formulas also offers several products in this category, each of which feature natural trans configured CoQ10. "The Q-asborb® products provide ubiquinol, the reduced form of CoQ10," he said. "It is a completely natural proliposome lipid-soluble delivery system clinically shown in humans to increase CoQ10 levels up to 400 percent over baseline."

Naturally, with so many options available, retailers have great opportunity to connect with shoppers. "Most customers are looking to reclaim strength and energy lost with age and see that potential within CoQ10," said Michael Hill, marketing and sales specialist, Reverseage Organics. "The majority of retailers are versed in the health benefits of ubiquinol and CoQ10 and many love the idea of combining CoQ10 with resveratrol, as we do in our Active Ubiquinol CoQ10 with Resveratrol."

Cheatham agreed there is growing demand among both retailers and consumers. "With the aging population, consumers are expressing their concerns about maintaining good health, especially cardiovascular health," he said. "Discerning retailers are not missing the opportunity to increase sales by providing CoQ10 as a solution to these consumer heart health concerns. Retailers are becoming knowledgeable about CoQ10 and its benefits."

Fortunately, the message for consumers is a simple one, Steinford said: "CoQ10 is manufactured by the human body and increased supplementation is important to maintain as we age. CoQ10 is found in every cell of the human body and is an integral part of the process to convert food into energy. The heart is the most energy consumptive organ in the body and requires more CoQ10 than any other organ."

At the same time, retailers should take the opportunity to become versed in the various health effects of CoQ10 and develop ways to converse with shoppers on the potential it poses. "Many retailers have some understanding of the science behind CoQ10, but not really all of the potential applications that this unique and valuable supplement has to offer," Bruno said.

Levin observed the level of knowledge among retailers runs the gamut, but there are opportunities to get educated, and share that knowledge. "Retailers can guide customers to a number of Web-based resources, from manufacturer Web sites to others like PubMed and SupplementInfo.org," he said. Steinford also recommended using educational promotion, such as literature and seminars, to educate consumers about the health effects of CoQ10.

However, Levin added an important caveat—let the research stand on its own to avoid overstepping the legal bounds in talking with customers about products. Under federal law, dietary supplements cannot be sold to treat, cure or mitigate a disease; using third-party literature can help educate customers on the health effects of CoQ10 without putting retailers and their staffs in a tenuous position.

To draw attention to the myriad CoQ10 products available, retailers can also tie them in to a store theme or promotion. "Retailers can effectively sell heart health products by tying them into the heart health themes already created by the media," Cheatham suggested. "Heart health products can be offered at discounted prices periodically and featured in store fliers, window showcases, end-aisles, countertop/floor displays, literature, posters and other POP material. Creative retailers can also utilize co-op advertising in print, radio and TV as a means of communicating the CoQ10 message to customers. In-store seminars, book signings, remote radio broadcasts and similar ingenious activity are also innovative vehicles to attract heart health customers into the store to build customer awareness of CoQ10."

With a little education and effort, retailers can help ensure CoQ10 products find a ubiquitous place in their customers' carts, supporting good health now and in the future.

References

Natural Products Marketplace – February 2010

“CoQ10 at the Heart of the Matter” References

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