CoQ10 Breakthrough: Our Most Potent Fat-Soluble Antioxidant Now Available in its Natural Reduced Form
Reduced, Electron-Rich Coenzyme Q10 is Now Here

Coenzyme Q10.

It’s a key molecule in one of the 20th century’s most significant Nobel Prize winning discoveries—solving the puzzle of how our cells make energy. It’s in every single one of the fifty trillion cells in our bodies, inside the mitochondria. It’s a potent antioxidant—the only fat-soluble antioxidant our bodies make—and there’s more of it in our cell membranes than any other lipid-based antioxidant.

It’s powerfully protective against cardiovascular disease, and can be of astonishing help to patients suffering heart failure. It may slow the onset of Parkinson’s and Huntington’s disease, and is an indispensable anti-aging nutrient.

It has been called one of the miracle nutrients of our time, and for good reason. Interest in this nutrient is now skyrocketing, with large, multi-center Phase III clinical trials scheduled in Parkinson’s, Huntington’s and Alzheimer’s diseases, and the publication this past June of a 200 page special issue of the journal Mitochondrion entirely devoted to CoQ10 (1).

And yet until now—in fact, for the last 30 years—CoQ10 has only been available as a supplement in its oxidized form. That form is called ubiquinone. To replenish our bodies by taking the supplement, we’ve had to swallow oxidized coenzyme Q10 and convert it to the antioxidant form, known as ubiquinol. Only a small percentage of a standard oral dose of regular CoQ10 is actually bioavailable, according to cardiologist Salvatore Pepe of the Department of Cardiothoracic Surgery at Alfred Hospital and Monash University in Australia (2). Even so, CoQ10 is so potent that the oxidized supplement alone has been the subject of over 1500 peer-reviewed studies on the supplement’s powerful protective health effects. In some studies, individuals have needed doses as high as 3,000 milligrams a day of ubiquinone to increase blood levels enough to make a difference in disease.

But now all that has changed. A new form of stable ubiquinol, the actual antioxidant form of coenzyme Q10, has been made available in a stable form for the first time. Ubiquinol is the form that is found 95% of the time in our blood, the form that actually quenches free radicals and helps prevent disease. It is also seems to have a higher degree of bioavailability. Initial studies and impressive word-of-mouth suggest the manufacture of ubiquinol is a major biochemical feat that will have far-reaching health consequences, and allow us to study CoQ10’s impact on aging and disease much more effectively.

In brief, here are a few impressive highlights of the new research:

• Ubiquinol is so readily bioavailable in comparison to ubiquinone (oxidized CoQ10) that plasma levels increased from .59 µg/ml to .91 µg/ml in young people, and from .82 µg/ml to 1.33 µg/ml in older healthy people after supplementation.
• When healthy volunteers in their fifties took regular CoQ10 for a year, they could not attain the plasma levels that similar volunteers attained in a mere 3 months with the new CoQ10.
• When individuals were given 300 milligrams daily of ubiquinol for four weeks, their blood levels increased eleven-fold over baseline, a remarkably high level.
• In a recent study, ubiquinol was given to children at both low and high doses—1 mg/kilogram of weight and 10 mg/kilogram of weight per day for one month. Blood levels were comparable to data from studies involving much higher doses of regular CoQ10 (2400 to 3000 mg/day).
• The highest net increase in blood levels in any study to date occurred using ubiquinol at a dose of 600 milligrams daily. Levels of 10.7 umol/L were achieved—higher than in any previous study of CoQ10.
• Early case reports indicate that ubiquinol packs a powerful punch and may save lives. In one report, a Class IV heart patient dying of heart failure, with an ejection fraction of only 15%, and little response to regular CoQ10, took ubiquinol and nearly tripled his ejection fraction.

The Power of CoQ10: Highlights of 30 Years of Remarkable Research

You probably know it well: that orange colored powder or gel supplement called coenzyme Q10, one of the most popular nutritional supplements of the last few decades, so effective that in 2006 health-conscious individuals bought over $400 million worth of the supplement. The nutrient has a remarkable safety profile, and as remarkable a history of benefiting individuals with heart disease, diabetes, and neurodegenerative diseases like Parkinson’s and Huntington’s. In a major NIH-funded study on Parkinson’s patients, CoQ10 supplements slowed disability by 44%.

CoQ10 is best known for its protective effect on the heart, with over 35 placebo controlled trials in cardiovascular disease. It contributes to 95% of the cellular ATP production to the heart muscle. In Japan it has been an approved drug for congestive heart failure for the last 30 years.

Even aging skin seems linked to decreased CoQ10. Between the ages of 30 and 80, levels of CoQ10 in the epidermis drop dramatically. CoQ10 may protect the skin against damage from UV radiation.

Coenzyme Q10 has two pivotal roles in our bodies: energy metabolism and lipid-soluble antioxidant protection. CoQ10 is a key factor in producing ATP, the universal energy currency of all living cells. In 1978, scientist Peter Mitchell was awarded the Nobel Prize for deciphering how electron transfer in cells is coupled to ATP synthesis. CoQ10 is an essential co-factor in this process. It is a carrier in the mitochondrial electron transport chain.

Interestingly, white blood cells contain high amounts of CoQ10, while red blood cells have very little. In one study it was found that there was a clear, dose-dependent relationship between CoQ10 and ATP in white blood cells. Scientists looked at ascorbic acid, vitamin E, riboflavin, thiamine, niacin, vitamin K and carnitine. But none had a significant effect on ATP synthesis. Only CoQ10 did.

Just as important is its lipid antioxidant ability, especially because it is inside the cell, the mitochondria, and in our cell membranes. It is the most important antioxidant nutrient in the mitochondria. As pharmaceutical scientist Randar S. Sohal and his colleagues at the University of Southern California note in the June issue of Mitochondrion (3), “Oxygen is the basis of our life on earth. And yet, paradoxically, it is a very toxic substance under a number of conditions. Oxygen radicals, such as hydrogen peroxide, singlet oxygen, and ozone, are called reactive oxygen species (ROS). But all organisms have antioxidant defense systems to limit ROS.”

Like all antioxidants, CoQ10 exists in an electron-rich (called “reduced”) form, which donates electrons to highly reactive, unstable molecules like peroxides—and stabilizes them. That’s ubiquinol. Once it has donated its electrons, it is oxidized. That’s ubiquinone. Then it needs to be recycled so it once again becomes electron rich (“reduced” back to the ubiquinol form).

Because of its energy-rich, antioxidant-rich ability, there can hardly be a more significant impact than CoQ10’s on aging and health. Biosynthesis of CoQ10 occurs in all tissues and cells in animals and is present in all membranes. It is found in particularly high levels in the heart, kidney, and liver, as well as the muscle, pancreas and thyroid (Figure 1).

When we are young and healthy, we synthesize CoQ10 entirely ourselves. As we age, we make less and less. And if we’re chronically ill, we rapidly deplete this essential substance. It’s hard to get CoQ10 from our diet (15 pounds of peanut butter contains 100 milligrams, a reasonable daily supplement; three pounds of sardines, a food ‘rich’ in CoQ10, provides 100 milligrams as well). And as we lose our ability to synthesize enough of it, we end up vulnerable to aging and ill health (Figure 2). As our CoQ10 stores fall because of increased metabolic demand, disease, deficiency of precursors and enzymes that synthesize it, and oxidative stress, we suffer. That slow, continuous decline becomes apparent around forty years of age, and according to Robert J. Barry, Ph.D., a former advisor for the National Institute of Health, and currently in Scientific Affairs at Kaneka Nutrients, the world’s leading supplier of CoQ10, is linked to age-related conditions such as heart disease, neurodegenerative diseases, cancer, diabetes, and the profound loss of stamina and energy that we all associate with growing old (4).

As Dr. Barry states: “It is very important to note that CoQ10 concentrations in the body decrease steadily as we age, and this decrease has been associated with the aging process itself, as well as age-related degenerative diseases”(5). According to Barry, levels start declining around age 20 and by age 40 the drop is noticeable. Peak values in the lungs, heart, spleen, liver, and kidneys are observed at 20 years of age (Figure 2).

“A steady, lifetime decrease in CoQ10 is far more common than we may have assumed,” states biochemist Magnus Bentinger of Stockholm University and the Rolf Luft Center for Diabetes and Endocrinology in Stockholm (6).

CoQ10 is the only lipid-soluble antioxidant we make, present in all membranes. Forty years of research has shown that CoQ10 prevents both lipid and protein oxidation, and even DNA oxidation (3). And it prevents both the initiation and the propagation of lipid peroxidation (unlike, for instance, vitamin E, which only inhibits propagation).

Because CoQ10 is essential for the production of cellular energy, supplementing it enhances stamina and health. Millions of people have taken CoQ10 supplements with no reported toxicity in over a thousand human and clinical trials. According to Dr. Barry, “Some reports say this decline in coenzyme Q10 becomes apparent around 40 years of age, some reports say as early as 20 years with slow but continuous decline.  The result is less cellular energy, slower conversion to the reduced form and subsequently diminished protection against oxidative insult.”

Ubiquinol: Why the Antioxidant Form of CoQ10 is So Potent

The antioxidant action of the reduced form of CoQ10 (ubiquinol) is now considered to be one of its most important protective functions in cellular systems. As pure as snow (because it is not oxidized, the familiar orange color of regular CoQ10), ubiquinol was first manufactured and commercially available in stable form in 2006, by Kaneka Pharmaceuticals, the world’s primary manufacturer of ubiquinone. Ubiquinol carries two additional hydrogen atoms—two extra electrons. Biologically, the difference between the two is therefore enormous.

Autopsies and fresh animal dissection show that ubiquinol is the main form of CoQ10 in tissues. And similarly, about 95% of CoQ10 in the blood is in the form of ubiquinol. In the blood, CoQ10 helps regenerate vitamin E. It protects against the oxidation of cholesterol—more powerfully than other major antioxidants including lycopene, beta-carotene, and tocopherol (7).

Disorders marked by oxidative stress cause large shifts in the amounts of ubiquinol and ubiquinone in the body. This is referred to as the ratio (ubiquinol:ubiquinone). In a 2005 Japanese study of diabetics, oxidative stress increased over the course of the day, while the ratio declined. Another 2005 study found that diabetics have an astounding 75% less ubiquinol overall compared to healthy individuals (Figure 3). The same profound loss of ubiquinol was found in people with chronic liver disorders such as hepatitis, cirrhosis and hepatoma.

Ubiquinol: Uniquely Bioavailable

Perhaps the most impressive aspect of the new ubiquinol data is how bioavailable the supplement is. It is absorbed quickly and in high amounts in older people—far higher than regular CoQ10. This is an extremely strong indication that the body needs and wants to assimilate ubiquinol. Based on recently published absorption studies, just 150 mg per day of ubiquinol would provide virtually the same high CoQ10 blood levels as 1200 mg of enhanced-delivery ubiquinone CoQ10. Human studies show that ubiquinol increases blood CoQ10 levels several times more efficiently than ubiquinone (8,9) (Figure 4).

According to a review in Mitochondrion by Hemmi Bhagavan and Raj Chopra (7), individuals taking 300 milligrams of ubiquinol for four weeks daily reached “a markedly high value of 8.413 umol/L, an 11-fold increase over baseline.” And according to the authors, when children were given either 1 milligram per kilogram of body weight per day, or a high dose of 10 milligrams per kilogram of body weight per day, after one month their blood levels were comparable to the levels achieved by much higher doses of ubiquinone (up to 3000 milligrams a day).

CoQ10 is better absorbed with fat (this was first discovered by asking patients to consume it with peanut butter). Soluble gel forms of CoQ10 are better absorbed overall. According to Bhagavan and Chopra, solubilized ubiquinone is “far superior to the powder-based” supplements, and “solubilized ubiquinol is even better.” In other words, solubilized ubiquinol seems to be best of all.

Aging is Dramatically Slowed by Ubiquinol in Special Mice Studies

Sometimes a picture literally is worth a thousand words. And this picture of 3 “senescence-accelerated mice” at age 14 months is just that (Figure 5) (10).

These are mice bred to age quickly, so that we can study markers of aging more effectively. Senescence-accelerated mice grow normally, but show early signs of aging, including markedly reduced physical activity, loss of hair glossiness, coarse skin, hair loss, lesions in and around the eye, and curvature of the spine. The control mouse looks painfully hunched and aged, the victim of severe degenerative changes. The mouse given regular CoQ10 looks a bit better, but still has aged rapidly. However, the mouse given ubiquinol is in far better shape than its peers.

It turns out that ubiquinol is 40% more effective than conventional CoQ10 in slowing aging markers in middle-aged senescent-accelerated mice, and over 50% more effective than no supplementation at all. At around three months of age, aging started to spike in the control group. When middle age set in (at about eight months), both ubiquinol and ubiquinone were helpful, slowing aging by about 45%.

It was at 10 months of age that the remarkable data showed up. By ten months, mice receiving ubiquinol aged 51% slower than the control group and 40% slower than the group receiving ubiquinone. And by twelve months, according to the researchers, the control mice were immobile and unresponsive, showing lesions in and around the eye, with spinal and limb deformities and a patchy, discolored coat. In contrast, the aging mice supplemented with ubiquinol were reported to be alert, responsive and energetic with no physical lesions or deformities, and a glossy coat resembling that of a young, healthy mouse (10).

In other unpublished research, the same scientists looked at the anti-fatigue effects of the ubiquinol and ubiquinone in aged rats. A control group receiving no CoQ10 showed a slight decline in treadmill running time. In a group receiving regular CoQ10, running times increased 60%. But the ubiquinol group outshone them all: their treadmill times increased a remarkable 150%. 

This is impressive news considering regular CoQ10’s already remarkable efficacy profile: A meta-analysis of the use of CoQ10 in randomized clinical trials in patients with congestive heart failure showed a significant and clinically relevant improvement of heart function, in some cases doubling the survival rate. What even more remarkable news might ubiquinol hold for the heart? According to Dr. Barry, “A cardiology group is submitting a case report to a refereed medical journal. Look at Figure 6: the patient was already on regular CoQ10, which helped to some degree. Three months later, after 450 milligrams of ubiquinol daily, his ejection fraction had almost tripled. The doctors said they had never seen this type of recovery before. Now other cardiology groups in the U.S. are interested and will be initiating their own studies.”

The Future: How Much Ubiquinol to Take

The importance of CoQ10 (ubiquinone) should not be disqualified and has nearly 30 years of research and clinical evaluation demonstrating its considerable health benefits and excellent safety profile, according to Dr. Barry. As a healthy twenty year old you are likely to readily biosynthesize all the ubiquinol (reduced CoQ10) you can use. But as you age, he says, “you produce less, and the result is less cellular energy, slower conversion to the reduced form and subsequently diminished protection against oxidative insult. Ubiquinol provides a strong first stage defense against cellular oxidative insult/disease and needs to be replenished to maintain optimum health.”

“In terms of dosages,” says Dr. Barry, “of course patients should always consult with their healthcare provider first before taking any supplement. Just as a general rule, and everyone is different, if you’ve never taken CoQ10 and are going to start taking ubiquinol, research shows that for the first two or three weeks, if you take 2-300 milligrams per day, the levels in your plasma plateau out during this period of time, and then 50-100 milligrams a day is a good maintenance dose. If you’re over age 40 or have any type of metabolic disease that would indicate an ongoing level of oxidative stress, ubiquinol may be more effective.”

If you are already on CoQ10, Dr. Barry notes that, “Case studies with cardiology patients show that higher levels of ubiquinol may be useful. The cardiology study used 450 milligrams a day. Doctors can have plasma levels taken.”

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