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46 VITAMIN RETAILER Celebrating 20 Years of Excellence 1994-2014 WWW.VITAMINRETAILER.COM FEBRUARY 2014 T his article will review some of the vital cellular functions and health/wellness applications for coenzyme Q10 (CoQ10), and address safety issues, as well as the difference between reduced (ubiquinone) and oxi- dized (ubiquinol) states of CoQ10, and the most effectively absorbed delivery forms. Vital Cellular Functions CoQ10 is best known for two functions. One is its role in the conversion of glu- cose and fatty acids to ATP (within the mitochondria of cells), the form of ener- gy used to power most body functions. 1 The other is its role as a powerful antioxi- dant in cells, inhibiting lipid peroxidation in cell membranes, DNA and low-density lipoproteins (LDL). 2 Various studies have shown that supplementation with 100 mg of CoQ10 daily is capable of signifi- cantly reducing oxidative damage. 3-5 [Note: CoQ10’s levels in skin decline with age 6 , which may also make skin more susceptible to oxidative damage.] Cardiovascular Disorders Angina In a review of the scientific literature, CoQ10 was shown to be used orally to treat various cardiovascular disorders including angina. 7 In one study, patients with acute myocardial infarction experi- enced a significant reduction in angina, arrhythmias (abnormal heartbeat) and poor heart function when supplemented with 120 mg of CoQ10 daily. 8 In another study, 150 mg of CoQ10 given to angina patients not only increased their blood levels of CoQ10, but also increased their ability to exercise longer. These results lead the researchers to conclude, “This study suggests that CoQ10 is a safe and promising treatment for angina pec- toris.” 9 [Note: Those with acute angina should only exercise in accordance to a physician-approved program.] Congestive Heart Failure A few researchers have said that in many cases, a lack of CoQ10 is the cause of congestive heart failure (CHF). Whether this is ultimately proven to be true, research certainly supports the use of this supplement by patients with CHF. A meta-analysis of eight controlled clini- cal trials of 100 to 200 mg/day CoQ10 treatment of CHF revealed a significant improvement in several important car- diac parameters. 10 Other research on CHF patients using CoQ10 has shown similar benefits, including the improve- ment of quality of life and survival. 11,12 High Blood Pressure Research indicates that CoQ10 affects blood vessels in a way that should cause a decrease in blood pressure. 13 In fact, this has been substantiated in a number of studies where CoQ10 significantly lowered blood pressure in people with hypertension. 14-17 All of these studies used at least 50 mg of CoQ10 taken twice daily. One should expect about 10 weeks of supplementation to pass before looking for results. CoQ10 also has been used successfully to treat diabetics with high blood pressure. In double-blind research, 200 mg and 120 mg were used. 18,19 Parkinson’s Disease In a multicenter, randomized, parallel- group, placebo-controlled, double-blind, dosage-ranging trial, 80 subjects with early Parkinson’s disease where randomly assigned to placebo or CoQ10 at dosages of 300, 600 or 1,200 mg daily for 16 months. The subjects underwent evaluation with the Unified Parkinson Disease Rating Scale (UPDRS), the change in which served as the primary response variable in the total score from baseline to the last visit. The results were that all doses of CoQ10 slowed function- al decline in people with early Parkinson’s disease, although this effect appears to be dose dependent. In addi- tion, the difference between the 1,200 mg and placebo groups were statistically significant. 20 Other research demonstrat- ed that CoQ10 slows function decline in Parkinson’s. 21,22 Diabetes Research has shown that some diabetic patients who use diet to control their SUPPLEMENTSCIENCE CoQ10 as Ubiquinone & Ubiquinol: For Cardiovascular Health & More By Gene Bruno

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46 VITAMIN RETAILER Celebrating 20 Years of Excellence 1994-2014 WWW.VITAMINRETAILER.COM ■ FEBRUARY 2014

T his article will review some of thevital cellular functions andhealth/wellness applications for

coenzyme Q10 (CoQ10), and addresssafety issues, as well as the differencebetween reduced (ubiquinone) and oxi-dized (ubiquinol) states of CoQ10, andthe most effectively absorbed deliveryforms.

Vital Cellular FunctionsCoQ10 is best known for two functions.One is its role in the conversion of glu-cose and fatty acids to ATP (within themitochondria of cells), the form of ener-gy used to power most body functions.1

The other is its role as a powerful antioxi-dant in cells, inhibiting lipid peroxidationin cell membranes, DNA and low-densitylipoproteins (LDL).2 Various studies haveshown that supplementation with 100mg of CoQ10 daily is capable of signifi-cantly reducing oxidative damage.3-5

[Note: CoQ10’s levels in skin decline withage6, which may also make skin moresusceptible to oxidative damage.]

Cardiovascular DisordersAngina

In a review of the scientific literature,CoQ10 was shown to be used orally totreat various cardiovascular disordersincluding angina.7 In one study, patientswith acute myocardial infarction experi-enced a significant reduction in angina,arrhythmias (abnormal heartbeat) and

poor heart function when supplementedwith 120 mg of CoQ10 daily.8 In anotherstudy, 150 mg of CoQ10 given to anginapatients not only increased their bloodlevels of CoQ10, but also increased theirability to exercise longer. These resultslead the researchers to conclude, “Thisstudy suggests that CoQ10 is a safe andpromising treatment for angina pec-toris.”9 [Note: Those with acute anginashould only exercise in accordance to aphysician-approved program.]

Congestive Heart FailureA few researchers have said that in

many cases, a lack of CoQ10 is thecause of congestive heart failure (CHF).Whether this is ultimately proven to betrue, research certainly supports the useof this supplement by patients with CHF.A meta-analysis of eight controlled clini-cal trials of 100 to 200 mg/day CoQ10treatment of CHF revealed a significantimprovement in several important car-diac parameters.10 Other research onCHF patients using CoQ10 has shownsimilar benefits, including the improve-ment of quality of life and survival.11,12

High Blood PressureResearch indicates that CoQ10 affects

blood vessels in a way that should causea decrease in blood pressure.13 In fact,this has been substantiated in a numberof studies where CoQ10 significantlylowered blood pressure in people with

hypertension.14-17 All of these studiesused at least 50 mg of CoQ10 takentwice daily. One should expect about 10weeks of supplementation to pass beforelooking for results. CoQ10 also has beenused successfully to treat diabetics withhigh blood pressure. In double-blindresearch, 200 mg and 120 mg wereused.18,19

Parkinson’s DiseaseIn a multicenter, randomized, parallel-group, placebo-controlled, double-blind,dosage-ranging trial, 80 subjects withearly Parkinson’s disease where randomlyassigned to placebo or CoQ10 atdosages of 300, 600 or 1,200 mg dailyfor 16 months. The subjects underwentevaluation with the Unified ParkinsonDisease Rating Scale (UPDRS), thechange in which served as the primaryresponse variable in the total score frombaseline to the last visit. The results werethat all doses of CoQ10 slowed function-al decline in people with earlyParkinson’s disease, although this effectappears to be dose dependent. In addi-tion, the difference between the 1,200mg and placebo groups were statisticallysignificant.20 Other research demonstrat-ed that CoQ10 slows function decline inParkinson’s.21,22

DiabetesResearch has shown that some diabeticpatients who use diet to control their

SUPPLEMENTSCIENCE

CoQ10 as Ubiquinone & Ubiquinol: For Cardiovascular Health & MoreBy Gene Bruno

blood sugar may have a deficiency ofCoQ10, which may be further exacerbat-ed by certain commonly used anti-dia-betic drugs. Such a CoQ10 deficiency inthe pancreas could impair aspects ofenergy metabolism, and the biosynthesisof insulin.23 Other research has demon-strated that CoQ10 levels are lower indiabetic patients, which can cause dia-betic cardiomyopathy. That sameresearch, however, also showed that thediabetic cardiomyopathy can also bereversed by CoQ10 supplementation.24

Further, research has also demonstratedthat CoQ10 exhibits an effective antiar-rhythmic (i.e., prevents abnormal heartbeat) in patients with diabetes.25 AndCoQ10 has also shown efficacy in treat-ing maternally inherited diabetes mellitusand deafness (MIDD), preventing pro-gressive hearing loss and improvingblood sugar metabolites after exercise.26

Physical PerformanceGiven its role in ATP production, it’s notsurprising that supplementation withCoQ10 has benefit for physical perform-ance. In a double-blind cross-overstudy27, 25 top-level cross-country skierswere given 90 mg/day of CoQ10. Theresults were that all measured indexes ofphysical performance (AET, ANT andVO2Max) improved significantly. Duringsupplementation, 94 percent of the ath-letes felt that the preparation had beenbeneficial in improving their performanceand recovery time vs. only 33 percent inthe placebo periods. Similar benefits inpower increases during exercise wereseen in other double-blind research with100 mg28 and 30 mg29 of CoQ10.

Reduced & Oxidized States CoQ10 can exist in three oxidationstates. The first is ubiquinol, fullyreduced form (CoQ10H2). The second isthe radical semiquinone intermediate(CoQ10H·), and the third is the fully oxi-dized ubiquinone (CoQ10). Most CoQ10products on the market today provideubiquinone, the oxidized version. [Note:Ubiquinone and Ubidecarenone are dif-ferent names for the same substance—CoQ10. Ubiquinone is a generic name.Ubidecarenone is the official name in theUnited States Pharmacopeia (USP)].

However, it is ubiquinol that providesvirtually all of benefits associated withCoQ10. When ubiquinone is supple-mented, the body must first convert it to

ubiquinol before the benefits can beenjoyed. In fact, ubiquinol may bethought of as the “active antioxidant”form of CoQ10. If ubiquinone has notbeen converted to ubiquinol, it is inac-tive as an antioxidant. That is not to saythat ubiquinone has no value. In fact, thebody will convert ubiquinone intoubiquinol30, in which case it will functionas fully active CoQ10.

So is there an advantage to choosingubiquinol over ubiquinone? Perhaps. It istrue that ubiquinol levels tend to declinein various important tissues of the body

in relation to age and disease.31,32

Therefore, supplementing with ubiquinolcan certainly help to compensate; butsupplementing with ubiquinone can alsodo the job. In fact, many if not mostCoQ10 studies have been conducted onolder and diseased people usingubiquinone, and the body convertsubiquinone to ubiqunol anyway. Oneargument in favor of ubiquinol is ahuman clinical study33, which found dailysupplementation with 150 mg ofubiquinol resulted in a 5.9 times increaseof ubiquinol levels after 28 days.

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Nevertheless, this may ultimately be anissue of solubility and absorption.

Therapeutic Value of UbiquinolIn addition to all of the research previ-ously discussed on CoQ10 asubiquinone, supplementation withubiquinol has been researched andfound to offer benefits. Following is abrief review of ubiquinol clinical research.

Down SyndromeChildren with Down syndrome have

decreased levels of ubiquinol com-pared to that of healthy children. Afterthree months of supplementation withubiquinol (10 mg/kg/day, equivalent to228 mg for a 50-lb. child), the averageubiquinol:total CoQ10 ratio increasedsignificantly in Down syndrome chil-dren, with 80 percent of individualratios changing to normal ranges.

Furthermore, ubiquinol supplemen-tation was effective in reducing theoxidative stress in children with Downsyndrome.34

Quality of LifeIn a pilot study, healthy elderly sub-

jects residing in a care home weretreated with 100 mg ubiquinol daily forsix months. The results of assessmentquestionnaires showed significantincreases in the “vitality” and “mentalhealth” scores. This was especially trueof subjects whose initial scores werelow, but markedly improved afterubiquinol therapy.35

CHFPatients with class IV CHF (the most

severe CHF, where patients should beat complete rest, confined to bed orchair; any physical activity brings on dis-comfort and symptoms occur at rest)originally received 450 mg of ordinaryubiquinone CoQ10 daily, but wereswitched to 580 mg of ubiquinol daily.The results were that the amount ofblood pumped out of the ventricle ofthe heart with each beat improved from22 up to 39 percent, and on averagepatients decreased from class IV to II(patients have only slight, mild limitationof activity; they are comfortable withrest or with mild exertion), and someeven decreased to class I (patients haveno limitation of activities; they suffer no

symptoms from ordinary activities).These improvements correlated with theincrease in ubiquinol levels.36

Supplementation & Absorption With CoQ10 benefits undisputed, thereal question is: what is the best way toobtain this critical substance?Surprisingly, diet is not a particularlyeffective means. Typically, dietary sourcesof CoQ10 such as dairy products, eggs,fish and vegetables do not significantlyaffect plasma concentrations ofCoQ10.37 It is possible, however, toincrease the CoQ10 status through theuse of dietary supplements.

CoQ10 powder in the form oftablets, two-piece capsules or soft gelcapsules containing an oil suspension,are the most commonly available typesof CoQ10 supplements on the market.It should be noted, however, that pureCoQ10 is insoluble in water and haslimited, although better, solubility in oilsand fats. As a result, powder-basedproducts tend to dissolve poorly in lab-oratory tests and show relatively poorbioavailability in human testing. Conse-quently, there are significant differencebetween the forms of dietary supple-ments used and the efficacy of CoQ10absorption.38

In a review38 of studies on theabsorption of CoQ10 supplements,large single doses of CoQ10 either as apowder or as an oil-suspension (softgel) resulted in practically no responsein human subjects or a marginalresponse. On the other hand, withongoing dosing there was a dose-dependent increase in plasma CoQ10administered as a soft gel, with a 2.8-fold increase at 30 mg, and a 6.5-foldincrease at 200 mg over a two to threemonth period. In another controlledtrial, supplementation with either 30 or100 mg CoQ10 as a soft gel for twomonths resulted in increases in serumCoQ10 values of 0.637 and 1.575mmol/l from baseline values of 1.483and 1.332 mmol/l, respectively. Whilethese increases sound relatively good,the limited solubility of CoQ10 has alsolimited bioavailability.

Absorption of Solubilized CoQ10To address this issue of limited solubility,a special solubilized form of CoQ10 was

created that allows for 90 to 100 percentof it to be dissolved. This meets the dis-solution standards of the USP—com-pared to 0 to 3 percent of regular, non-soubilized CoQ10, which fails USP stan-dards.39 If it seems that the solubilizedform of CoQ10 would have greaterbioavailability, you are correct. Considerthat solubilized formulations of CoQ10resulted in much higher plasma values,increasing from 0.579 to 3.834 mmol/lwith the solubilized formulation, com-pared to only 0.579 to 1.587 mmol/l witha regular soft gel in just three weeks (seechart).40 This certainly indicated thesuperiority of the solubilized formulationof CoQ10 with regard to bioavailability.

ConclusionCoQ10 is a popular dietary supple-ment, with multiple applications tohuman health, including cardiovascularhealth, Parkinson’s disease, diabetesand physical performance. In addition,CoQ10 is available in the oxidized andreduced states of ubiquinione andubiquinol, respectively—with eitherform offering a viable option for sup-plementation. Furthermore, the use ofeither ubiquinione or ubiquinol in asolubilized form has been shown inresearch to offer considerably betterabsorption/bioavailability than ordi-nary, non-solubilized forms. VR

For a full list of references, visitwww.vitaminretailer.com

SUPPLEMENTSCIENCE

Gene Bruno, MS, MHS, the dean of aca-demics for Huntington College of HealthSciences, is a nutritionist, herbalist,writer and educator. For more than 30years he has educated and trained natu-ral product retailers and health care pro-fessionals, has researched and formulat-ed natural products for dozens of dietarysupplement companies, and has writtenarticles on nutrition, herbal medicine,nutraceuticals and integrative healthissues for trade, consumer magazinesand peer-reviewed publications.