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Optimizing Cholesterol Levels (The Cholesterol Balancing Act)

Steve Myers
06/11/2008

Cholesterol is a “four-letter word” with 11 letters. The immediate connotation is something bad, a monster out to wreak havoc on the circulatory system. However, presence alone is not the nightmare, but the proliferation of certain types of cholesterol can contribute to the progression of heart disease, the number one killer in America and other parts of the world.

As its name suggests, cholesterol is a sterol, an unsaturated waxy solid. Considering a sterol is a combination of steroid and alcohol, cholesterol’s public image could be worse. It is a lipid manufactured in the body and has important functions relative to cell membrane management. Plus, it is known to help produce bile to digest fats, and can also assist in metabolizing fat-soluble vitamins.

The key to why cholesterol can be problematic is the transportation of these lipids, which occurs in the bloodstream. Many factors contribute to atherosclerosis (hardening of arteries by build-up and eruption of plaques in the artery walls), with excessive cholesterol in the blood being only one culprit.

Cholesterol is made in tissue membranes or derived through the diet. Herein lies the basis for “good” and “bad” cholesterol. Cholesterol is not very soluble in water, so it needs a transporter in the blood stream. Cholesterol made in tissue membranes is transported by high-density lipoprotein (HDL), which delivers it to the liver. It is hypothesized that HDL also removes cholesterol from arteries and delivers it back to the liver for processing. Increased levels of HDL have been deemed protective against heart disease.

On the other side, dietary cholesterol is transported by low-density lipoprotein (LDL), which carries cholesterol from the liver to the tissue membranes. This doesn’t make LDL-bound cholesterol inherently bad; the danger is the amount of cholesterol in the wrong place at the wrong time. Excessive amounts of cholesterol and LDL in the arteries can contribute to plaques that damage the arteries over time, leading to heart attack, stroke or some other manifestation of heart and vascular diseases. There seems to be a correlation between risk of atherosclerosis and the size of LDL particles, with the smaller LDL being considered more problematic. Even still, science is showing oxidized LDL is more likely to end up trapped in the web of matter that collects in arteries to become a plaque.

For these reasons, cholesterol management for heart and vascular health focuses on lowering LDL cholesterol, especially small LDL, and limiting LDL oxidation, often called lipid peroxidation. Often overlooked is the value of raising HDL cholesterol levels, which can improve removal of cholesterol from dangerous locations in the arteries. Further still, very low density lipoprotein (VLDL) contain triglycerides—a compound with three fatty acids—that are commonly packaged with cholesterol and released for use as energy; however, high levels of triglycerides have correlated to high total cholesterol and low HDL, so lowering triglycerides has become part of the cholesterol management spectrum of goals.

A Natural Approach

The diet greatly influences health, and addressing macro- and micro-nutrients is a good place to start influencing cholesterol health. Macro-nutrients that affect cholesterol include fiber, protein and fats. Micro-nutrients include vitamins and minerals, particularly those with potent antioxidant mechanism that can affect lipid peroxidation.

Fiber has long been a recommendation of the American Heart Association (AHA), with the emphasis being on soluble fiber, such as oats and barley. Oats and whole oat products were approved for a heart health claim by FDA in 1995, due to the amount of research showing that adding oat bran to the diet can lower total and LDL cholesterol levels, while raising HDL levels.1,2

Specific oat fiber products on market have turned in positive results. Adding just 6 g/d oat beta glucans as OatVantage™, a branded ingredient made by GTC Nutrition and found in cholesterol management finished products, has significantly lowered total and LDL cholesterol in 75 hypercholesterolemic study subjects.3 Likewise, the same amount of oat glucans, this time as Nutrim™, an ingredient from FutureCeuticals, consumed in conjunction with the AHA’s Step Diet more effectively lowered LDL than did diet alone in men with mild to moderate hypercholesterolemia.4 In a similar vein, between 3 g/d and 5 g/d of barley beta glucans—as Barliv™, from Cargill—taken for six weeks decreased LDL by as much as 15 percent.5

For the more adventurous, a fiber from the Opuntia ficus indica cactus branded as NeoPuntia®, from Bio Serae laboratories, may raise HDL levels and lower triglycerides, when adding as little as 1.6 g/d of the fiber ingredient to the diet.6

Fiber can be straightforward, whereas the trick with protein is always in finding a good source without the saturated fat and cholesterol that can negate any of the macronutrient’s benefits. Whey protein may be animal-based, but it has been shown, to lower LDL cholesterol, at least when taken in hydrolyzed form.7 However, many people have looked to soy to provide cholesterol-managing protein. In fact, FDA approved a health claim in 1999 for soy protein and decreased heart disease risk. While this does not specifically reward soy for its cholesterol lowering actions, studies showing 25 g/d of soy reduces LDL by as much as 10 percent went a long way to support the FDA claim.

The science on soy and cholesterol is robust, but is still not definitive. Soy protein can lower triglycerides and both total and LDL cholesterol, while raising HDL levels.8,9 It may do so via several mechanisms, including affecting expression of genes involved in fat metabolism.10

Like cholesterol itself, fat gets a bad rep. But, as the world is slowly learning, there are good fats and bad fats, and it isn’t even that simple. There is much debate over the ideal ratio of omega-6s to omega-3s, both considered good fats. The lesson? With cholesterol and fats, it’s not just about the good and the bad, but how much of each kind is in the body.

As far as cholesterol management via natural products, marine polyunsaturated fats (PUFAs) appear to be the heroes. Researchers learned eating fish twice or more per week can lower triglycerides and raise HDL significantly more than eating fish only once per week or less.11 The primary PUFAs in fish are docosahexaenoic acid (DHA) and eicosapentaenoic acid (EPA). FDA even approved a prescription therapeutic dose of 2 to 4 g/d EPA and DHA for regulating very high triglyceride levels (>500mg/dL).12

Douglas MacKay, N.D., research advisor to Nordic Naturals, stressed fish oil does not reduce LDL, as all the clinical trials show fish oil reduces triglycerides—by as much 30 percent. “What fish oil does for cholesterol is it changes the ratio and quantity of the cholesterol sub-particles,” he explained. “Fish oil supplementation leads to more large, buoyant cholesterol sub-particles (reduces the risk for cardiac event), and less small, dense cholesterol sub-particles that could increase the risk for a cardiac event.”

Newer to the marine omega scene is krill oil, from shrimp-like crustaceans. In fact, krill oil has compared favorably to fish in lowering cholesterol levels. A Canadian trial found 1 to 3 g/d krill oil lowered triglycerides, and both total and LDL cholesterol, in addition to raising HDL, more effectively than 3 g/d fish oil (3:2 EPA:DHA ratio) or placebo.13

For retailers and consumers searching for a one-two punch, many manufacturers have combined omega-3s with other heart healthy ingredients, such as fatty alcohols (from plant waxes) and phytosterols (the plant version of cholesterol).

Of four interventions in a Canadian trial—fish oil, sunflower seed oil, fish-oil-sterol combo and plant oil-sterol combo—the fish oil, combined with plant sterols, best increased HDL levels, although both sterol interventions lowered LDL cholesterol and total:HDL ratio.14 Plant sterols alone have demonstrated beneficial cholesterol management properties, especially when incorporated into fatty foods,15,16 although encapsulated plant sterols have shown similar benefits.17

Omega-3s and omega-6s, combined with policosanol, a fatty alcohol derived from sugar cane, have shown promise in boosting HDL levels while lowering non-HDL levels,18 especially in subjects with diabetes, a disease that goes hand-in-hand with heart disease.19

On the smaller level of dietary approach, micro-nutrients, such as vitamins and minerals, can be very helpful to natural cholesterol management. Vitamin E tops many heart doctors’ nutrient interventions, based on study reports that supplementing with the vitamin can help lower LDL cholesterol and risk of atherosclerosis, the formation of plaques.20

Vitamin E can be found as tocotrienol or tocopherol compounds; both have shown promise against cholesterol. Tocotrienols from annatto, palm and rice have shown the ability to lower total and LDL cholesterol, in addition to increasing HDL levels in some trials.21,22,23 Tocopherols might have similar actions, dependent on the form, either alpha- or gamma-tocopherol. The alpha form has helped researchers raise HDL levels in statin therapy,24 while gamma-tocopherols have reduced LDL cholesterol and platelet aggregation (blood cell adhesion leading to clotting).25 Exemplifying a team mentality, a mixture of tocopherols and tocotrienols from palm oil decreased overall cholesterol levels more than did tocotrienols or carotenoids alone.26

One of vitamin E’s biggest contributions to cholesterol health is antioxidant activities, which seem to thrive in combination with vitamin C.27 In fact, an antioxidant combination of 400 IU/d vitamin E and 500 mg/d vitamin C for six weeks in youth with hypercholesterolemia or hyperlipidemia (raised levels of lipids or lipoproteins in the blood) improved endothelial function and inhibited progression of atherosclerosis.28

B vitamins also play a role in cholesterol management, including protection against lipid peroxidation. Folate supplementation in vivo has kept homocysteine in check and guarded LDL and VLDL from oxidation.29

Fellow B vitamin niacin contributes in a non-antioxidant mechanism, lowering LDL cholesterol and triglycerides; however, it’s most notable for its ability to significantly raise HDL, an important, if not overlooked, aspect of cholesterol management.30

Niacin combined with chromium might offer adjunctive benefits, as this intervention has led to improvements to mechanisms of cholesterol transport between the tissues and liver.31 Researchers reported the combination therapy in hyperlipidemic animals reversed increased lipid peroxidation and increased aortic levels of an important endogenous antioxidant, glutathione.

As for other minerals, copper and selenium have shown promise in fighting oxidative stress and lipid peroxidation in the cardiovascular system.32,33

Free Radicals, Free Your Health

The theory of limiting oxidative stress and lipid peroxidation in the arteries is a popular component of cardiovascular disease cholesterol management. While micro-nutrients provide a good level of protection from oxidation, a large contingent of the antioxidant cavalry comes from botanicals, from flavonoids to carotenoids.

Flavonoids and other polyphenols are the roots of cholesterol care for many botanical-based products, including cocoa, tea and fruit. The flavanols in cocoa provide its defense against cholesterol, including its ability to decrease LDL and increase HDL.34 However, chocolate enriched with plant sterols and stanols more effectively reduced total and LDL concentrations than did non-enriched chocolate, according to researchers.35

As in cocoa, the main cholesterol oxidation retardants in green tea are its flavanol catechins. In one cardio trial, subjects in the high-catechin group experienced greater LDL reduction than those in the low-catechin group.36 Another study has shown less effect by tea catechins on LDL, but marked effects on raising HDL.37

Citrus bioflavonoids also weigh in on antioxidant cholesterol management. Combined with the antioxidant vitamin E tocotrienols, citrus bioflavnoids can reduce total cholesterol by as much as 30 percent, LDL by as much as 27 percent and triglycerides by as much as 34 percent.38

Fruit is another source of polyphenols for cholesterol monitoring. Grape polyphenols such as anthocyanins provide those on a high-cholesterol diet a means of lowering triglycerides and VLDL levels, via alteration of cholesterol metabolism in the liver.39 And grape seed extract containing between containing 200 mg or 400 mg of proanthocyanidins can help limit LDL oxidation.40

Pomegranate, another anthocyanin-rich fruit, has also delivered solid antioxidant results on cholesterol, reducing not only LDL levels but also LDL oxidation rates, in addition to moderating other characteristics of atherosclerosis development.41

Beyond flavonoids, botanicals such as garlic contain other antioxidant constituents, including organosulfur compounds. Aged garlic extract (AGE) has turned in some startling results on cholesterol, restricting diet-induced high cholesterol in one trial,42 and safeguard against oxidation of LDL particles in another trial.43 While many have focused on AGE’s allicin content, some research has suggested saponins in garlic are to credit for the herb’s ability to lower total and LDL cholesterol while maintaining HDL levels.44

French pine bark extract, also known as Pycnogenol, counts bioflavonoids, catechins, phenolic acids and other compounds for its various benefits, including the area of cholesterol health. One study confirmed Pycnogenol supplementation for six weeks significantly increased HDL levels while reducing LDL levels.45

Plants and certain algae are also home to carotenoids, which provide colorful pigments as well as antioxidant punch against cholesterol problems. Lycopene, most known as the tomato carotenoid, has inhibited lipid peroxidation in hypertensive patients.46 Early in vitro work suggests lycopene confers its benefits by reducing macrophage foam cell formation (a key step in formation of plaques) thereby decreasing lipid synthesis.47

From the garden to the pond, astaxanthin is a carotenoid common to microalgae and may help retard oxidation of cholesterol lipids.48 This carotenoid has also reduced triglycerides and increased HDL levels in subjects with metabolic syndrome.49 In proprietary research from Cyanotech, has shown BioAstin brand astaxanthin can drop total and LDL cholesterol by as much as 17 percent and triglycerides by 24 percent.50

Guiding Consumers’ Cholesterol Shopping

As with other areas of the typical health food store, the shelves devoted to cardiovascular health are crowded with all types of heart products, not to mention formulas tailored specifically for cholesterol. As big a deal as cholesterol management has become, is there room for a bunch of single-ingredient formulas, or do multiple-ingredient products make more sense for both economy of space and maximized benefits for consumers?

“We definitely know that multiple ingredient formulas work much more effectively,” said Gary Stanton, president, New Health Corp., which makes Heart Savior—plant sterols, policosanol, guggulipid and red yeast rice and selenium and coenzyme Q10 (CoQ10). “For example, plant sterols are great at blocking dietary cholesterol, but do nothing for cholesterol produced by the liver; red yeast rice, policosanol and niacin have different mechanisms of action that reduce cholesterol produced by the human body by inhibiting the production of cholesterol in the liver. We are seeing consumers ... opting for a combination of ingredients over single ingredient products.”

Similarly, CholestSolve 24/7™ from American Biosciences focuses on plant sterols—which have been a popular mainstay in cholesterol-lowering margarines—but also benefits from the researched lipid-control actions of CoQ10 and various flavonoids from wine, grapes and green tea. Ditto for Country Life, which offers Total Lipid Control formula, a combination of cholesterol modifying plant sterols with omega-3 EPA and DHA, as CardiaBeat™ branded ingredient from Enzymotec.

MacKay advised the best combination is exercise, a fiber supplement, fish oil, and one specific cholesterol lowering ingredient (niacin, red yeast rice or policosanol). “If the one ingredient does not seem to do the trick, switch to another,” he said. “I have found that these products work for some but not others, so switching is key.”

Another concern for consumers is whether the products they are taking for cholesterol are having the intended health benefit. As with many natural products, changing the course of cholesterol is not an overnight feat. However, without regular cholesterol screening/testing, consumers have no idea of any true changes. Thus, it is good for retailers to be aware of the average time-to-effect of products in this category, so that they can inform consumers when to expect changes in their cholesterol test results.

“Most of our customers are expecting to see some benefit within 60 days,” Stanton said, noting quality ingredients in the proper form and dosage can absolutely deliver measurable benefits in this time frame. “Within 60 days, results are clearly evident.”

MacKay confirmed: “You can not feel your cholesterol go up or down; cholesterol is tested in the blood. Typically you should give any treatment plan for cholesterol three months and then have your blood re-tested—you will then know if it is working.”

Retailers, consumers and their health care providers might not associate creatine with cholesterol, but the research is telling the tale. All American’s Kre-Alkalyn, a stable, pH-adjusted creatine product has recently been shown in scientific research to help with cholesterol care. “We sort of stumbled onto this [benefit],” Archer admitted. “The research is showing some positive results on cholesterol, namely that Kre-Alkalyn can lower bad cholesterol and raise good cholesterol.” He noted previously, creatine has shown an ability to help with good cholesterol, but never with bad cholesterol, until now.

Whether a single- or multiple-ingredient approach, there are many well-researched ways to help consumers keep cholesterol levels in check, lowering the bad, while raising the good. Keeping inventory tied to the vitamins, minerals, herbs and specialty supplements shown by science to affect cholesterol and triglyceride levels is a way for retailers to send a strong, well-supported message to consumers about their heart health preventive care.

References

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