Natural Approaches to HDL, LDL and Total Cholesterol #4

Continued from 01.11.11

From heat to sweet, policosanol is a cholesterol-lowering natural product derived from sugar-cane wax with a therapeutic range from 5 to 20 mg/d. Policosanol from honeybee’s wax or rice bran is also available on the market. Policosanol is a combination of long-chain fatty alcohols, including octacosanol, triacontanol, dotriacontanol, tetratriacontanol, hexacosanol, heptacosanol and nonacosanol. Several research studies showed policosanol from sugar cane is effective at reducing cholesterol levels. A 2002 study published in the American Heart Journal reviewed the literature on placebo-controlled lipid-lowering studies using policosanol, and found doses of 10 to 20 mg/d lowered cholesterol by 17 percent to 21 percent and LDL by 21 percent to 29 percent, and raised HDL by 8 percent to 15 percent.12 A year later, a clinical study compared policosanol to the statin drug lovastatin on 28 patients with intermittent claudication.13 Patients who took 10 mg/d of policosanol for 20 weeks experienced a 17.5-percent drop in total cholesterol, a 31-percent drop in LDL cholesterol, and a 31.5-percent rise in HDL cholesterol, while those who took 20 mg/d lovastatin reduced total cholesterol by 18 percent and LDL cholesterol by 22.6 percent. Five lovastatin patients, but none from the policosanol group, experienced adverse events.

Also from the plant cholesterol-lowering area, phytosterols (plant sterols) have attracted a great deal of interest for their effects on cardiovascular health, especially after FDA authorized a claim that allows phytosterol-enriched foods to assert they may reduce the risk of coronary heart disease (CHD) when combined with a diet low in cholesterol and saturated fats. Phytosterols are structurally similar to cholesterol, which makes them compete with cholesterol during absorption in the digestive tract, thereby lowering plasma cholesterol levels.14 According to one review, many clinical trials have proven plant sterols can effectively decrease high serum total and LDL cholesterol by reducing intestinal absorption of cholesterol.15 And an earlier review of 16 published human studies that used phytosterols to reduce plasma cholesterol levels in 590 subjects found phytosterol therapy was accompanied by an average 10-percent reduction in total cholesterol and 13-percent reduction in LDL cholesterol levels.16 Most recently, a 2010 study found daily consumption of plant stanols up to 9 g reduced serum LDL cholesterol concentrations up to 17.4 percent.17

References:

12. Gouni-Berthold I, Berthold HK. “Policosanol: clinical pharmacology and therapeutic significance of a new lipid-lowering agent.” Am Heart J. 2002 Feb;143(2):356-65.
13. Castaño G, et al. “Effects of policosanol and lovastatin in patients with intermittent claudication: a double-blind comparative pilot study.” Angiology. 2003 Jan;54(1):25-38.
14. Heinemann T, Axtmann G, von Bergmann K. “Comparison of intestinal absorption of cholesterol with different plant sterols in man.” Eur J Clin Invest. 1993 Dec;23(12):827-31.
15. Reiner Z, Tedeschi-Reiner E. “[The effects of plant sterols on hypercholesterolemia] [Article in Croatian]” Lijec Vjesn. 2007 Aug-Sep;129(8-9):276-81.
16. Ling WH, Jones PJ. “Dietary phytosterols: a review of metabolism, benefits and side effects.” Life Sci. 1995;57(3):195-206.
17. Mensink RP, et al. “Plant stanols dose-dependently decrease LDL-cholesterol concentrations, but not cholesterol-standardized fat-soluble antioxidant concentrations, at intakes up to 9 g/d.” Am J Clin Nutr. 2010 Jul;92(1):24-33.

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Natural Approaches to HDL, LDL and Total Cholesterol #3

In 1986, Asaf Qureshi at the University of Wisconsin isolated alpha-tocotrienol from barley and found it had cholesterol-lowering properties;4 later, he found delta- and gamma-tocotrienol were the most potent inhibitors of endogenous cholesterol synthesis of all tocotrienols,5 and tocopherol-free tocotrienol worked better in lipid reduction than tocopherol/tocotrienol mixtures.6

A 2006 chicken study on the tocotrienol-rich-fraction (TRF) of palm oil found it produced a dose-response (50 to 2,000 ppm) lowering of serum total and LDL cholesterol levels by 22 percent and 52 percent respectively, compared with the control group.7 Alpha-tocopherol did not affect total or LDL-cholesterol levels, but supplemental alpha-tocotrienol within the 50 to 500 ppm range produced a dose-response lowering of total (17 percent) and LDL (33 percent) cholesterol levels. The more potent gamma and delta isomers yielded dose-response (50 to 2,000 ppm) reductions of serum total (32 percent) and LDL (66 percent) cholesterol levels. HDL cholesterol levels were minimally impacted by the tocotrienols; as a result, the HDL/LDL cholesterol ratios were markedly improved (123 to 150 percent). The researchers concluded the safe dose of various tocotrienols for human consumption might be 200 to 1,000 mg/d based on this study.

Qureshi also reviewed tocotrienol-rich fraction (TRF25) of stabilized and heated rice bran in 90 hypercholesterolemic human subjects and found a dose of 100 mg/d of TRF25, along with the AHA Step-1 diet, produced maximum decreases of 20 percent, 25 percent, 14 percent and 12 percent, respectively, in serum total cholesterol, LDL-cholesterol, apolipoprotein B and triglycerides compared with the baseline values.8

Both SourceOne Global and KGK Synergize Inc. combine palm tocotrienols with polymethoxylated flavones (PMFs) in product formulations. PMFs, one of the main active ingredients in Sytrinol® (manufactured by KGK Synergize Inc. and exclusively marketed by Proprietary Nutritionals), and PMF-Source ™ (SourceOne Global), are a group of compounds derived from the peels of citrus fruits. The two most common are tangeretin and nobiletin, which are potent bioflavonoids. A study conducted by KGK Synergize Inc. found diets containing 1-percent PMFs significantly reduced serum total by 19 to 27 percent and very LDL by 32 to 40 percent.9 That study also found comparable reductions were achieved by feeding a 3-percent mixture of hesperidin and naringin (1:1, w/w), implying a lower potency of hesperidin/naringin versus PMFs.

PMFs were shown to have enhanced bioavailability when offered in soft gels (manufactured by Soft Gel Technologies Inc.) in a clinical trial. The company tested absorption rates of Sytrinol it soft gel form and found tangeretin and nobiletinwere four times more bioavailable compared to powder-filled, two-piece hard shell capsules. Further, the company said this form of Sytrinol was shown in several clinical trials to lower total cholesterol by 20 percent, LDL cholesterol by 22 percent and triglycerides by 28 percent.

Along with vitamin E, another letter vitamin, B3, aka niacin, has been shown to increase HDL cholesterol and decrease overall cholesterol when used in conjunction with statins.10 One unfortunate side effect of niacin is “flushing,” or warmth, tingling and itching of the skin. Flushing can range from minor warm or itchy facial skin to major body discomfort. However, flushing may be reduced by using a time-release formula.11

Dietary enzymes help to increase levels of HDL cholesterol, according to Triarco’s research, which the company said was being prepared for publication at press time. It said a patented blend of digestive protease (as Aminogen®) added to whey protein significantly reduced the increase in LDL and total cholesterol levels seen when whey was consumed without Aminogen®. Aminogen® also increased levels of HDL cholesterol when added Natural

References:

4. Qureshi AA, et al. “The structure of an inhibitor of cholesterol biosynthesis isolated from barley.” J Biol Chem. 1986 Aug 15;261(23):10544-50.
5. Pearce BC, et al. “Hypocholesterolemic activity of synthetic and natural tocotrienols. J Med Chem. 1992 Oct 2;35(20):3595-606.
6. Qureshi AA, et al. “Lowering of serum cholesterol in hypercholesterolemic humans by tocotrienols (palmvitee).” Am J Clin Nutr. 1991 Apr;53(4 Suppl):1021S-1026S.
7. Yu SG, et al. “Dose-response impact of various tocotrienols on serum lipid parameters in 5-week-old female chickens.” Lipids. 2006 May;41(5):453-61.
8. Qureshi AA, et al. “Dose-dependent suppression of serum cholesterol by tocotrienol-rich fraction (TRF25) of rice bran in hypercholesterolemic humans.” Atherosclerosis. 2002 Mar;161(1):199-207.
9. Kurowska EM, Manthey JA. “Hypolipidemic effects and absorption of citrus polymethoxylated flavones in hamsters with diet-induced hypercholesterolemia.” J Agric Food Chem. 2004 May 19;52(10):2879-86.
10. Ceska R, et al. “[Hyperlipoproteinaemia and dyslipoproteinaemia II. Therapy: non-pharmacological and pharmacological approaches]. [Article in Czech]” Vnitr Lek. 2010 Jul;56(7):647-54.
11. Norris RB. “’Flush-free niacin’: dietary supplement may be ‘benefit-free’. Prev Cardiol. 2006 Winter;9(1):64-5.

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What can you tell me about Cholesterol? #2

Statins lower cholesterol by blocking the enzyme responsible for cholesterol production (3-hydroxy-3-methyl-glutaryl-CoA reductase or HMGR) in the liver. Statins may also help the body reabsorb cholesterol that has built up in plaques on artery walls, preventing further blockage in blood vessels and heart attacks.

However, in blocking HMGR, statins also inhibit the production of other important intermediates downstream in the pathway, including coenzyme Q10 (CoQ10), dolichols, hemes and other proteins. Since these intermediates are inhibited by statins, many patients experience side effects ranging from myopathy to anemia and chronic fatigue syndrome, and even temporary memory loss. Patients on statins must also keep in mind most people take them for the rest of their lives. Side effects may be minor, but they could be there forever.

Those who use statins to manage cholesterol levels are often concerned with CoQ10 levels because it shares the biosynthetic pathway with cholesterol. CoQ10 is produced by the human body and is necessary for the basic functioning of cells. Statin usage is known to deplete CoQ10 levels,1 so supplementation is encouraged for those on these drugs. Healthy levels of CoQ10 can reduce the oxidation of LDL cholesterol–the first step in the formation of arterial plaque.2 Further, Italian research showed CoQ10 has a “direct, anti‐atherogenic effect,” and dietary supplementation with CoQ10 resulted in increased levels of ubiquinol‐10 within circulating lipoproteins and increased resistance of human LDL to lipid peroxidation.3

Tocotrienols also inhibit HMGR’s cholesterol synthesis, but does it farther downstream in the process rather than by competitive inhibition. Tocotrienols are members of the vitamin E family and come in alpha, beta, gamma and delta forms. Vitamin E is also made up of four tocopherols (alpha, beta, gamma and delta). Tocotrienols are found in select vegetable oils, wheat germ, barley, saw palmetto, and certain types of nuts and grains.

Tocotrienols work differently than statins by “dialing down” cholesterol synthesis downstream in the process rather than by competitive inhibition. Unlike statins, American River Nutrition pilot studies showed CoQ10 levels increased by 20 percent when patients were taking 75 mg/d of its DeltaGold® tocopherol-free tocotrienol ingredient. Company studies have also shown 75 mg/d annatto tocotrienol/d decreased total cholesterol by 13 percent and LDL by 15 percent, while HDL levels showed a small, but insignificant increase.

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What can you tell me about Cholesterol? #1

Natural Approaches to HDL, LDL and Total Cholesterol

It’s that time of year when consumers buckle down and try to reduce. They want to cut calories, frivolous spending and bad habits. In the past, one of the yearly New Year’s goals may have been to reduce all forms of cholesterol; however, this is not the case anymore as the complexity of cholesterol is continually being explored in medical journals and doctors’ offices. Research has taught us the error of thinking that “getting the numbers down” is the only cholesterol goal. Not all cholesterol is unhealthy; in fact, some even need to work to balance their levels.

Cholesterol is a soft, waxy substance found in the bloodstream. It aids biological functions, such as the production of hormones, and is an essential component of cell membranes. It’s measured in three ways: high-density lipoprotein (HDL), low-density lipoprotein (LDL) and total. LDL cholesterol is known as the "bad" or “lousy” cholesterol. When too much of it circulates in the blood, it can clog arteries, increasing the risk of heart attack and stroke. LDL cholesterol is produced naturally by the body, but many people’s genes tell their bodies to make too much. Others can’t blame their parents because diets rich in saturated fat, trans fats and dietary cholesterol also increase LDL levels.

HDL, termed “good” or “healthy” cholesterol, helps keep LDL cholesterol from getting lodged into artery walls. A healthy level of HDL may also protect against heart attack and stroke, while low levels of HDL (less than 40 mg/dL for men and less than 50 mg/dL for women) have been shown to increase the risk of heart disease.

Cholesterol is either made by the body or consumed from food. The liver and other cells make about 75 percent of blood cholesterol found in the human body; the other 25 percent comes from eating animal products. For many Americans—102 million, according to the American Heart Association—total cholesterol is too high.

Consumers are starting to understand the differences between total, HDL and LDL, and learning how too much of one type—or not enough of another—can put them at risk for coronary heart disease, heart attack or stroke. Cholesterol screenings measure levels of HDL and LDL. If HDL is too low or LDL is too high, health care professionals may prescribe getting regular physical activity, quitting smoking, reducing trans fat consumption and eating a balanced, nutritious diet. If those don’t work, they may write a prescription for a statin, such as atorvastatin (Lipitor), simvastatin (Zocor) or rosuvastatin (Crestor).

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