POLICOSANOL

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LE Magazine June 2001

 

 

 

A Natural Anti-Cholesterol Dietary Supplement

 

POLICOSANOL

 

Heart attack and stroke have been associated with high levels of a type of

cholesterol known as low-density lipoprotein (LDL) (“bad” cholesterol) and low

levels of high-density lipoprotein (HDL) (“good” cholesterol). Reversing these

trends can lower the risk for these and other artery-related diseases.

 

Policosanol is a supplement that can normalize cholesterol as well or better

than drugs, without side effects.(1) Efficacy and safety have been proven in

numerous clinical trials, and it has been used by millions of people in other

countries. Policosanol can lower LDL cholesterol as much as 20% and raise

protective HDL cholesterol by 10%. This compares favorably with

cholesterol-lowering drugs which have the drawback of side effects such as liver

dysfunction and muscle atrophy. Policosanol is free of these side effects.

 

Policosanol works by blocking the synthesis of cholesterol. It does not inhibit

the HMG-CoA enzyme like the “statin” cholesterol-lowering drugs, but it may

inhibit a different enzyme. Its exact mechanism is not known.

 

What makes policosanol exciting is that it has other actions against heart

disease in addition to lowering cholesterol. Like statin drugs, policosanol

helps stop the formation of artery lesions.(2) This was proven in studies on

rabbits fed a diet designed to create high cholesterol:

 

“In most policosanol-treated animals, atherosclerotic lesions were not present,

and in others, thickness of fatty streaks had less foam cell layers than in

controls.”(3)

One of policosanol’s important actions is to inhibit the oxidation of LDL.(4)

Oxidized LDL is dangerous. It promotes the destruction of blood vessels by

creating a chronic inflammatory response. Oxidized LDL can also provoke

metalloproteinase enzymes.(5) These enzymes promote blood vessel destruction,

partly by interfering with HDL’s protective effect. Studies show that rats

treated with policosanol have fewer foam cells, reflecting less inflammatory

response causing less blood vessel destruction.(6,7)

 

Another action of policosanol is to reduce the proliferation of cells. Healthy

arteries are lined with a smooth layer of cells so that blood can race through

with no resistance. One of the features of diseased arteries is that this layer

becomes thick and overgrown with cells.

As the artery narrows, blood flow slows down or is blocked completely.

Policosanol was tested for its ability to stop the proliferation of these

cells.(8) According to the results, policosanol’s ability to stop cell

overgrowth “is in agreement with the antiproliferative effects reported for

other lipid-lowering drugs, such as most of the statins.”(9)

 

Policosanol is a natural supplement made from sugar cane.

Policosanol also inhibits the formation of clots, and may work synergistically

with aspirin in this respect. In a comparison of aspirin and policosanol,

aspirin was better at reducing one type of platelet aggregation (clumping

together of blood cells). But policosanol was better at inhibiting another type.

Together, policosanol and aspirin worked better than either alone.(10,11) A

related effect is that significant reductions in the level of thromboxane occur

in humans after two weeks of policosanol.(12) Thromboxane is a blood

vessel-constricting eicosanoid produced by platelets. (Note: eicosanoids are

powerful chemicals created in cells that can do things like create fever to kill

infections, make blood vessels in lungs expand so you can breathe, and reduce

inflammation. The body could not function without eicosanoids. Problems arise

when eicosanoid reactions are disrupted by drugs, disease, poor diet and other

factors that interfere with their natural balance).

 

Drug interactions

 

As for interfering with other heart medication, policosanol doesn’t appear to

cause any problems. Adverse reactions do not occur with blood thinners or

beta-blockers, except that policosanol may enhance the blood pressure-lowering

effect of propranolol.(13) No direct studies have been done combining

policosanol with other drugs. However, during clinical trials policosanol was

given to people taking calcium antagonists, diuretics, vasodilators, NSAIDs,

meprobamate, thyroid hormones, digoxin, anticoagulants, ulcer drugs,

neuroleptics, antidepressants and anxiolytics (anti-anxiety drugs) without any

problems.(14)

 

Highlights of clinical trials

 

Policosanol has undergone as many clinical trials as most drugs. In studies on

people with high cholesterol at high risk of heart disease, policosanol lowered

LDL cholesterol 20% in 6 to 12 weeks at 10 mg/day. Total cholesterol was reduced

15%, and HDL increased 7%-28%. Taking 20 mg/day reduced LDL about 28%, total

cholesterol about 20%, and elevated HDL 7%-10%. Triglycerides don’t respond to

policosanol.

 

The 10 mg dose has undergone long-term testing (2+ years), with no ill effects

reported. The 20 mg dose (and higher) is still undergoing long-term trials.

(Note: as in most trials of cholesterol-lowering drugs, policosanol was tested

in conjunction with a low-cholesterol diet).

 

Policosanol holds its own against statin drugs. LDL and total cholesterol

lowering is similar, with policosanol performing better on elevating HDL. In a

side-by-side comparison study from Chile, for example, 10 mg of policosanol

reduced LDL 24% compared with 22% for lovastatin (Mevacor) at 20 mg, and 15% for

simvastatin (Zocor) at 10 mg. This is similar to findings in other studies.(15)

 

A combination of policosanol and gemfibrozil (Lopid) works better than either by

itself, according to one study.(16) Another study combined policosanol with

bezafibrate, a cholesterol- and fibrinogen-lowering drug. Policosanol

dramatically enhanced the ability of bezafibrate to lower LDL and total

cholesterol.

 

In a study involving over 3000 people taking policosanol, only 26 dropped out

because of side effects. The side effect complained of most frequently was

weight loss. (Average time in the study 2.5 years).

In short-term, placebo-controlled trials, complaints of side effects from the

placebo exceeded those for policosanol in every category except abdominal pain

(which was reported equally in both). Policosanol appears to have good side

effects rather than bad ones. One of the noted side effects of the large study

above was that people taking policosanol had significantly lower rates of

hospitalizations in special care units. Serious coronary events were reduced in

the people taking

policosanol compared to placebo.

 

Non-toxic

 

 

Policosanol is a natural supplement made from sugar cane. The

main ingredient is octacosanol. Octacosanol is an alcohol found in the waxy film

that plants have over their leaves and fruit. The leaves and rinds of citrus

fruits contain octacosanol, and so does wheat germ oil. Caviar, which reportedly

has health benefits, contains high amounts of octacosanol.

 

Octacosanol is a “long chain fatty alcohol” (similar to cholesterol which is

also an alcohol). Policosanol is a combination of octacosanol and several other

long chain fatty alcohols — hence the name “poli”-cosanol. Keeping octacosanol

together with other naturally-occurring fatty alcohols makes it more stable.

There is evidence that octacosanol also works better when it’s combined with

other fatty alcohols.

 

Fatty alcohols are converted to fatty acids, and vice-versa. The beneficial

fatty acids in fish, for example, are made from octacosanol and other long chain

fatty alcohols. Fatty alcohols are required for the

synthesis of myelin, the insulation around nerves, as well as other important

bio-substances in the body.

 

Policosanol is very safe. When rats were given 1724 times what a human would

take, no toxicity occurred.(17) Monkeys and dogs have also been given high doses

of policosanol long-term without toxicity.(18) No cancer has ever resulted in

rodents given large amounts for extended periods or time, nor does policosanol

appear to interfere with drug metabolism (it doesn’t affect the liver’s

cytochrome p450).

 

Exercise enhancement

 

In studies dating back to the 1960s, octacosanol has shown its ability to

enhance endurance and oxygen utilization during exercise. Research shows that

octacosanol is taken up by muscles.(19) It appears that muscles store

octacosanol and convert it to an energy source. Energy mobilization and

metabolism are enhanced by octacosanol. When octacosanol is first given, most of

it goes to the liver, but after three days of treatment, it starts accumulating

in muscle.(20)

 

In studies from Japan, octocasanol caused rats to be more active and exercise

more. It also increased their endurance. When people with heart disease are

given 10 mg/day of policosanol, aerobic capacity and oxygen uptake increase, and

ischemia decreases. Improvement on treadmill exercise-ECG tests occurs after

treatment with policosanol. These results in heart patients confirm studies in

healthy people undergoing exercise programs who were also able to increase

reaction time and strength with octacosanol.

 

Libido enhancement (maybe)

 

Unlike cholesterol-lowering drugs that can induce impotency, policosanol may

have a libido-enhancing effect. Studies in male rats show that policosanol

increases sexual activity without increasing testosterone. The same results

appear to be true for monkeys, but the studies are too few to be definitive.

Unfortunately, very high amounts of policosanol had to be taken to get these

effects. However, the bright side is that when policosanol is taken at

recommended doses, it doesn’t interfere with a person’s sex life, which gives it

an advantage over many cholesterol-lowering drugs.

 

Other conditions respond to policosanol

 

 

Policosanol has been tested in postmenopausal women at risk for heart disease,

people over 60 years old, and people with intermittent claudication (blockage of

arteries, usually in the lower extremities). All showed good results. In studies

on postmenopausal women, policosanol (10 mg/day) reportedly reduced total

cholesterol by 17% and LDL by 25%. HDL increased 28%. These results are similar

to those reported in people over 60 who took 10 mg/day of policosanol. In

studies on people with intermittent claudication, policosanol (20 mg/day)

reduced lameness and increased the distance a person could walk. The percentage

of serious complications in the policosanol group was 9.7% compared to 38.7% in

the group getting a placebo. This significant reduction in intermittent

claudiction-induced complications indicates that policosanol exerted beneficial

effects beyond cholesterol modulation.(21)

 

Total cholesterol levels should be kept below 200 mg per deciliter of blood.

Cholesterol levels above 240 are especially dangerous. The dosage for

policosanol is 5-20 mg/day. It can be taken with other drugs, and seems to

enhance the effects of statin drugs, especially in conjunction with aspirin. No

serious side effects have ever been reported for this cholesterol modifying

supplement. Although it shows benefits for cholesterol, LDL and HDL, policosanol

doesn’t appear to affect triglycerides. Serum triglyceride levels may be lowered

by other supplements such as fish oil. One of the very striking benefits of

policosanol is that it not only lowers LDL, it keeps it from oxidizing. This and

other actions of this natural product give it potential as the number-one choice

for people with artery disease—or those who want to prevent it.(22-23)

 

Purchase POLICOSANOL from LEF

 

References

 

1. Mas R, et al. 1999. Effects of policosanol in patients with type II

hypercholetserolemia and additional coronary risk factors. Clin Pharmacol Ther

65:439-47.

 

2. Noa M, et al. 1995. Effect of policosanol on lipofundin-induced

atherosclerotic lesions in rats. J Pharm Pharmacol 47:289-91.

 

3. Arruzazabala ML, et al. 2000. Protective effect of policosanol on

atherosclerotic lesions in rabbits with exogenous hypercholesterolemia. Braz J

Med Biol Res 33:835-40.

 

4. Menendez R, et al. 1999. Oral administration of policosanol inhibits in vitro

copper ion-induced rat lipoprotein peroxidation. Physiol Behav 67:1-7.

 

5. Xu XP, et al. 1999. Oxidized low-density lipoprotein regulates matrix

metalloproteinase-9 and its tissue inhibitor in human monocyte-derive

macrophages. Circulation 99:993-8.

 

6. Noa M, et al. 1996. Effect of policosanol on foam-cell formation in

carrageenan-induced granulomas in rats. J Pharm Pharmacol 48:282-5.

 

7. Lindstedt L, et al. 1999. matrix metalloproteinases-3, -7, and -12, but not

-9, reduce high density lipoprotein-induced cholesterol efflux from human

macrophage foam cells by truncation of carboxyl terminus of apolipoprotein A-I.

Parallel losses of pre-beta particles and the high affinity component of efflux.

J Biol Chem 274:22627-34.

 

8. Noa M, et al. 1998. Effect of olicosanol on damaged arterial wall induced by

forceps in rabbits. J Electron Microsc 4:629-30.

 

9. Negre-Aminou P, et al. 1996. Antiproliferative potencies of 6 vastatins in

cultured human cells: involvement of the ras-mediated signalling pathway. 66th

Cong Eur Atheroscler Soc (July 13-17, Florence): 120.

 

10. Arruzazabala ML, et al. 1997. Comparative study of policosanol, aspirin and

the combination therapy policosanol-aspirin on platelet aggregation in healthy

volunteers. Pharmacol Res 36:293-7.

 

11. Stusser R, et al. 1998. Long-term therapy with policosanol improves

treadmill exercise-ECG testing performance of coronary heart disease patients.

Int J Clin Pharmacol Ther 36:469-73.

 

12. Carbajal D, et al. 1998. Effect of policosanol on platelet aggregation and

serum levels of arachidonic acid metabolites in healthy volunteers. Prost Leuk

Essen Fatty Acids 58:61-4.

 

13. Molina V, et al. 1998. Effect of policosanol on arterial blood pressure in

rats. Study of the pharmacological interaction with nifedipine and propranolol.

Arch Med Res 29:21-4.

 

14. Carbajal D. 1998. Interaction policosanol-warfarin on bleeding time and

thrombosis in rats. Pharmacol Res 38:89-91.

 

15. Prat H, et al. 1999. [Comparative effects of policosanol and two HMG-CoA

reductase inhibitors on type II hypercholesterolemia]. Published in Spanish. Rev

Med Chile 127:286-94.

 

16. Castaño G, et al. 1998. Comparative study of policosanol, gemfibrozil and

policosanol-gemfibrozil combination therapy in the treatment of type II

hypercholesterolemia. Rev CENIC Cien Biol 29:17-23.

 

17. Aleman CL, et al. 1994. A 12-month study of policosanol oral toxicity in

Sprague Dawley rats. Toxicol Lett 70:77-87.

 

18. Rodriguez-echenique C, et al. 1994. Effects of policosanol chronically

administered in male monkeys (Macaca arctoides). Food Chem Toxicol 32:565-75.

 

19. Kabir Y, et al. 1994. Distribution of radioactive octacosanol in response to

exercise in rats. Nahrung 38:373-7.

 

20. Kabir Y, et al. 1995. Tissue distribution of (8-14C)-octacosanol in liver

and muscle of rats after serial administration. Ann Nutr Metab 39:279-84.

 

21. Castano G, et al. 1999. a double-blind, placebo-controlled study of the

effects of policosanol in patients with intermittent claudication. Angiology

50:123-30.

 

22. Mas R, et al. 1999.Pharmacoepidemiologic study of policosanol. Curr Ther Res

60:458-67.

 

23. Mas R. 2000. Policosanol. Drugs of the Future 25:569-86.

 

Purchase POLICOSANOL from LEF

 

 

 

 

 

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