Natural Medications for CVD -- 2006
Niacin:
The finding that niacin lowered cholesterol was soon confirmed by Parsons, Achor, Berge, McKenzie and Barker (1956) and Parsons (1961, 1961a, 1962) at the Mayo Clinic which launched niacin on its way as a hypocholesterolemic substance. Since then it has been found to be a normalizing agent, i.e. it elevates high density lipoprotein cholesterol, decreases low density and very low density lipoprotein cholesterol and
lowers triglycerides. Grundy, Mok, Zechs and Berman (1981) found it lowered cholesterol by 22 percent and triglycerides by 52 percent and wrote, "To our knowledge, no other single agent has such potential for lowering both cholesterol and triglycerides."
Flavonoids:
Many in-vitro studies show that the flavonoids possess strong antioxidants and metal chelating properties and may therefore protect cells and tissue structures - lipids, proteins and DNA against reactive oxygen species ROS ( hydroxyl OH, superoxide
anions O2, singlet oxygen O1) and nitrogen species peroxynitrate initiating the following pathologic conditions:
(1). Oxidation of LDL which is thought to be the initiating event in atherosclerosis
(3) Diabetes due to the destruction of the B-cells in islets of Langerhans in the pancreas.
(4) Contributing to insulin resistance and inhibiting action
(5) Rheumatoid arthritis by releasing the various inflammatory mediators
The body’s endogenous antioxidant defenses are not always sufficient to counteract completely against ROS and nitrogen species, and diet derived antioxidants are important in protecting against chronic diseases. The principal polyphenols found in green tea are catechins (epigallo catechin , and epigallocatechin gallate (EGCG)) and flavins. The polymerized catechins in black tea following fermentation yield theaflavins
(TF) and thearugabins. Several epidemiological and animal studies have shown an association between increased tea consumption and reduced incidence of cardio vascular diseases (CVD). However, human studies have not been clear cut and have shown contradictory results from a positive lowering of systolic blood pressure in Norwegian men consuming black
tea to no reduction in Japanese consuming green tea, or Australians consuming five cups of green or black tea. A British study showed that men or women consuming six
cups of black tea showed no lowering in blood pressure. Recently, several carefully controlled studies with particular attention to confounding factors of dietary lifestyles
showed an inverse relationship between increased tea consumption and CVD.
Researchers have postulated that the reason some studies with green tea showed no possible health correlation was possibly due to an absence of theaflavins. In other words, a possible synergy between catechins and theaflavins was suspected.
Theaflavins combine the benefits of green tea phytochemicals and black tea to give a synergistic effect for cardiovascular health.
Pantethine (Pantethine is definitely diabetic safe)
Pantethine is not to be confused with simple calcium pantothenate/pantothenic acid (vitamin B5). Rather, the making of Pantethine is the very reason the body needs B5 in the first place. That is, pantothenic acid’s whole purpose in the body is to serve as a raw material for the synthesis of Pantethine, which is the “business end” of the critical Coenzyme A (CoA). The real “work” done by CoA is accomplished by Pantethine as
CoA’s active site. CoA, in turn, is used by the body in a wide variety of functions, including regulating cholesterol synthesis. Thus, optimal Pantethine levels are a key factor in maintaining optimal blood lipid balance.
Pantethine is not to be confused with simple calcium pantothenate/pantothenic acid (vitamin B5). Rather, the making of Pantethine is the very reason the body needs B5 in the first place. That is, pantothenic acid’s whole purpose in the body is to serve as a raw material for the synthesis of Pantethine, which is the “business end” of the critical Coenzyme A (CoA). The real “work” done by CoA is accomplished by Pantethine as
CoA’s active site. CoA, in turn, is used by the body in a wide variety of functions, including regulating cholesterol synthesis. Thus, optimal Pantethine levels are a key
factor in maintaining optimal blood lipid balance.
Know How Much You’re Getting
It’s important to note that these effects are achieved at dosages of at least 600 milligrams per day of active Pantethine ion. Most trials, in fact, have used 900 milligrams, although persons choosing to take more than one lipid-balancing nutrient
may find that they get good results at the lower dose. But health-conscious persons should be careful in selecting a Pantethine product, making sure that they know what they’re getting. While Pantethine is still uncommon on the shelves of North American health food stores, some companies are selling it, and many Pantethine products contain far too little Pantethine to be effective.
Guggulipid:
Commiphora mukul or Guggul is a small, thorny tree closely related to the Biblical myrrh and found widely in India. The resin of the Guggul plant is a mainstay of rasayan, the vast medicine chest of herbs, mineral extracts, and medicinal foods painstakingly collected by untold generations of physicians working with Ayurveda, the traditional medical system of India. Guggul is used for a broad variety of conditions in Ayurveda,
including nutritional support in inflammatory conditions and for supporting healthy body weight: the weight loss appears to be due to the botanical’s ability to support healthy thyroid function. But the best-backed such application is in maintaining a healthy cholesterol balance.
Guggul’s place as herbal support for healthy cholesterol balance is on solid ground. It appears to work through several mechanisms, including inhibition of HMG-CoA reductase (the enzyme that controls the body’s synthesis of cholesterol), increasing the release of excess lipids through the feces (an action similar to the drug cholestryramine (Questran®)), and its support of thyroid hormone production.
L-Arginine:
The amino acid Arginine was first characterized in 1886 by the Swiss Chemist Ernst Schulze. Little research was conducted subsequently and there was widespread belief that adequate amounts of arginine could be synthesized in the body which undoubtedly delayed further research. In the 1930's research showed that arginine deprivation decreased the rate of growth and/or lead to severe metabolic disorders and even death.
Extensive studies have demonstrated arginines antiatherogenic, antiischaemic and antithrombic properties. The eventual consequence is formation of plaque in the arteries, which leads to compromised endothelial function which in turn leads to reduced vasodilation. Arginine has been shown to not only prevent further progression but also even regression of plaque formation! An interesting study by Boger and colleagues
compared the effects of standard cholesterol drug lovastatin (Mevacor) with arginine in cholesterol fed rabbits. Lovastatin reduced cholesterol by 32%, but had only a weak effect on formation of plaque. Interestingly, arginine had no effect on cholesterol yet completely blocked the formation of plaque.
Niacin No-Flush Inositol Hexanicotinate (IHN – also sometimes called inositol hexaniacinate) is the true “flushless niacin.” Unlike “sustained-release” niacin, which is just regular niacin in a pill which dissolves more slowly, IHN is a niacin complex, formed with the B-vitamin-like inositol. When you take an IHN supplement, the central inositol ring gradually releases
niacin molecules, one at a time – delivering true niacin, but in a controlled fashioned governed by the kinetics of the hydrolysis of the molecule itself.
Niacin is also the only proven way to reduce levels of lipoprotein(a) (Lp[a] – a littleknown, but especially deadly lipoprotein. (One exception: estrogen therapy in menopausal women often restores lower Lp(a) levels). Recently, for instance, a randomized, controlled comparison with lovastatin
(Mevacor®) found that niacin lowers LDL to a similar degree (23% (niacin) vs 32% (statin)), while elevating HDL considerably more (33% vs. 6%). And niacin lowers lipoprotein(a) (Lp[a]) by an astounding 35%, while lovastatin therapy has no effect.
But niacin doesn’t just change the amount of cholesterol floating around in your blood: it also changes the biochemical composition of that cholesterol in heart-healthy directions.
It’s well-known that the LDL “bad” cholesterol is much more likely to form atherosclerotic plaques when it’s been oxidized (damaged by free radicals). And the smaller and denser
your LDL particles are, the more likely they are to become oxidized. Niacin converts the dense, easily-oxidized LDL particles to larger, more oxidation-proof ones. Likewise, the “good” cholesterol, HDL, is more effective at clearing cholesterol out of your cells when it’s rich in a protein called apolipoprotein A-I. Niacin increases the concentration of apolipoprotein A-I in HDL, boosting its cholesterol-clearing powers.
Safe for Diabetics
New research has dispelled an old myth about niacin. For a long time, it was believed that one drawback to the use of this niacin for cholesterol balance was that it would
raise the blood sugar levels of diabetics, thereby worsening their condition. This situation was ironic in the extreme, since diabetics typically have exactly the lipid imbalance combination that most closely match up with niacin’s beneficial properties as a dietary supplement: high LDL, low HDL, and – especially – high triglycerides. But the belief that niacin and diabetes don’t mix was based entirely on a handful of case reports and small-scale, poorly controlled experiments. Recently several large, well-controlled trials have found that niacin does not elevate blood sugar to a clinically significant
degree in either diabetics or healthy individuals when administered on a long-term basis (60 weeks).
B-12, Folic Acid, B1, B6, Magnesium, Lycopene
Some concern has been raised by a recent report, which found that niacin raises homocysteine levels. But in fact, this finding represents yet further proof of niacin’s benefits for heart health, and an opportunity to make them even stronger. That is, since persons taking niacin alone, even with this Hcy-raising effect, still end up with lower rates of both heart attack and death than those not receiving the supplement, it is
reasonable to speculate that taking niacin with homocysteine-lowering nutrients may result in even greater reductions in risk. Hcy-lowering nutrients include the
vitamins B6, B12, and folic acid, along with trimethylglycine (TMG) – and, to a lesser extent, B2 (riboflavin). Animal studies confirm that B vitamins lower Hcy without inhibiting niacin’s cholesterol-balancing function.
To convert homocysteine to harmless (or even useful) amino acids, the body requires folic acid, vitamin B-6 and vitamin B-12. It is important to get at least 800 micrograms of
folic acid, 25 milligrams of vitamin B-6 and 100 micrograms of vitamin B-12. Although a good broad spectrum vitamin supplement will probably supply the necessary B-6 and B-12, it is usually necessary to take a separate folic acid supplement to get adequate folic acid to minimize homocysteine formation. Folic acid has many important benefits at high doses. Although 800 micrograms is the largest folic acid dose generally available in the United States without a prescription, 5000 microgram (5 mg.) folic acid tablets are available in many other countries.
It is important to have one's homocysteine levels measured occasionally. Many people with an adequate intake of folic acid and vitamins B-6 and B-12 still have high homocysteine levels.
Those individuals need to take enough trimethyglycine (TMG) to
keep their homocysteine levels low. TMG is a readily-available nutritional supplement. Sadenosylmethionine (SAM-e) can also reduce homocysteine levels. Creatine (the supplement often used for muscle building) has also been shown to significantly reduce homocysteine levels. To reduce oxidation of cholesterol from LDL, you need at least 100 units of vitamin E, 25,000 units of beta carotene (and/or 5 mg. lycopene), and 500 mg. of vitamin C per day, along with other dietary antioxidants. (These are absolute minimums.) It is important to get a broad spectrum of fat-soluble and water-soluble antioxidants.
Many single antioxidants, taken alone, will actually generate free radicals that must be de-activated by other antioxidants.
A very important antioxidant in preventing heart disease and many cancers is lycopene, which is very similar to beta carotene, but which has finally become available in pure
form as a nutritional supplement.
The best food sources of lycopene are canned tomato juice, or juices such as V8 that are high in tomato juice. Aspirin
In case all of the above fail, it is important for most people to take 1/4 aspirin tablet (81 mg.) per day. Low dose aspirin is the simplest and least expensive method of heart attack prevention. Low dose aspirin, by itself, reduces the risk of heart attack by at least 40%. Low dose aspirin will also reduce the risk of colon cancer, one of the deadliest and most common forms of cancer, by at least 40%. Policosanol (May not be safe for people taking coumarin, warfarin or blood thinning agents)
Octacosanol (an ingredient of Policosanol) Beats Statins
While you may not have heard of it, a substance called octacosanol is more effective than the statin drugs in lowering cholesterol, and it has other benefits also. This is the main component of a complex called Policosanol, and the research is impressive. In studies doing direct comparisons with statin drugs, the octacosanol was superior.
Octacosanol is a waxy alcohol derived from sugar cane or wheat germ. In a study of octacosanol and Pravachol (pravastatin), 10 mg daily of either product lowered LDLcholesterol by 19.3 percent, the drug only 15.6 percent, it lowered total cholesterol by 13.9 percent (the drug only 11.8). The drug did not affect triglycerides or HDL, but octacosanol raised the good HDL by 18 percent, and lowered the triglycerides by 14
percent. Vitamins, E, C, Quercetin, Chromium, Garlic, L-Carnitine Vitamins E and C reduce total cholesterol and raise HDL levels, but not as much as octacosanol. They also protect the LDL from oxidation, and in clinical studies they reduce heart disease. It is impossible to get therapeutic levels of vitamin E (400 to 800 IU) from the diet. Vitamin C is easier to find in foods, and on a diet rich in raw fruits and vegetables it is possible to get over 2000 mg daily, but it is likely that you will need supplements to get this amount. The bioflavonoid quercetin is anti-inflammatory and inhibits oxidation of LDL.
Chromium supplements in the range of 200 to 400 mcg daily reduce total cholesterol and raise HDL levels, and up to 1000 mcg also help control blood sugar levels. As diabetes is a heart risk factor, this in itself is an important benefit.
In earlier issues, I have discussed the benefits of red yeast rice, pantethine, garlic, and L-carnitine, but octacosanol appears to be one of the best supplements for the heart,
particularly when combined with exercise and a mostly vegetarian diet (plus fish with omega-3 oils), and soy foods such as tofu, tempeh, and soymilk.
Eating Fish
Eating omega-3 oils, particularly from fish, reduces the risk of heart disease. A new review shows that 1 to 2 fish meals a week lowers the incidence of heart attacks, and people who have had heart attacks have reduced overall mortality, as well as
fewer recurrent heart attacks (Nordoy A, et al., n-3 polyunsaturated fatty acids and cardiovascular diseases. Lipids 2001;36 Suppl:S127-9.) Omega-3 oils are also in ground flaxseeds, flaxseed oil, and walnuts, and these foods also reduce cardiac risk.
Olive Oil
Monounsaturated fats and medium chain triglycerides (MCT) are safer types of fats. MCT can dramatically improve LDL/HDL ratios and can be used as a substitute for ordinary fats in many applications. MCT is difficult to use in frying, though, because it decomposes (and smokes) at a lower temperature than other fats. (See the Fats in Your Foods chapter of this manual.) Some types of fats, such as the omega-3 fatty
acids in fish oil, are good for you and are very important substances for life extension.
COQ10
DHEA (dehydroepiandrosterone) also often lowers LDL and raises HDL. For those with who require a cholesterol-lowering drug, lovastatin (Mevacor) is very effective (as are the other "statin" drugs), but it is mandatory to take at least 30 mg.
of coenzyme Q-10 daily since all statin drugs block the liver's production of coenzyme Q-10. Coenzyme Q-10 is a substance essential for proper muscle functioning, especially functioning of the heart muscle. The 30 mg. coenzyme Q-10 is a minimum dose: 60 mg. to 120 mg. is a better dose. (Doses of coenzyme Q-10 larger than 200 mg. should only be taken under medical supervision.)
Most people taking a cholesterol-lowering drug would find inositol hexanicotinate to be safer and just as effective, but they should not make the switch except under a physician's supervision and with regular blood chemistry tests. It is prudent to take supplementary coenzyme Q-10 with inositol hexanicotinate.
Green Tea and Booze
An average intake of about one ounce of alcohol per day in men, or 1/4 ounce per day in women, will raise HDL levels. Even though a little alcohol is good for most people, a little more than this amount can produce very adverse consequences. The differences between the optimal amount for men and women are more than just a matter of differences in average body weight. Men and women metabolize alcohol very differently.
For example, the optimal alcohol intake for the average man will increase the breast cancer risk for the average woman. If the alcohol is consumed in the form of red wine, the olyphenols in the red wine will raise the body's level of natural antioxidants. Green tea contains similar polyphenols.
Beta Glucan and Oats.
With all the significant advances in medical science and nutrition, cardiovascular disease continues to be the leading cause of death in developed nations. Cardiovascular disease results from the culmination of several risk factors including
high cholesterol, high blood pressure, overweight/obese, smoking, and diabetes.
Many of these factors are treatable either through lifestyle changes or through medications, often with dramatic improvements. In fact it has been estimated that a 10% reduction in total cholesterol levels could result in an estimated 30% reduction in the incidence of coronary heart disease (Center for Disease Control and Prevention, 2000).
Blood cholesterol levels are affected mainly by genetics and lifestyle (primarily diet and exercise). While there is not much a person can do about genetics, it is possible to
improve their diet and exercise habits. Dietary fiber, particularly soluble fiber, has been shown to help decrease cholesterol levels, however most adults only eat about 15g of
fiber eat day, which is about half of the 28-35g per day recommended by the Institute of Medicine (IOM).
Potassium
Potassium is a mineral that is often recognized as one of the body’s many resident electrolytes. Deficiencies in potassium can be caused by magnesium deficiency, refined glucose intake, alcohol, exercise-induced water loss, dieting (decreased dietary intake), gastrointestinal losses (i.e. diarrhea), and many other dietary factors. Potassium deficiencies have become much more common today because of refined high salt diets and the increasing levels of alcohol consumption. Low levels of potassium directly result in an electrolyte imbalance in the heart (salt concentrations in the heart muscle increase.) Even mild deficiencies in potassium may result in nervous disorders, insomnia, and irregular heartbeat. Also, potassium has a
definite impact upon blood pressure. In study after study, the efficacy of using potassium supplementation for lowering blood pressure has been established.
Magnesium
When a magnesium deficiency arises, the result is high blood pressure. In a 1988 study on the prevalence of magnesium deficiency, it was reported that “Magnesium is the most under-diagnosed electrolyte abnormality...” (Whang, R: Prevalence of magnesium deficiency, Clifton, N.J., Oxford Health Care Inc., pg. 5-6). How prevalent are magnesium deficiencies? In a nationwide study conducted by the U.S. Department of Agriculture in 1977-78, only 25% of 37,785 people surveyed had magnesium intake at or greater than the RDA. That means 75% of the population was deficient!
Taurine
Taurine is the most abundant free amino acid in the blood of mammals. Within the heart muscle, taurine is again the most abundant amino acid. A variety of studies have shown taurine to be an effective modulator of heart activity, although the mechanism still has not been clarified.
Nutritional research has been gathered upon taurine’s effects on the cardiovascular system. Some of the results are astounding, especially for an unpopular (but well researched) amino acid: hypotensive activity, membrane stabilizing effects, and antiarrhythmic activity. In repeated studies, taurine has been effective in minimizing the injurious effects of congestive heart failure.
The beneficial effects of taurine reach past cardiovascular system: taurine protects the cellular membranes from being damaged by toxic compounds, such as oxidants, bile acids, and xenobiotics. The cellular membranes are protected by taurine because it:
1) Acts as a Direct Antioxidant: It protects tissues from oxidative stress because of its ability to scavenge free radicals.
2) Acts as an indirect antioxidant by preventing the disruption of ion transport and membrane permeability that results from oxidative damage. It protects the heart against
3) free radical damage by its ability to stabilize the membranes.
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