Grapefruit Lowers Cholesterol

Grapefruit contains pectin, a form of soluble fiber that has been shown in animal studies to slow down the progression of atherosclerosis. In one study, animals fed a high-cholesterol diet plus grapefruit pectin had 24% narrowing of their arteries, while animals fed the high-cholesterol diet without grapefruit pectin had 45% narrowing.Both blond and red grapefruit can reduce blood levels of LDL ("bad") cholesterol, and red grapefruit lowers triglycerides as well, shows a study published in the Journal of Agricultural and Food Chemistry.Israeli researchers from the Hebrew University in Jerusalem first tested the antioxidant potential of blond and red grapefruits and then their cholesterol-lowering potential in humans. The test tube research showed that red grapefruit contains more bioactive compounds and total polyphenols than blond, but both grapefruits are comparable in their content of fiber, phenolic and ascorbic acids, and the flavonoid, naringinen, although red grapefruit contains slightly more flavonoids and anthocyanins.In this recent study, participants added either red grapefruit, blond grapefruit or no grapefruit to their daily diet. The results indicated that both types of grapefruit appeared to lower LDL cholesterol in just 30 days: total cholesterol by 15.5% in those eating red grapefruit and 7.6% in those eating blond grapefruit; LDL cholesterol by 20.3% and 10.7% respectively; and triglycerides by 17.2% and 5.6% respectively. No changes were seen in the control group (those that didn't eat any grapefruit).Both red and blond grapefruits both positively influenced cholesterol levels, but red grapefruit was more than twice as effective, especially in lowering triglycerides. In addition, both grapefruits significantly improved blood levels of protective antioxidants. Red grapefruit's better performance may be due to an as yet unknown antioxidant compound or the synergistic effects of its phytonutrients, including lycopene.In response to this rapid and very positive outcome, the researchers concluded that adding fresh red grapefruit to the diet could be beneficial for persons with high cholesterol, especially those who also have high triglycerides.One caveat, however: Compounds in grapefruit are known to increase circulating levels of several prescription drugs including statins. For this reason, the risk of muscle toxicity associated with statins may increase when grapefruit is consumed. (See our Individual Concerns section for more information.)

Precautions: Research indicates that individuals taking statin drugs should avoid grapefruit. Grapefruit increases the amount of statin drug that reaches the general circulation in two ways. First, grapefruit contains a compound called naringenin, which inactivates an enzyme (cytochrome P450 3A4) in the small intestine that metabolizes statin drugs. Secondly, grapefruit also inhibits P-glycoprotein, a carrier molecule produced in the intestinal wall that would normally transport the statin drug back to the gut. The end result of these two mechanisms is that much more of the statin drug enters the systemic circulation than would normally be the case, leading to a build up in statin levels that can be quite dangerous, and may trigger a rare but serious statin-associated disease called rhabdomyolysis. Rhaddomyolysis affects muscle tissue, usually causing temporary paralysis or weakness, unless the muscle is severely injured.

Danger of Grapefruit: if you take Zocor (simvastatin), Lipitor (atorvastatin) and Pravachol (pravastatin) you should not eat grapefruit or drink grapefruit juice

Supplement​s against statins side effects

Most of the negative side effects caused by statins are due to the way these drugs deplete the body of the potent antioxidant CoQ10.

You see, statins work in the liver by blocking an enzyme pathway that leads to the creation of cholesterol. Unfortunately, that same enzyme pathway is the one your body uses to create CoQ10. So statin takers need to be especially aware of the fact that they’re not producing CoQ10 at the levels they would be if they were taking no medication. When your body lacks CoQ10, energy production will lag and cell function will suffer.

Here’s a list of nutrients I recommend to all statin users. Because of the CoQ10 connection, it’s at the top of the list. But because CoQ10 is so intimately involved in cellular energy production, I also recommend including complementary nutrients in your daily regimen. You’ll find many of these nutrients in a quality multivitamin and mineral formula. Others, like CoQ10, ribose, and broad spectrum carnitine, must be purchased separately and can be found in health food stores and most grocery stores.

· CoQ10, 100–200 mg (hydrosoluble softgel) daily. CoQ10 serves as a raw material for the production of adenosine triphosphate (ATP), the primary source of cellular energy. Also a potent antioxidant, CoQ10 helps to neutralize the free radicals generated during the ATP production cycle.

· Broad spectrum carnitine, 1–2 g daily. This nutrient shuttles the fatty acids necessary for ATP production into the cells and transports waste material out.

· Ribose, 5 g twice a day. Ribose allows used ATP molecules to be recycled more quickly. A simple sugar made in every cell, ribose is depleted by heart disease. When taken as a supplement, it rapidly re-energizes heart patients.

· Magnesium, 400–800 mg daily. In the body, magnesium helps activate and regulate more than 350 enzymatic reactions. It is also required to stabilize and store ATP.

· Vitamin E (100–200 IU of mixed tocopherols daily),

· Vitamin C (200 mg daily), and

· Alpha lipoic acid (50–100 mg daily).

These three major antioxidants protect your cells from free-radical damage and are able to penetrate the inner mitochondrial membrane.

· Copper (500 mcg to 1 mg daily),

· Zinc (15–30 mg daily),

· Molybdenum (75–150 mcg daily), and

· Manganese (2–4 mg daily).

All four are vital minerals for ATP production and cellular health and repair.

Read more: http://www.drsinatra.com/cholesterol-meds-statin-nutrient-depletion#ixzz2fAQQRlL0

Cholesterol medications: Consider the options

By Mayo Clinic staff
A healthy lifestyle is the first defense against high cholesterol. But sometimes diet and exercise aren't enough, and you may need to take cholesterol medications. Cholesterol medications may help:

• Decrease your low-density lipoprotein (LDL) cholesterol, the "bad" cholesterol that increases the risk of heart disease
• Decrease your triglycerides, a type of fat in the blood that also increases the risk of heart disease
• Increase your high-density lipoprotein (HDL) cholesterol, the "good" cholesterol that offers protection from heart disease

Your doctor may suggest a single drug or a combination of cholesterol medications. Here's an overview of benefits, cautions and possible side effects for common classes of cholesterol medications.

Drug class and drug names	Benefits	Possible side effects and cautions
Statins Altoprev (lovastatin) Crestor (rosuvastatin) Lescol (fluvastatin) Lipitor (atorvastatin) Mevacor (lovastatin) Pravachol (pravastatin) Zocor (simvastatin)	Decrease LDL and triglycerides; slightly increase HDL	Constipation, nausea, diarrhea, stomach pain, cramps, muscle soreness, pain and weakness; possible interaction with grapefruit juice
Bile acid binding resins Colestid (colestipol) Questran (cholestyramine/ sucrose) Welchol (colesevelam)	Decrease LDL	Constipation, bloating, nausea, gas; may increase triglycerides
Cholesterol absorption inhibitor Zetia (ezetimibe)	Decreases LDL; slightly decrease triglycerides; slightly increase HDL	Stomach pain, fatigue, muscle soreness
Combination cholesterol absorption inhibitor and statin Vytorin (ezetimibe-simvastatin)	Decreases LDL and triglycerides; increases HDL	Stomach pain, fatigue, gas, constipation, abdominal pain, cramps, muscle soreness, pain and weakness; possible interaction with grapefruit juice
Fibrates Lofibra (fenofibrate) Lopid (gemfibrozil) TriCor (fenofibrate)	Decrease triglycerides; increase HDL	Nausea, stomach pain, gallstones
Niacin Niaspan (prescription niacin)	Decreases LDL and triglycerides; increases HDL	Facial and neck flushing, nausea, vomiting, diarrhea, gout, high blood sugar, peptic ulcers
Combination statin and niacin Advicor (niacin-lovastatin)	Decreases LDL and triglycerides; increases HDL	Facial and neck flushing, dizziness, heart palpitations, shortness of breath, sweating, chills; possible interaction with grapefruit juice
Omega-3 fatty acids Lovaza (prescription omega-3 fatty acid supplement) Vascepa (Icosapent ethyl)	Decrease triglycerides	Belching, fishy taste, increased infection risk

Most cholesterol medications lower cholesterol with few side effects, but effectiveness varies from person to person. If you decide to take cholesterol medication, your doctor may recommend periodic liver function tests to monitor the medication's effect on your liver. Also remember the importance of healthy lifestyle choices. Medication can help control your cholesterol — but lifestyle matters, too.

Flaxseed against cholesterol

Flax seed oil is a rich source of essential fatty acids, most notably omega-3 fatty acids. Also known as polyunsaturated fatty acids, these compounds are necessary for healthy growth and development. According to the University of Maryland Medical Center, they are also critical for proper brain function and cardiovascular health.

Various flaxseed preparations - including ground flaxseed, partially defatted flaxseed, and flaxseed bread and muffins - seem to significantly reduce total cholesterol and the “bad cholesterol,” low-density lipoprotein (LDL) cholesterol, in people with normal cholesterol levels and in men and pre-menopausal women with high cholesterol. But flaxseed doesn’t have much effect on “good cholesterol,” high-density lipoprotein (HDL) cholesterol. Most flaxseed preparations don’t affect triglyceride levels either, but unfortunately partially defatted flaxseed (flaxseed without as much alpha-linolenic acid content) can increase triglycerides by approximately 10%.

 

Flaxseed might slow blood clotting. Taking flaxseed along with medications that also slow clotting might increase the chances of bruising and bleeding.

Some medications that slow blood clotting include aspirin, clopidogrel (Plavix), diclofenac (Voltaren, Cataflam, others), ibuprofen (Advil, Motrin, others), naproxen (Anaprox, Naprosyn, others), dalteparin (Fragmin), enoxaparin (Lovenox), heparin, ticlopidine (Ticlid), warfarin (Coumadin), and others.

 

Red Rice Yeast Instead of Statins?

Cardiologists David Becker, M.D., and Ram Gordon, M.D., Chestnut Hill Cardiology, studied 62 patients with high cholesterol in the first randomized, double-blinded placebo-controlled trial to evaluate red yeast rice in patients with a history of statin-associated myalgias (side effects that include muscle pain and weakness). Thirty-one of the patients took three 600-mg capsules of red yeast rice twice per day over the course of six months, and the other half received identical placebo tablets. The red yeast rice patients also participated in weekly meetings for the first three months, where they were taught about heart disease and how to incorporate heart-healthy nutrition, exercise and stress management into their lives.

At the conclusion of the study, the research found:

- Low-density lipoprotein cholesterol (also known as "bad cholesterol") levels decreased more in the patients receiving the red yeast rice (average decrease, 35 mg/dL) than in patients receiving the placebo (average decrease, 15 mg/dL).

- Total cholesterol levels improved more in the red yeast rice group than in the placebo group.

- Muscle pain scores, weight loss, HDL cholesterol (high-density lipoprotein or "good cholesterol") and liver or muscle enzyme levels did not differ between the two groups.

Red Yeast Rice, a staple of Chinese medicine for more than a thousand years, is derived from a fungus that grows on rice. A series of compounds within the red yeast rice have been found to slow the production of cholesterol in the liver. The medical community, however, has been slow to consider its potential use as an alternative treatment therapy for patients with statin-associated myalgias because the supplement is not regulated by the Food and Drug Administration.


Question to Andrew Weil M.D.:
Now that a scientific study has found that red rice yeast supplements work as well as statin drugs for cholesterol control I'm wondering if I should switch from the statin I now take. What's your recommendation?

Answer (Published 6/30/2009)

You're referring to a study published in the June 16, 2009 issue of the Annals of Internal Medicine showing that a red rice yeast supplement worked as well to lower LDL ("bad") cholesterol as prescription statin drugs. The study included 62 patients, all of whom quit taking statins because of muscle pain, the most common side effect of these drugs. Half the 62 patients in the study received a red rice yeast supplement; the other half were given a placebo. After three months, average LDL levels among those taking the red rice yeast had dropped an average of 27 percent compared with six percent among the placebo group. All the participants were taught how to eat well, exercise and otherwise maintain a healthy lifestyle. Only seven percent of the patients taking the supplement developed muscle pain; among statin users, at least twenty percent experience muscle pain initially but many improve once their bodies get used to the drug.

Red rice yeast (Monascus purpureus) is a natural source of statins, but unlike pharmaceutical products, it provides a mix of these compounds rather than a single one. The complex mixture interacts with the body more smoothly and is less likely to cause toxicity.

One active ingredient in red rice yeast extract, monacolin K, is the active component of the FDA approved statin Mevacor. The lead researcher of the new study, David Becker, M.D., of Chestnut Hill Cardiology in Pennsylvania, said that because the dose of monacolin K in the red rice yeast supplement used in the study was five times smaller than the amount in a typical Mevacor prescription, "something else is having a powerful lipid-lowering effect." Healthy lifestyle changes among the study participants probably didn't account for the difference.

This is a valuable study, but I wouldn't recommend switching from a statin to red rice yeast without your physician's approval and supervision. Because supplements are unregulated and the demand for quality ingredients is growing, some products will not actually contain any red rice yeast extract and, as a result, won't be effective.

I have put many patients on red rice yeast products with excellent results and have seen only two patients who could not tolerate them because of side effects. Note that anyone taking statins, either as red rice yeast or prescription drugs, should be on daily supplements of coenzyme Q10 (CoQ10). Statins inhibit the body's production of this coenzyme along with lowering cholesterol. CoQ10 is necessary for optimum function of muscles, including heart muscle.

Andrew Weil, M.D.

Berberine against Cholesterol

Berberine is a quaternary ammonium salt from the protoberberine group of isoquinoline alkaloids.

It is found in such plants as Berberis [e.g. Berberis aquifolium (Oregon grape), Berberis vulgaris (barberry), Berberis aristata (tree turmeric)], Hydrastis canadensis (goldenseal), Xanthorhiza simplicissima (yellowroot), Phellodendron amurense^[2] (Amur cork tree), Coptis chinensis (Chinese goldthread), Tinospora cordifolia, Argemone mexicana (prickly poppy), and Eschscholzia californica (Californian poppy). Berberine is usually found in the roots, rhizomes, stems, and bark

During the last few decades, many studies have shown berberine has various beneficial effects on the cardiovascular system and significant anti-inflammatory activities.^[18] A Canadian report suggested berberine can effectively reduce intracellular superoxide levels in LPS-stimulated macrophages. Such a restoration of cellular redox by berberine is mediated by its selective inhibition of gp91phox expression and enhancement of SOD activity.^[19]

Berberine exerts up-regulating activity on both the low-density-lipoprotein receptor (LDLR) and the insulin receptor (InsR). This one-drug-multiple-target characteristic might be suitable for the treatment of metabolic syndrome.^[20][21]

Berberine lowers elevated blood total cholesterol, LDL cholesterol, triglycerides and atherogenic apolipoproteins (apo B) (Apo B),^[41] but the mechanism of action is distinct from statins.^[42][43][44] Berberine reduces LDL cholesterol by upregulating LDLR mRNA expression posttranscriptionally while downregulating the transcription of proprotein convertase subtilisin/kexin type 9 (PCSK9), a natural inhibitor of LDL receptor (LDLR),^[45] and increasing in the liver the expression of LDL receptors through extracellular signal-regulated kinase (ERK) signaling pathway,^[46] while statins inhibit cholesterol synthesis in the liver by blocking HMG-CoA-reductase. This explains why berberine does not cause side effects typical to statins. Berberine and plant stanols synergistically inhibit cholesterol absorption in hamsters.^[47]

Berberine seems to improve the arterial endothelial function in humans.^[26][48] Berberine activates AMP-activated protein kinase (AMPK),^[49] specifically extracellular signal-regulated kinases (ERK),^[50] which plays a central role in glucose and lipid metabolism,^[51][52] suppresses proinflammatory cytokines,^[53] and reduces MMP-9 and EMMPRIN expression,^[54] which are all beneficial changes for heart health.

Lp(a) and cardiovascular diseases

Many large-scale studies have explored the relationship between Lp(a) and cardiovascular diseases, consistently finding an association between high Lp(a) levels and atherosclerosis, heart attacks, or stroke; Lp(a) has been validated as a significant, independent risk factor for heart disease.

Lp(a) promotes the recruitment of immune cells called monocytes to the intima, the innermost layer of blood vessels and arteries facing the blood stream. Once monocytes have migrated to the intima, they can become engorged with oxidized LDL—becoming “foam”cells—and initiate atherosclerotic lesion formation.

Lp(a) contributes to thrombosis (blood clot formation) that could result in a heart attack or stroke. Clot formation in the arterial wall, called “mural thrombosis,” contributes to the growth of atherosclerotic lesions; “occlusive thrombosis,” on the other hand, blocks an artery and triggers a heart attack or stroke. Lp(a) may also enhance coagulation, which could further contribute to thrombotic events.

Lp(a) is found in few species, mainly those that do not synthesize vitamin C. Since the absence of detectable Lp(a) in most species—almost all of which synthesize vitamin C—does not seem to be biologically disadvantageous, it was also proposed that vitamin C serves as a surrogate for Lp(a).

As a surrogate for vitamin C and owing to its pro-clotting functions, Pauling and his colleague suggested that Lp(a) might help repair lesions in the arterial wall caused by mechanical stress, free radicals, and/or sub-optimum collagen synthesis when vitamin C concentrations are insufficient. However, atherosclerosis results from the chronic, pathological deposition of Lp(a). A corollary is that adequate vitamin C status in humans, such as that achieved by sufficient intake, may help prevent arterial damage and reduce the need for the deposition of Lp(a) and/or lower its levels, thus preventing the development of atherosclerotic plaque.

Depletion of vitamin C increases the permeability of the vascular wall, thereby contributing to the infiltration of Lp(a) and leading to plaque formation and mural thrombosis. In chronic vitamin C insufficiency, the prolonged action and accumulation of Lp(a) may result in the development of plaque (mural thrombosis)

 

Lysine—by binding to Lp(a)—may quickly remove Lp(a) from plaque and also prevent its deposition in developing plaque.

Unfortunately, no controlled clinical trials have yet been published to validate or refute this.

Lysine is found in the diet, and it can be used in the body as a precursor to synthesize carnitine, an amino acid critical for mitochondrial energy production in cells. In his first case report on the amelioration of angina with vitamin C and lysine, Pauling noted that vitamin C is important in the hydroxylation reactions that synthesize carnitine from lysine. A number of studies have found that carnitine supplementation, as an adjunct to conventional therapy, is useful in treating heart disease, including heart attacks, heart failure, angina, and peripheral arterial disease.

 

Source:

Linus Pauling Institute | Oregon State University

Stephen Lawson
LPI Administrative Officer

VITAMIN C, LYSINE, AND LIPOPROTEIN(a) IN ATHEROSCLEROSIS AND ANGINA PECTORIS