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Life Extension Magazine August 2012
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Pycnogenol®: Multi-Modal Defense Against Aging

By Janet Sarto

Pycnogenol® for Heart and Artery Health

Pycnogenol® for Heart and Artery Health

More than 27 million Americans have heart disease; nearly 600,000 die from it each year.18 Age-related dysfunction of the endothelium (the layer of cells lining arteries and smaller vessels), is to blame for many cardiovascular diseases. A malfunctioning endothelium can't properly control blood flow and pressure.

Excessive platelet function is another cause of heart disease and stroke. When platelets are overactive, clots form inside blood vessels, blocking blood flow.

The result of endothelial dysfunction and platelet activation can be a heart attack or stroke. Pycnogenol® improves both conditions.

Pycnogenol's® antioxidant function helps protect endothelial cells from damage.19 In addition, it may bind to proteins in blood vessel walls, helping to "seal" them and prevent capillary leakage.20 Studies demonstrate how these effects play out in human subjects with endothelial dysfunction. When patients with high blood pressure were given 100 mg/day of Pycnogenol® for 12 weeks, they were able to reduce their blood pressure medication.21

In another study, 125 mg Pycnogenol®/day helped normalize blood pressure in 58% of hypertensive diabetic patients, while cutting their need for blood pressure medication by 50%.6 Supplementation can also reduce the fluid accumulation that is a common side effect of blood pressure medications.22 Insight into how Pycnogenol® works to lower blood pressure comes from human studies using ultrasound to measure blood flow. Healthy young men treated with 180 mg/day of Pycnogenol® had a 41% increase in blood flow response to the vascular-response neurotransmitter acetyl choline indicating significantly lower risk for cardiovascular complications.23

A similar study done in patients with existing coronary artery disease

A similar study done in patients with existing coronary artery disease, (who were considered at high risk for heart attacks) showed that 200 mg of Pycnogenol® per day along with standard cardiovascular therapy, produced a 32% increase in coronary blood flow, but no change occurred in placebo patients.24 Another benefit of improved blood flow is better erectile function in men. A dramatic study showed that a combination of L-arginine aspartate and Pycnogenol® intake for one month restored erectile dysfunction to normal, and doubled the frequency of intercourse.25 Along the way, cholesterol and blood pressure were also reduced.

The physiology behind the improvement in erectile function is important, and applies equally to men and women. That's because nitric oxide, a signaling compound, is essential in dilating blood vessels, not only to allow a normal erection, but also to control blood pressure throughout the body. Our bodies relax their arteries by increasing nitric oxide levels in the vessels' lining cells, or endothelium.26

Pycnogenol® beneficially modulates nitric oxide production.27 In endothelial cells, Pycnogenol® boosts levels of endothelial nitric oxide synthase (eNOS), the enzyme system that produces vessel-relaxing nitric oxide in response to blood flow and blood pressure.28 That effect is powerful enough to overcome the vessel-constricting, blood pressure-elevating effects of adrenaline and other stress-induced compounds.28 The result is an increase in blood flow to vital tissues, and a decrease in blood pressure.27

Animal and human studies have repeatedly shown that treatment of hypertension with Pycnogenol® results in lowered blood pressure and reduced damage to blood vessels and organs such as the kidney.27,29 And the positive elevation of nitric oxide in endothelial tissue can also inhibit LDL cholesterol oxidation, slowing the early development of atherosclerotic plaques.28

Pycnogenol® Protects Against Five Mechanisms of Aging

Among the most exciting developments with Pycnogenol® and nitric oxide are studies showing that Pycnogenol® can mitigate the effects of congestive heart failure. In this condition, chronically elevated pressures within the heart cause the muscle to become floppy and ineffective. Victims become weak, fluid accumulates in their tissues, and death often results from increasingly insufficient blood flow.

Changes in heart structure during congestive heart failure are the direct result of impaired nitric oxide production. Supplementing animals with Pycnogenol® reverses that remodeling in congestive heart failure, reduces the gradual degradation of heart muscle proteins, and restores the heart's ability to pump blood normally.30,31

Boosting nitric oxide in endothelial cells and platelets also gives Pycnogenol® impressive effects on platelet function. It reduces their “stickiness,” which lowers the risk that these tiny blood cells will produce a deadly clot in one of your vessels.28

Smokers, who are at high risk for blood clots, participated in a study that showed 200 mg of Pycnogenol® was sufficient to reduce over-activated platelet function.32 This effect is likely due to reduction in thromboxane, a clot-inducing protein that is elevated in many high-risk conditions including diabetes and obesity.33

Pycnogenol® Protects Against Five Mechanisms of Aging
Mechanism Problem Resulting Diseases Pycnogenol® Effects
Oxidant Stress Oxidant stress releases free radicals that "burn" cells and tissues. That damages DNA and cell membranes, and triggers dangerous inflammation. Oxidant stress underlies neurocognitive disorders like Alzheimer's and Parkinson's diseases, as well as atherosclerosis and cancer. Pycnogenol® reduces free radical production, boosts cells' natural antioxidant systems, and scavenges free radicals, preventing the development of oxidant-related diseases.2,47,55-58
Membrane Damage Damage to membranes of cells and their internal organelles disrupts cellular structure and communication. Damage to cell and mitochondrial membranes is implicated in chronic obstructive pulmonary disease (COPD) and congestive heart failure. Pycnogenol® stabilizes membranes, protects them against toxic injury, restores their normal characteristics, and prevents their rupture and leakage.4,5,19,59
DNA Damage Damaged DNA can fail to produce working proteins, and can lose control over cell replication. The best-known consequence of DNA damage is cancer, but it is also involved in Alzheimer's disease, attention deficit/hyperactivity disorder (AHDH) and atherosclerosis. Pycnogenol® reduces DNA damage by its antioxidant effect and possibly other mechanisms.3,58,60,61
Inflammation Chronic inflammation damages almost every component of cells and their organelles. Inflammation is involved in every chronic, age-related disease, including atherosclerosis, osteoporosis, kidney disease, arthritis, and cancer, to name just a few. Pycnogenol® fights inflammation by switching off a central inflammation-generating system and reducing the production of inflammatory cytokine molecules.8,54,62-64
Glycation Proteins and fats become “glycated” when sugar molecules bond to them. Glycated molecules function abnormally and trigger oxidation and inflammation. Glycation is implicated in cancer, cardiovascular disease, Alzheimer's disease, osteoporosis, and arthritis. It also contributes to obesity, itself a cause of inflammation and chronic disease. Pycnogenol® prevents glycation by lowering blood sugar levels and preventing sugar absorption in the intestine.6,38,65,66

Five major molecular mechanisms contribute substantially to aging and chronic diseases.
Studies show that Pycnogenol® combats all five mechanisms and prevents disease.

When you sit still for long periods of time (for example, on a long airplane flight), you are at risk for developing dangerous blood clots in your legs. These clots can travel, eventually blocking major arteries from the heart to the lungs, and cause sudden death.

Pycnogenol® shows a unique ability to prevent these so-called thrombotic events. When a group of 99 long-haul airline passengers were given 200 mg of Pycnogenol® before departure, and another 200 mg 6 hours later, then 100 mg next day, they had zero thrombotic events, compared with 5 such events in a similar-sized group of placebo patients.34

Pycnogenol® Helps Control Diabetes

Figure 3: In Type II diabetics not requiring medication, 50-200 mg of Pycnogenol® lowered both fasting and after meal glucose levels.

Figure 3: In Type II diabetics not requiring medication, 50-200 mg of Pycnogenol® lowered both fasting and after meal glucose levels.35

People with diabetes are in a constant state of accelerated aging, vulnerable to all five of the key mechanisms described on the preceding page. Controlling blood sugar levels is vital to prevent these age-enhancing effects.

Pycnogenol® supplementation lowers blood sugar levels, especially in the critical after-meal period when high sugar leads most powerfully to heart disease.35,36 One way Pycnogenol® works is by blocking starch breakdown in the intestine.37 This slows glucose absorption (we get much of our glucose from breaking down starch), and helps level off the blood sugar flux throughout the day. Pycnogenol® also stimulates cells to take up excess glucose from the blood, reducing blood sugar even more.38,39 Patients treated with 125 mg/day of Pycnogenol® saw a drop in fasting blood sugar of 23.7 mg/dL, compared with a decrease of just 5.7 in controls. Hemoglobin A1c, a marker of long-term blood sugar levels, dropped by 0.8% in supplemented patients, compared with just 0.1% in controls. LDL (bad) cholesterol dropped by 12.7 mg/dL as well.6 In a second study involving 30 individuals with type II diabetes who were not on conventional therapy, Pycnogenol® showed dose dependent lowering of blood sugar levels.35 The participants were administered 50 mg of Pycnogenol® for 3 weeks, followed by 100 mg for 3 weeks, and finally 200 mg for 3 additional weeks. As little as 50 mg per day of Pycnogenol® had significant blood sugar lowering effects not just on fasting blood sugar but post-meal blood sugar as well. However, the benefit of taking 100 mg or 200 mg of Pycnogenol® was even more dramatic. Many people with diabetes need to lose weight. Strict control of blood sugar and weight loss will reduce, but not eliminate, the risk of diabetic complications. Many of these complications result from small blood vessel damage in the eye, the skin, and the nerves.

Pycnogenol® slows progression of blood vessel disease in the eye (diabetic retinopathy) by reducing capillary damage in the retina and improving blood flow.39-41

Figure 4: Pycnogenol® use has afforded improvements in visual acuity on the Snellen chart by an average 21.4%, even for those already afflicted with serious eye disease such as retinopathy.

Figure 4: Pycnogenol® use has afforded improvements in visual acuity on the Snellen chart by an average 21.4%, even for those already afflicted with serious eye disease such as retinopathy.41

One study using 150 mg/day for 2 months completely blocked the loss of retinal function in diabetic patients.20 Placebo patients just got worse. Supplemented patients showed no deterioration of retinal function, instead experienced a significant recovery in visual acuity (ability to see according to the standard “Snellen” eye chart).20 Blood vessel studies in supplemented patients demonstrated improved distribution of blood vessels, and a reduction in the "leakiness" of capillaries that damages vision.

An independent study at a different hospital showed similar results.41 Eighteen out of 24 patients had subjective improvement in their vision, and the average visual acuity on the Snellen chart improved by 21.4% after just 2 months of treatment. No change was found in the placebo group.

Diabetic damage to capillaries in the skin (microangiopathy) produces skin breakdown and ulcers. Oral Pycnogenol® at 150 mg/day can produce complete healing of ulcers in up to 85% of patients.42,43

Prolonged exposure to elevated glucose damages nerves, producing a painful condition called diabetic neuropathy. People with this condition experience burning, stinging sensations; meanwhile, their nerves conduct impulses more slowly than normal.

Pycnogenol® has been shown to slow declines in nerve conduction velocity, even under diabetic conditions.36