The History Of Pycnogenol

Pycnogenol® is a natural plant extract from the bark of the Maritime Pine, pinus maritima, growing along the coast of south-west France, in the Landes of Gascony. Pycnogenol® is a water-soluble flavonoid extract with highly bioavailable procyanidins, catechins, taxifolins and the typical spectrum of phenolic acids.

Pycnogenol® is among the ten most popular supplements in America and is touted for its impressive history with decades of European research and safety studies, patents and medicinal use.

In 1947, a student at the biological and medical faculty of the University of Bordeaux, France named Jack Masquelier was assigned the task of determining whether or not the red inner skin of peanuts was toxic. For his doctoral dissertation, Masquelier undertook a series of experiments to answer this question. Fairly early in his investigations, Masquelier was able to determine that in fact peanut skins were not toxic. In the course of his research, however, he came upon a colorless substance in peanut skin which called for further examination. By 1948, he had succeeded in isolating that substance, oligomeric proanthocyanidin (OPC), from peanut skin, and had identified that it possessed vasoprotective (protective of blood vessels) potential. After casting about among many possible sources, he found what he was searching for in the bark of Landes pine trees, a waste product of the lumber industry typically used as a mulch for gardens. This new source yielded sufficient quantifies of OPC to be useful for manufacturing purposes.

In 1979 Masquelier "coined the word Pycnogenol to create a little order in this highly complex chemistry." Pycnogenol is a blend of flavonoids patented by Horphag International and imported into the United States from France.

"The invention provides a method for preventing and fighting the harmful biological effects of free radicals in the organism of warm blooded animals and more especially human beings, namely cerebral involution, hypoxia following atherosclerosis, cardiac or cerebral infarction, tumour promotion, inflammation, ischaemia, alterations of the synovial liquid, collagen degradation, among others."

There are over 60 diseases in which free radicals are implicated. Pycnogenol has the ability to neutralize free radicals, aid cell regeneration, and assist DNA cells to reproduce again. Pycnogenol is becoming and increasingly valuable aid in fighting many diseases.

At an annual meeting of the scientists researching the patented product, several studies were presented to substantiate claims that Pycnogenol combats aging and heart disease. David F. Fitzpatrick, associate professor of pharmacology and therapeutics at the University of South Florida College of Medicine in Tampa, reported that the supplement can prevent damage to blood vessels and a decrease in blood clotting, both of which are linked to heart disease. Another study found that Pycnogenol's unique combination of natural vitamin-like compounds known as flavonoids, inhibits excessive metabolizing of nitric oxide, a process that has been linked to inflammation, arthritis, and Alzheimer's.

Since OPC is an antioxidant, research shows it fights cholesterol by discouraging deposits from forming on artery walls. OPC's anti-inflammatory activity may help relieve inflammatory conditions, including arthritis, allergies, bronchitis, and asthma. OPC also corrects dangerous blood clotting tendencies that trigger heart attacks and strokes. Dr. Ronald Watson, a researcher at the University of Arizona, recently confirmed that OPC (Pycnogenol) normalizes platelet aggregation -- blood stickiness leading to hazardous blood clots. He showed that when people smoked, their platelets clumped together in a tendency to form clots. But about twenty minutes after taking OPC, their platelets returned to normal.

Nitrogen monoxide (NO) has diverse physiological roles and also contributes to the immune defense against viruses, bacteria, and other parasites. However, excess production of NO is associated with various diseases such arthritis, diabetes, stroke, septic shock, autoimmune, chronic inflammatory diseases, and atheriosclerosis. Cells respond to activating or depressing stimuli by enhancing or inhibiting the expression of the enzymatic machinery that produce NO. Thus, maintenance of a tight regulation of NO production is important for human health. Phytochemicals have been traditionally utilized in ways to treat a family of pathologies that have in common the disregulation of NO production. Here we report the scavenging activity of Pycnogenol (the polyphenols containing extract of the bark from Pinus maritima) against reactive oxygen and nitrogen species, and its effects on NO metabolism in the murine macrophages cell line RAW 264.7. Macrophages were activated by the bacterial wall components lipopolysaccharide.

(LPS) and interferon (IFN-gamma), which induces the expression of large amounts of the enzyme nitric oxide synthase (iNOS). Preincubation of cells with physiological concentrations of Pycnogenol significantly decreased NO generation. It was found that this effect was due to the combination of several different biological activities, i.e., its ROS and NO scavenging activity, inhibition of iNOS activity, and inhibition of iNOS-mRNA expression. These data begin to provide the basis for the conceptual understanding of the biological activity of Pycnogenol and possibly other polyphenolic compounds as therapeutic agents in various human disorders.

A surprising use of OPC has arisen among people suffering from that bewildering disorder in concentration and attention known as attention deficit disorder (ADD), or attention deficit hyperactivity disorder (ADHD). It is said to have begun quite accidentally when people with ADD took OPC for another purpose, such as allergies, and noticed an improvement in concentration and mental focus, classic symptoms of attention deficit. Others started using it. Word spread, and the ADD remedy has achieved high visibility on the Internet and at natural products trade shows.

The use of OPC for this purpose has not been widely studied but a preliminary study by Marion Sigurdson, Ph.D., a psychologist in Tulsa, Oklahoma, who specializes in treating attention deficit disorder, has found striking benefits from OPC. Using a blend of pine bark and grape seed (Dr. Masquelier's OPC product), Dr. Sigurdson found that it worked just as well as the commonly prescribed stimulant medications, including Ritalin, on thirty children and adults diagnosed with ADD. The subjects were given a battery of computerized and behavior tests to judge their attention, concentration, and other important factors in ADD under various circumstances: when they were either on or off their usual stimulant medications, or on the OPC alone. When they were off their medications, their ADD deteriorated. On their medications, they were much improved. But when they took daily doses of the OPC grape seed-pine bark mixture, their scores and behavior were just as improved as when they took stimulant drugs. In other words, the OPC equaled the drugs in most subjects.

There is growing interest in the biologic activities of plant extracts such as that obtained from the bark of the French maritime pine Pinus maritima, Pycnogenol. Pycnogenol (PYC) is a standardized extract composed of a mixture of flavonoids, mainly procyandins and phenolic acids. Studies indicate that PYC components are highly bioavailable. Uniquely PYC displays greater biologic effects as a mixture than its purified components do individually indicating that the components interact synergistically. PYC has been reported to have cardiovascular benefits, such as a vasorelaxant activity, angiotensin-converting enzyme (ACE) inhibiting activity, and the ability to enhance the microcirculation by increasing capillary permeability. Investigations of the cellular mechanisms of these therapeutic effects have demonstrated that PYC has strong free radical-scavenging activity against reactive oxygen and nitrogen species. The oligomeric components of PYC contribute significantly to the ESR free radical signal. PYC also participates in the cellular antioxidant network as indicated by its ability to regenerate the ascorbyl radical and to protect endogenous vitamin E and glutathione from oxidative stress. PYC modulates NO metabolism in activated macrophages by quenching the NO radical and inhibiting both iNOS mRNA expression and iNOS activity. The spectrum of different effects of NO in the circulation and the nervous system suggest the potential applications of PYC in immune and circulatory disorders as well as in neurodegenerative disease. PYC can bind to proteins, altering their structure and thereby modulating the activity of key enzymes and proteins involved in metabolic pathways. PYC effects redox-sensitive signal transduction pathways and alters gene expression.

Studies carried out at the Pasteur Institute in Lyon, France, have shown it to be nontoxic to humans. In one study, daily doses of up to 35,000 mg were given for six months, with no adverse effects. Pycnogenol should be viewed as a completely safe nutrient.

See also: Proanthocyanidins

  • Jack Masquelier, "A Lifetime Devoted to OPC and Pycnogenols," Dr. Jack Masquelier's Premier American Scientific Address, Baltimore, USA (1996).
  • DR. JACK MASQUELIER, PATENT INVENTOR, United States Patent 4,698,360 (1987)
  • Dianne Lange, "The Body News: Power Pill," Allure Magazine (November 1997).
  • Virgili F; Kobuchi H; Packer L. Procyanidins extracted from Pinus maritima (Pycnogenol): scavengers of free radical species and modulators of nitrogen monoxide metabolism in activated murine RAW 264.7 macrophages. Free Radic Biol Med, 24(7-8):1120-9 1998 May
  • Packer L; Rimbach G; Virgili F. Antioxidant activity and biologic properties of a procyanidin-rich extract from pine (Pinus maritima) bark, pycnogenol. Free Radic Biol Med, 27(5-6):704-24 1999 Sep
  • Steven Lamm, M.D. and Gerald Secor Couzens, "Younger at Last: The New World of Vitality Medicine," Simon & Schuster.

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