Description 

• Date back to the bitter winter of 1534, French explorer Jacques Cartier and his 110-man crew were blocked by ice near Quebec. Lacking fresh fruit and vegetables they got what is now known as scurvy. Soon scurvy killed 25 and affected more than 50 others. Fortunately, Quebec Indians rescued them by giving them a tea from the needles and bark of Canadian pine trees. It had a miracle effect and saved most of the crew from death by scurvy. This life saving event was noted by Explorer Jacques Cartier in his book Voyages Au Canada which provided the basis of the today’s health product Pycnogenol.
• Extensive research work have been carried out in France, England, Italy, Finland, Germany, Holland, Denmark, Portugal, Spain, Switzerland, Romania, Argentina, Australia, New Zealand, Japan, China, Singapore, Korea and the U.S.A etc. over the last thirty years.
• Pycnogenol is a standardized extract of the bark of the French maritime pine, Pinus pinaster Ait., that has multiple biological effects, including antioxidant, anti-inflammatory and anticarcinogenic properties.
  

Chemistry of Pycnogenol

• The active compounds are a group of bio-flavonoids with recognized antioxidant (free radical scavenging) properties and with the ability to inhibit the activity of certain enzymes which cause inflammation and some disorder in the body. They include water-soluble proanthocyanidins and procyanidins consisting of catechin and epicatechin units linked by C-C bonds to form dimers, trimers and other oligomers up to a chain length of 6-7 molecules and phenolic acids and its glucose derivatives. It also contains active compounds such as caffeic acid, ferulic acid, p-coumaric acid, p-hydroxybenzoic acid, vanillic acid and protocatechic acid etc.
  
• Each kind of plant and each plant species produces a different procyanidin pattern. Extracts from different sources may contain different components. Pycnogenol^® contains a number of active compounds proved to be beneficial to human health.

Pharmacological and Physiological Activities of Pycnogenol

• Pycnogenol is a powerful scavenger of free radical which now is well known to cause body damage that can lead to more than 50 disease conditions including accelerating aging, cancer, heart disease and arthritis.
• In vitro studies show that Pycnogenol is 50 times more powerful than vitamin E and 20 time more powerful than vitamin C. In vivo studies also prove that Pycnogenol is extremely effective as an antioxidant, but comparisons are much more difficult to evaluate.
• Plant flavonoids are generally not soluble in water. Pycnogenol, produced solely by warm-water extraction under pressure, is water-soluble. This means that Pycnogenol is well-absorbed and bioavailable. This is why it is so effective as a powerful antioxidant and capillary strengthener.
• Human and animal studies have proved the rapid uptake and distribution of Pycnogenol throughout the body. Being water soluble and acidic, after taking by mouth it is absorbed through the gastrointestinal tract and enters the blood stream. Eventually its nutrient content binds to collagen fibers in the subcutaneous layer of the skin.
• Pycnogenol can readily cross the blood-brain barrier to provide antioxidant protection to central nervous system tissue. This is the difference of Pycnogenol from the other known antioxidants.
• Pycnogenol interferes with pathological cardiovascular processes which either are normal aging reactions or are prematurely enhanced by stress and life style.
• Pycnogenol acts especially on leaky capillary vessels which can be considered as a defective network of collagen fibers. Pycnogenol enhances vitamin C activity in capillary wall membranes and strengthens collagen in the capillaries. Furthermore, some Pycnogenol constituents demonstrate: antiviral effects, anti-inflammatory activity, antiproliferative action, antimutagenic potential and protect the human skin against the damage of UV-radiation. Natural killer cell cytotoxicity was increased with Pycnogenol treatment.
• Inflammation and some aging symptoms can occur due to a bioflavonoid deficiency which make capillaries porous, or due to free radicals and other oxygen species which can initiate the inflammatory response. Pycnogenol has been shown to strengthen capillaries and quench free radical attack.
• During the inflammation process, the enzymes collagenase and elastase are released which damage the skin proteins collagen and elastin. Studies have shown that Pycnogenol bioflavonoids bind to these skin proteins and protect them against degradation by the collagenase and elastase enzymes. Another damaging enzyme is hyaluronidase, a mucopolysaccharide-splitting enzyme which is related to increase permeability of capillaries and other blood vessels, as well as to inflammation. Two of the bio-flavonoids of Pycnogenol, catechin and proanthocyanidin B-2 inhibit hyaluronidase. Thus Pycnogenol protects hyaluronic acid, a basic constituent of connective tissue and creates more youthful, undamaged structures of the face and other body areas. Elasticity and flexible strength is restored to connective tissue.
  

Clinical Experience of Pycnogenol

• The use of Pycnogenol in human subjects showed health benefits and to reduce risk of more than 50 radical-related diseases such as:
  • preventing cardiovascular degeneration or disease,
  • restorating and preventing leaky capillaries,
  • strengthening capillaries, arteries and veins,
  • improving circulation and enhancing cell vitality,
  • slowing aging and improving skin smoothness and elasticity,
  • improving vision,
  • enhancing immune response and reducing inflammation in arthritis,
  • an antiviral effect in patients with recurrent herpes glutealis after application of a topical ointment.
• Some clinical reports are as follows:
  • In another study, 31 persons were given 90 mg. of Pycnogenol daily for two months. Their capillary resistance improved markedly.
  • Dr. F. Feine-Haake studied the benefit of 30 mg.x 3/daily of Pycnogenol on 100 persons having varicose veins. 80% showed a clear improvement. Additionally, among the 40 individuals in that group who had nightly leg cramps, 90% reported that Pycnogenol prevented the cramping.
  • Another study involved 110 persons having nocturnal leg cramps or pain. They were given 90 mg. Pycnogenol daily for five days, and then half this amount for nine days. The symptoms disappeared completely in 50% and were significantly relieved in another 31%.
  • Pycnogenol has been licensed in France for years for treating diabetic retinopathy. French physicians have concluded that Pycnogenol is the first choice in the treatment of diabetic retinopathy.
  • Dr. G. Maynard reported benefits of Pycnogenol on the damage of retina caused by the microbleeding of the eye capillaries due to diabetes. 40 patients were given 80 to 120 mg. of Pycnogenol daily for a week, and then maintained on 40 to 80 mg. daily for 1.5 to 4 months. The microbleeding of the capillaries decreased remarkably in 90% of the patients and their eyesight improved noticeably.
  • Dr. Miklos Gabor of Szent-Gyorgyi Medical University in Hungary has researched capillary resistance and permeability for about 40 years and is considered the world’s expert on the relationship between flavonoids and capillaries. He has researched the effect of Pycnogenol on capillaries since 1979. He has found Pycnogenol protects capillaries against many of the stimuli that can cause an inflammatory response.
  • The anti-platelet activity of Pycnogenol was established in new preclinical and clinical research, initiated by Dr. P. Rohdewald, University of Munster, Germany and confirmed by Dr. R. R. Watson, University of Arizona, USA. In a two-armed clinical study, Pycnogenol was administered versus Aspirin to smokers. Smoking caused stress to healthy volunteers, detectable in relevant biochemical parameters. The results of the clinical studies showed that only 100 mg oral Pycnogenol reduced blood clotting without prolonging the bleeding time, whereas with at least 500 mg oral Aspirin, the same blood clotting reduction was obtained, but with the unwanted side effect of prolongation of the bleeding time. This research was recognized as an invention and published in the recent US. Patent (5720956) on 24th February 1998. Therefore, Pycnogenol is also called THE SUPER ASPIRIN.
  • Dr. Wang Shiwen et al. of The Institute of Geriatric Cardiology in China reported a placebo-controlled, double-blind, randomized trial in 60 patients with coronary artery diseases (CAD). They indicated that Pycnogenol could inhibit the adhesion and aggregation of platelets, enhance the diameter of microcirculation perfusion, and some extent prevent and improve the myocardial ischemia in patients with coronary artery diseases. There were no severe side effects and toxicity to vital organs such as liver and kidneys when used in routine dosage. It can be used as a beneficial health protection agent to prevent cardiovascular damage and thrombotic CAD.
  • Dr. Pavlovic of the U.S.A. reported that Pycnogenol significantly improved endurance of athletes compared to the control.
  • Dr. Kohama of Japan reported the treatment of gynaecological disorders with Pycnogenol. They indicated that menstrual cramps, abdominal pain and tenderness were reduced in a significant percent of patients ranging between 66% and 100%. They concluded that Pycnogenol resulted to be useful to partly relieve the most troublesome findings of gynaecological problems.
  • Dr. Roseff of the U. S. A. reported that the potent antioxidant Pycnogenol significantly improved sperm morphology in a small group of subfertile men.

Toxicology of Pycnogenol

• Extensive studies carried out in Pasteur Institute and Huntington Institute and others over many years confirmed its purity and safety.
• Pycnogenol is non-toxic (acute and chronic toxicity studies in mice, rats, guinea pigs, dogs; reproduction studies). The LD50 is 3g per kilogram of body weight. Nutritional supplementation is usually 20 to 150 mg daily.
• Pycnogenol is non-carcinogenic and non-mutagenic which was shown in several conventional test systems. It was even shown to inhibit mutagenesis induced by the classical mutagen benzo(a)-pyrene.
• Pycnogenol is also non-teratogenic and non-antigenic.

Dosage

Pycnogenol^® (20 mg Pycnogenol/tablet)

2-4 tablets a day

Pycnogenol Strongl^® (40 mg Pycnogenol/tablet)

1-2 tablets a day

Package

Pycnogenol Strongl^® (40 mg Pycnogenol/tablet)

60 tablets/18g

References

1. Inhibition of NF-kappaB activation and MMP-9 secretion by plasma of human volunteers after ingestion of maritime pine bark extract (Pycnogenol).
   Grimm T et al.
   J Inflamm (Lond). 2006 Jan 27;3(1):1 [Epub ahead of print]
2. Venous ulcers: microcirculatory improvement and faster healing with local use of pycnogenol((r)).
   Belcaro G, et al.
   Angiology. 2005 Nov-Dec;56(6):699-705.
3. Inhibition of COX-1 and COX-2 activity by plasma of human volunteers after ingestion of French maritime pine bark extract (Pycnogenol).
   Schafer A, et al
   Biomed Pharmacother. 2005 Oct 26; [Epub ahead of print]
4. Prevention of edema in long flights with Pycnogenol
   Cesarone MR et al.
   Clin Appl Thromb Hemost. 2005 Jul;11(3):289-94.
5. Pycnogenol as an adjunct in the management of childhood asthma.
   Lau BH, Riesen SK, Truong KP, Lau EW, Rohdewald P, Barreta RA.
   J Asthma. 2004;41(8):825-32.
6. Pycnogenol((R)) accelerates wound healing and reduces scar formation.
   Blazso G, Gabor M, Schonlau F, Rohdewald P.
   Phytother Res. 2004 Jul;18(7):579-81.
7. The effect of Pycnogenol on the erythrocyte membrane fluidity.
   Sivonova M, Waczulikova I, Kilanczyk E, Hrnciarova M, Bryszewska M, Klajnert B, Durackova Z.
   Gen Physiol Biophys. 2004 Mar;23(1):39-51.
8. Antioxidant activity and inhibition of matrix metalloproteinases by metabolites of maritime pine bark extract (pycnogenol).
   Grimm T, Schafer A, Hogger P.
   Free Radic Biol Med. 2004 Mar 15;36(6):811-22.
9. Protection from inflammation, immunosuppression and carcinogenesis induced by UV radiation in mice by topical Pycnogenol.
   Sime S, Reeve VE.
   Photochem Photobiol. 2004 Feb;79(2):193-8.
10. Pycnogenol, French maritime pine bark extract, improves endothelial function of hypertensive patients.
    Liu X, Wei J, Tan F, Zhou S, Wurthwein G, Rohdewald P.
    Life Sci. 2004 Jan 2;74(7):855-62.
11. Sharma SC, Sharma S, Gulati OP.
    Pycnogenol inhibits the release of histamine from mast cells.
    Phytother Res. 2003 Jan;17(1):66-9.
12. Devaraj S, Vega-Lopez S, Kaul N, Schonlau F, Rohdewald P, Jialal I.
    Supplementation with a pine bark extract rich in polyphenols increases plasma antioxidant capacity and alters the plasma lipoprotein profile.
    Lipids. 2002 Oct;37(10):931-4.
13. Hosseini S, Pishnamazi S, Sadrzadeh SM, Farid F, Farid R, Watson RR.
    Pycnogenol in the Management of Asthma.
    J Med Food. 2001 Winter;4(4):201-209.
14. Schonlau F, Rohdewald P.
    Pycnogenol for diabetic retinopathy. A review.
    Int Ophthalmol. 2001;24(3):161-71.
15. Ni Z, Mu Y, Gulati O.
    Treatment of melasma with Pycnogenol.
    Phytother Res 2002 Sep;16(6):567-71
16. Roseff SJ.
    Improvement in sperm quality and function with French maritime pine tree bark extract.
    J Reprod Med 2002 Oct;47(10):821-4
17. Feng WH, Wei HL, Liu GT.
    Effect of PYCNOGENOL on the toxicity of heart, bone marrow and immune organs as induced by antitumor drugs.
    Phytomedicine 2002 Jul;9(5):414-8
18. Rohdewald P.
    A review of the French maritime pine bark extract (Pycnogenol), a herbal medication with a diverse clinical pharmacology.
    Int J Clin Pharmacol Ther 2002 Apr;40(4):158-68
19. Koch R.
    Comparative study of Venostasin and Pycnogenol in chronic venous insufficiency.
    Phytother Res 2002 Mar;16 Suppl 1:S1-5
20. Spadea L, Balestrazzi E.
    Treatment of vascular retinopathies with Pycnogenol.
    Phytother Res 2001 May;15(3):219-23
21. Araghi-Niknam M, Hosseini S, Larson D, Rohdewald P, Watson RR
    Pine bark extract reduces platelet aggregation.
    Integr. Med. 2000 Mar 21;2(2):73-77
22. Hasegawa N
    Inhibition of lipogenesis by pycnogenol
    Phytother Res 2000 Sep;14(6):472-3
23. Hasegawa N
    Stimulation of lipolysis by pycnogenol.
    Phytother Res 1999 Nov;13(7):619-20
24. Huynh HT, Teel RW
    Selective induction of apoptosis in human mammary cancer cells (MCF-7) by pycnogenol.
    Anticancer Res 2000 Jul-Aug;20(4):2417-20
25. 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 1999 Sep;27(5-6):704-24
26. Liu FJ, Zhang YX, Lau BH
    Pycnogenol enhances immune and haemopoietic functions in senescence-accelerated mice.
    Cell Mol Life Sci 1998 Oct 54:10 1168-72
27. Petrassi C, Mastromarino A, Spartera C
    PYCNOGENOL in chronic venous insufficiency
    Phytomedicine 2000 Oct;7(5):383-8