DEFINITION
Pycnogenol is a brand name for a plant extracts obtained from the bark of the Pinus maritima pine tree, known for their antioxidant properties. It’s a standardized extract composed of a mixture of flavonoids, mainly procyandins and phenolic acids which have very high oxidizing power, also present in many plants and fruits, such as green tea and Virginia creeper. Procyanidins are biopolymers of catechin and epicatechin subunits which are recognized as important constituents in human nutrition. Pycnogenol contains a wide variety of procyanidins that range from the monomeric catechin and taxifolin to oligomers with 7 or more flavonoid subunits. The phenolic acids are derivatives of benzoic and cinnamic acids. Studies indicate that these components are highly bioavailable. Uniquely pycnogenol displays greater biologic effects as a mixture than its purified components do individually indicating that the components interact synergistically. The active ingredients in pycnogenol can also be extracted from other sources, including peanut skin, grape seed, and witch hazel bark.
A review of the French maritime pine bark extract (Pycnogenol), a herbal medication with a diverse clinical pharmacology, 2002
DISCOVERY
Hundreds of years ago, it originated from a pine bark and pine needle potion that Native North American medicine men were using to treat what we now know was scurvy. In 1535, a French expedition to Canada had to stop at the native American villages of Stadacona and Hochelaga for the winter as the Hudson Bay had frozen. When they ran out of fresh supplies, 25 of them died from scurvy, with at least another 50 becoming seriously ill. A member of the expedition, Jacques Cartier became friends with the Native American chief who prepared a concoction of bark and needles to make a tea which he recommended be drunk several times a day by the men suffering from scurvy.
Miraculously, the men recovered within a week or two. It wasn’t until the mid-1900s that scientists wanted to find out exactly why a tree bark extract cured these explorers and that is when the research began.
GENERAL BENEFITS
Pycnogenol demonstrates antioxidant and anti-inflammatory action. Pycnogenol is one of nature’s most versatile supplement. It produces more health benefits than any other single antioxidant including:
* Protection against free radicals which speed up the ageing process;
* Reduction in the risk of heart disease;
* Stronger blood vessel walls and improved circulation which helps prevent blood clots from forming;
* Protection against stress;
* Stronger immune system;
* Reduced inflammation, improving joint flexibility;
* Reduction of menstrual disorders;
* Improved healing;
* It can help attention deficit hyperactive disorder (ADHD);
* Youthful skin – making the skin tighter, smoother with fewer lines, more elasticity and less discolouration;
* Protection against deep vein thrombosis;
* Relief from allergies such as hay fever – by inhibiting the release of histamine;
* Anti-inflammatory action helps asthmatics breathe more easily;
* Improvement in sexual function and erectile dysfunction;
* Improvements in oral health such as periodontitis;
* Research on the effect Pycnogenol may have on Alzheimer’s disease is on-going but looking very encouraging, and it has been shown to improve memory retention and learning ability.
* Improvement in athletic endurance
* Improvemnet in retinopathy
* Improvements in diabetes
* Reduced ringing in the ears
* Improvement in endometriosis
Pharmaceutical and nutraceutical effects of Pinus pinaster bark extract, 2011
Antioxidant activity and biologic properties of a procyanidin-rich extract from pine (Pinus maritima) bark, pycnogenol, 1999
ANTIOXIDANT AND ANTI-INFLAMMATORY ACTIVITY
Pycnogenol acts as an antioxidant by scavenging reactive oxygen and nitrogen species and suppressing production of peroxides (H2O2). It protects against oxidative stress in several cell systems by doubling the intracellular synthesis of anti-oxidative enzymes and by acting as a potent scavenger of free radicals. It has the ability to regenerate the ascorbyl radical, to recycle and regenerate vitamin C, vitamin E and the carotenoids, to increase the endogenous antioxidant enzyme systems and to protect glutathione from oxidative stress. It modulates NO metabolism in activated macrophages by quenching the NO radical and inhibiting both iNOS mRNA expression and iNOS activity. It can bind to proteins, altering their structure and thereby modulating the activity of key enzymes and proteins involved in metabolic pathways. Pycnogenol gets quickly absorbed from the gastrointestinal tract due to its excellent water solubility. The compound fixes rapidly to cell menmbranes in veins and capillaries and connective tissues where it exerts a stabilizing effect on cellular membranes of all types. The high affinity of pycnogenol to collagen and elastin, the main tissue constituents, is an advantage over other antioxidants, because pycnogenol will be fixed in the areas where we need it, in the tissues. Another advantage of pycnogenol is that it stabilizes red blood cell membranes. This also aids in distributing pycnogenol throughout the body. An in vivo stydy showed a 40 percent increase in antioxidant potency in blood following 3 weeks supplementation with 150 mg a day.
It is widely known that during inflammation, oxygen radicals are produced. Most recent studies examine the relationship between free radicals and the inflammation process, and the role of pycnogenol. There is good correlation between the free-radical scavenging and the anti-inflammatory activity of pycnogenol against the superoxide and hydroxyl radicals. It was also shown that pycnogenol supplementation (150 mg a day for five days) during an inflammatory situation inhibites 5-lipoxygenase (5-LOX) and cyclooxygenase-2 (COX-2) gene expression and phospholipase A2 (PLA2) activity. Interestingly, Pycnogenol suspendes the activity of 5-LOX by inactivating protein (FLAP) expression. Pycnogenol supplementation reduced leukotriene production but did not leave prostaglandins unaltered with a decline of COX-2 activity in favour of COX-1. infact Cox-1 is a constitutive enzyme always present in the body while cox-2 is present only in case of inflammation. Moreover bioavailable active principles of Pycnogenol exert anti-inflammatory effects by inhibition of proinflammatory gene expression inhibited matrix metalloproteinase 9 (MMP-9) release from human monocytes and NF-kappaB activation.
The anti-inflammatory pharmacology of Pycnogenol in humans involves COX-2 and 5-LOX mRNA expression in leukocytes, 2009
Inhibition of NF-kappaB activation and MMP-9 secretion by plasma of human volunteers after ingestion of maritime pine bark extract (Pycnogenol), 2006
Pycnogenol -- Safe and Effective: An Interview with Professor Peter Rohdewald
Antioxidant activity and biologic properties of a procyanidin-rich extract from pine (Pinus maritima) bark, pycnogenol, 1999
MAIN DISEASES
TUMOURS
Pycnogenol may guard against the formation of tumours or another cell mutations caused by free radicals and may help protect against degenerative diseases like cancer. In vitro studies show antimetastatic effects of pycnogenol extraxt. It has the ability to induce apoptosis and slow down the proliferation of leukemia, ovarian and breast cancer cells. Moreover it prevents activation of NF-KB, a transcription factor that is generally overactive in cancer cells and it inhibits the enzyme monooxygenase, preventing the formation of highly carcinogenic diole epoxide of benzopyrene.
The main action is to alleviate adverse effects in oncologic treatment. In an important study several radiotherapy patients receiving pycnogenol were compared to other patients receiving placebo. In the first patients most apparent improvements of acute side effects related to decreased soreness and ulceration in the mouth and throat as well as less dryness of the mouth and the eyes. Also a decreased incidence of nausea /vomiting, diarrhoea, edema and weakness was noticed, which was reflected by semi-quantitative evaluation suggesting that severity was only half or even less pronounced than in the control group. Moreover several chemotherapy patients were supplemented with Pycnogenol and another patients were in the control group. For all patients this was the first chemotherapy treatment period. The most prominent improvements were found for nausea, vomiting, diarrhoea and weight loss and semi-quantitative evaluation showed that here again symptom severity was half or less pronounced than in the control group.
Pycnogenol reduces talc-induced neoplastic transformation in human ovarian cell cultures, 2007
Pycnogenol induces differentiation and apoptosis in human promyeloid leukemia HL-60 cells, 2005
Selective induction of apoptosis in human mammary cancer cells (MCF-7) by pycnogenol, 2000
Pycnogenol may alleviate adverse effects in oncologic treatment, 2008
HEART AND CIRCULATION
The most positive improvements are in pheripheral circulation where it helps to protect capillaries by binding to blood vessels walls and reducing permeability. It inhibits superoxide radicals and might improve blood flow. The majority of the beneficial effects of Pycnogenol for heart health instead are likely related to the enhanced generation of nitric oxide in cells lining blood vessel walls and to the decrement of endothelin-1 concentrations. The nitric oxide relieves arterial constriction and this releases the pressure build-up in the vascular system. Patients with systolic blood pressures of 140 mmHg are considered borderline hypertensive and they don’t take medication but a study showed that, after taking Pycnogenol for eight weeks, their blood pressures went down significantly, bringing it close to 130 mmHg. Consequently pycnogenol might have a protective effect for heart failure and it is useful in patients with stable coronary artery disease. In hypertensive people infact the heart needs more force to pump blood. The heart chamber wall wears out and the heart gradually loses the ability to pump sufficient amounts of blood to meet the organ’s metabolic demand. This can turn into fatal problems. Pycnogenol gives also a protection against the cardiovascualr risk of thrombotic events by preventing the clotting of blood platelets caused by smoking and inhibits the nicotine-induced constriction of blood vessels. So pycnogenol preventes platelets in smokers from getting sticky as effectively as aspirin but it doesn’t cause the longer bleeding time that aspirin does.
Hypertension is a major side effect of diabetes, which can be considered a “heart disease” due to the frequency of such clinical consequences. A study showed that in diabetics whose hypertension is only partially controlled by pharmaceutical drug pycnogenol is so effective that their blood pressures are under good control and the need for pharmaceutical drugs for hypertension is dramatically lowered. Probably equally exciting is the point that adding Pycnogenol to their standard anti-diabetic regimens (which includes the drugs glitazides and metformin) helpes their blood glucose finally reach healthy levels. In the placebo group, none of these benefits were found.
Pycnogenol Is Protective Against Heart Disease, Diabetes and Inflammation:An Interview with Ronald Ross Watson, Ph.D., 2011
Effects of Pycnogenol on endothelial function in patients with stable coronary artery disease: a double-blind, randomized, placebo-controlled, cross-over study, 2012
OSTEOARTHRITIS
People living with osteoarthritis usually only have the option of taking pain killers. Chronic use of pain killers eventually leads to stomach ulcers but people will continue to use them to control pain of the joints. In osteoarthritic patients in addition to the standard pain medication pycnogenol significantly decreased joint pain and improved joint function. In a study it was investigated the anti-inflammatory and antioxidant activity of Pycnogenol against elevated C-reactive protein (CRP) and plasma-free radicals. Elevated CRP levels have been suggested to be associated with disease progression in osteoarthritis. Comparison of blood specimens drawn at baseline and after 3-month treatment showed that Pycnogenol significantly decreased plasma free radicals to 70.1% of baseline values. Plasma CRP levels decreased from baseline 3.9 mg/l to 1.1 mg/l in the Pycnogenol group whereas the control group had initial values of 3.9 mg/l which decreased to 3.6 mg/l. Also Fibrinogen levels were found to be lowered to 62.8% of initial values. So osteoarthrtritic patients require significantly less pain medication with a significant improvement of quality life.
Variations in C-reactive protein, plasma free radicals and fibrinogen values in patients withosteoarthritis treated with Pycnogenol, 2008
Pycnogenol Is Protective Against Heart Disease, Diabetes and Inflammation:An Interview with Ronald Ross Watson, Ph.D., 2011
ASTHMA
Pycnogenol is also very useful to treat inflammation in patients with allergic asthma. It decreases nitric oxide production and reduces the interleukine -1β and IL-6 levels in cells. It also reduces the expression of inducible nitric oxide synthase (iNOS) and matrix metalloproteinase -9 and enhances the expression of hemeoxygenase (HO)-1. It decreases the inflammatory cell count and the levels of IL-4, IL-5, IL-13, and immunoglobulin (Ig) E in serum attenuating the airway inflammation and mucus hypersecretion. So pycnogenol has potential as a therapeutic agent for the treatment of allergic asthma.
Inhibitory effects of Pycnogenol® (French maritime pine bark extract) on airway inflammation in ovalbumin-induced allergic asthma, 2013
ERECTYLE DISFUNCTION
Erection requires the relaxation of the cavernous smooth muscle, which is triggered by NO. Pycnogenol in combination with L-arginine may cause an improvement in sexual function in men with erctyle disfunction. It enhances NO production which leads an improvement in blood vessel dilation and an increase in blood flow and oxygen supply to muscles. Moreover decrease in blood pressure, aspartate transaminase and γ-glutamyl transpeptidase (γ-GTP), and a slight increase in salivary testosterone are observed.
Clinical assessment of a supplement of Pycnogenol® and L-arginine in Japanese patients with mild to moderate erectile dysfunction, 2012
CHRONIC VENOUS INSUFFICIENCY
Pycnogenol is very useful in the treatment of chronicvenous insufficiency (CVI) and related venous disorders such as deep vein thrombosis (DVT), post-thrombotic syndrome, long haul air-travel-related leg oedema, venous ulcers and acute haemorrhoids. Clinical studies have shown that it can reduce oedema of the legs in CVI, reduce the incidence of deep venous thrombosis during long haul flights and enhance the healing of venous ulcers and haemorrhoidal episodes by topical application and/or oral administration.
Pycnogenol® in chronic venous insufficiency and related venous disorders, 2014
DOSING BY MOUTH
- For allergies: 50 mg twice daily.
- For asthma in children: 1 mg per pound of body weight given in two divided doses.
- For poor circulation: 45-360 mg daily, or 50-100 mg three times daily.
- For diseases of the retina, including those related to diabetes: 50 mg three times daily.
- For mild high blood pressure: 200 mg of pycnogenol daily.
- For improving exercise capacity in athletes: 200 mg daily.
SIDE EFFECTS AND INTERACTIONS
Pycnogenol is possibly safe when taken in doses of 50 mg to 450 mg daily for up to 6 months even if it can cause dizziness, gut problems, headache, and mouth ulcers.
Medications that decrease the immune system (Immunosuppressants) interacts with pycnogenol which seems to increase the immune system. By increasing the immune system pycnogenol might decrease the effectiveness of medications that decrease the immune system. It’s best to avoid using pycnogenol in case of “auto-immune diseases” such as multiple sclerosis (MS), lupus (systemic lupus erythematosus, SLE), rheumatoid arthritis (RA), or other conditions.
Moreover preliminary research suggests pycnogenol might be safe in late pregnancy but until more is known, pycnogenol should be avoided by women who are pregnant or breast-feeding.
