Pycnogenol Antioxidant Activities

Pycnogenol® is the extract of the bark of the French pine tree (Pinus pinaster). It is a strong antioxidant and a potent free-radical scavenger. Pycnogenol contains approximately 85% proanthocyanidins (OPC’s). Oligomeric Proanthocyanidin is the major active ingredient in Pycnogenol and Grape seed extract. In vitro and animal-based studies demonstrate that pycnogenol has antioxidant, immunostimulant, anti-inflammatory, and neuroprotective activities.

Pycnogenol Antioxidant Benefits

Pycnogenol is a unmatched blend of bioflavonoids not found in any other supplement. It has been found to be much more powerful than vitamin C and E, grape seed extract, Coenzyme Q10 and lipoic acid. Pycnogenol decreases free radical production, enhances cells’ natural antioxidant systems, and scavenges free radicals, preventing the development of oxidant-related diseases. Pycnogenol decreases DNA damage by its antioxidant activity and probably other mechanisms.

Antioxidants are substances that protect cells from oxidative damage caused by molecules called free radicals. Free radicals are unstable molecules that attack normal cells and damage membranes. Cell death caused by free radicals contributes to a variety of diseases, including heart disease, some forms of cancer and nervous system disorders such as Alzheimer’s. Elevated antioxidant amounts in the body may protect against damage to cells and cellular components, thus helping to reduce the risk of many chronic degenerative diseases. Pycnogenol is a powerful antioxidant which consists of a highly bioavailable flavonoid called proanthocyanidin. Pycnogenol, acts  as an antioxidant by scavenging reactive oxygen and nitrogen species and suppressing production of peroxides. It increases the activities of antioxidant enzymes by increasing the intracellular glutathione amount.  Pycnogenol also, it recycles vitamin C, regenerates vitamin E and increases the endogenous antioxidant enzyme system.

Pycnogenol may guard against the formation of tumors or another cell mutations caused by free radicals and may help protect against degenerative diseases like cancer. Pycnogenol has been recognized as an anti-oxidant and for its ability to prevent activation of  NFkappaB, a transcription factor that is generally overactive in cancer cells. New research by Dr. Stewart Brown of the “University of  Nottingham” shows that its radical scavenging effect slows cancer mutagenesis. Dr. D. White of the University of Nottingham explained that it inhibits the enzyme monooxygenase, thereby preventing the formation of highly carcinogenic diole epoxide of benzopyrene.

Pyncogenol gets quickly absorbed from the gastrointestinal tract due to its excellent water solubility. The compound fixes rapidly to cell membranes in veins and capillaries and connective tissue where it exerts a stabilizing effect  on cellular membranes of all types. Outside and inside the membranes it counteracts destructive oxidation by free radicals from this solubility property. This super antioxidant; It can be retained for as 72 hours while it neutralizes free radicals and prevents oxidation. An in vivo study showed a 40 percent increase in antioxidant potency in blood following 3 weeks supplementation with 150 mg pycnogenol a day.

Experiment has showed that Pycnogenol flavonoids exhibited an anti-enzyme property which prevented the breakdown of collagen and elastin, the very compounds which keep skin firm and inhibit the formation of wrinkles. Also, pycnogenol lightens up dark spots on the skin that are due to over-pigmentation.

Pycnogenol helps to protect capillaries by binding to blood vessels walls and reducing permeability. Pine Bark Extract contains substances that might improve blood flow. Has been shown to improve endothelial function and blood flow. Pycnogenol, inhibits superoxide radical in blood flow, and protects blood vessel walls. Double blind placebo controlled studies have indicated that participants suffering from circulatory insufficiencies and diseases of the lymph system demonstrated important improvement in pain control and vessel elasticity after taking these flavonoids.

Antiviral Effects of Olive Leaf

Olive Leaf extract has anti-viral, anti-bacterial and anti-fungal effects. Oleuropein and hydroxytyrosol are considered as main polyphenolic compounds in olive leaf. Oleuropein is converted into elenolic acid in the body which may prevent  bacteria and viruses  from replicating. Olive leaf extract has been shown to be effective against herpes, flu and colds, bacterial infections, vaginal yeast infections, malaria, and hepatitis. In 1969 scientists showed olive leaf constituents are strong in vitro inhibitors of numerous viruses, including parainfluenza, pseudorabies, herpes, and some forms of polio. Almost every virus tested, including several cold and influenza viruses, was inactivated when exposed to a constituent of olive leaf extracts (OLE), calcium elenolate. Olive leaf extract (Oleuropein) has been patented in the United States for antiviral activity against viral diseases, including hepatitis and herpes.

Antiviral and Antibacterial Activity

First researches by the pharmaceutical company Upjohn found extracts from olive leaves to be effective in treating infection caused by a large number of viruses as well as bacteria and parasitic protozoans. Oleuropein is able to stop viruses in their tracks, by neutralizing the enzymes that are important for the virus to replicate itself and spread. The major constituent of olive leaf is the phytochemical oleuropein, which is broken down to elenolic acid, has a potent anti-bacterial activity, and the ability to interfere with critical amino acid production essential for viruses. Investigators have showed olive leaf  constituents, especially elenolic acid and its salt, calcium elenolate, are effective in vitro against many viruses investigated, including parainfluenza, pseudorabies, Herpes simplex, Varicella zoster, coxsackie virus, myxoviruses, rhinoviruses, encephalomyocarditis, 2 strains of  leukemia virus and some forms of polio.

Olive leaf extract interacts with the protein in cold and flu virus particles to halt infection, according to a research reported in “Alternative Medicine Review“. In lab experiments, olive leaf extract has shown virucidal effect like herpes simplex 1 and 2 and herpes zoster. Research conducted in 1969, proved that a compound of oleuropein from the olive leaf could kill all viruses, including the herpes, against which it was investigated. In 1992 French scientists found that all of the herpes viruses were inhibited or killed by extracts from olive leaf.

Lab studies have a shown that olive leaf extracts can influence proteins that prevent cell death that may prove effective against the HIV (Human Immunodeficiency Virus).  Anti-HIV effects of  leaf extract include up-regulation of the expression of apoptosis inhibitor proteins as well as protein kinase signaling molecules. Cell-to-cell transmission of HIV was inhibited in a  dose-dependent manner with EC50s of 0.2 µg/ml, and HIV replication was inhibited in an in vitro experiment. The olive leaf extract indicates antiviral effect against viral haemorrhagic septicaemia rhabdovirus (VHSV). A study in reported 2003 edition of  Biochemical and Biophysical Research communications concluded that oleuropein helped the prevent the adherence of the hemorrhagic septicaemia virus to normal healthy cells, and reduce the infectivity of the virus by up to 30%.  Oleuropein, inhibited the in vitro infectivity of the viral haemorrhagic septicaemia virus. Incubation of virus with oleuropein before infection reduced the viral infectivity to 10 and 30%, respectively.

Olive leaf extracts has been found to kill a number of microorganisms including, yeasts, bacteria and fungi. Olive leaf extract (oleuropein) has been shown to have strong antimicrobial effect against both Gram Negative and Gram-positive bacteria as well as mycoplasma. Research reported by the “American Society for Microbiology“, found that OLE (olive leaf extract) inhibited the growth of every virus, bacteria, fungi and protozoa it was tested against.

An aqueous extract of olive leaf was bactericidal against Klebsiella pneumoniae, Pseudomonas aeruginosa, E. coli, and Staphylococcus aureus. Researches in Israel found the extract efficacious against Streptococcus by damaging the cell membrane of the bacteria, and therefore allowing intercellular substances like potassium, phosphorus and glutamate toleak out, disabling the bacteria. A study reported in the Apr 2003 edition of  “Mycoses” explored the effects of olive leaf extract against strains of various bacteria and fungi in vitro. Within 3 hours, olive leaf extracts killed nearly all bacteria, and within 24 hours, it completely destroyed candida, the yeast-like fungus responsible for vaginal yeast infections. New researches demonstrated the antimicrobial activity of olive leaf extracts against Campylobacter jejuni, H. pylori and MRSA (methicillin-resistant Staphylococcus aureus). According to a study reported in in May 2009  in the International Journal of Antimicrobial Agents OLE (olive leaf extract) may reduce levels of the bacteria H. pylori and Campylobacter jejuni in the digestive tract.

Oleuropein Natural Hypertension Remedy

Olive leaves come from the olive tree (Olea europae), which is native to the Mediterranean. Oleuropein is a non-toxic secoiridoid found in the leaves and fruits of olive. One of these bioactive compounds is the secoiridoid oleuropein, which can constitute up to 6-9% of dry matter in the leaves.

Olive Leaf Hypertension and Heart Health Effects

Olive leaf extracts and their oleuropein constituents are best known for their blood pressure-lowering properties. Hypertension thought to be responsible for 50% of all heart attacks and strokes. Oleuropein, favorably modulates arterial resistance or stiffness, high blood pressure’s core mechanism. Research found that olive leaf extract causes relaxation of the arterial walls and reduces high blood pressure. It is oleuropein that is largely responsible for the useful effect on high blood pressure. The oleuropeoside, which was isolated from olive leaf during the twenties, caused important hypotension in rats, due to prolonged peripheral vasodilatation of  isolated aorta. Olive leaf water extract proposed property as an inhibitor of the ACE (angiotensin converting enzyme) has been showed in vitro.

Scientists designed a study to compare its effects to Captopril, a blood pressure medication known as an ACE-inhibitor. A study reported in the Feb 2011 edition of  Phytomedicine sought to compare the effects of  OLE (olive leaf extract) against captopril. For 8 weeks, subjects either took the medication or 500 mg of  olive leaf extracts twice a day. All subjects experienced important drops in both systolic and diastolic blood pressure. Although they utilize different mechanisms of action, both olive leaf extracts (oleuropein) and captopril function inside the vasculature to lessen the tension in the walls of blood vessels and promote widening of the vessels, eventually lowering blood pressure. This study demonstrate olive leaf extract may be as effective as captopril for treating Stage 1 high blood pressure.

Taking 1000mg of a specific olive leaf extract (EFLA®943) can lower blood pressure in people with mild hypertension. To test this in humans, scientists from Germany and Switzerland carried a pilot study with 20 identical (monozygotic) twin pairs who had an increased blood pressure. Identical twins were used to help keep the data consistent, because genetic differences can make people respond differently to the same therapies. Participants were either given placebo capsules or capsules containing doses of 500mg or 1000mg of leaf extract EFLA®943. At the study’s conclusion, those who took the highest daily dosage of  EFLA®943 (1000 mg) received the highest benefits. At the end of the 8-week study, the group that took 1000 mg per day had dropped their systolic blood pressure by an average of 11 points.

Preliminary research findings demonstrate that compounds in olive leaf may help by assisting normal platelet aggregation, which may in turn play a role in helping to prevent the formation of clots. Olive leaf extracts appears to lower levels of deleterious blood fats, called triglycerides, known to raise the risk of  heart attacks and strokes. In a study, participants who took the olive leaf pill for 8 weeks saw a significant reduction in blood pressure readings and triglyceride levels.  Oleuropein shows anti-atherogenic activity. In 2003, researchers reported that oleuropein reduces monocytoid cell adhesion to stimulated endothelium as well as vascular cell adhesion molecule-1 (VCAM-1) mRNA and protein. Compounds found in olive leaves have been shown to help directly avoid the formation of arterial plaques in 2 ways. 1) They reduces the production and activity of a series of adhesion molecules. 2) they reduce platelet aggregation by multiple mechanisms, which reduces the risk that tiny clots will form at sites of plaque to produce a stroke or heart attack.

Anticancer Effects of Olive Leaf

Oleuropein is the most important phenolic compound in the fruit of olive tree. In-vitro studies show that oleuropein induces apoptosis in numerous cancers, including leukemia, breast cancer and colon cancer, and inhibits proliferation and metastasis. Scientists demonstrated that oleuropein aglycone is the most strong phenolic compound in decreasing breast cancer cell viability. Although oleuropein has shown strong anticancer activity the underlying action mechanism remains largely unknown.

Olive Leaf Extract and Cancer

Oleuropein, is a potent antioxidant and anti-angiogenic agent. Oleuropein inhibit the proliferation and migration of advanced-grade tumor cell lines in a dose-responsive manner. Olive-leaf extracts were found to inhibit cell proliferation of human breast adenocarcinoma (MCF-7), and human urinary bladder carcinoma. Oleuropein exhibits specific cytotoxicity against breast cancer cells, with higher effect on the basal-like MDA-MB-231 cells than on the luminal MCF-7 cells. Latterly, researchers reported that 200 lg/mL of oleuropein remarkably decreases  the viability of MCF-7 cells and reduces  the number of  MCF-7 cells by inhibiting the rate of cell proliferation and inducing cell apoptosis.

When oleuropein was administered orally to mice that had developed tumors, it regressed the tumors in 9 to 12 days. In an experiment, oleuropein irreversibly rounded cancer cells, preventing their replication, motility, and invasiveness; these effects were reversible in normal cells. When administered orally to mice that developed spontaneous tumors, oleuropein completely regressed tumors in 9-12 days. This experiment; reported by Biochemical and Biophysical Research Communications. A version of oleanolic acid, found in olive leaf, substantially reduced the growth of liver tumors in lab animals, according to scientists from “Johns Hopkins University and Dartmouth Medical School“. In their study, the use of small amounts of the  OLE (olive leaf extract), a triterpenoid analog called CDDO-Im, yielded a greater than 85% diminution in the volume of liver tumors.“Even at low-doses, CDDO-Im induces cell protecting genes, inhibits DNA damage by aflatoxin and dramatically blocks development of liver tumors,” according to Melinda Yates lead author of the study.

Quercetin as an Prostatitis Treatment

Prostatitis is inflammation of the prostate. Usually causes painful or difficult urination. Quercetin has anti-inflammatory and antioxidant properties and may decrease symptoms of chronic prostatitis. It is occasionally coupled with papain and bromelain, have anti-inflammatory effect, but also help to improve the absorption of quercetin.

Quercetin Prostatitis Benefits

Quercetin is a polyphenolic flavonoid that may benefit men with chronic prostatitis/chronic pelvic pain syndrome (CP/CPPS) through antioxidant and anti inflammatory  mechanisms. In vitro and animal studies have shown quercetin to improve symptoms of chronic nonbacterial prostatitis in mice. According to “Mount Sinai Hospital“, quercetin is an effective cure for chronic prostatitis. The studies shows symptoms begin to disappear after a few months of daily use. Current Urology Reports in July 2007 reported an article pointed out that the new method of therapy of prostatitis have some findings of efficacy include compounds such as quercetin phytotherapeutic.

A study showed that 500 mg of quercetin twice daily for at least 2 weeks significantly improved symptoms in 59% of men with chronic prostatitis. The results of an clinical trial reported in the Dec 1999 edition of  “Urology” shows that quercetin helps to reduce chronic pelvic pain in men with chronic prostatitis. In this study, investigated the effects of 500 mg of quercetin, taken twice daily, in thirty men with chronic prostatitis. After the one-month, study was over, 67% of the men taking the quercetin reported a measurable improvement in symptom. Papain and bromelain promote absorption of quercetin and have anti-inflammatory effects as well. Investigators at the “Institute for Male Urology” gave men with prostatitis 1000 mg of quercetin daily for 1 month. Two-thirds of the men had at least a 25% diminution in symptoms. When the  researchers added papain and bromelain to enhance quercetin absorption, 82% of the patients got better.