Phenolic Compounds: Going Beyond Vitamins and Minerals
Oleuropein taken via olive leaf extract, first cold-pressed organic olive oil or organic olive leaf tea is fundamental to human health and longevity regardless of DBS/IBS or any of the dozens of autoimmune disorders it will assist in correcting. Little consideration is given to the mechanism of action regarding phenolic compounds, but this is about to change with this comprehensive overview of what I consider to be the most fundamental phenolic compound.
Oleuropein is derived from the botanical name of the olive tree, which is Olea europaea. It is found in olive leaves, olive oil and the green skin of olives which is removed to make them palatable. Oleuropein is what gives all olive products, their bitter flavor, and when it comes to the benefits of olive products, bitter is better. Implementation of the following represents improved #mentalhealth better numbers on our #GutHealth checklist and overall better numbers on our Emotional Checklist which represents #depression, #anxiety, #stress and 14 other issues we measure and improve.
Candida (Yeast) Overgrowth Inflammation Disease and Ageing
Candida albicans is a normal part of the composition of the gut microbiota (bacteria). Candida is, however, an opportunistic yeast that can and will multiply when there is a disruption in the balance of the microbiota. There are many causes for this with the most obvious being stress and antibiotics. Other causes include diet alcohol environmental toxins, and in my case, a severe parasitic infection. The bottom line is once the microbiota is out of balance and candida begins to take over it causes an immune response that can be propelled into an autoimmune response. Once an autoimmune response is initiated and not immediately addressed, it can have a cascading effect which can initiate more autoimmune responses. These autoimmune responses can lead to a myriad of diseases.
Depending on the severity of a yeast infection, the microbiota can be very difficult to get back into balance, and this is, of course, if your MD recognizes that the microbiota is out of balance. The vast majority of autoimmune disorders are not treated from the root cause, which is a microbiota out of balance. Functional Medicine practitioners are currently the only group who are trained to take this approach.
The other major dilemma is false negatives when getting tested. I could see the yeast in the stool, so I insisted on being tested for candida overgrowth yet blood, urine, and three stool tests, one of which was comprehensive did not indicate an infection. This led me to a theory given the opportunistic nature of candida that this is a primary issue that must be addressed in any gut or an autoimmune issue. I am unaware of any instance in the medical literature where there was a case of a disrupted microbiota and candida was not a part of the equation. Even if one does not believe that candida is an issue because of negative test results, I believe it still must be addressed.
After ten years of experimentation with antifungals, probiotics, biofilm disrupters, and a perfect diet, I was still having neurological issues. At one point, I realized that IgG4 food antigens were an issue and lettuce was on this list, which meant I also stopped using olive oil as I consider olive oil a cold use oil.
After my first coconut oil fast followed up by an olive oil liver gallbladder flush, I passed a significant amount of yeast. At the time, I assumed this was a result of the coconut oil until I did a flush without doing a coconut oil fast. This led me to research oleuropein, which is a primary phenolic compound of olive oil and olive leaf.
An in vitro study showed that olive leaf aqueous extracts destroyed 15% of C. Albicans within 24 hours.155 Some discount this study because it was in vitro, but I have first-hand experience of how effective it is. There is a question however of how effective olive leaf extract supplements are, but I feel the 40% Oleuropein that I took was effective, but this is a subjective opinion. I also used Organic Olive Leaf Tea, which I found to be very effective. Even though olive leaf has the highest concentration of oleuropein, I found taking 2 to 3 tablespoons of olive oil on an empty stomach with an equal amount of lime or lemon juice caused the most significant die-off.
Why Oleuropein is the Definitive Biofilm Disrupter and Candida Killer
The problem with virtually all of the biofilm disrupters I have taken including monolaurin, HICA, and even coconut oil is that they only took me so far. I would see improvement and then it would plateau and went no further. I did not know if NAC was effective or if I was getting sick from it because it was a deregulated pharmaceutical that was giving me a bad reaction. Because of its previous pharmaceutical status, I did not want to risk it
I started dosing with oleuropein with 3 capsules of olive leaf extract per day. To try and find a therapeutic amount, I added one ounce of olive oil with an equal amount of lime juice twice a day. After the third day of this, I suffered a significant die-off and took a day off to recalibrate. When I ran out of the olive leaf extract capsules, I switched to Organic Olive Leaf Tea. I found this to be much more potent than the capsules but calibrating the tea and olive oil was a constant juggling act because of die-off.
I did not realize how effective olive oil was until I stopped eating it for a while and then reintroduced it. There was nothing I took over 5 years of trying to kill off this yeast infection that has been as effective as olive oil and olive leaf. My theory is that olive oil is not only a super candida killer but unlike coconut oil, it stimulates the release of bile, which gives the pathogens a double whammy. Unlike a capsule or pill, olive oil can be taken every day for an indefinite period of time with virtually no negative effects except for die-off from breaking down biofilm and killing pathogens and parasites.
The bottom line is that biofilm disrupters are the absolute foundation for resolving DBS/IBS. One must be aware of other biofilm disrupters that may not be obvious as this can increase die-off symptoms. Stevia which is used for Lyme disease biofilm is the best example of this because many people will use stevia as a replacement for sugar, and it will intensify the effects of other biofilm disrupters one may be using. There are issues with virtually all sweeteners, so I do not use any. Honey is the least offensive of all sweeteners in my opinion; however, it will stimulate the production of insulin and is a FODMAP.
Getting Worse Before Getting Better
The downside to using olive leaf extract, olive oil or olive leaf tea is that there are several mechanisms at play which have the potential of making symptoms worse. It is counterintuitive to take something that makes you worse, but on the upside, oleuropein is a food, and there are no known contraindications to it as there are with antibiotics, antifungals antivirals or deregulated pharmaceuticals.
Olive oil is a primary component of the Mediterranean Diet and scientist are now coming to realize that it is the use of olive oil in food preparation and not necessarily the diet itself that enables people to live healthy lives over the age of 100.
Testing for Candida
One test other than the standard IgG, IgA, and IgM antibody tests I also recommend the IgG4 test. You can also do a comprehensive stool analysis along with a urine test. Even though I passed a significant amount of yeast after a liver gallbladder flush, all of these tests came back negative for me. In my opinion, this is one of the reasons yeast overgrowth is at epidemic levels. I believe most people trust the tests and this can literally be a fatal mistake.
I believe it is reasonable to assume that if you have DBS/IBS or an autoimmune disease yeast overgrowth is a significant part of the equation if not the origin of the disease. Because of the false-negative tests, not to mention the fact that there are many other health benefits to using olive oil adults should take a minimum of two tablespoons of olive oil with an equal amount of lime on an empty stomach in the morning every day after acclimation. I am not saying you should limit yourself to two tablespoons per day; this is just a recommended minimum.
Counterfeit Olive Oil
In 2012 an estimated 70% of olive oil randomly pulled off grocery store shelves for testing was diluted with other cheaper oils. This was down to approximately 50% by 2015. I use Trader Joes First Cold-Pressed Organic Olive Oil, Whole Foods 365 Organic Olive Oil, and Lucini Reserve Organic Olive Oil. All of these have been confirmed as pure. If you are unsure about the olive oil, you are using you can go to https://www.aboutoliveoil.org/certified-olive-oil-list to see if it has recently been tested for purity.
A Multifaceted Phenolic Compound
Oleuropein exhibits multiple activities beyond being the most effective candida killer I have found. I suspect this is why after two months, I am still trying to increase the amount I am taking, which is beyond three tablespoons of olive oil a day.
A surprise effect was a neurological one. After back surgery in 1999, I experienced significant electrical impulses in my right leg. At times I would wake up, and I would be numb from the waist down or be consistently awakened by electrical jolts or buzzing in my right or both legs. This went on for 20 years then suddenly after taking a calibrated amount olive oil, olive leaf extract and olive leaf tea it suddenly and permanently went away.
I also noticed a thrashing on my right side in the vicinity of the liver and large intestine then on the left side. This was consistent with a tapeworm that I had passed a couple of years earlier. I initially wrote it off as a muscle spasm but then thought I would try three ounces of shredded coconut twice a day and the thrashing on the left side stopped within 24 hours with the thrashing on the right side significantly reduced than all but completely gone within a week. This led me to take a look at yet another issue that Oleuropein might be effective for, and that was parasites. I did not find anything specific to tapeworms, but I did find a study on Giardia lamblia and a comparison between olive leaf and metronidazolen which is an antibiotic used to treat a range of bacterial, fungal and protozoan infections. An in vitro test indicated olive leaf extract was more effective in killing the Giardia lamblia cysts.156 As I discovered it is not only important to take what is most effective but also something you can take indefinitely.
Below I list several more issues that Oleuropein is effective at addressing. Important to keep in mind that Oleuropein addresses the root cause of autoimmune disorders which are responsible for a wide range of diseases including Lupus, Celiac disease, Multiple sclerosis, Peripheral neuropathy and dozens of others.
Oleuropein potently and dose-dependently inhibits copper sulfate-induced oxidation of low-density lipoproteins. Oleuropein has both the ability to scavenge nitric oxide and to cause an increase in the inducible nitric oxide synthase (iNOS) expression in the cell.
Oleuropein increases the ability of LDL to resist oxidation and at the same time reduces the plasma levels of total, free, and esterified cholesterol.
Additionally, the potential protective effects of oleuropein have been investigated in isolated rat hearts. The organs were subjected to 30 min of no-flow global ischemia and then reperfused. At different intervals, the coronary heart effluent was collected and assayed for creatine kinase activity and reduced and oxidized glutathione.157
Oleuropein increases nitric oxide (NO) production in macrophages challenged with lipopolysaccharide through induction of the inducible form of the enzyme nitric oxide synthase, thus increasing the functional activity of these immunocompetent cells. It is well known that oleuropein elicits anti-inflammatory effects by inhibiting lypoxygenase activity and the production of leukotriene.157
Reflow in ischemic hearts was accompanied by a prompt release of oxidized glutathione; in ischemic hearts pretreated with oleuropein, this release was significantly reduced and was accompanied by prevention of membrane lipid peroxidation, which is considered a key factor in the pathogenesis of atherosclerosis.157
A plethora of minor constituents in olive oil has been identified as effective agents in mitigating the initiation, promotion, and progression of multistage carcinogenesis.
Oleuropein inhibits growth of LN-18 cells, a poorly differentiated glioblastoma cell line; TF-1a, a erythroleukemia; and tumor cell lines derived from Advanced-grade human tumors (786-O, renal cell adenocarcinoma; T-47D, infiltrating ductal carcinoma of the breast pleural effusion; RPMI-7951, malignant melanoma of the skin-lymph node metastasis; and LoVo, colorectal adenocarcinoma cells) in Swiss albino mice with soft tissue sarcoma.
Oleuropein aglycone is the most potent phenolic compound in decreasing breast cancer cell viability.
Secoiridoids deacetoxy oleuropein aglycone, ligstroside aglycone, and oleuropein aglycone induce strong tumoricidal effects within a micromolar range by selectively triggering high levels of apoptotic cell death in HER2-overexpressing breast carcinomas.
Oleuropein remarkably reduces the viability of MCF-7 cells and decreases the number of MCF-7 cells by inhibiting the rate of cell proliferation and inducing cell apoptosis (programmed cell death).
Antiproliferative activity of crude extracts and phytochemicals were exhibited (the dominant compound of the extracts is oleuropein) against cell lines at low micromolar concentrations. These extracts inhibit cell proliferation of human breast adenocarcinoma (MCF-7), human urinary bladder carcinoma (T-24) and bovine brain capillary endothelial (BBCE).157
Oleuropein has been shown to have strong antimicrobial activity against both Gram-negative and Gram-positive bacteria as well as mycoplasma. Phenolic structures similar to oleuropein seem to produce its antibacterial effect by damaging the bacterial membrane and/or disrupting cell peptidoglycans. Effective interference with the production procedures of certain amino acids necessary for the growth of specific microorganisms has also been suggested.
Oleuropein and hydrolysis products are able to inhibit the development and production of enterotoxin B by Staphylococcus aureus, the development of Salmonella enteritidis, and the germination and consequent development of spores of Bacillus cereus. Oleuropein and other phenolic compounds (p-hydroxybenzoic, vanillic and p-coumaric acids) completely inhibit the development of Klebsiella pneumoniae, Escherichia coli, and B. cereus.
Antimicrobial activity of commercial Olea europaea (olive) leaf extracts (abundantly oleuropein) was shown against Campylobacter jejuni, Helicobacter pylori, and methicillin-resistant Staphylococcus aureus (MRSA). These extracts play a role in regulating the composition of the gastric flora by selectively reducing levels of H. pylori and C. jejuni. 157
In a U.S. patent, it has been claimed that oleuropein has potent antiviral activities against herpes mononucleosis, hepatitis virus, rotavirus, bovine rhinovirus, canine parvovirus, and feline leukemia virus. Studies have also shown that oleuropein exhibits significant antiviral activity against respiratory syncytial virus and para-influenza type 3 virus.
There is also one anecdotal report that olive leaf extracts augment the activity of the HIV-RT inhibitor 3TC. The olive leaf extracts were investigated for their antiviral activity against viral hemorrhagic septicemia virus (VHSV), a salmonid rhabdovirus, and against HIV-1 infection and replication. 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.
One of the suspected targets for olive leaf extract (mainly oleuropein) action is HIV-1 gp41 (surface glycoprotein subunit), which is responsible for HIV entry into normal cells. 157
The phenol components of olive oil have a direct antioxidant action on the skin, especially oleuropein, which acts as a free radical scavenger at the skin level.
Normal human fibroblasts undergo replicative senescence (cell deterioration) due to both genetic and environmental factors. The proteasome, a multicatalytic nonlysosomal protease, has impaired function during aging, while its increased expression delays senescence in human fibroblasts. Oleuropein enhances proteasome activities in vitro more effectively than other known chemical activators, possibly through conformational changes of the proteasome. Moreover, continuous treatment of early passage human embryonic fibroblasts with oleuropein decreases the intracellular levels of reactive oxygen species (ROS), reduces the amount of oxidized proteins through increased proteasome-mediated degradation rates and retains proteasome function during replicative senescence. Importantly, oleuropein-treated cultures exhibit a delay in the appearance of senescence morphology, and their life span is extended by approximately 15%.157
According to the free radical theory, aging is the result of oxidative injury, mainly to mitochondria, over the lifetime of an individual. Some of the oxidative damage cannot be entirely counteracted, which leads to cellular dysfunction. Mitochondrial membranes are very sensitive to free radical attack because of the presence of a double bond carbon-carbon in the lipid tails of its phospholipids, which leads to the production of cognitive and neurodegenerative disease.
In vitro and epidemiological studies have pointed out the positive impact of naturally extracted polyphenols on the incidence of age-related disorders, such as dementia. One study has reported that oleuropein decreases or even prevents Aβ aggregation, which is inherent to Alzheimer’s disease (AD). The potential effect of oleuropein on brain function in AD is analogous to atherosclerosis because they both are age-dependent diseases in which abnormal accumulation of a normal metabolite (cholesterol and Aβ, respectively) precedes clinical symptoms and leads to disease.
The link between heart disease, hypercholesterolemia, and AD is due to similar mechanisms of pathogenesis of these disorders. The circumstantial evidence that cholesterol-related interventions can alter Aβ deposition suggests that oleuropein might be promising in the management of AD. Furthermore, the importance of inflammatory processes in the clinical manifestation of AD, combined with the epidemiological evidence of a protective effect of anti-inflammatory agents against AD, suggest that a polyphenolic natural extract, such as oleuropein, could prove effective against age-dependent disease.157
Further pharmacological activity of oleuropein includes diverse healing properties due to its vasodilatory, anti-platelet aggregation, hypotensive, anti-rheumatic, diuretic, and antipyretic effects. Prevention of free radical formation by oleuropein occurs through its ability to chelate metal ions, such as Cu (copper) and Fe (iron), which catalyze free radical generation reactions, and through its inhibitory effect on several inflammatory enzymes like lipoxygenases. Previously, oleuropein was reported to have an anti-hyperglycemic effect in diabetic rats. Oleuropein inhibits hyperglycemia and oxidative stress induced by diabetes, which suggests that the administration of oleuropein is helpful in the prevention of diabetic complications associated with oxidative stress.
The Bottom Line
There are many moving parts to the development of a disease, and no rock should be left unturned, but I consider oleuropein to be a foundational protocol regardless of whether you are battling a disease or not.
About Kelly Burris, PhD, MBC