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Methylene blue (MB) is an antioxidant with high redox activity, able to rapidly "oscillate" between its oxidized and reduced forms, much like that seen in vitamin C. A small molecule with fat- and water-soluble characteristics, it reaches all areas and cells of the body, and it especially concentrates in the brain and central nervous system. Like vitamin C, MB is highly effective in maintaining a healthy distribution of electrons already in the body, along with the distribution of new electrons assimilated from the nutrients in a healthy dietary regimen.

MB has a unique ability among antioxidants and other biomolecules to relay electrons from the first complex in the energy-generating Krebs cycle in the mitochondria directly to the fourth complex. This allows the energized fourth complex to then produce ATP without the additional expenditure of energy in the steps of the electron transport chain that was bypassed. As such, MB allows dysfunctional mitochondria to produce healthy levels of ATP while producing less oxidative stress in the process, an optimal way both heal those mitochondria while promoting healing anywhere in the body. Photodynamic therapy (PDT) can also directly activate the energy production of the fourth complex in the electron transport chain.

Like vitamin C, MB is also a very powerful anti-pathogen. It has been documented to salvage even late-stage COVID patients supported on ventilators with hypotension secondary to septic shock. For viruses in general, MB has the unique ability to attack the circulating virus, to block its binding of the virus to the cells of the body, and to stop the proliferation of the virus inside the infected cell. When administered as recommended MB is exceptionally well-tolerated, with a safety profile that extends now over a period of more than 100 years of clinical use.

Methylthioninium chloride, commonly called methylene blue, is a salt used as a dye and as a medication.

Methylene blue is one of the oldest organic dyes ever produced. In 1876, Heinrich Caro synthesized this pure blue dye to stain wool for the textile industry. But it wasn’t long before medical researchers discovered uses for methylene blue far beyond fabric coloring.

METHYLENE BLUE: A BRIEF HISTORY

During the second World War, methylene blue was given to soldiers as an antimalarial drug. It is considered one of the most, if not THE most, effective drug for the disease to this day. Only within the past couple of decades, have scientists decoded exactly how methylene blue provides its benefits to the brain and body, spanning all the way down to the molecular level in mitochondria.

In 1880, microbiologist Robert Koch pioneered the use of methylene blue for staining cells and microbes for easier visualization under a microscope. Not only is methylene blue capable of staining the Malaria-causing parasite, but it was found also to be capable of killing it. Paul Ehrlich in 1891 published a case study on two Malaria patients who were cured using methylene blue. Its use for the treatment of Malaria awarded methylene blue the honor of being the first pharmaceutical drug in history.

Methylene blue is the first drug to be tested and used in humans. Chemically known as methylthioninium chloride, it was first synthesized in 1876, and it was used as an industrial dye. It was later found to be an excellent dye for staining microbes and human tissues as well. In 1891 it was found to be very effective as an anti-malarial agent by Paul Ehrlich. Of note, Ehrlich first coined the term "magic bullet" to refer to how effectively MB targeted and accessed the nervous system. It has since been established to have a selective affinity for the nervous system, although it is highly effective in reaching all cells in the body.

As a powerful antioxidant with the ability to target the brain, MB was used as an antipsychotic drug for 50 years before phenothiazine became the first "official" antipsychotic drug. It continues to be used as a dye for the staining of biological tissue specimens as well as a diagnostic tool in surgical procedures. It has also been established to have numerous and very significant therapeutic purposes for a wide range of medical conditions. Some of the more significant conditions to be consistently and successfully treated by MB include the following:

  • Infections, from minimal to life-threatening, including those having progressed to septic shock. Also, acute respiratory distress syndrome (ARDS) and hypoxemia secondary to COVID or any of multiple different pathogens; also used for disinfection of plasma to be used for transfusion.

  • Mitochondrial dysfunction.

  • Depression, dementia, psychosis, impaired memory, as well as multiple acute and chronic neurological conditions.

  • Methemoglobinemia, in which the oxygen-carrying capacity of the blood is critically depleted. MB has FDA approval as a first-line therapy for this condition.

Methylene blue works by directly increasing mitochondrial respiration through its interactions with the electron transport chain—a series of four protein complexes that sit inside the mitochondrial membrane, are responsible for producing ATP—a process called oxidative phosphorylation. Methylene blue can act as an alternative electron carrier when any of the mitochondrial complexes I – IV are dysfunctional.

All diseases are metabolic in nature, and methylene blue selectively targets cells and tissues that have dysfunctional metabolism.

3 WAYS METHYLENE BLUE INHIBITS NITRIC OXIDE

  • Inhibits nitric oxide synthesis.

  • Disassociates nitric oxide from the cytochrome c oxidase enzyme.

  • Scavenges existing nitric oxide.

METHYLENE BLUES EFFECTS ON METABOLISM

  • Increases oxygen consumption and ATP production.

· Increases glucose consumption.

  • Increases the NAD/NADH ratio.

  • Decreases lactic acid production.

  • Is a potent antioxidant—acts similarly to vitamin E.

  • Inhibits monoamine oxidase (MAO).

  • Acts as an alternative electron carrier in the mitochondrial electron transport chain.

METHYLENE BLUE EFFECTS ON HORMONES

  • Inhibits prolactin.

  • Inhibits estrogen. Increases thyroid hormone and lowers TSH.

  • Increases testosterone.

METHYLENE BLUE AND THE BRAIN

Methylene quickly concentrates in the brain, once injected into animals. It has been under investigation for its potential use in dementia and other neurodegenerative related disorders.

METHYLENE BLUE TARGETS DISEASED TISSUES

Methylene blue has the ability to selectively target diseased tissues in the body. The cells with the greatest dysfunction metabolically receive aid first. Referring to methylene blue, Paul Ehrlich coined the term “magic bullet,” which is still in use today.

METHYLENE BLUE REDOX TEST FOR MILK

In the 1940s and 1950s, the methylene blue redox test was used to determine the freshness of milk by indirectly revealing how much oxygen is inside the milk.

METHYLENE BLUE REDOX SKIN TEST

Similar to the milk test, if you put a drop of methylene blue on your skin, the quicker it disappears, the more starved for oxygen (hypoxia) that local tissue is. Since methylene blue substitutes for oxygen, the more hypoxic the skin tissue, the quicker it gets used. If the methylene blue drop on your skin completely disappears in less than six hours, it indicates local hypoxia.

THE TOP 10 BENEFITS OF METHYLENE BLUE

1. An antidote for chemical poisoning and overdose.

2. The greatest anti-malarial drug ever discovered.

3. The pathogen warrior.

4. Forget Dementia, Alzheimer’s, Parkinson’s.

5. Cognitive enhancement: A brain-boosting powerhouse.

6. Depression no more.

7. Hope for Autism.

8. The great pain reliever.

9. A healthier heart.

10. Cancer.

Methylene blue is always present as the main antidote required in emergency and critical care units. Methylene blue is so essential and routinely used in hospital emergency rooms that scientists from the United States, Japan, Greece, Italy, and Canada have stressed the importance of stockpiling it.

Methylene blue is routinely used in hospital emergency rooms for: circulatory shock, neuroprotection, anaphylaxis (severe allergic reactions), and overdoses and chemical poisonings. Cyanide and carbon monoxide poisoning victims in critical care units worldwide have been treated successfully using MB.

Methylene blue has been shown to have renewable auto-oxidizing properties, which acts as an electron cycler that allows MB to redirect electrons to the mitochondrial electron transport chain. This enhances ATP energy production and promotes cell survival. This means MB directly gives electricity to the mitochondria, the powerhouse of the cell, and helps regenerate the cells. MB reduces reactive oxygen species production from the mitochondrial electron transport chain.

The antioxidant and electron donor property of MB is unique and can be utilized for photodynamic cancer treatment, neuro-regeneration, antiaging, and pain relief. It has antimalarial, antiviral and antidepressant properties.

MB enhances cytochrome c oxidase activity to produce more ATP in cells under normal oxygen conditions. MB replaces oxygen as the oxidant to sustain ATP generation under low oxygen conditions, while simultaneously reducing oxidative stress. MB is one of the most effective compounds to delay senescence.

MB AND CANCER

MB photodynamic therapy (PDT) has been shown to induce massive cell death in breast cancer models, while having no effect on healthy cells. PDT has been effective in melanoma, basal cell carcinoma, prostate cancer, and Kaposi sarcoma. On the PubMed website, the entry "cancer methylene blue" results in about 2,500 references.

The articles that appear address primarily the role of MB in:

  • Localizing (staining) of cancerous tissues and/or identifying as many involved lymph nodes as possible.

  • The inhibition, inactivation, or killing of a wide array of different cancer cells in vitro, with and without the application of PDT.

  • The superiority of MB in treating mice tumors over traditional chemotherapy.

  • In combination with PDT, the complete resolution of AIDS-related Kaposi's sarcoma skin lesions that had been unresponsive to chemotherapy with MB and toluidine blue.

  • The direct treatment of cancer in dogs.

  • The direct treatment of cancer in humans. While treating different types of cancer, the author asserted that MB reliably stopped pain secondary to cancer, improved general health, and added years of longevity. This was reported in 1907! Another article asserted that MB was found to have anticancer effects over a century ago. NO significant clinical applications of methylene blue on cancer patients were found other than the 1907 study cited above.

The efficacy of an inexpensive and safe agent like MB in many different and even advanced medical conditions make it an ideal general add-on or even stand-alone treatment most of the time. Furthermore, its potent anti-cancer effects in vitro make it especially puzzling why straightforward clinical studies on cancer patients with MB alone or in combination with other agents have not been reported. Even the positive effects of the much-ignored vitamin C on cancer patients have been published in many articles, yet the wonderful properties of MB have been known much longer now than vitamin C. The literature even suggests that MB could play a positive role in the treatment of cancer patients.

ANTIOXIDANT EXTRAORDINAIRE

An ideal antioxidant is one that is equally stable chemically in either its reduced or oxidized state, while having physical access to all the oxidized biomolecules in the body. Such a quality allows the continued giving and taking of electrons throughout the cellular and extracellular spaces, as that molecule does not resist being either reduced or oxidized. This redox (reduction-oxidation) property helps to conduct electron flow inside the cells.

This helps to generate and sustain the microcurrents (a current is literally an electron flow) that have been identified inside cells, which work to maintain healthy transmembrane voltages. A sick cell always has a low transmembrane voltage, which directly reflects a redox balance skewed toward oxidation, with a limited influx of new antioxidant (nutrient) molecules available to deal with any new pro-oxidant (toxic) molecules. Normal transmembrane voltages are critical in maintaining healthy ion channels, transporters, pumps, and enzymes in the cell. They are also critical for the optimal synthesis of ATP.

A toxin always works to cause oxidation wherever it is found or ends up. It is always pro-oxidant in its chemical impact, as it seeks to oxidize a biomolecule and then keep the electron it has "robbed." The electron it acquires makes the toxin much more stable chemically, and such a reduced toxin will not give up the electron again to another oxidized, or electron-depleted, biomolecule. This means that the electron-sated toxin will never re-donate its electron to an oxidized biomolecule, as would occur with an electron-sated, or reduced, antioxidant molecule.

In addition to increasing the numbers of oxidized biomolecules, this retention of electrons by toxins also impedes/decreases electron flow (microcurrents) since the newly acquired electrons are tightly held and never again released in the manner of an antioxidant that is continually giving and taking electrons. An antioxidant like vitamin C decreases the total number of oxidized biomolecules and supports optimal microcurrents, and a toxin does the opposite.

It is the antioxidant properties of MB that results in the impressive clinical impact it has on so many conditions. In this regard, there is a striking parallel in what MB can do in the body with what vitamin C can do. Both vitamin C and MB are small molecules, and they effectively reach every cell in the body. However, MB requires no active or passive cell membrane transporters as does vitamin C, and it has both lipid-soluble and water-soluble characteristics. Because of this, MB passes easily through lipid-rich cell membranes, after which it disseminates throughout the water-based cell. Also, while both MB and vitamin C access the brain, MB has been found to have a brain concentration up to tenfold higher than in the serum as quickly as one hour after intravenous administration. Uptake is very rapid in the other organs as well.

MB also has well-documented antitoxin properties like vitamin C, but the studies documenting them are much less prolific than those showing the similar effects of vitamin C on pro-oxidants, and other poisons. MB helps protect the kidneys against the toxicity of the chemotherapeutic agent, cisplatin. MB has also been shown to protect the brain against the toxicity of another chemotherapeutic agent, ifosfamide. It also was shown to effectively treat the encephalopathy induced by ifosfamide after it had developed. And even though there is not an abundance of articles demonstrating the ability of MB to neutralize toxins and repair toxic damage, multiple researchers recommend it be routinely available as a general emergency antidote.

Many toxins also inflict harm in some individuals by the formation of methemoglobin with a reduction of oxygen delivery to the tissues. Such toxin excesses or poisonings can be effectively treated with MB, as it is already the treatment of choice by many clinicians for methemoglobinemia. MB is always a good partner to be administered along with vitamin C for any excess toxin or overdose. The addition of magnesium with MB and vitamin C to overdose patients offers additional protection against the development of fatal arrhythmias that can occur before the MB and vitamin C can resolve and block further toxic impact.