During my studies, I have been fascinated by vitamin C, both because of its effects on human physiology and its history of constant conflict with traditional medicine.
And it is from the history of this extraordinary molecule that we are going to begin our journey, giving the reader independent information, free from any kind of conflict of interest.

A LITTLE HISTORY

The vitamin C theme, chemically called ascorbic acid, was born in a very far era, millions of years ago when our progenitors primates, along our family tree, stopped producing it. We are among the very rare animals, in fact, along with other primates, India’s piglets and a few species of frugivorous bats that lost the gene for the L-gulono-gamma-lactone oxidase enzyme, the enzyme required in the last step for the ascorbate’s synthesis.

During the course of human evolution, the gene responsible for this vitally important enzyme underwent innumerable mutations until it ceased to function [1],

according to some hypotheses this is because being primates that consumed huge amounts of fruit with huge amounts of vitamin C, the need to independently produce it ceased.

Vitamin C intake became vital, and since then we have been exposed to chronic deficiency, which resulted in the extinction of many species, including the famous Neanderthals, which use to eat only meat.

Obviously, we were unaware of this deficiency and we did not know anything about this molecule and its effects on our physiology until Homo sapiens realized that without consuming fruit, they died of a terrible illness, scurvy. The first meeting with scurvy occurred in ancient Egypt around 1500 BC but we have to wait for explorers’ sea trips from 1500 to 1800 to reach the first casual medical considerations.

The famous worldwide circumnavigation in 1520, which saw Ferdinando Magellano as the protagonist, ended with 80% of the crew decimated by the alleged disease. Offshore for several months, and without conservation techniques it was impossible to load fruits and vegetables as food supply.

After about a month without vitamin C intake, the sailors showed the brutal symptoms of scurvy like widespread hemorrhage, bleeding gums and falling teeth due to the breakdown of the protein that makes up the matrix of human tissues, collagen, whose synthesis depends merely on vitamin C intake.

In many books and diaries on board, these poor sailors are described in total agony, literally falling apart and bleeding everywhere, basically because their cells were no longer held together by collagen. Death was inevitable.

Since then, the importance of ascorbic acid was understood, and the ships before any journey were loaded with cedar tea and returning from long exploration trips, the sailors who were treated with vitamin C-rich foods usually got back to life.

EARLY SCIENTIFIC STUDIES

But for more concrete studies on ascorbic acid and its therapeutic uses we have to wait for the ’30s, the period when the polio virus begins to spread like wildfire, killing more than half a million people in the world every year.

In 1935, experimental evidence showed that the polio virus was inactivated when in vitro combined with small amounts of ascorbic acid and this compound injected into the rhesus monkeys did not cause disease [2].

Based on this evidence, experimental studies regarding vitamin C and polio went on and in the late 1940s, the American physician from Austria, Frederik Klenner, wrote a scientific article in which he reported 60 cases of bulbous polio, treated with high doses of Vitamin C, administered simultaneously by mouth, intramuscularly and intravenously [3].

The scientist claimed to be able to cure bulbous polio in 96 hours, as long as Vitamin C is administered uninterruptedly and at high doses. His findings, although confirmed by other well-known colleagues, were completely ignored, albeit Albert Sabin himself, who will become famous for the anti-polio oral vaccine, has used Vitamin C to treat monkeys in the lab.

THE GOLDEN AGE OF ASCORBIC ACID

But in the ’70s began the golden age of vitamin C, first with Irwin Stone and later with Linus Pauling.
Irwin Stone, with a series of scientific articles and a book titled “The healing factor”, brings to the attention the problem of “hypoascorbemia”, the chronic Vitamin C deficiency and its related issues [4-8].

The American biochemist, through comparative physiology studies (comparing human production of vitamin C to that of other animals), finds that our vitamin C requirements are not in the order of milligrams, but grams per day.

As explained above, man is unable to produce vitamin C and since diet alone can not reach quantities in the order of grams, all of us are in a subacute deficiency condition of Vitamin C, which Irwin Stone defines “chronic subclinical scurvy”, considering it to be responsible for all diseases affecting the humankind, especially cardiovascular diseases and cancer [5,6,8].

LINUS PAULING AND HIGH DOSES OF VITAMIN C

With Linus Pauling, the Nobel Prize for Chemistry and Peace (the only man in the world twice awarded the Nobel Prize) begins another era for ascorbic acid.

Pauling is the most fervent and vigorous supporter of using high doses of vitamin C to cure virtually all illnesses, including cancer [9,10].

And it is the use of mega doses of vitamin C in cancer care that becomes the main topic of scientific research in the 1970s.
From 1976 to 1978, along with Ewan Cameron, Pauling publishes two articles that show that 10 grams per day of vitamin C, initially administered intravenously and then orally, prolong survival and improve the quality of life of patients with terminal cancer [11,12].

Always Linus Pauling in one of his books “Vitamin C and the Common Cold” demonstrates through scientific evidence and experiments that the high doses of vitamin C are particularly effective in the prevention and treatment of common cold [13].

But this is a serious blow to the drug industry and in the specific case, to that of chemotherapies, now becoming the standard therapy for cancer treatment. From this moment how it ever happened before, vitamin C will literally be defamed and its miraculous effects ignored.

Two subsequent articles published on The New England Journal of Medicine by Cregan and Mortel oncologists reported a total failure of vitamin C in cancer treatment and the results are entirely accepted by the international medical community as a definitive test for the inefficiency of vitamin C to treat cancer [14,15].

Obviously the studies are disguised and Pauling makes it clear to the authors. In the first study, patients who had previously undergone chemotherapy were enrolled, despite Pauling recommending this type of patient because their immune system, compromised by chemotherapy, is no longer able to respond to the stimulating action of Vitamin C [14].

In the second study, only patients with colon-rectal cancer were enrolled, while Cameron and Pauling had enrolled patients with different types of cancer. In addition, contrary to the standard clinical trial procedures, all enrolled patients are informed of the treatment to which they would be subjected [15].

The conclusion of both studies is that sodium ascorbate (vitamin C to neutral ph) is not superior to placebo and therefore ineffective in treating cancer.

The system reacts and Big Pharma defends itself. Only two trials are enough in order to destroy years of honest scientific research and definitively silence vitamin C and its miraculous health effects.

VITAMIN C AND CANCER: BIG PHARMA’S HEGEMONY IS IN DANGER

But almost 30 years after the publication of the studies by Creagan and Moertel, vitamin C and its anti-tumor effects come back to the scene again, with in vitro experiment that unequivocally demonstrate the devastating power of high doses of ascorbic acid in killing cancer cells [16 ].

From now on, clinical trials designed to demonstrate the effectiveness of vitamin C are going to spread. In vivo studies are also conducted, but there are still problems, mainly related to the mode of administration and some aspects that need to be better investigated.

Big Pharma is in serious danger and is increasingly claiming that high-dose Vitamin C can be used, but only in combination with standard chemotherapy [17].

But why does ascorbic acid, alias vitamin C, despite the many scientific evidence in its favor, is has been always obstructed in preventing treatment, cancer and many other diseases treatment?

Vitamin C as a natural molecule, which is very effective in selectively killing cancer cells, is affordable at low cost and is not patentable, unlike the active ingredients of endless drugs and chemotherapists, the latter highly toxic, unbelievable expensive and above all of dubious effectiveness.

Pharmaceutical companies do not and will never have any interest in promoting such a cure that does not profit, and much less, to fund scientific research to deepen the effects of ascorbic acid.

The ascorbic acid controversy remains open until 2015 when Science publishes an article that shows that in rectal cancer cancers (those used by Creagan and Moertle oncologists to evaluate the efficacy of Vitamin C) with mutations of KRAS and BRAF genes, the mega doses of ascorbic acid doses selectively destroys cancer cells [18].

Linus Pauling was right but despite the fact that the miraculous therapeutic effects of vitamin C have already been widely demonstrated as anticancer therapy [19-31], there are no studies on the human being. The system imposes chemotherapy as a standard procedure and vitamin C infusions can only be complementary therapy.

We just have to wait for state funds to support vitamin C research and the approval of ethics committees to be able to treat cancer patients in order to see a turning point in tumor care.

But I think it would be easier, by absurdity, to make ascorbic acid patentable in order to capture the interest of pharmaceutical companies.

If you have read the first part of the article, you will have understood well the extraordinary effects of vitamin C. Every physician should recommend it, especially in winter when influenza viruses return and become overbearing and we tend to consume less fruit and vegetables. So far, nothing would be wrong if it were not for the RDA, or the recommended daily “ridiculous” amounts. If you also think that with an orange a day you have covered your need for ascorbic acid, you are completely wrong.

The food guidelines, nutritionists and all the so-called experts in the field continue to recommend 60 to 110 milligrams a day despite the scientific literature has amply shown that the dosages in the order of grams are necessary in order to maintain good health, prevent and even treat some diseases.

Let’s make it clear. The RDA of vitamins and minerals are the minimum daily doses for the survival of our body and not for being in good health. In the case of vitamin C, those 60-110 milligrams a day is the amount necessary to avoid dying of scurvy.

In the ’70s, despite Irwin Stone and Linus Pauling bringing to light the problem of hypoascorbemia, or in easier words the chronic deficiency of Vitamin C with the related problems and having shown that our requirement of vitamin C is in the order of grams, the medical community continues to recommend a couple of oranges a day.

While drugs and medications have free way, the importance of vitamin C is ignored and high doses are not recommended because they could promote kidney stones and even cause cancer, although there are no studies that support these hypotheses and the existing literature states the opposite.

THE ROLE OF ASCORBIC ACID IN HUMAN PHYSIOLOGY

Like all micronutrients, vitamin C is involved in countless and very important physiological functions. The main ones are:

  • the biosynthesis of collagen, a very important protein;
  • the synthesis of noradrenaline (neurotransmitter);
  • the synthesis of carnitine, essential for the transfer of fatty acids into the mitochondria for energy production;
  • biosynthesis of bile acids;
  • activation of folic acid in tetrahydrofolic acid (FH4), biologically active form;
  • the biosynthesis of steroid hormones in the adrenal cortex; in fact, when the hormonal need increases in the cortex there is a depletion of both cholesterol and vitamin C;
  • intestinal iron absorption, its transfer from plasma transferring to tissue fereritin and the increased intracellular availability favoring iron-ferritin bond and increasing the stability of the complex itself;
  • reduce the toxicity of some minerals (Ni, Pb, V, Cd, Se), which in their reduced form are absorbed more easily or excreted faster;
    the reduction of free radicals and other powerful oxidants, protecting the structure of DNA, proteins and membranes from damage that these oxidants could cause;
  • the constitution, together with vitamin E, of a system of protection against oxidative damage caused by free radicals;
  • the strengthening of immune function.
  • In fact it has been observed experimentally that vitamin C is able to:
    • stimulate the production of interferons, which protect cells from viral attacks,
    • stimulate the proliferation of neutrophils;
    • protect proteins from inactivation by free radicals produced during oxidative processes occurring in neutrophils,
    • stimulate the synthesis of IgG and IgM class antibodies.

From these and many other unlisted functions, we can understand how vitamin C plays a vitally important role in the human organism. Not taking enough vitamin C and then following the food guidelines of 60-110 milligrams a day is compromising your health.

Let’s take a look at the role that ascorbic acid plays on the synthesis of collagen, a protein equivalent to 33% of our body weight and that in vertebrates constitutes more than 50% of all the body’s proteins. Arteries and veins, joints, bones and skin, muscles are all structures composed of collagen whose deficiency results respectively in hypertension, stroke, infarct, atherosclerosis, arthritis and arthrosis, osteoporosis and wrinkles, sarcopenia.

Collagen is everywhere and its lack leads to a worsening of the physical and mental condition. The so-called “ailments” of age are nothing but the degradation of tissues (usually caused by free radicals and hormonal decreases) resulting from an ever-decreasing amount of collagen available.

Another key point of the role of vitamin C is the strengthening of the immune system. A weak immune system means to open the door to all the pathologies brought by viruses and bacteria as well as to dangerous fungi and infections.

Vitamin C therefore plays a vital role in the prevention of almost all diseases.

It should be noted that all the other animals are not affected by all these diseases that affect us humans. And the case is that all the other animals produce an average of 10 grams of ascorbic acid per day (for 70 kg of weight) and that the production of the latter increases in case of infections, wounds and exposure to stress.

Furthermore, Vitamin C is naturally also the most powerful of all antioxidants.

Anti-oxidants are those molecules that block Free Radicals, which are in turn molecules that “oxidize” cells. Cells get sick, get old and die just because of oxidation. Taking a proper amount of Antioxidants with food is always vitally important.

RECOMMENDATIONS

The way of taking vitamin C is quite special and we need to know that every 3-4 hours the human body expels it through the urine regardless of the amount we have taken (in fact an excellent practice for those with bladder diseases such as inflammation, cystitis and others even more serious, it is to hold back urine for a while, to allow the ascorbic acid to act on it).

This means that in order to keep its antioxidant level high and optimize its benefits, it should be taken every 3-4 hours (particularly important with ongoing illnesses).

In our experience we have found remarkable benefits taking 500 or 1000 mg together with each meal for a total ranging from 1 to 3 grams a day. ATTENTION: we always refer to HEALTHY SUBJECTS, a PREVENTIVE PURPOSE and to MAINTAIN AN OPTIMAL FUNCTIONING OF THE ORGANISM.

Obviously if we are in the presence of disease with 2 grams a day we do very little. Here we talk about prevention and if you read the first part of the article forget that you can treat cancer simply by taking orally vitamin C.

For this purpose, very high blood concentrations of ascorbic acid are required, impossible to reach except by medical practices such as direct infusions of potassium ascorbate.

In fact, of those 2-4 grams that you will take orally in the bloodstream will inevitably reach a much lower amount but still sufficient to maintain an excellent state of health and prevent the ailments of time.

Think of those ridiculous 80 milligrams of vitamin C that have always been recommended. Do you know how many actually get into the blood and then into your cells where ascorbic acid would perform its valuable functions? A truly ridiculously small amount, useless.

In the case of a cold, as Linus Pauling suggests, take 1 gram every hour for 24 hours or adjust the dosages up to intestinal tolerance, for instance when you will have flutolence and diarrhea (the only side effect of high doses of ascorbic acid that simply disappears by reducing the doses). We always refer to HEALTHY SUBJECTS!

We recommend vitamin C supplements with added citrus bioflavonoids or rose hip, while for high doses we recommend 100% active ingredient powder to avoid ingesting high doses of caking agents, stabilizers and anything else used for the construction of the tablets.

There is much more to say but we must stop here as not to bore you and not to go too specific in order to make reading more or less understandable for everyone.
Do not hesitate to contact us for more information.

EVOplus - Lifestyle Revolution

REFERENCES

1. Nishikimi M, Fukuyama R, Minoshima S, Shimizu N, Yagi K. Cloning and chromosomal mapping of the human nonfunctional gene for L-gulono-gamma-lactone oxidase, the enzyme for L-ascorbic acid biosynthesis missing in man. J Biol Chem. 1994; 269:13685–13688. [PubMed: 8175804]
2. Claus W. Jungeblut, m.d. Inactivation of poliomyelitis virus in vitro by crystalline vitamin c (ascorbic acid) From the department of bacteriology, college of physicians and surgeons, Columbia University, New York (received for publication, July 3, 1935)
3. Klenner FR. The treatment of poliomyelitis and other virus diseases with vitamin C. South Med Surg. 1949 Jul; 111(7):209-14. No abstract available. PMID: 18147027.
4. Stone Irwin. Hypoascorbemia, the genetic disease causing the human requirement for exogenous ascorbic acid. Perspect Biol Med. 1966 Autumn;10(1):133-4.
5. Stone Irwin. On the genetic etiology of scurvy. Acta Genet Med Gemellol (Roma). 1966 Oct;15(4):345-50.
6. Stone Irwin. The genetic disease, Hypoascorbemia. A fresh approach to an ancient disease and some of its medical implications. Acta Genet Med Gemellol (Roma). 1967 Jan;16(1):52-62.
7. Stone Irwin. Sudden death. A look back from ascorbate’s 50th anniversary. Australas Nurses J. 1979 Jul;8(9):9-13, 39.
8. Stone Irwin. Homo sapiens ascorbicus, a biochemically corrected robust human mutant. Med Hypotheses. 1979 Jun;5(6):711-21.
9. Cameron E, Campbell A. The orthomolecular treatment of cancer. II. Clinical trial of high-dose ascorbic acid supplements in advanced human cancer. Chem Biol Interact 1974;9:285-315.
10. Cameron E, Campbell A, Jack T. The orthomolecular treatment of cancer. III. Reticulum cell sarcoma: double complete regression induced by high-dose ascorbic acid therapy. Chem Biol Interact 1975;11:387-93.
11. Cameron E, Pauling L. Supplemental ascorbate in the supportive treatment of cancer: prolongation of survival times in terminal human cancer. Proc Natl Acad Sci U S A 1976;73:3685-9.
12. Cameron E, Pauling L. Supplemental ascorbate in the supportive treatment of cancer: reevaluation of prolongation of survival times in terminal human cancer. Proc Natl Acad Sci U S A 1978;75:4538-42.
13. L. Pauling - Vitamin C and Common Cold – 1970.
14. Creagan ET, Moertel CG, O’Fallon JR, et al. Failure of high-dose vitamin C (ascorbic acid) therapy to benefit patients with advanced cancer. A controlled trial. N Engl J Med 1979;301:687-90.
15. Moertel CG, Fleming TR, Creagan ET, et al. High-dose vitamin C versus placebo in the treatment of patients with advanced cancer who have had no prior chemotherapy. A randomized double-blind comparison. N Engl J Med 1985;312:137-41.
16. Qi Chen†, Michael Graham Espey‡, Murali C. Krishna‡, James B. Mitchell‡, Christopher P. Corpe, Garry R. Buettner, Emily Shacter†, and Mark Levine. Pharmacologic ascorbic acid concentrations selectively kill cancer cells: Action as a pro-drug to deliver hydrogen peroxide to tissues. © 2005 by The National Academy of Sciences of the USA.
17. Bryan G. Allen et al. O2 and H2O2-Mediated Disruption of Fe Metabolism Causes the Differential Susceptibility of NSCLC and GBM Cancer Cells to Pharmacological Ascorbate. Cancer Cell Volume 31, Issue 4, p487–500.e8, 10 April 2017.
18. Jihye Yun, Edouard Mullarky et al. Vitamin C selectively kills KRAS and BRAF mutant colorectal cancer cells by targeting GAPDH. Science. 2015 December 11; 350(6266): 1391–1396. doi:10.1126/science.aaa5004.
19. Chen Q, Espey MG, Sun AY, Lee J, Krishna MC, Shacter E et al. Ascorbate in pharmacologic concentrations selectively generates ascorbate radical and hydrogen peroxide in extracellular fluid in vivo. Proc Natl Acad Sci USA 2007;104:8749–54.
20. Yeom CH, Lee G, Park JH, Yu J, Park S, Yi SY et al. High dose concentration administration of ascorbic acid inhibits tumor growth in BALB/C mice implanted with sarcoma 180 cancer cells via the restriction of angiogenesis. J Transl Med 20097:70.
21. Verrax J, Calderon PB. Pharmacologic concentrations of ascorbate are achieved by parenteral administration and exhibit antitumoral effects. Free Rad Biol Med 2009;47:32–40.
22. Levine M, Espey MG, Chen Q. Losing and finding a way at C: new promise for pharmacologic ascorbate in cancer treatment. Free Rad Biol Med 2009;47:27–9.
23. Ohno S, Ohno Y, Suzuki N, Soma G, Inoue M. High-dose vitamin C (ascorbic acid) therapy in the treatment of patients with advanced cancer. Anticancer Res 2009;29:809–15.
24. Takemura Y, Satoh M, Satoh K, Hamada H, Sekido Y, Kubota S. High dose of ascorbic acid induces cell death in mesothelioma cells. Biochem Biophys Res Commun 2010;394:249–53.
25. Pollard HB, Levine MA, Eidelman O, Pollard M. Pharmacological ascorbic acid suppresses syngeneic tumor growth and metastases in hormone-refractory prostate cancer. In Vivo 2010;24:249–55.
26. Du J, Martin SM, Levine M, Wagner BA, Buettner GR, Wang SH et al. Mechanisms of ascorbate-induced cytotoxicity in pancreatic cancer. Clin Cancer Res 2010;16:509–20.
27. Fromberg A, Gutsch D, Schulze D, Vollbracht C, Weiss G, Czubayko F et al. Ascorbate exerts anti-proliferative effects through cell cycle inhibition and sensitizes tumor cells towards cytostatic drugs. Cancer Chemother Pharmacol 2011;67:1157–66.
28. Klingelhoeffer C, Kammerer U, Koospal M, Muhling B, Schneider M, Kapp M et al. Natural resistance to ascorbic acid induced oxidative stress is mainly mediated by catalase activity in human cancer cells and catalase-silencing sensitizes to oxidative stress. BMC Complement Altern Med 201212:61.
29. Putchala MC, Ramani P, Sherlin HJ, Premkumar P, Natesan A. Ascorbic acid and its pro-oxidant activity as a therapy for tumours of oral cavity: a systematic review. Arch Oral Biol 2013;58:563–74.
30. Rawal M, Schroeder SR, Wagner BA, Cushing CM, Welsh JL, Button AM et al. Manganoporphyrins increase ascorbate-induced cytotoxicity by enhancing H2O2 generation. Cancer Res 2013;73:5232–41.
31. Kawada H, Kaneko M, Sawanobori M, Uno T, Matsuzawa H, Nakamura Y et al. High concentrations of L-ascorbic acid specifically inhibit the growth of human leukemic cells via downregulation of HIF-1 transcription. PLoS ONE 20138:e62717.