MELATONIN: The Miracle Molecule

Written by PIERPAOLI, M.D., Walter

What is melatonin?

In our bodies, melatonin is the molecule naturally produced within the pineal gland, the glandular organ nestled between the cerebral hemispheres that the great French philosopher Descartes once proposed to be the “seat of the soul.”

We find melatonin everywhere in the biological world, from unicellular organisms to the vertebrates. Melatonin is the “Master Hormone-Modulating Molecule” but it is misleadingly called a “hormone.” This is because it is the body’s regulator of all hormones, the molecule which controls the production of almost every other human hormone. Melatonin also helps regulate our “sleep/wake”, or circadian cy-cles.

Melatonin production reaches its peak in puberty and then continues to decrease as we grow older, resulting in the physically degenerative condition commonly referred to as “aging”. As we “age”, our bodies become vulnerable to a host of illnesses and diseases, including insomnia, immune dysfunc-tions, heart disease and cancer. But research shows that taking small doses of synthetic melatonin supplements at the time of life when naturally produced melatonin levels decline can halt and even reverse the negative effects of aging.

Melatonin and sleep

Sleep is crucial to our health and well-being; we need it as much as we need oxygen. It allows our bodies to rest and refuel and gives the body’s cells a chance to repair and regenerate. The average adult needs between 8 and 9 hours of sleep per night to allow for the completion of this regeneration process. But most adults get less than 7!

Study upon study continues to show that people who don’t get adequate sleep are at increased risk for a myriad of health problems and illnesses including obesity, diabetes, immune-system dysfunction, as well as impaired job performance, concentration and productivity in many other activities. The sleep cycle stems form an interaction between how much sleep you get (hours) and the circadian cycle -the 24 hour sleep/wake cycle of light and darkness created by the rotation of the earth.

The pineal gland, a pea-sized structure at the center of the brain, works with the hypothalamus gland to control your sleep/wake cycles. At night, in darkness, the pineal gland produces melatonin, which causes your heart rate to slow down and your body temperature to drop- physiological conditions that allow for deep, restful sleep. As we age, the amount of melatonin produced by our body lessens, re-sulting in the sleep disturbances. Numerous scientific studies have shown that taking synthetic melatonin as a supplement can help correct the irregularities in the body’s circadian cycle that prevent a good night’s sleep.

Melatonin supplements have worked wonders in the treatment of insomnia, sleep disturbances, jet lag and seasonal affective disorder. But sleep isn’t melatonin’s only story. In extensive clinical trials, I (Walter Pierpaoli) have discovered that the benefits of taking synthetic melatonin supplements reach far beyond a good night’s sleep. So far, in fact, you might call it “The Miracle Molecule”.</p

Melatonin and the aging clock

In my groundbreaking scientific study, “The Aging Clock: The Pineal Gland and Other Pacemakers in the Progression of Ageing and Carcinogenesis”, I have proved that conventional wisdom regarding how we age is flawed. Aging is not the inevitable result of passing years; it is actually a degenerative physical condition that can be slowed down, stopped and even reversed by simply re-setting your “ag-ing-clock”. Through exhaustive research I and my colleagues have discovered that the pineal gland, in its role as the producer/keeper of melatonin, functions as the body’s “aging clock”. A young pineal gland, through its master molecule, melatonin, sends a message of “youth” throughout the body, keeping the body healthy and strong. As the pineal gland ages, however, the message it sends to the body is “slow down, you’re old” and subsequently, the body systems comply, following closely the “master,” growing older and older until we eventually die. This aging-preventing and aging-promoting role of the pineal gland has been most dramatically demonstrated by transplanting the pineal gland from young into old animals and from old animals into young animals. The story of the discovery has also been illustrated in the popular book “The Melatonin Miracle”, Simon & Schuster, New York, 1995. In addition, exten-sive clinical trials have shown that melatonin supplements in aging subjects restored pineal glands to their youthful, productive states, restored balance to the body and literally reversed the aging process.

It’s the 21st century and stress is part of our daily lives. We are subjected to it constantly, in many cases plagued by it. But what exactly is stress? The body’s stress response can be likened to an air-plane getting ready for take-off. Virtually all body systems, (e.g., the heart and blood vessels, the immune system, the lungs, the digestive system, the sensory organs, and brain) are modified to ready us to “fight or flee” – a physiological response mechanism left over from prehistoric times, when we literally had to fight or flee to survive. In the brain, the HPA (hypothalamic-pituitary-adrenal) system is activated, triggering the production and release of corticosteroids, including the primary stress hormone cortisol. Corticosteroids are in-volved in a wide range of physiological systems including: stress response, immune response and regulation of inflammation, carbohydrate metabolism, protein catabolism, blood electrolyte levels and behavior. Numerous scientific studies have proven that sleep deprivation leads to an abnormal elevation in corticosteroids. Prolonged exposure to elevated levels of corticosteroids can:

  • Raise blood sugar levels, increasing the risk of diabetes and obesity.
  • Damage the heart.
  • Weaken the bones, leaving the vulnerable to breaks and fractures.
  • Damage the brain and affect our ability to think clearly and retain information in memory.
  • Suppress and damage the immune system by decreasing the number of active white blood cells in our bodies.

Clinical trials show that melatonin supplementation normalizes corticosteroid levels in our bodies. But taking melatonin doesn’t just protect us against the negative effects of stress by keeping corticosteroid levels in check. Melatonin actually works with endorphins, special stress-reducing, pain relieving chemicals produced by the immune system. Melatonin enhances the effect of endorphins, thereby aiding the body to withstand stress and promote a greater sense of general well-being.

Melatonin and the immune system

The immune system is, quite possibly, the most intricate and dynamic system in the human body. It is designed to respond to protect you against the millions of external, unwanted bacteria, microbes, parasites and viruses that can attack and destroy your body. T-cells (thymus cells, white blood cells that attack virus-infected cells, foreign cells and cancer cells) play a pivotal role in immune response. T-cells also produce a number of substances that regulate the immune response. A multitude of healthy, active T-cells are necessary for our healthy survival. As we age, the thymus gland, the gland that stores and controls T-Cells, deteriorates, causing the T-cells to become less effective. Our immune system gradually breaks down, leaving us vulnerable to the onset of disease. Clinical trials show that melatonin supplementation increases the weight of the thymus, as well as the activity of the T-cells. Clinical trials also show that melatonin works to strengthen the body’s antibody response, helps fight against viruses and improves thyroid function – all of which boost and support the immune system.

Melatonin as cancer prevention and treatment

Improving T-cell function doesn’t just bolster your immune system. T-cells are the body’s primary cancer fighters. Cancer is a group of disease in which the body’s cells are abnormal and divide without control. Cancer cells may invade nearby tissues and/or spread through the bloodstream and lymphatic system to other parts of the body. There is strong evidence that in its role as the “master regulatory molecule”, i.e., the regulator of other hormones, melatonin may help prevent hormone-dependent cancers (including breast cancer and prostate cancer). Melatonin is also a strong tool in the prevention of cancer in its role of strengthening the immune system, (the body’s ability to identify and destroy ab-normal cells that may turn cancerous). Melatonin prevents the age-related decline in your immune system that leaves your body vulnerable to cancer. Clinical trials have shown that melatonin can diminish the effects of hormones that trigger cer-tain cancers, including breast cancer and prostate cancer. Melatonin also hinders spindle formation, which can potentially slow down cell division. If you already have cancer, supplementing melatonin before and after, but not during the course of your chemotherapy, could be a beneficial treatment support. Clinical trials have shown that melatonin supplements taken can protect bone marrow cells from the ravaging effects of chemotherapy. But in such cases you should always ask your doctor beforehand.

Melatonin’s other miracles

Our research and research of many other scientists also showed that melatonin can:

Help maintain a healthy heart by:

  • Stabilizing cholesterol and other essential blood lipids. Clinical trials indicate that melatonin can reduce the effect of cholesterol intake on blood levels of cholesterol.
  • Protect against high blood pressure. By slowing down the “aging clock”, melatonin can help stay the tendency for blood pressure levels to rise as we age. In addition, melatonin’s role as a “sleep aid” can help keep the body in the restful restorative sleep state that allows blood pres-sure levels to drop.
  • Counteracting the harmful effects of stress. Melatonin stabilizes the production of corticoster-oids, harmful stress hormones that have been proven to damage the heart.

Help maintain a healthy sex life by:

  • Restoring both male and female sex organs and drive to their youthful “peak performance” levels. Clinical trials show melatonin can prevent age-related deterioration of sexual organs, which has been linked to impotency, sexual dysfunction and lack of desire.
  • Restoring libido-enhancing sex hormones to their youthful “peak performance” levels as the body’s “master molecule.”
  • Promoting and supporting prostate health. Clinical trials show melatonin to be an inhibitor of the 5-alpha-reductase enzyme, which can stimulate the growth of prostate cells, (resulting in an enlarged prostate). Melatonin also has been shown to restore and maintain normal zinc levels, es-sential to maintaining a healthy prostate.
  • Preventing arteriosclerosis, in which the arteries or the heart become clogged with plaque. Through its role in normalizing cholesterol levels, melatonin may also protect against this age-related disease, which is one of the leading causes of male impotency.
  • Stabilizing and synchronizing couples’ sleep/wake cycles.

And although further research must be done before we can be sure, melatonin shows to hold great promise in the treatment and prevention of dozen of other conditions, diseases and illnesses including asthma, diabetes, menopause, Alzheimer’s Disease, Parkinson’s Disease, Multiple Sclerosis, Down Syndrome and AIDS.

WHY Dr. Pierpaoli’s melatonin?

The development of Melatonin Zn-Se â has been designed to be the purest, most effective form of synthetic melatonin available; each tablet has been scientifically tested for biological activity and chemical purity. Synthetic melatonin is produced by synthesis from pharmaceutical grade ingredients, starting from serotonin extracted from coffee beans, and is molecularly identical to the melatonin pro-duced in the human body and it is never ever “bovine”, “animal” or “natural” grade melatonin. These grades of melatonin contain the actual extracts of the pineal gland and derive from animal tissue, which means it could contain viruses or proteins that could cause an undesired antibody response.

Dr. Pierpaoli and his colleagues have investigated the possible mechanisms and also the molecules which presumably cooperate and synergize with melatonin in the regulation and re-synchronization of fundamental immunological and hormonal functions which are lost or deranged in the course of aging. During recent studies and long-term experiments with old rodents, it has been observed that zinc can correct completely aging-dependent immunodepression and several other hormonal and metabolic alterations typical of aging. It has been found that the low zinc levels in aging animals can be restored to normal values with nocturnal administration of melatonin or transplantation of the pineal gland from young into older animals. Zinc is an essential component of more than 200 enzymes and one of the most relevant trace elements in the body. It is thus clear that additional zinc must be supplemented daily to the body of an aging organism with a low zinc balance, in order that melatonin can better exert its anti-aging activities on the entire hormonal and immune systems! This important and novel scien-tific observation of the powerful anti-aging and immuno-enhancing activity of the combination of zinc and melatonin has now resulted into the development of Melatonin Zn-Seâ.

Also selenium is a fundamental trace element of the body and possesses powerful anti-cancer effects. Modern agriculture and alimentary habits have dramatically decreased the daily input of selenium from the diet. Selenium is essential for the enzymatic reaction responsible for the synthesis of glutathione, a powerful physiological molecule which constantly protects the body from oxidative damage. A lack of selenium will thus result into a loss of the detoxification capacity of the body, immunodepression and onset of degenerative diseases and cancer. This is the reason why Melatonin Zn-Se â combines, in a unique synergistic combination, three fundamental anti-aging molecules, where melatonin plays the master role for reactivation and restoration of its natural night peak to juvenile levels, this resulting into normalization of all measurable immunological and endocrine functions in the course of aging. The positive aging-postponing, metabolic and immunological effects of Melatonin Zn-Se â can be easily measured by anybody by means of a normal periodic check-up!

Although synthetic melatonin is one of the least toxic substances in existence and produces almost no side effects, it does produce somnolence (sleepiness) in most of the population at higher dose. Mela-tonin should not be taken with MAOI drugs, as MAOIs inhibit the breakdown of melatonin in the body. Melatonin should not be taken during pregnancy or while nursing. Melatonin should not be taken with alcohol, NSAIDS (anti-inflammatory medications) or beta-blockers.


• Dr. Pierpaoli’s groundbreaking research on the pineal gland and melatonin was presented at the Third Stromboli Conference on Aging and Cancer and published in 1994 by the Annals of the New York Academy of Sciences under the title: “The Aging Clock: The Pineal Gland and Other Pace-makers in the Progression of Aging and Carcinogenesis” and in the Proceedings of the National Academy of Sciences, 1994.

• In 1995, “The Melatonin Miracle”, co-authored by Dr. Pierpaoli and Dr. William Regelson (with Carol Coleman) and based on Dr. Pierpaoli’s research, was published by POCKET BOOK, a divi-sion of Simon and Schuster.

• All clinical trials in Dr, Pierpaoli’s study were conducted on laboratory mice and all claims made in the study were based on those trials. Scientists choose mice for medical research because the manner in which illnesses present in mouse bodies virtually duplicates the pathology of the same illnesses in human bodies. In addition, mice are subject to the same biological rhythms as hu-mans. At present, results of many clinical studies with melatonin are being published in the scien-tific literature supporting and fully confirming the findings reported with mice and other rodents.