What are enzymes?
Enzymes are proteins that speed up chemical reactions. There are estimated to be between 50,000 and 70,000 different enzymes in your body that regulate every metabolic function in your body. Without enzymes, all of these metabolic functions would progress through the same steps, but would go too slowly to sustain life. In essence, enzymes make life happen where otherwise there would be none.
Most people, when they think of enzymes, think of digestive enzymes, and in the world of alternative health, that usually means digestive enzyme supplements. But as we’ve already mentioned, there are tens of thousands of different enzymes in the human body, and 99.999% have nothing to do with digestion.
An important concept to understand is that digestive enzyme formulas and systemic/metabolic, proteolytic enzyme formulas, although they may share many of the same enzymes (protease, papain, bromelain, etc.), are not the same thing.
- When you take a digestive enzyme formula with your meal, the enzymes work on speeding up the breakdown of the food in your stomach.
- When you take a proteolytic enzyme formula between meals, the enzymes do not get stuck working in your stomach or wrapped up with your food and passed out through the colon. Instead, they quickly enter your bloodstream. Once in the bloodstream, they help optimize your blood, plus they make their way to all of the tissues throughout your body, where they assist with intelligent, adaptive healing.
Primary benefits of taking systemic proteolytic enzymes center around their ability to:
- Control inflammation throughout the body, not just in your joints.
- Repair and rebuild the cardiovascular system.
- Optimize blood flow.
- Prevent and dissolve blood clots.
- Dissolve plaque in your arteries and dental plaque in your mouth.
- Clean up your immune system.
- Minimize the impact of allergies.
- Improve the ability to exercise and speed up recovery times.
And all of these benefits stem from one simple ability: proteolytic enzymes facilitate the breakdown of rogue proteins in your bloodstream and in the soft tissues of your body.
Understanding Proteolytic Enzymes
The vast majority of metabolic enzymes in your body, the enzymes that regulate everything from liver function to the immune system, are proteases, or proteolytic enzymes. Proteolytic is a catchall phrase for hydrolytic enzymes that specifically facilitate the chemical breakdown of proteins by severing the bonds between the amino acids that make up those proteins.
Proteolytic enzymes occur naturally in all organisms and constitute 1-5% of all genetic content. They are different from other enzymes in the body in that they are able to adapt to changing needs. For example, the same proteolytic enzyme can meet both digestive and metabolic needs in the body. This is the reason that you will see some of the same proteolytic enzymes in both digestive enzyme formulas and systemic metabolic formulas.
The bottom line is that a healthy supply of these protein specific enzymes is essential for sustaining and maintaining optimal health.
Types of Proteolytic Enzymes
There are six classifications or groups of proteases in the human body:
- Serine protease
- Threonine protease
- Cysteine protease
- Aspartate protease
- Glutamic acid protease
Most of the proteases that we’re going to talk about in this report are serine proteases. Serine proteases are enzymes that break peptide bonds in those proteins in which the amino acid serine plays a key role at the enzyme’s active site.1 In humans, serine proteases are responsible for coordinating various physiological functions including digestion, immune response, blood coagulation, inflammation, and reproduction. Equally important, serine proteases are widely distributed in nature and found in all kingdoms of cellular life as well as many viral genomes. The ability to break down serine protein bonds in invading viruses carries some obvious advantages when it comes to defending your body.
The two exceptions that commonly figure in supplemental enzyme formulas are bromelain and papain, which are cysteine proteases. In humans, cysteine proteases are responsible for cell aging and cell death, and certain immune responses.2 Thus, enzymes that regulate and enhance those reactions provide a perfect complement in any systemic, proteolytic enzyme formula. In addition, cysteine proteases play a role in bringing macrophages back into line when they are misprogrammed and attacking collagen and elastin at sites of inflammation such as arterial walls in atherosclerosis and lung tissue in emphysema.
Which leads us to the next piece of the puzzle.
Proteolytic Enzymes and Illness
Just about everything that makes us sick is either a protein or is protected by a protein and is therefore subject to control by proteolytic enzymes. For example:
- Your DNA stores the code for all of your body’s proteins and enzymes. In essence, your DNA is a protein manufacturing plant. Genetic diseases are the result of your DNA no longer producing those proteins and enzymes accurately or doing it insufficiently or excessively.
- Bacteria, viruses, yeasts, and fungi are all protected by proteins. Attacking those proteins is key to destroying the invaders.
- Food allergens are almost all proteins.
- Cancer cells are protected by proteins.
Proteolytic enzymes have the ability to digest and destroy the protein based defense shield of each and every pathogen, allergen, and rogue cell, thereby leading to their ultimate elimination. In addition, established cancers reprogram the production of enzymes in the body to both accelerate their own growth and protect themselves from the immune system. Supplemental proteolytic enzymes have the ability to alter that dynamic.
And then there are CIC’s (Circulating Immune Complexes). CIC’s start out as extra-large protein molecules (primarily from wheat, corn, dairy, and soy) that are only partially digested in the small intestine and are absorbed into the bloodstream. Once in the bloodstream, the immune system treats them as invaders because they are too large to be metabolized, provoking an immune reaction. Antibodies couple with these foreign protein invaders to form CIC’s. At first, these CIC’s may be neutralized by the immune system, then eliminated through the lymphatic system and the kidneys. But over time, as too many CIC’s are created, they overwhelm the body’s ability to eliminate them. At that point, the body has no choice but to “store” them in its own soft tissues, where the immune system continues to attack them as allergens, which leads to inflammation3 and, ultimately, autoimmune disorders such as lupus.4 In fact, studies have shown that diseases that present high CIC-levels can be improved or even cured by eliminating excess CICs.5
It is here that proteolytic enzyme supplements come into play. They compensate for your dietary inadequacies and errors by making their way into your bloodstream, where they set to work breaking down CIC’s in your blood and soft tissues — eventually passing the waste out through your kidneys and lymphatic system.
And finally, some proteolytic enzymes such as nattokinase and seaprose-S are very specialized. They work on specific protein related tasks such as optimizing blood, reducing pain and inflammation, and cleaning out the lungs. (We’ll talk more about those later.)
Why You Need to Supplement?
In a perfect world, we would all eat raw (organic) unprocessed foods that are naturally high in active enzymes.
But this isn’t a perfect world.
Most people eat food that is enzyme deficient (cooking and processing destroy enzymes) and fail to chew food adequately (saliva contains amylase) so their bodies must compensate. The body is forced to divert its production of metabolic proteolytic enzymes into the production of large amounts of pancreatic enzymes in order to break down all of the dead food in our diets. Short term, this is not a problem. Your body can easily handle it. But the long-term consequences of this diversion are enormous. It can lead to everything from a weakened immune system to thickened blood, from pain and inflammation to cardiovascular disease, and from reduced athletic performance to difficulty breathing. Supplementing with proteolytic enzymes offsets this devastating diversion and restores balance.
Proteolytic enzymes are indicated in inflammatory conditions and to support the immune system. Proteolytic enzymes (or proteases) refer to the various enzymes that digest (break down into smaller units) protein. These enzymes include the pancreatic proteases chymotrypsin and trypsin, bromelain (pineapple enzyme), papain (papaya enzyme), fungal proteases, and Serratia peptidase (the “silk worm” enzyme). Preparations of proteolytic enzymes have been shown to be useful in the following situations:
- Digestion support
- Fibrocystic breast disease
- Food allergies
- Hardening of the arteries (atherosclerosis)
- Hepatitis C
- Herpes zoster (shingles)
- Inflammation, sports injuries and trauma
- Pancreatic insufficiency
- Multiple sclerosis
- Rheumatoid arthritis and other
- Sinusitis, asthma, bronchitis, and autoimmune disorders chronic obstructive pulmonary disease
How do the proteolytic enzymes help autoimmune conditions like rheumatoid arthritis?
The benefits in some inflammatory conditions appears to be related to helping the body breakdown immune complexes formed between antibodies produced by the immune system and the compounds they bind to (antigens). Conditions associated with high levels of immune complexes in the blood are often referred to as “autoimmune diseases” and include such diseases as rheumatoid arthritis, lupus, scleroderma, and multiple sclerosis. Higher levels of circulating immune complexes are also seen in ulcerative colitis, Crohn’s disease, and AIDS. 4-6
How are Proteolytic enzymes used in cancer therapy?
Proteolytic enzymes have a long history of use in cancer treatment. In 1906, John Beard, a Scottish embryologist, reported on the successful treatment of cancer using a pancreatic extract in his book The Enzyme Treatment of Cancer and its Scientific Basis. Proteolytic enzymes have been promoted by numerous alternative cancer practitioners for many years, but most recently by Nicholas Gonzalez, M.D., who is evaluating the benefit of proteolytic enzymes in patients with advanced pancreatic cancer in a large-scale study, funded by the National Institute of Health’s National Center for Complementary and Alternative Medicine, with collaboration from the National Cancer Institute. This larger trial is a follow-up to a smaller study that showed dramatic improvements in these patients.
How do Proteolytic enzymes work to fight cancer?
Once absorbed the body prevents digestion of proteins in the blood and other body tissues producing antiproteases. The production of these antiproteases is critical to the mechanism of action of proteolytic enzymes. These antiproteinases block the invasiveness of tumor cells as well as prevent the formation of new blood vessels (angiogenesis). Proteolytic enzymes exert a number of other interesting anticancer mechanisms including the inhibition of metastasis (the spread of cancer) and the enhancement of the immune response. 1
What clinical research has been done with proteolytic enzymes in cancer?
The clinical research that currently exists on proteolytic enzymes suggests significant benefits in the treatment of many forms of cancer.2 Specifically these studies have shown improvements in the general condition of patients, quality of life, and modest to significant improvements in life expectancy. Studies have consisted of patients with cancers of the breast, lung, stomach, head and neck, ovaries, cervix, and colon; lymphomas and multiple myeloma. These studies involved the use of proteolytic enzymes in conjunction with conventional therapy (surgery, chemotherapy and/or radiation) indicating that proteolytic enzymes can be used safely and effectively with these treatments. Proteolytic enzymes are not recommended for at least two days before or after a surgery as they may increase the risk of bleeding. Proteolytic enzymes have been shown to be quite helpful in speeding up post-surgical recovery and relieving a complication of surgery and radiation known as lymphedema. (SEE TABLE 1-2)
What other conditions might proteolytic enzymes be helpful for?
The list of conditions benefited by pancreatic enzyme supplementation seems to be growing all the time. For example, one potential use is in the treatment of viral related illness including hepatitis C and herpes simplex infections. For example, in one study in the treatment of herpes zoster (shingles) an orally administered proteolytic enzyme preparation was more effective than the standard drug therapy (acyclovir).8 In a study in patients with hepatitis C, proteolytic enzymes were shown to be slightly superior to alphainterferon in improving laboratory values and symptoms.9 Proteolytic enzymes also appear to be quite helpful in recovery from surgery, fibrocystic breast disease, acute and chronic sinusitis and bronchitis, and chronic obstructive pulmonary disease and asthma.10-13
Can taking proteolytic enzymes actually improve digestion?
Yes, in fact, using enzyme preparations to support proper digestive function is used in conventional
medicine in cases of pancreatic insufficiency and cystic fibrosis (a rare inherited disorder). Pancreatic insufficiency is characterized by impaired digestion, malabsorption, nutrient deficiencies, and abdominal discomfort.
Are proteolytic enzymes actually absorbed?
Yes. One of the outdated arguments against the effectiveness of orally administered proteolytic enzymes was that they either got digested or they were too large to be absorbed. Absorption studies with the various proteolytic enzymes have confirmed that they are absorbed intact. In fact, they appear to be actively transported across the gut wall.3 Since stomach acid can destroy proteolytic enzymes, the best formulas are “enteric coated” – meaning that the pills have a coating around them to prevent the pill from being broken down in the stomach. An enteric-coated pill passes into the small intestine, where due to the pH change it will break down there.
Do the proteolytic enzymes digest blood proteins?
NO! There are special factors in the blood that block the enzymes so that they do not digest blood proteins.
What proteolytic enzyme product do you recommend?
In order to get the most out of proteolytic enzymes it is essential to use a high quality product at an adequate dosage. To judge the quality of an enzyme preparation it is important to know what you are looking for. Most of the proteolytic enzymes have well established guidelines developed by the United States Pharmacopoeia (USP) or the Food Chemical Codex (FCC). The product that I recommend contains the following ingredients per enteric-coated tablet. It is more than twice as potent as other popular preparations:
Pancreatin(8X) 200 mg.
Papain (30,000 USP/mg) 120 mg.
Peptizyme SP (200,000 SPU/g) 52 mg.
Bromelain (1,200 MCU/g) 50 mg.
Pancreatin refers to pancreatic enzyme preparations prepared from fresh hog pancreas. The two primary proteases of pancreatin are chymotrypsin and trypsin (also available from ox bile). Papain and bromelain are proteolytic derived from papaya and pineapple, respectively. Peptizyme SP (a special serrapeptase) is derived from a bacteria that resides in the intestines of silk worms. It is also called “silk worm” enzyme as it is the enzyme used to breakdown the cocoon of the silk worm.
The Miracle Enzyme
Dr. Hans Nieper, a legendary medical doctor known for his extensive use of proteolytic enzymes, called serrapeptase the “Miracle Enzyme.” Dr. Nieper used the enzyme primarily to open up clogged arteries supplying the brain. This enzyme is more powerful than the pancreatic enzymes chymotrypsin and trypsin. It has been used in Europe and Japan for over 25 years. As evident in Table 1, good clinical results have been demonstrated in clinical trials. In addition to its general anti-inflammatory effects, it is particularly beneficial in fibrocystic breast disease as well as upper respiratory tract conditions like sinusitis, bronchitis, asthma, and chronic obstructive pulmonary disease due to its ability to improve the structure and function of the mucus lining.10-13
Are proteolytic enzymes preparations safe?
Proteolytic enzymes are generally well-tolerated and are not associated with any significant side effects. Even in people with presumably normal pancreatic function, taking proteolytic enzymes produced no untoward side effects nor did it reduce the capacity for these subjects to produce their own pancreatic enzymes.14 However, my recommendation is to utilize these preparations only when there is apparent need.
Although no significant side effects have been noted with any of the proteolytic enzymes, allergic reactions may occur (as with most therapeutic agents). Pancreatic enzymes should not be used by anyone allergic to pork; bromelain should not be used in anyone allergic to pineapple; and papain should not be used in anyone sensitive to papaya.
1. Rubinstein E, et al.: Antibacterial activity of the pancreatic fluid. Gastroenterol 1985;88:927-32.
2. Ambrus JL, et al.: Absorption of exogenous and endogenous proteolytic enzymes. Clin Pharmacol Therapy 1967;8:362-8.
3. Kabacoff BB, et al.: Absorption of chymotrypsin from the intestinal tract. Nature 1963;199:815-7.
4. Martin GJ, et al.: Further in vivo observations with radioactive trypsin. Am J Pharm 1964;129:386-92.
5. Avakian S: Further studies on the absorption of chymotrypsin. Clin Pharmacol Therap 1964;5:712-5.
6. Liebow C and Rothman SS: Enteropancreatic circulation of digestive enzymes. Science 1975;189:472-4.
7. Oelgoetz AW, et al.: The treatment of food allergy and indigestion of pancreatic origin with pancreatic enzymes.
Am J Dig Dis Nutr 1935;2:422-6.
8. Carroccio A, et al.: Pancreatic enzyme therapy in childhood celiac disease. A double-blind prospective randomized
study. Dig Dis Sci 1995;40:2555-2560.
9. Innerfield I: Enzymes in Clinical Medicine. McGraw Hill, New York, 1960.