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Enzyme supplements offer digestive and systemic health benefits

Without enzymes, not too much would happen in the body. Almost all processes in a biological cell require enzymes, so without them, cell activity stops. That would make life pretty boring. To name a few things these little catalysts do for us: “Enzymes are the spark of life; they facilitate many functions within the body, from muscle contractions to blinking of the eyes,” said Guy Devin, Ph.D.

Enzymes convert our food to energy, dissolve arterial plaque buildup, eliminate viruses, dissolve scar tissue and reduce blood clots and intimately purify our blood.”

Thankfully, enzymes give us some action in life. Enzymes are catalysts for biochemical reactions, meaning they speed up reactions using lower activation energy than would be necessary for the process to go on without the enzyme. Food can sit out at room temperature and biodegrade over a few days; but, enzymes in the digestive track speed up that process, so humans can get all of the nutrients during the course of a day or so. Enzymes also have a unique shape, which allows a lock-and-key method with the molecules involved in their reactions. This means enzymes are highly selective, only causing specific reactions.

Digestion is a major function of enzymes in all living creatures. Food processing starts in the mouth where salivary glands secrete carbohydrate digestive enzymes. In the gastrointestinal (GI) track, digestion continues with the secretion of hydrochloric (HCl) acid, the enzyme pepsin, and additional starch and protein hydrolases (another type of enzyme). Then, the small intestine secretes alkaline bicarbonate buffers and pancreatic enzymes to further the process. Specific enzymes target specific types of foods for digestion; for example, amylase digests carbohydrates, lipase tackle fats, protease target proteins and cellulase handlesfiber.

When these enzymes aren’t present or don’t work correctly, GI abnormalities can result, including constipation, diarrhea, malnutrition, irritable bowel syndrome (IBS), dyspepsia, Crohn’s disease, maldigestion, malaria, cystic fibrosis, multiple sclerosis and cancer, to name a few.

With most of today’s food grown in the depleted soil of corporate farms, we have lost the enzyme-rich foods our ancestors enjoyed. We are also living longer than our forefathers, and as we age, our bodies don’t produce as many enzymes. A study published in Gastroenterology found advancing age is associated with reduced enzyme output independent of atrophic gastritis, H. pylori infection and smoking.1

Add to that overeating, smoking, drinking alcohol, diseases (patients with cirrhosis have a lower maximal enzyme output than that of healthy subjects),2 and a genetic predisposition, and consumers may look to supplement their diets with enzymes to help reduce the aforementioned ailments and other enzyme-deficiency illnesses.

People are becoming more educated in how enzymes work, and the main driving force for that interest is the continuing increase in the number of individuals with digestive issues and the severity of those issues, despite the availability of multiple pharmaceutical products.

After practicing chiropractic and enzyme replacement nutrition for 24 years, Dr. Paul S. Inselman, chiropractic physician, internal digestive health specialist, said he has noticed a tremendous shift in consumers’ overall interest in natural enzyme supplements and credits three driving forces. “First, I am finding people are dissatisfied with the traditional medical model of just being given drugs,” he said. “Second, people are realizing enzymes are essential nutrients that have been systematically removed from our food supply in order to increase shelf life. This removal of enzymes causes our bodies to have to work harder and eventually break down. Lastly, I believe consumers want to use safe and natural products that promote normal function, which is what enzymes do; they digest food and nourish the immune system.”

Digesting the Facts

People are looking for ways to reduce their digestive woes, and are willing to put money toward a better gut feeling. Digestion issues continue to be one of the most compelling problems that people have. Due to lack of enzymes in food, many consumers can benefit from an enzyme supplement. Enzymes may affect all aspects of digestion from occasional heartburn, gas, acid indigestion to poor nutrient absorption.

Originally, pancreatic enzymes were the first choice for digestive issues. Today, blends of plant and microbial source enzymes are preferred. Plant enzymes include extracts of pineapple stem (bromelain) or papaya latex (papain). The microbial enzymes are derived by submerged or surface fermentation of fungal or bacterial organisms.

Bromelain has demonstrated the ability to enhance the absorption of drugs, particularly antibiotics, as well as to reduce swelling, inflammation and formation of blood clots after oral administration in vitro and in vivo.3 That same article noted a wide range of therapeutic benefits has been claimed for bromelain, such as inhibition of platelet aggregation, chest pain, bronchitis and sinusitis.

Another chief digestive enzyme is pepsin, which is secreted by the cells in the stomach lining and is one of the first protein digestive enzymes secreted in the GI tract beginning the hydrolytic process of protein catabolism. It converts protein foodstuffs into water-soluble material and degrades food proteins into peptides. Other pancreatic enzymes (amylase, lipase and protease) secreted by the acinar cells of the pancreas are the major digestive agents in the GI tract. These pancreatic enzymes digest starches, lipids and proteins to absorbable forms in the small and large intestine.

Enzymes such as amylase, protease, lipase, cellulase, lactase, acid protease, bromelain, amyloglucosidase, hemicellulase, alpha galactosidase, invertase, peptidase, and two probiotic strains (L-acidophius and B. Bifidum), ensure better breakdown and absorption of proteins, carbohydrates, fats, plant fibers, beans and dairy while supporting gut function, stability and immune system modulation.

Many enzyme products are vegetarian, reflecting an increased consumer demand for animal-free supplements.

Keeping enzymes plant-based may also help increase efficacy, as one study stated application of non-animal enzymes derived from Aspergillus and other microbial species may prove valuable in a broad range of conditions associated with digestive weaknesses, such as pancreatic enzyme insufficiency, maldigestion, malabsorption, steatorrhea, lactose intolerance, celiac disease and food sensitivities.4 The researchers hypothesized non-animal enzymes may be particularly well-suited for human use due to their ability to break down (hydrolyze) physiologically and/or pathologically important substrates over a wide pH range.

Systemic Changes

The health benefits of enzymes don’t stop with digestion. Supplemental enzymes fall into one of two categories, digestive or systemic formulations. Systemic enzymes include every health condition besides digestion, but tend to concentrate on inflammation, cardiovascular and immune health.

Systemic enzymes are an exciting area of investigation. Systemic enzymes are predominantly protease enzymes. One of the oldest and best known is bromelain, which is derived from the stem of pineapples. Newer protease enzymes include nattokinase, serratiopeptidase and blended combinations that employ one or both of these with other proteases. These two enzymes, in particular, exhibit profound fibrinolytic as well as anti-inflammatory activity. The potential for use in inflammatory and cardiovascular conditions is significant.” Smith added the demand for systemic enzymes is increasing as the Baby Boomers hit their 60s and face common age-related issues like joint disorders and cardiovascular disease (CVD).

Inflammation is a culprit in both joint discomfort and heart problems. “Somewhat new is the awareness that enzymes can play significant roles in supporting normal inflammatory responses,” noted Dallas Clouatre, Ph.D.. “For such purposes, it is best to take an enzyme product such on an empty stomach with a full glass of water.”

Much research has been underway, especially in Europe, regarding the utilization of enzymes as natural anti-inflammatories in sports medicine and cardiovascular support. Some studies show, for example, that bromelain when taken with food helps to break down proteins; however, taken between meals, it may act to reduce pain and inflammation allowing speedier healing.

Indeed, a study from Pakistan reported an oral enzyme combination containing rutosid (a bioflavonoid) and the enzymes bromelain and trypsin can be considered an effective and safe alternative to nonsteroidal anti-inflammatory drugs (NSAIDs), such as diclofenac, in the treatment of painful episodes of osteoarthritis (OA) of the knee.5 Similarly, short-term evaluation indicated the same enzyme-rutosid combination was found to be an effective and safe alternative to diclofenac in the treatment of painful gonarthritis (inflammation of the knee),6 as well as hip OA.7

Joint issues can be reduced by more than just the bromelain and trypsin enzymes. A study from the Case Western Reserve University, Cleveland, found protease therapy had anti-inflammatory efficacy in the early (inflammatory) phase of collagen-induced arthritis, similar to the NSAID ibuprofen.8

Serratiopeptidase, a protease enzyme, produced a significant reduction of cheek swelling and pain intensity in patients whose molars were surgically removed in a prospective, intra-individual, randomized, double blind, crossover study.9 The group that received 5 mg of serrapeptase experienced improvement during the second, third and seventh post-op days compared to placebo (P<0.05). Additionally, University of Naples, Italy, researchers found serrapeptase had anti-inflammatory, anti-oedemic and fibrinolytic activity in a multicenter, double blind, placebo-controlled study of 193 subjects suffering from acute or chronic ear, nose or throat disorders.10

Reducing pain can help fuel athletes, and studies show enzymes provide this benefit as well. A Texas study found protease supplementation seemed to reduce muscle strength losses after eccentric exercise by regulating leukocyte activity and inflammation.11

Enzymes with protease reduced muscle soreness after downhill running; and researchers noted supplementation may also facilitate muscle healing and allow for faster restoration of contractile function after intense exercise.12

Enzymes may also help sports players by increasing the amount of protein digested. A clinical study published in the Journal of the International Society of Sports Nutrition showed a combination of enzymes increased amino acid levels by 100 percent, branched‐chain amino acid levels by 250 percent and nitrogen retention – an indicator of protein absorption –by 32 percent.13 This can translate into real benefits such as building lean muscle, supporting muscle recovery after exercise, and promoting weight management.

Studies on enzymes have also shown heart-health benefits. A German study found incubation of bromelain decreased platelet count in blood samples of 10 healthy male non-smokers.14 Excess platelets in the blood can cause clotting. In a 2008 study, researchers said bromelain revealed a novel mechanism of cardioprotective action, and was a potential therapeutic target against ischemia-reperfusion (deficient blood flow) injury.15 Aortic flow increased and blood clotting was decreased in bromelain-treated rats compared with those untreated. A separate German study found bromelain, orally applied at 60 mg/kg body weight, inhibited blood clot formation in a time-dependent manner.16

Nattokinase, a potent serine proteinase enzyme found in the traditional fermented food called natto, can also help the heart. Oral administration of nattokinase decreased certain factors of blood clotting and lipids that are associated with an increase risk for CVD (fibrinogen, factor VII and factor VIII) in a Taiwan study,17 and reduced systolic blood pressure and diastolic blood pressure in a Korean study.18

Some enzymes act as antioxidants in the body, reducing free radical damage. In comparison to vitamin C, people taking enzymes showed significant increases in the ability to clear caffeine as well as elevating cysteine levels, indicating the liver’s antioxidative capacities were increased; improved baseline measurements of detoxification systems; significant improvement over baseline measurements in three of the liver’s detoxification pathways (sulfation, glycination and glucuronidation); and impressive results in free radical markers.

The benefits of enzymes don’t stop there, as studies have recommended hydrolytic enzymes should be included in the therapy of HIV-positive patients to improve the immune system,19 found pancreatic enzyme extracts significantly prolonged the survival of mice with human pancreatic cancer xenografts and slowed the tumor growth,20 and shown complementary treatment of oral enzymes in colorectal cancer patients improved quality of life by reducing both the signs and symptoms of the disease and the adverse reactions associated with adjuvant therapies.21

Enzyme Entry

With all these health benefits, it becomes obvious that enzymes are needed by people. So far, the delivery system has mostly been through tablets and capsules and not much else. The reason? There are several formulation hurdles.

Enzymes present several challenges in regard to their use in product delivery forms other than capsules and tablets. They are activated by water, so their use in beverages or foods with any degree of water content has been problematic. New and innovative coating technologies may soon open many doors for the use of enzymes in a wide variety of applications.

Microencapsulation of enzymes allows for a convenient sprinkle delivery system. This delivery is excellent for individuals who have trouble swallowing capsules. Microencapsulation allows enzymes to maintain stability after being added to wet foods, and does not interfere with taste.

People are also becoming more educated in enzyme technology, which includes demands for enzymes to be non-GM (genetically modified), gluten-free and, whenever possible ... kosher.

Enzymes must also be deactivated before they get to to the consumer. Enzymes are proteins and a protein is a long chain of amino acids bound to each other by peptide bonds. However, this chain of amino acids is not in a straight line, it has twists and turns that give shape to the molecule. It is this shape that creates active sites on the protein molecule that allows it to do work. A slight change to the shape of the molecule renders it inactive or ‘denatured.’ Heat, sunlight, extremes of pH can denature the enzyme.

1. Feldman M, et al. “Effects of aging and gastritis on gastric acid and pepsin secretion in humans: a prospective study.” Gastroenterology. 1996 Apr;110(4):1043-52.
2. Lo WC, et al. “Gastric secretion in Chinese patients with cirrhosis.” J Clin Gastroenterol. 1996 Dec;23(4):256-60.
3. Maurer HR, et al. “Bromelain: biochemistry, pharmacology and medical use.” Cell Mol Life Sci. 2001 Aug;58(9):1234-45.
4. Rachman B. “Unique Features and Application of Non-Animal Derived Enzymes.” Clinical Nutrition Insights. Vol 5 No 10. 1997;5(10):1-4. 
5. Akhtar NM, et al. “Oral enzyme combination versus diclofenac in the treatment of osteoarthritis of the knee--a double-blind prospective randomized study.” Clin Rheumatol. 2004 Oct;23(5):410-5. Epub 2004 Jul 24.
6. Klein, G.; Kullich, W. “Short-Term Treatment of Painful Osteoarthritis of the Knee with Oral Enzymes: A Randomised, Double-Blind Study versus Diclofenac” Clinical Drug Investigation: January 2000 - Volume 19 - Issue 1 - pp 15-23
7. Klein G et al. “Efficacy and tolerance of an oral enzyme combination in painful osteoarthritis of the hip. A double-blind, randomized study comparing oral enzymes with non-steroidal anti-inflammatory drugs.” Clin Exp Rheumatol 2006 Jan-Feb;24(1):25-30
8. Chintalacharuvu SR, et al. “Treatment of collagen induced arthritis by proteolytic enzymes: immunomodulatory and disease modifying effects.” J Rheumatol. 2001 Sep;28(9):2049-59.
9. Al-Khateeb TH, Nusair Y. “Effect of the proteolytic enzyme serrapeptase on swelling, pain and trismus after surgical extraction of mandibular third molars.” Int J Oral Maxillofac Surg. 2008 Mar;37(3):264-8. Epub 2008 Feb 12.
10. Mazzone A,et al. “Evaluation of Serratia peptidase in acute or chronic inflammation of otorhinolaryngology pathology: a multicentre, double-blind, randomized trial versus placebo.” J Int Med Res. 1990 Sep-Oct;18(5):379-88.
11. Buford TW, et al. “Protease Supplementation Improves Muscle Function after Eccentric Exercise.” Med Sci Sports Exerc. 2009 Sep 2.
12. Miller PC, et al.” The effects of protease supplementation on skeletal muscle function and DOMS following downhill running.”  J Sports Sci. 2004 Apr;22(4):365-72.
13. Oben J, Kothari SC, Anderson ML. “An open label study to determine the effects of an oral proteolytic enzyme system on whey protein concentrate metabolism in healthy males.” J Int Soc Sports Nutr. 2008 Jul 24;5:10.
14. Gläser D, Hilberg T. “The influence of bromelain on platelet count and platelet activity in vitro.” Platelets. 2006 Feb;17(1):37-41.
15. Juhasz, B. “Bromelain induces cardioprotection against ischemiareperfusion injury through Akt/FOXO pathway in rat myocardium” Am J Physiol Heart Circ Physiol. 2008 March
16. Metzig C, et al “Bromelain proteases reduce human platelet aggregation in vitro, adhesion to bovine endothelial cells and thrombus formation in rat vessels in vivo.” In Vivo. 1999 Jan-Feb;13(1):7-12.
17. Hsia CH, et al. “Nattokinase decreases plasma levels of fibrinogen, factor VII, and factor VIII in human subjects.” Nutr Res. 2009 Mar;29(3):190-6.
18. Kim JY, et al. “Effects of nattokinase on blood pressure: a randomized, controlled trial.” Hypertens Res. 2008 Aug;31(8):1583-8.
19. Stauder G, et al. The use of hydrolytic enzymes as adjuvant therapy in AIDS/ARC/LAS patients.” Biomed Pharmacother. 1988;42(1):31-4.
20. Saruc M, et al. “Pancreatic enzyme extract improves survival in murine pancreatic cancer.” Pancreas. 2004 May;28(4):401-12.
21. Popiela T, et al. “Influence of a complementary treatment with oral enzymes on patients with colorectal cancers--an epidemiological retrolective cohort study.” Cancer Chemother Pharmacol. 2001 Jul;47 Suppl:S55-63.
22. Zentler-Munro PL, Northfield TC. “Review: pancreatic enzyme replacement--applied physiology and pharmacology.” Aliment Pharmacol Ther. 1987 Dec;1(6):575-91.
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