Bromelain

Bromelain Bodybuilding Wonder Supplement

This is a
rather long article. I was turned on to Bromelain by a Pharm MD freind of mine,
who uses this as an anti-inflammatory.

My interest is to enhance recouperation from the reduced inflammation
properties of Bromelain supplementation.

This
article makes it look like a wonder drug and I will be doing a controlled study
with myself to accurately assess it’s effectiveness in accomplishing this in
the next few months and will define the dosing and protocol use when
done-including some accurate notes from the log book.

I am planning on doing back to back comparisons with the only variable being
the added Bromelain itself to accurately assess it’s effect.

Everything will be planned to be kept the same in each study. Training style,
DIET (food), supplementation, and possibly no AAS or if so , Enhanced HRT doses
only. I’ll do my best to keep stress and other things to a minimum.

Oh yea plus blood work before and after each study to see the effects on tha
blood. (Thank God for www.directlabs.com)

Read up and comment please.

“Bromelain: A Literature Review and Discussion of its Therapeutic
Applications

Gregory S. Kelly, N.D.

Abstract

First introduced as a therapeutic compound in 1957, bromelain’s actions
include: (1) inhibition of platelet aggregation; (2) fibrinolytic activity; (3)
anti-inflammatory action; (4) anti-tumor action; (5) modulation of cytokines
and immunity; (6) skin debridement properties; (7) enhanced absorption of other
drugs; (8) mucolytic properties; (9) digestive assistance; (10) enhanced wound
healing; and (11) cardiovascular and circulatory improvement. Bromelain is well
absorbed orally and available evidence indicates that it’s therapeutic effects
are enhanced with higher doses. Although all of its mechanisms of action are
still not completely resolved, it has been demonstrated to be a safe and
effective supplement. (Alt Med Rev 1996;1(4):243-257)

Description

Pineapple has been used as a medicinal plant in several native cultures and
bromelain has been known chemically since 1876. In 1957, bromelain was
introduced as a therapeutic compound when Heinicke found it in high
concentrations in pineapple stems.

Bromelain is a general name for a family of sulfhydryl proteolytic enzymes
obtained from Ananas comosus, the pineapple plant. It is usually distinguished
as either fruit bromelain or stem bromelain depending on its source, with all
commercially available bromelain being derived from the stem.1 The term
bromelain will be used to refer to stem bromelain in the remainder of this
article.

Bromelain’s primary component is a sulfhydryl proteolytic fraction. Bromelain
also contains a peroxidase, acid phosphatase, several protease inhibitors, and
organically bound calcium. When the proteolytic fraction of bromelain is
purified and extracted, the result is a potent proteolytic enzyme in vitro;
however, this component has been shown to be physiologically inactive in vivo
for many of the conditions where bromelain has a beneficial effect.2 It appears
that a great deal of the physiological activity of bromelain is not accounted
for in its proteolytic fraction and it is likely that the beneficial effects of
bromelain are due to multiple factors, not to one single factor that can be
isolated.

To date, eight basic proteolytically active components have been detected in
the stem. The two main components have been labeled F4 and F5. The proteinase
considered to be the most active fraction has been designated as F9, which
comprises about 2% of the total proteins. It is estimated that 50% of the
proteins in F4 and F5 are glycosylated, whereas F9 was found to be
unglycosylated. The optimal pH for the F4 and F5 fractions is between 4.0 and
4.5 and for F9 close to a neutral pH.3 The entire extract of bromelain has been
shown to exhibit its activity over a pH range of 4.5 to 9.8.4

Since bromelain is derived from a natural source, different sources can exhibit
variability in their physiological activity, even when their proteolytic
activity is the same. Bromelain is not heat stable so it’s physiological
activity can be further reduced by improper processing or storage conditions.

Absorption and Availability

Bromelain is absorbed intact through the gastrointestinal tract of animals,
with up to 40% of the high molecular weight substances detected in the blood
after oral administration. The highest concentration of bromelain is found in
the blood 1 hour after administration; however, its proteolytic activity is
rapidly deactivated,5 probably by the normal plasma protease controls and serum
alpha2-macroglobulin.

A variety of designations have been used to indicate the activity of bromelain;
with published research varying in the designation utilized. Rorer units
(R.U.), gelatin dissolving units (G.D.U.), and milk clotting units (M.C.U.) are
the most commonly used measures of activity. One gram of bromelain standardized
to 2000 M.C.U. would be approximately equal to 1 gram with 1200 G.D.U. of
activity or 8 grams with 100,000 R.U. of activity.

Platelet Aggregation, Fibrinolysis and Anti-Inflammatory Activity

The first conclusive evidence that bromelain prevents aggregation of blood
platelets was reported in 1972. Bromelain was administered orally to 20
volunteers with a history of heart attack or stroke, or with high platelet
aggregation values. Bromelain decreased aggregation of blood platelets in 17 of
the subjects and normalized values in 8 of the 9 subjects who previously had
high aggregation values.6 In vitro studies have demonstrated that bromelain
inhibits platelet aggregation stimulated by ADP or epinephrine, as well as by
prostaglandin precursors, in a dose-dependent manner.7

Bromelain is an effective fibrinolytic agent in vitro and in vivo; however, its
effect is more evident in purified fibrinogen solutions than in plasma. This is
probably due to the antiproteases present in plasma. A dose-dependent reduction
of serum fibrinogen level is seen in rats following administration of
bromelain, and at the highest concentrations of bromelain, both prothrombin
time (PT) and activated partial thromboplastin time (APTT) are markedly
prolonged.8 Bromelain’s fibrinolytic activity has been attributed to the
enhanced conversion of plasminogen to plasmin, which limits the spread of the
coagulation process by degrading fibrin.9

Bromelain seems to have both direct as well as indirect actions involving other
enzyme systems in exerting its anti-inflammatory effect. Both etodolac and
bromelain inhibit the inflammatory pain in rats in a dose-dependent manner.10
Bromelain was the most potent of nine anti-inflammatory substances tested on
experimentally-induced edemas in rats;11 while prednisone and bromelain have
been shown to be comparable in their ability to reduce inflammation in rats.12
Treatment with bromelain and emorfazone has been shown to decrease
significantly the heat-evoked immunoreactive substance P release and subsequent
edema in a rat model.13

Mechanism of Action

Surface contact, by collagen or platelets, activates the kinin system and the
clotting cascade by stimulating the conversion of Hageman factor to an active
protease (factor XIIa). Factor XIIa then activates the kinin system by
converting plasma prekallikrein into kallikrein, and continues the intrinsic
path of the clotting cascade by converting factor XI to its active form.
Kallikrein, in an autocatalytic loop, accelerates the activation of Hageman
factor, which continues to potently activate both the kinin system and the
clotting cascade. In addition, Kallikrein cleaves (HMWK) to produce bradykinin,
a potent stimulator of both increased vascular permeability and pain. The
activation of the clotting cascade will culminate in the conversion of
fibrinogen to fibrin (see Figure 1). Fibrin then forms a protective matrix
around the injured area. This matrix inhibits tissue drainage, promotes edema
and blocks circulation of blood flow.

In order to determine the effects of bromelain on the plasma kallikrein system,
bradykinin levels and plasma exudation at the inflammatory site were examined
in rats. Bromelain (5 and 7.5 mg/kg) caused a dose-dependent decrease of
bradykinin levels at the inflammatory site and a parallel decrease of the
prekallikrein levels in sera. Plasma exudation was also reduced dose
dependently. Bradykinin-degrading activity in sera was elevated after treatment
with bromelain, although it was unchanged in the pouch fluid.14 The levels of
high molecular weight (HMW) kininogen and pre-kallikrein in rat plasma were
markedly reduced after single injection of bromelain (10 mg/kg, i.v.) and
gradually recovered over a 72 hour period. The level of low molecular weight
(LMW) kininogen was not changed during this period.15

Bromelain-treated rats also show a reduction in Factor X and prothrombin, both
of which are needed for the activation of fibrinogen to fibrin through the
common pathway of the intrinsic and extrinsic cascade.16 This indicates that
bromelain’s action is in part a result of inhibiting the generation of
bradykinin at the inflammatory site via depletion of the plasma kallikrein
system, as well as limiting the formation of fibrin by reduction of clotting
cascade intermediates. These actions result in significant reduction in pain
and edema, as well as enhanced circulation to the injured site.

After the formation of a clot, vessel repair begins with the conversion of
plasminogen to plasmin, which then acts to degrade fibrin into smaller
components which can be removed by monocytes and macrophages. In rats,
bromelain has been shown to stimulate the conversion of plasminogen to plasmin,
resulting in increased fibrinolysis. This minimizes venous stasis, facilitates
drainage, increases permeability and restores the tissue’s biological
continuity.16

The therapeutic effect of bromelain may also be due to its ability to
selectively modulate the biosynthesis of thromboxanes and prostacyclins; two
groups of prostaglandins with opposite actions which ultimately influence
activation of cyclic-3,5-adenosine (cAMP), an important cell-growth modulating
compound.

The binding of epinephrine, collagen, or thrombin to platelets activates the
enzymes phospholipase C and phospholipase A2 which release arachidonic acid
from membrane phospholipids (phosphatidylcholine and phosphatidylinositol).
Table 1 lists the inflammatory actions of arachidonic acid metabolites.

Plasminogen, which is activated to plasmin by the oral administration of
bromelain, has been shown to inhibit the release of arachidonic acid from cell
membranes, resulting in decreased platelet aggregation and modulation of the
series 2 prostaglandins.17 It is also hypothesized that bromelain therapy leads
to a relative increase of the endogenous prostaglandins, PGI2 and PGE2 over
thromboxane A2.18

Non-steroidal anti-inflammatory drugs inhibit cyclooxygenase, which is required
for the synthesis of series 2 prostaglandins, resulting in a decrease in both
pro and anti-inflammatory prostaglandins. Rather than blocking the arachidonic
acid cascade at the enzyme cyclooxygenase, like NSAIDs, bromelain may
selectively decrease thromboxane generation and change the ratio of thromboxane/prostacyclin
(PGI2) in favor of prostacyclin (see Figure 2). Bromelain, similar to NSAIDs,
has been shown to inhibit PGE2, however, its action is significantly weaker.16
Table 2 lists bromelain’s impact on selected mediators of inflammation.

Antitumor

The first documented use of oral bromelain on cancer patients was in 1972.
Twelve patients with ovarian and breast tumors were given 600 mg of bromelain
daily for from 6 months to several years, with reported resolution of some of
the cancerous masses and a decrease in metastasis.19 Bromelain in doses of over
1000 mg daily has been combined with chemotherapeutic agents such as 5-FU and
vincristine, and has been reported to result in tumor regression.19,20

Bromelain has also decreased lung metastasis of Lewis lung cancer cells
implanted in mice in a dose-dependent manner. This antimetastatic potential was
demonstrated by both the active and inactive bromelain, with or without
proteolytic and anticoagulant properties.21,22

Cytokine Induction

The successful initiation of an immune response depends on T cells and
macrophages, along with the polypeptide factors they produce, called cytokines,
which play a key role in communication during normal immunological response as
well as infectious, inflammatory, and neoplastic disease states. Table 3 lists
cytokines and their activities.

Bromelain, papain, and amylase have all been demonstrated to induce cytokine
production in human peripheral blood mononuclear cells. Treatment leads to the
production of tumor necrosis factor-alpha (TNF-alpha), interleukin-1-beta (IL-1
beta), and interleukin-6 (IL-6) in a time and dose-dependent manner.
Interferon-alpha (IFN-alpha) and interferon-gamma (IFN-gamma), which had no
effect alone, synergistically increased TNF-alpha production when applied
together with the enzymes.23,24 The tryptic but not the autolytic fractions of
papain and bromelain have a higher (10- to 40-fold) inducing capacity for TNF
production than the untreated enzyme.25 Trypsin alone had only a small inducing
effect.

The ability to induce cytokine production may explain the antitumor effects
observed after oral administration of polyenzyme preparations.

Immunity

Bromelain has been shown to remove T-cell CD44 molecules from lymphocytes and
to affect T-cell activation. The highly purified bromelain protease F9 was
tested on the adhesion of peripheral blood lymphocytes (PBL) to human umbilical
vein endothelial cells (HUVEC). Both bromelain and protease F9 reduced the
expression of CD44, but F9 was about 10 times more active than bromelain;
having about 97% inhibition of CD44 expression. The results indicate that F9
selectively decreases the CD44 mediated binding of PBL to HUVEC.26

Debridement

Bromelain applied topically as a cream (35% bromelain in a lipid base) can be
beneficial in the elimination of burn debris and in acceleration of healing. A
non-proteolytic component of bromelain is responsible for this effect. This
component, referred to as escharase, has no hydrolytic enzyme activity against
normal protein substrates or various glycosaminoglycan substrates and its
activity varies greatly from preparation to preparation.27

Topical bromelain has achieved complete debridement on experimental burns in
rats in an average of 1.9 days as compared to collagenase, which required an
average of 10.6 days for similar results.28

Topical bromelain separates eschar at the interface with living tissue. It is
hypothesized that bromelain activates collagenase in living tissue which then
attacks the denatured collagen in the eschar. This produces a demarcation
between living and dead tissue. With very little scraping, using a tongue
depressor, all of the eschar can be removed and a bed suitable for grafting
results. By using bromelain, grafting can occur as soon as 24 hours after the
accident. Utilizing bromelain cream in the treatment of burns usually results
in minimal or no scar tissue formation.

The applicability of topical bromelain in frostbite eschar removal was
extrapolated and investigated. In the initial trial, no debridement other than
that of the superficial layers of the eschar was noted. Although third degree
burn injuries debrided to a graftable bed after two topical applications of
bromelain, frostbite injuries remained unaffected.29

Potentiation of Antibiotics

Antibiotic potentiation is one of the primary uses of bromelain in several
foreign countries. Bromelain can modify the permeability of organs and tissues
to different drugs. It prolongs sleeping time in mice administered
pentobarbital30 and increases spinal levels of penicillin and gentamycin in
rats. In humans, bromelain has been documented to increase blood and urine
levels of antibiotics16 and results in higher blood and tissue levels of
tetracycline and amoxycillin when they are administered concurrently with
bromelain.31

Treatment of 18 women with 80 mg of bromelain concurrently with amoxycillin or
tetracyclin resulted in increased serum levels and concentrations of both
antibiotics in uterus, ovarian tubes, and ovaries as compared with controls.
This effect was not generated by indomethacin, an anti-inflammatory drug which
acts as a cyclooxygenase inhibitor, which indicates that bromelain has some
undetermined activity that enhances absorption and tissue distribution of
antibiotics.32 A three-fold increase in the level of tetracycline in serum
after oral ingestion of 540 mg of enterically-coated bromelain has also been
demonstrated in a double blind test.33

Combined bromelain and antibiotic therapy was instituted for 53 hospitalized patients
with the following conditions; pneumonia, bronchitis, cutaneous staphylococcus
infection, thrombophlebitis, cellulitis, pyelonephritis and perirectal and
rectal abscesses. Twenty three of the patients had been on antibiotic therapy
without success. Bromelain was administered four times a day along with the
following antibiotics either alone or in combination; penicillin,
chloramphenicol, erythromycin or novobiacin. A control group of 56 patients was
treated with antibiotics alone. Of the 23 patients who had been unsuccessfully
treated with antibiotics, 22 responded favorably to the combined treatment. In
every disease state studied there was a significant reduction in morbidity when
the combination of bromelain and antibiotics was used as opposed to antibiotics
alone. Another group of 106 cases was treated with bromelain alone, with
results comparable to those obtained with antibiotic treatment.34

Forty eight patients with acute sinusitis were placed on standard therapy,
which included antihistamines and analgesic agents, along with antibiotics if
indicated. Twenty three of the patients received bromelain four times daily,
while the remaining 25 received a placebo. Of the patients receiving bromelain,
83% had complete resolution of nasal mucosal inflammation compared with only
52% in the placebo group. Improvement in breathing occurred in 78% of those
receiving bromelain as compared to 68% in those receiving placebo. In the
patients not receiving antibiotic treatment, 85% of patients receiving bromelain
had complete resolution of inflammation of the nasal mucosa and complete
resolution of breathing difficulties. Only 40% of the placebo group had a
similar outcome with respect to inflammation, while 53% reported resolution of
breathing difficulty.35

The potentiation of antibiotics and other medicines by bromelain may be due to
enhanced absorption, as well as increased permeability of the diseased tissue
which enhances the access of the antibiotic to the site of the infection. It is
also thought that the use of bromelain may provide a similar access to specific
and non-specific components of the immune system, therefore, enhancing the
body’s utilization of its own healing resources.

Mucolytic Properties

The topical use of the enzymes, bromelain or papain, to remove excessive
cervical mucus was demonstrated in 1954. Observations following its use
demonstrated that pseudo and actual space-occupying lesions could be more
positively identified, and inflammatory changes of the canal and its glands
could be visualized with greater accuracy.36

Effects of bromelain on rabbit sputum consistency were investigated in vitro
and in vivo. Of the enzymes tested, bromelain exerted the most potent lowering
effect on sputum viscosity and also showed a tendency to increase the sputum
volume.37

In a clinical study of 124 patients hospitalized with chronic bronchitis,
pneumonia or bronchopneumonia, bronchiectasis, or pulmonary abscess, those
receiving bromelain orally showed a decrease in the volume and purulence of the
sputum.17 These results support the effectiveness of bromelain in decreasing
the viscosity of sputum so that it can be more easily cleared from the
respiratory tract.

Digestive Aid

Bromelain has been used successfully as a digestive enzyme following pancreatectomy,
in cases of exocrine pancreas insufficiency and in other intestinal
disorders.38 Because of its wide pH range, bromelain has activity in the
stomach as well as the small intestine. It has also been shown to be an
adequate replacement for pepsin and trypsin in cases of deficiency. The
combination of ox bile, pancreatin and bromelain is effective in lowering stool
fat excretion in patients with pancreatic steatorrhoea. In addition, this
combination resulted in a gain in weight in most cases as well as an enhanced
subjective feeling of well being. Symptomatic improvement was also noted in
relation to pain, flatulence and stool frequency.39

Bromelain has been reported to heal gastric ulcers in experimental animals.40
In an extensive study of the effect of bromelain on the gastric mucosa, it was
found that bromelain increased the uptake of radioactive sulfur by 50% and
glucosamine by 30 -90%. Increased uptake of these substances may allow the
gastric mucosa to heal more rapidly under the influence of bromelain.41

In a study designed to examine the effect of bromelain on enterotoxin receptor
activity in porcine small intestine, orally administered bromelain inhibited
enterotoxin attachment to pig small intestine in a dose-dependent manner.
Attachment was negligible after treatment. Serum biochemical analysis and
histopathological examination of treated piglets showed no adverse effects with
the bromelain treatment. Administration of bromelain may therefore be useful
for preventing enterotoxin-induced diarrhea.42

Surgical Procedures and Musculoskeletal Injuries

Bromelain also has therapeutic effects in the treatment of inflammation and
soft tissue injuries. An early clinical trial on bromelain was conducted on 74
boxers with bruises on the face and haematomas of the orbits, lips, ears, chest
and arms. Bromelain was given four times a day for 4 days or until all signs of
bruising had disappeared. A control group of 72 boxers were given a placebo. In
58 of the boxers taking bromelain, all signs of bruising cleared completely in
four days, with the remaining 16 requiring 8-10 days for complete clearance. In
the control group, only 10 had complete clearance within four days, with the
remainder requiring seven to fourteen days for resolution.43

The edema-reducing property of bromelain was investigated in
traumatically-induced hindleg edema in rats. After enteral application of
bromelain a significant reduction of the edema could be observed, however,
parenteral application only resulted in a minimal therapeutic effect. Although
enterally-applied enzymes are thought to be degraded in the gut, the better
results were obtained after oral administration of bromelain, supporting the
observation that bromelain can be absorbed by the gut without losing its
biological properties.11

Fifty-five pre-surgical patients were divided into two groups. Group one,
consisting of 22 patients, took bromelain four times a day for 48-72 hours
prior to surgery and continued for 72 hours after surgery. Group two,
consisting of 33 patients, took bromelain starting on the day of surgery, with
the first dose administered one hour prior to surgery. Fifty percent of group
one and 42.4% of group two had complete disappearance of pain and inflammation
within 72 hours. Pain and inflammation persisted past 72 hours in only one
member of the group supplemented with bromelain for three days prior to
surgery, as opposed to five members of the group that started supplementation
one hour prior to surgery. In a separate study, supplementation of bromelain
starting 48-72 hours prior to surgery reduced the average number of days for
complete disappearance of pain from 3.5 to 1.5, and disappearance of
inflammation from 6.9 to 2.0 days, as compared with controls receiving no
bromelain.44

Sixteen patients undergoing oral surgery were given bromelain four times a day
starting 72 hours prior to surgery. At 24 hours after surgery, 75% of these
patients were evaluated as having mild or no inflammation, in contrast to only
19% of a group receiving a placebo. Twenty-four hours after surgery, pain was
either absent or mild in 38% of bromelain-treated patients, as opposed to 13%
receiving placebo. After 72 hours, this increased to 75% of those in the
bromelain group, as compared to only 38% in the placebo group.45

In an observation study involving 59 patients with blunt injuries to the
musculoskeletal system, the efficacy and tolerability of high-dose bromelain,
in addition to the usual therapeutic measures, was investigated. Treatment with
bromelain resulted in a clear reduction in all four parameters tested;
swelling, pain at rest and during movement, and tenderness.46

Cardiovascular and Circulatory Applications

Research has indicated that bromelain prevents aggregation of human blood
platelets in vivo and in vitro, prevents or minimizes the severity of angina
pectoris and transcient ischemic attacks (TIA), is useful in the prevention and
treatment of thrombosis and thrombophlebitis, may break down cholesterol
plaques, and exerts a potent fibrinolytic activity. If administered for
prolonged time periods, bromelain also exerts an anti-hypertensive effect in
experimental animals.2,47

Administration of 400-1000 mg/day of bromelain to 14 patients with angina
pectoris resulted in the disappearance of symptoms in all patients within 4 to
90 days.48 Similar results have been observed in patients taking between
500-700 mg/day of bromelain. After discontinuing bromelain, angina attacks
reappear after a variable period of time, often triggered by stressful
experiences.2

A drastic reduction in the incidence of coronary infarct after administration
of potassium and magnesium orotate along with 120-400 mg of bromelain per day
has also been reported.49

In a study involving 73 patients with acute thrombophlebitis, bromelain, in
addition to analgesics, was shown to decrease all symptoms of inflammation;
including, pain, edema, tenderness, skin temperature, and disability.40

The ability of bromelain to influence these conditions may be due to its
ability to breakdown fibrinous plaques. Bromelain has been shown to dissolve
arteriosclerotic plaque in rabbit aorta in vivo and in vitro.2 It is likely
that bromelain also increases vessel wall permeability to oxygen and nutrients
while increasing blood fluidity, both of which aid in these conditions.

Toxicity, Side Effects and Allergic Reactions

Bromelain is considered to have very low toxicity, with an LD50 greater than
10g/kg. Toxicity tests on dogs, with increasing levels of bromelain up to 750
mg/kg administered daily, showed no toxic effects after six months. Dosages
of1.5 g/kg/day administered to rats show no carcinogenic or teratogenic
effects. 51

In human clinical tests, side effects have not been observed. Bromelain
supplementation up to 460 mg has been shown to have no effect on heart rate or
blood pressure; however, increasing doses up to 1840 mg have been shown to
increase the heart rate proportionately. In some cases an increase of up to 80%
of the baseline has been reported, which may be a result of bromelain’s
influence on IL-1 and TNF production. Maximum effects were seen at 2 hours but
some residual effect remained at 24 hours. At doses above 700 mg, palpitations
and subjective discomfort have been reported. Blood pressure changes have not
been demonstrated in humans at any dosage level.52

The allergenic potential of proteolytic enzymes should not be underestimated,
for they cause, in particular, IgE-mediated respiratory allergies of both the
immediate type and the late-phase of immediate type with predominantly respiratory
symptoms. Allergy to bromelain has been reported in workers of a blood-grouping
laboratory, and investigation indicates that (1) bromelain is a strong
sensitizer, (2) sensitization usually occurs due to inhalation and not to
ingestion, (3) bromelain allergy is occupationally acquired, and adequate
precautions are necessary.53 The risk of sensitization to enzymes due to
inhalation as a result of occupational exposure is very high (up to 50%).54

Bromelain has been shown to cross-react with the sera in about 28% of persons
with IgE allergic response to honeybee venom.55 Bromelain, along with
horseradish peroxidase and ascorbate oxidase are recognized by the IgE of sera
from patients who are hypersensitive to olive tree pollen.56

Bromelain and papain, due to their use as a meat tenderizer and to clarify
beer, are considered as potential ingestive allergens and may represent an
unrecognized cause of an allergic reaction following a meal. As with other food
substances, a small segment of the population, particularly those with a
sensitivity to pineapple, may be sensitive to oral supplementation with
bromelain. As contact allergens, the enzymes play a minor role; however, it is
thought that skin testing with isolated proteases like bromelain may induce
systemic reactions in susceptible individuals, even at very high dilution.53,57

Indications for the Use of Bromelain

There are several compelling reasons for supplementation with oral bromelain.

1. It inhibits blood platelet aggregation, favorably modulates prostaglandin
formation and minimizes risk of coronary atherosclerotic disease.

2. It continues to provide a desired physiological action for as long as it is
administered, with no evidence indicating that a tolerance develops.

3. It is considered to be non-toxic and lacking in side effects, so it can be
used without concern in doses from 200 to 2000 mg for prolonged periods of
time.

4. It is a protein and seems to be as easily metabolized as other dietary
proteins.

5. It is well absorbed and seems to have greater therapeutic impact when
administered orally as opposed to intravenously

6. While effective for inflammation and injury, it is even more effective if
administered prior to a traumatic event, i.e. surgery or athletic competition.

7. It seems to enhance the absorption of and improve the action of other
substances when they are administered in combination.

8. Because of its impact on the cytokine system, particularly IL-1 and TNF,
which stimulate fever and acute phase response, and its demonstrated ability to
increase the heart rate, bromelain may assist in generating an acute-stage
healing response.

Bromelain has a wide range of conditions for which it has well documented
therapeutic efficacy (see Table 4).

Dosage and Prescription Instructions

Available research does not demonstrate an enhanced efficacy of bromelain when
it is administered between meals. It is generally recommended that bromelain be
taken away from food unless it is being used as a digestive aid, because it is
believed that otherwise, it will tend to act as a digestive enzyme and its
therapeutic benefit may be diminished. While this may in fact be the case, the
clinical studies conducted on bromelain have not followed this protocol.

Bromelain has shown therapeutic benefits in doses as small as 160 mg/day;
however, it is thought that, for most conditions, best results occur starting
at a dose of 750-1000 mg/day. Most research on bromelain has been done
utilizing divided doses, usually four per day, and findings indicate that results
are dose-dependent. See Table 5 for a summary of prescription instructions.

Conclusion

Bromelain has been used for a variety of clinical applications for more than 35
years. Although its mechanisms of action has not been completed resolved,
bromelain has demonstrated a beneficial effect on the kinin system, the
coagulation cascade, the cytokine system, and prostaglandin synthesis.
Bromelain is believed to enhance the absorption of flavonoids and has been
shown to increase absorption of glucosamine, so bromelain supplemention should
be considered when these nutrients are given. It may also enhance absorption
and utilization of many other substances; however, to date research in this
area has focused primarily on antibiotics. Bromelain has been shown to exert a
beneficial effect at doses as low as 160 mg/day, however, there is a general
consensus among researchers that the best results occur when bromelain is given
in doses above 500 mg per day and that results improve in a dose-dependent
manner with higher levels of bromelain supplementation. Bromelain has been
demonstrated to be well absorbed after an oral dose and has been shown to be
safe at high doses for prolonged periods of time. For the conditions discussed
in this review, bromelain has shown itself to be an effective supplement.”


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