Dr. Clouatre's
Corner
Dallas L. Clouatre, Ph.D.
Dallas is a well-established author and consultant in the
alternative and complimentary medicine and nutrition field,
Mr. Clouatre is a Member of the American College of
Nutrition and has published in peer-reviewed medical
journals.
HCA Thoughts:
• HYDROXYCITRIC ACID as a Lipogenesis
Inhibitor and Much More*
Publications:
• The Prostate Miracle: New Natural
Therapies That Can Save Your Life
• FAQs All about Grape Seed Extract
• Anti-Fat Nutrients: Safe and
Effective Strategies for Increasing Metabolism, Controlling
Appetite, and Losing Fat in 15 Days
• Glucosamine Sulfate and Chondroitin
Sulfate
• Getting Lean With Anti-Fat
Nutrients
• SAM-E: THE ULTIMATE METHYL
DONOR.(S-adenosyl-L-methionine) : An article from: Health
Products Business [HTML]
• Glucosamine: Changing the Delivery
for Superior Benefits. : An article from: Original
Internist [HTML]
• FAQs All about SAM-E
• Users Guide to Weight-Loss
Supplements: Learn How to Sort Through All the Fads and
Supplements and Successfully Lose Weight (Basic Health
Publications User's Guide)
• The Diet and Health Benefits of
Hca: How This All-Natural Diet Aid Promotes Weight Loss and
Inhibits Fat Production (Hydroxycitric Acid : How This All
Promotes Weight Loss and Inhibits Fat Production)
Research:
• Hydroxycitric acid delays
intestinal glucose absorption in rats
• HYDROXYCITRIC ACID as a Lipogenesis
Inhibitor and Much More*
Inhibitors of lipogenesis are substances that slow the
production of fats from the metabolism of carbohydrates and
proteins. This means inhibiting, for instance, the
synthesis of triglycerides and/or cholesterol, and likewise
preventing the storage of fat in fat cells. Some known
drugs, such as Triton, inhibit lipogenesis, but these drugs
have many side effects and they lose their effectiveness
with continued use. Safe and effective natural alternatives
are now being discovered. One such natural alternative is
(–)-hydroxycitric acid (HCA), which is usually made
available combined with a mineral, as in calcium
(–)-hydroxycitrate. HCA is extracted primarily from
the dried pericarp (rind) of the fruit of Garcinia
cambogia, native of South Asia. Related species of trees
also produce HCA. Crude extracts of Garcinia are popularly
employed in cooking as flavoring and souring agents,
including in the preparation of curries. Garcinia extract
also is used as a preservative, as a purgative for the
treatment of intestinal worms and parasites, and for
bilious digestive conditions.113 Interestingly, in the
areas where it traditionally is used, G. cambogia is said
to make meals more “filling.” However, in the
West until quite recently HCA has been a disappointment as
a diet aid. Research over the past few years indicates that
purity and delivery methods are at fault and that when
these are corrected, HCA may at last live up to its
promise.
How HCA Blocks Fat
HCA is remarkable for its ability to reduce the body's own
synthesis of fats. During the normal metabolism of meals,
carbohydrate calories which are neither used immediately
for energy nor stored as glycogen are converted into fats
in the liver by the enzyme ATP-citrate lyase. HCA inhibits
this enzyme, and by doing so it also reduces the formation
of acetyl coenzyme A, a biochemical which plays a key role
in carbohydrate and fat metabolism. As a result, the
production of low-density lipoprotein (LDL) and
triglycerides is inhibited. The net effect is that fat
production and storage is reduced. The appetite is
controlled, food consumption is cut and thermogenesis may
be enhanced.
HCA has been studied extensively for a period of more than
two decades. Numerous animal trials conducted at major
universities and described in peer-reviewed journals have
demonstrated both the safety and the efficacy of HCA in
inhibiting the production of fats from carbohydrate
calories. The results of these trials have been so
impressive that one of the world's largest pharmaceutical
firms, Hoffmann-La Roche, not only sponsored much of the
work, but also sought synthetic patentable versions of HCA
to market as diet drugs. To date, no such synthetic
products are available.
Quality control is of major importance inasmuch as the
desired effect is dosage-dependent. As it turns out, it is
quite difficult to establish the exact amount of HCA
present in an extract. Many companies which claim to have a
concentration of 50% HCA actually have mistakenly counted
tartaric, citric and other organic acids present in the
rind as part of the HCA content. Also important is the form
of HCA used. In animal trials, the lactone form of HCA has
proven to be less effective than the salt form. According
to data from Hoffman-La Roche, the rate of conversion of
free HCA in solution into its lactone is approximately 10%
per week at low room temperature with an equilibrium point
(usually 20 – 25% lactone) reached depending on
concentration. Virtually all the pharmaceutical trials
employed a pure trisodium (–)-hydroxycitrate
containing no absorption-impeding gums, pectins or other
such compounds. Similarly, current thinking is that calcium
as part of an HCA salt impedes absorption and/or otherwise
reduces the activity of the compound. Readers should keep
these points in mind inasmuch as the forms of HCA available
in the health food market seldom approach the optimal level
of quality.
Current Controversies
Despite claims to the contrary, the employment of HCA for
weight loss is not a modern Western pharmaceutical
invention. In some parts of Malaysia, the fruit of Garcinia
species is used to make a soup that is eaten before meals
for weight loss. This is a traditional remedy in the
villages, not the cities. Note that this means that very
large amounts of HCA are consumed via a liquid food, not
small amounts via capsules. Moreover, a bowl of light soup
before lunch and supper does seem to make HCA work better.
HCA increases the body’s own satiety signal, so it is
best to slow down how quickly meals are eaten. This
strategy gives the body a chance to respond to the signal
that enough has been eaten. Never skip meals and do not
take HCA in place of a meal – it requires food to
work. Those who are sensitive to citric acid (i.e., to
oranges, tomatoes, etc.) may be sensitive to Garcinia
extracts as well.
The best recent evidence suggests that the newly available
HCA potassium salts are both much more effective and more
effective for a greater percentage of users than are the
HCA calcium salts. Liquid Garcinia extracts likewise appear
to be more readily absorbed and more active despite the
lactone issue. Concurrent use of nutrients such as green
tea extract or L-carnitine may improve results, especially
when the fat content of the diet is not closely regulated.
However, HCA definitely should not be taken at the same
time as fiber (glucomman, guar gum, etc.) inasmuch as the
fiber will bind the HCA.
HCA presently is very controversial as a weight loss aid.
In large part, this is because of purity and delivery
issues. Significant failings in the Hoffmann-La Roche
pharmaceutical research also turn out to be at fault, for
these failings have led to the inappropriate use of HCA for
weight loss. The proper use of HCA is explained below.
However, first the verdict on current HCA products.
All the major US and European trials have yielded either
marginal or negative results with regard to actual weight
loss. These trials have employed HCA salts from the leading
suppliers of such products to the US. In a marketing push,
one company is now claiming that HCA increases brain
serotonin levels based upon evidence of in vitro tests
using rat brain slices. The problem here is that Hoffman-La
Roche long ago showed that HCA does not cross the
blood-brain barrier. Even an increase in blood serum
serotonin levels in vivo would be largely meaningless
because peripheral serotonin is used entirely or almost
entirely peripherally, i.e., outside of the brain. This
same company is claiming very good weight loss results in a
clinical trial using 2,800 mg HCA/day given in three
divided doses thirty minutes before meals. Unfortunately,
only the protocol of the study was done in the US. The
trial was conducted entirely in India under Indian
conditions with all oversight, data collection, etc.
performed locally and with the participants eating a
low-fat diet (25 percent or less) rather than
American-style fare. Hence this was a non-US study and its
results cannot be assumed to be valid under American
conditions with American eating habits. Therefore, as of
2003, HCA as a weight loss compound still awaits clinical
validation in a trial conducted in the United States or
Europe under Western conditions and Western standards of
evidence.
The salts of HCA other than potassium, sodium and some
specialty compounds not yet on the market are mostly bound
by bile acids, fiber and/or other components in the diet
and excreted from the body. Studies performed at the
University of California at Berkeley with a leading
potassium/calcium HCA showed that uptake on an empty
stomach was only 20% at best under fasting conditions and
that taking food thirty minutes after ingesting the HCA
reduced absorption by 60%. Calcium appears to reduce the
activity of HCA. Free HCA is extremely ionic and thus does
not easily cross the intestinal wall into the blood stream.
There are several ways one might attempt to solve this
issue. One way is to try to alter the ionic quality of the
extract in the gut. An international patent application
suggests that the inclusion of the Garcina anthocyanin
“garcinol” with the HCA salt makes the HCA more
effective, perhaps by improving uptake or by some other
mechanism, although the results claimed are distinctly
underwhelming.
Delivering the Promise of
(–)-Hydroxycitrate
It is now known that Roche made some major mistakes with
regard to the mechanisms of action of HCA. Yes, the
compound does inhibit the synthesis of fats from
carbohydrates. It also does much more. HCA actually has two
quite distinct actions in the body, one involving gastric
emptying and satiety, the second involving the metabolism.
In the case of appetite suppression, HCA slows the emptying
of the stomach to make one feel fuller faster and
longer––very important for dieters. Roche
maintained that all of HCA’s effects upon appetite
came from the activation of glucose receptors found in the
liver, but data from Swiss researchers published in 2001
proved that this is not the case. The best available
evidence indicates that HCA activates receptors in the
stomach itself and in the duodenum, the first few inches of
the small intestine. These receptors, in turn, activate
cholecystokinin (CCK), which is a satiety compound produced
in the body that requires the presence of food for its
actions. The implication is that HCA must be fully and
completely exposed to stomach receptors either just before
food is ingested or with some source of carbohydrates that
activate sugar sensors. Given that the active HCA salts
will bind to food components if left exposed to these,
achieving significant appetite suppression is quite
difficult. Without a delivery technology, the only
published means of accomplishing this is to take
approximately two grams of a potassium or potassium/calcium
salt and dissolve this in about eight ounces of tomato
juice just before drinking it some 30 minutes before meals.
Inconvenient, to say the least. New technologies promise to
solve this issue. (The action of HCA on gastric emptying
and the delivery forms necessary to optimize this action
are US Patent Pending.)
The metabolic effect of HCA is separable from its appetite
suppressing effect and requires several weeks to come into
its own. The dosage of HCA necessary to reliably enhance
energy metabolism also is higher than that necessary to
reduce appetite and must be aimed at achieving blood levels
rather than influencing stomach receptors. Human trials
have demonstrated that a short-term reduction in caloric
intake of about 15% with HCA led to very little weight
loss, whereas a long-term (three months) intake of HCA that
had no effect on appetite or caloric intake nevertheless
led to slow, yet significant weight loss. The key for most
dieters is to combine these effects, effects involving both
the appetite and the metabolism, into one package. Again,
new delivery technologies promise to solve this problem.
(Some delivery methods for improving HCA blood levels are
protected in US Patent 6,447,807 and others are US Patent
Pending.)
How Is It Available and How Should It Be
Taken?
Since all Garcinia products on the market are extracts and
not pure HCA, consumers should look for the actual HCA
content. For instance, 500 mg. of calcium
(–)-hydroxycitrate standardized as 50 percent HCA
will provide 250 mg. of actual HCA. The effective dosage of
actual HCA probably begins at 1,000 mg. taken two to three
times per day in conjunction with a low fat/low alcohol,
high complex carbohydrate diet. Three grams of HCA is a
good starting dosage if derived from the HCA potassium
salt. There is no good evidence available to support
dosages below three grams HCA per day, and the authors
themselves have seldom heard positive feedback with dosages
below 11–12 grams of the calcium salt. HCA is
included as a minor ingredient in quite a number of
products as a “label palliative,” but there is
no reason to believe that this practice leads to any
benefits. A fully reacted potassium
(–)-hydroxycitrate is roughly three times as
effective as is calcium (–)-hydroxycitrate. One of
the authors was involved in a pilot clinical trial with
morbidly obese patients weighing between roughly two
hundred and four hundred pounds and found that three grams
of HCA derived from five grams potassium
(–)-hydroxycitrate led to weight loss of about three
pounds per week during the three weeks of the trial.
Ideally, dieters should take HCA with a small snack about
an hour before lunch and supper and, if hungry, again
before bedtime. This can be accomplished in several ways.
The least convenient is to mix an HCA powder into 8-10
ounces of juice. Another method is to take an instantly
releasing tablet or capsule with that same juice, although
this requires that a sophisticated coating be applied to
the HCA and that the tablet be specially formulated. Yet
another method is to build a specially coated HCA into
snacks, such as bars or liquids. This is not easily
accomplished because HCA binds to the ingredients found in
foods.
For the best results, two deliveries are required, one
instant to achieve an effect in the stomach for satiety,
and a second one that is controlled for release only in the
small intestine to achieve maximal HCA blood levels. Purity
and delivery are exceptionally important if results are to
be found using HCA. VERY IMPORTANT: Do not take HCA with
red pepper sauces or other capsaicin (capsicum)-containing
supplements. Capsaicin negates the effects of HCA on
gastric emptying.
Cautions
Those who are diabetic or borderline diabetic may find that
the amounts of HCA that are necessary to induce weight loss
will also alter blood glucose levels. Individuals taking
medication for diabetes/blood glucose regulation should
supplement with the effective amounts and forms of HCA,
especially the potassium salt, only under the supervision
of a physician. This had not previously been recognized as
an issue because of the poor quality of the available HCA
salts and inadequate dosages. The use of HCA for blood
glucose and insulin regulation is under patent protection.
(US Patent 6,207,714) Similarly, individuals being treated
for blood pressure disorders may find that effective
amounts and forms of HCA, especially the potassium salt,
may augment the actions of hypotensive medications. (US
Patent Pending) Again, HCA influences the levels of
circulating glucocorticoids. (US Patent 6,474,071, which
also covers claims regarding leptin and several other
hormones) Reducing the chronic levels of these compounds is
usually to be desired, but individuals being treated
therapeutically with cortisol, dexamethasone or other
corticosteroids may find that the effectiveness of their
medications is reduced. Although HCA itself is an extremely
safe compound, as the foregoing indicates, it is likely to
indirectly influence the actions of several drugs.
*Adapted from Dallas Clouatre and William Karneges,
Anti-Fat Nutrients (4th edition).