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120 Bodybuilding Supplement Guide

Guggulsterones: Turn Up the Heat to

Burn More Fat

by Derek Cornelius

as guggul. Just as that plant has

unique and interesting names, so it

also has unique and interesting effects

on the human body.

Guggul is a tree that grows in India that exudes a

resinous sap from its bark. The resin has been used

for centuries in India’s traditional Ayurveda

medicine. In our modern world of advanced chem-

istry the sap is processed and purified and then

standardized for its active constituents—Z and E

guggulsterones. The two compounds are plant

sterols that have a high degree of human bioactivity

and have been shown in studies to affect many bio-

logical processes, including thyroid metabolism,

cholesterol management and dermal, or skin, func-

tion. In each of those areas guggulsterones were

shown to be highly effective modulators with near-

druglike potency.

Bodybuilders are concerned with not only build-

ing solid muscle tissue but also reducing the

amount of fat deposits. You may weigh 240 pounds

and have a tremendous amount of muscular devel-

opment, but if you have two inches of subcuta-

neous fat all over your body, you won’t look all that

great. You definitely won’t be aesthetically pleas-

ing, and some people might even call you dough-

boy. A thyroid-stimulating substance might be

exactly what you need.

I first became interested in guggulsterones when

I noticed studies on their thyroid-stimulating prop-

erties. I discovered that guggulsterones have a di-

rect stimulating action on the thyroid gland through

enzymatic mechanisms. One study concluded that

they’re a viable option for the treatment of hy-

pothyroidal conditions. The warm feeling, the

sweating and the rise in body temperature confirm

guggulsterone’s thyroid-stimulating ability. That’s

good news for those of us who are trying to lose

weight—especially adipose tissue, or fat stores.

When the thyroid gland is stimulated, it produces

more thyroid hormones, such as thyroxin, which

have a profound effect on the rate of metabolism,

including a direct catabolic effect on adipose tis-

sue. That means guggulsterones will stimulate

your thyroid to produce more thyroid hormones,

which in turn will raise your metabolic rate and

burn more fat.

Guggulsterones by themselves have been shown

to work very well for fat loss, but I’ve found a

combination that’s nothing short of amazing—

guggulsterones and an ECA stack such as

Adipokinetix. We already know that Adipokinetix

is an extremely potent fat burner, but it does its

work outside the realm of the thyroid. It made

sense to me that if one could combine the fat-burn-

ing effects of the thyroid hormones with those of

the adrenergic hormones (e.g., adrenaline), some-

thing very dramatic would result. Also, ECA

stacks tend to decrease the amount of thyroid hor-

mones circulating in the blood over time. Guggul-

sterones do a great job of inhibiting that reduction,

thus keeping all physiological fat-burning systems

operating at a maximum level.

The final ways in which guggulsterones can ben-

efit in the fight to burn fat involve ketogenic diets

and growth hormone use. Over time ketogenic

diets tend to reduce the thyroid’s effectiveness by

reducing the conversion of T4 to the more potent

T3. Guggulsterones won’t do anything to increase

the conversion, but they will cause more T4 re-

lease, which in turn should increase T3 to some ex-

tent. Furthermore, although T4 is not as potent a

metabolic regulator, it is functional and should in-

herently help boost the metabolic rate. Regarding

GH use, anyone who has taken this potent hor-

mone knows that it vastly reduces the amount of

thyroid hormones that are produced by the thyroid

gland. Again, although I’ve never tried it and don’t

know of anyone who has, guggulsterones should

help lessen the thyroid-hormone-reducing effect.

Although their fat-burning properties are what

we’re most interested in, guggulsterones also have

an extremely beneficial effect on cholesterol and

122 Bodybuilding Supplement Guide

Bodybuilding Supplement Guide 123

C ommiphora mukul is an herb known

Guggulsterones

have a direct

stimulating

action on the

thyroid gland

through

enzymatic

mechanisms.

One study

concluded that

they’re a viable

option for the

treatment of

hypothyroidal

conditions.

triglyceride levels. Numerous clinical studies have shown that they

cause a 14 to 27 percent decrease in total cholesterol in a four-to-12-

week period, while triglyceride levels drop 22 to 30 percent. Even more

interesting is the fact that guggulsterones support a high high-density

lipoprotein (HDL), or “good” cholesterol, level and a low low-density

lipoprotein (LDL), or “bad” cholesterol, level. Study after study con-

firms that guggulsterones are as potent as many of the current prescrip -

tion drugs for lowering LDL cholesterol. Unlike their drug

counterparts, though, guggulsterones have absolutely no negative side

effects.

The cholesterol-reducing effect is important for anyone who’s inter-

ested in keeping a healthy cardiovascular system—especially those

who use steroidal compounds. Anabolic/androgenic steroids increase

not only total cholesterol but also the ratio of LDL to HDL.

It’s hard to imagine a compound that beneficial having any more ben-

efits, but guggulsterones have also been proven as effective as the drug

tetracycline in treating acne. In a 1994 study published in the Journal of

Dermatology , 20 patients with nodulocystic acne were randomly given

either tetracycline or guggulsterones. Both were taken daily for three

months, and both produced a progressive reduction in the lesions in the

majority of the patients. Tetracycline reduced them by 65.2 percent,

while the guggulsterones produced a 68 percent reduction.

Who can benefit from guggul’s effects? Well, who wouldn’t like a

better complexion? That’s especially true for people on anabolic/andro-

genic steroids, as those drugs tend to increase the skin’s oiliness and po-

tential for acne.

Where else can you find a compound that will help you lose fat, im-

prove your cholesterol profile and at the same time improve your com-

plexion? I’ve

looked long and

hard and have yet

to find even one

competitor. You

should take 30 to

60 milligrams three

times per day with

meals, and always

use a product that

contains the high-

potency, naturally

extracted guggul.

Editor’s note:

Derek Cornelius is

a respected bio -

chemist and the

owner of Syntrax

Innovations Inc.

Adipokinetix: Faster Fat Burning

T h rough Biochemistry

Adipokinetix is a supplement that mobilizes and burns

fat tissue without sacrificing muscle and organ tissue. You

should be familiar with the ECA stack—a combination of

ephedrine, caffeine and aspirin. Adipokinetix is similar to

ECA but is a vast improvement. It takes fat mobilization

and burning to a new level. Adipokinetix contains precise

ratios of 1R,2S norephedrine HCl, caffeine, yohimbine HCl

and now 50 milligrams of theophylline. The aspirin is left

out because some people are sensitive to

it. Furthermore, aspirin is cheap, easy to

get and can be easily added to the stack

if you can tolerate it.

The first two compounds—1R,2S

norephedrine and caffeine—work to-

gether in much the same way ephedrine

and caffeine work. The difference is that

studies have shown norephedrine to be

the most potent and most thermogenic

of the ephedrine alkaloids.

Norephedrine also lacks some of the

central-nervous-system-stimulating ef-

fects of ephedrine. In practical terms

that means an individual will still feel a

little wired but not nearly as much as he

or she will feel with ephedrine. Another

plus for norephedrine is that it doesn’t

have the negative associations that

ephedrine has—there are no Food and Drug Administr a-

tion restrictions and no negative publicity. In the coming

years norephedrine will definitely be the compound of

choice for easy, effective weight loss—instead of the ECA

stack, you’ll hear about the NCA stack.

Norephedrine and caffeine work synergistically to drasti-

cally increase the body’s production of adrenaline and no-

radrenaline—the adrenergic hormones—which bind to the

adrenergic receptors. There are a number of different

adrenergic receptors: the alpha sub 1, alpha sub 2, beta sub

1, beta sub 2 and beta sub 3. We are mainly interested in the

alpha-sub-2, beta-sub-2 and beta-sub-3 receptors—for

they’re the ones that mainly affect fat loss and mobiliza-

tion.

Among other things, the beta-sub-2 and beta-sub-3 re-

ceptors are responsible for the mobilization and burning of

adipose tissue; so they are the receptors that you want to

stimulate, for they ultimately affect fat loss in a positive

way. Another positive benefit of stimulating the beta-sub-2

receptors is an anticatabolic effect on proteinaceous tis-

sues. Thus, you simultaneously lose fat without sacrificing

much or any muscle tissue.

The other receptor that we’re interested in is the alpha-

sub-2 receptor. Studies have shown that it blocks the mobi-

lization of adipose tissue. In terms of fat loss it’s the bad

guy. In fact, it’s the receptor that causes

women to have a harder time losing adi-

pose tissue—especially in their lower bod-

ies. Women have many more alpha-sub-2

receptors than men, and they have an

even greater number in their lower bodies.

To combat those nasty receptors, we need

a compound that’s naturally occurring,

easy to get, potent, lacking negative side

effects and able to block them. Yohimbine

is the answer.

Yohimbine does all of the above with an

added bonus—it’s a proven aphrodisiac.

Thus, with Adipokinetix you can lose fat,

preserve muscle tissue and at the same

time increase your sex drive—regardless

of your gender. Both men and women

benefit. Yohimbine vastly improves the ef-

fectiveness of the norephedrine and the

caffeine by allowing the increased adrenergic hormones to

do their job. Basically, it cripples your body’s negative feed-

back loop for maintaining your bodyfat.

The new formula also includes 50 milligrams of theo-

phylline per capsule. The interesting thing about theo-

phylline is its potent diuretic effect. When it’s used in

combination with an ephedrine alkaloid, a dual leaning ef-

fect ensues—you burn excess bodyfat and eliminate excess

fluid, reducing fluid retention.

Currently, there’s no other product on the market like

Adipokinetix. I t’s unique and destined to be the future of

fat-loss pills.

—Derek Cornelius

Editor’s note: Adipokinetix is available from Home Gym

Warehouse, 1-800-447-0008.

124 Bodybuilding Supplement Guide

Bodybuilding Supplement Guide 125

Boost Your Stagnant Metabolism

by Daniel Gwartney, M.D.

vent a decrease in T3 and an increase in resting metabolism in subjects

who are on low-energy diets. 7 That, in addition to phosphates’ positive

effects on creatine storage, buffering lactic acid and increasing ATP,

firmly establishes the value of including phosphates in Thyro Stak.

The product contains niacin, selenium and magnesium. Niacin plays

a role in supporting the co-factors necessary for energy production,

such as NAD(H) and NADP(H). More than 200 enzymes require NAD

and NADP. NAD is involved in energy production, while NADP(H) is

If you aren’t

bringing in

enough

calories, your

body turns its

thermostat

down and

you burn

fewer

calories. It

makes sense,

especially if

you think of

long-term

survival.

main goals—and possibly the most

frustrating. After long periods of diet-

ing you often hit a plateau. What hap-

pens when fat loss comes to a

screeching halt? You redouble your efforts. You

fumble around with your diet, supplements, cardio

and so on, trying to increase your caloric expendi-

ture and metabolic rate.

Despite the best intentions, however, many of

those efforts are self-defeating. People who are try-

ing to lose weight often experience a decrease in

basal metabolic rate, or BMR, which is the number

of calories you burn at rest. The frustrating part is

that it happens following long periods of low-calo-

rie dieting; stimulant use, including ephedra and

caffeine; and excessive physical activity. Do any of

those scenarios sound familiar?

The decrease in BMR is directly related to the

level of thyroid hormone activity, which refers to

the levels of two hormones released by the thyroid

gland, thyroxine, or T4, and triiodothyronine, or

T3. T4 is a low-activity thyroid hormone, and T3 is

a highly active one. The overall thyroid hormone

activity involves the total amount of thyroid hor-

mones and their relative proportions. Optimal thy-

roid activity depends on necessary levels of the

hormones and the rate of conversion of T4 to T3.

Most thyroid hormone is released in the form of

T4 and needs to be converted to T3, a process that

takes place in the liver and is regulated by caloric

intake, rather than caloric expenditure. In simple

terms, if you are bringing in lots of fuel—i.e.,

food—you can turn up the heat, literally and figu-

ratively. If, however, you aren’t bringing in enough

calories, your body turns its thermostat down and

you burn fewer calories. It makes sense, especially

if you think of long-term survival.

So what can you do? Some advances have been

made in terms of useful training methods and sup-

plements. You can do your cardiovascular work

first thing in the morning, possibly after consum-

ing 200 to 400 milligrams of caffeine, along with

plenty of water. Unfortunately, some of the effec-

tive thermogenic supplements have been taken off

the market. The ECA (ephedrine, caffeine, aspirin)

combinations provided good results for many peo-

ple, but some people abused them. Most of the

other so-called fat-burners lack much promise.

Some products have been shown to be effective,

including essential fatty acids, soy-protein isolates

and the use of low-glycemic-index carbohydrates.

New, theoretically thermogenic combinations are

being introduced almost daily, including such

agents as yohimbine, tyrosine and phenylalanine.

Typically, they are added to ECA or a chemically

related compound like synephrine or pseu-

doephedrine, so we may end up seeing the same

problems.

All of those products, with the exception of soy-

protein isolates, interfere with thyroid activity.

That fact led to the development of Thyro Stak. It

includes five ingredients that have been shown to

support or enhance thyroid activity even in low-

calorie environments.

The main ingredient is an herb that has received

little attention in Western medicine, though it’s

been used in Ayurvedic medicine for many cen-

turies. Commiphora mukul contains a class of ac-

tive compounds known as guggulsterones, 1,2,3,4,5,6

and, while there isn’t a great deal of published re-

search on the compounds, what there is indicates

that guggulsterones, specifically guggulsterones Z

and E, have thyroid-stimulating activity. 5,6 Subjects

in those studies showed an increase in thyroid hor-

mone levels and an increase in the conversion of

T4 to T3. They showed lower cholesterol and

blood triglyceride levels as well, further indicating

increased thyroid activity.

Thyro Stak also contains phosphates, which are

found in such high-energy compounds as ATP and

phosphocreatine. Thyroid activity is closely linked

to the amount of energy you have, so it’s a good

idea for everyone to take an ample amount of phos-

phates daily. Numerous studies have shown the ef -

fect of phosphate supplementation on metabolic

rate. Of particular interest is a study published in

1996, which demonstrated that phosphates can pre-

Daniel Gwartney, M.D.

126 Bodybuilding Supplement Guide

Bodybuilding Supplement Guide 127

L osing bodyfat is one of a bodybuilder’s

Thyroid

activity is

closely linked

to the

amount of

energy you

have, so it’s a

good idea for

everyone to

take an

ample

amount of

phosphates

daily.

used in a variety of processes, including fatty acid synthesis, glutamate

oxidation and antioxidant activity. Niacin has also been shown to de-

crease cholesterol levels. Some people are sensitive to the flushing ef-

fect of high doses of niacin, but the effect is short-lived, and it’s

possible to build up a tolerance with continued usage.

Selenium is a mineral that has received a great deal of attention in re-

cent years. Selenium appears to have a major regulatory impact on the

enzyme 5’-deiodinase, which converts T4 to T3. 9 Low levels of seleni-

um can impair thyroid conversion—but excess selenium also has a neg-

ative effect on thyroid conversion.

Magnesium is present in more than 300 identified enzymatic reac-

tions. 10 It’s involved in glycolysis, the Krebs cycle and creatine phos-

phate production, among others. Magnesium even has a role in protein

synthesis. Subjects in a 1992 study showed increases in strength and

lean body mass after a few weeks of increasing their magnesium in-

take. 11

There are a lot of valuable products available to bodybuilders these

days. Thyro Stak is the first supplement designed to optimize thyroid

function and metabolic control, and, as such, it can be help you break

through those maddening diet plateaus.

Magnesium

even has a

role in protein

synthesis.

Subjects in a

1992 study

showed

increases in

strength and

lean body

mass after a

few weeks of

increasing

their

magnesium

intake.

References

1 Griffin, J., and Ojeda, S. Textbook of Endocrine Physiology , 3rd. ed.

New York: Oxford University Press. 1996

2 Nityanand, S., et al. (1989). Clinical trials with gugulipid. A new hy-

polipidaemic agent. J Assoc Physicians India . 37.5:323-328.

3 Gopal, K., et al. (1986). Clinical trials of ethyl acetate extract of

gum gugulu (gugulipid) in primary hyperlipidemia. J Assoc Physicians

India . 34.4:249-251.

4 Agarwal, R., et al. (1986). Clinical trials of gugulipid—a new hy-

polipidemic agent of plant origin in primary hyperlipidemia. Indian J

Med Res . 84:626-634.

5 Tripathi, Y.B., et al. (1984). Thyroid stimulating action of Z-guggul-

sterone obtained from Commiphora mukul. Planta Med. Feb(1):78-80.

6 Tripathi, Y.B., et al. (1988). Thyroid stimulating action of Z-guggul-

sterone: mechanism of action. Planta Med. 54(4):271-277.

7 Nazar, K., et al. (1996). Phosphate supplementation prevents a de-

crease of triiodothyronine and increases resting metabolic rate during

low-energy diet. J Physiol Pharmacol. 47.2:373-383.

8 Kohrie, J. (1994). Thyroid hormone deiodination in target tissues—a

regulatory role for the trace element selenium? Exp Clin Endocrinol.

102.2:63-89.

9 Englisch, R., et al. (1995). Induction of glucose transport into rat

muscle by selenate and selenite: comparison to insulin. Diabetologia.

38.1(suppl):A133.

10 Shils, M.E.; Olson, J.A.; and Shuke, M. Modern Nutrition in Health

and Disease , 8th ed. Philadelphia: Lea and Febiger. 1994. 164-184.

11 Brilla, L.R., and Haley, T.F. (1992). Effect of magnesium supple-

mentation on strength training in humans. J Amer Col Nutr. 11.3.

128 Bodybuilding Supplement Guide

Bodybuilding Supplement Guide 129

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