Supplement Edge - The Most Effective Supplements for Fat Loss

Obesity results from an excess of energy intake over energy expenditure. So, if the obese individual wants to shred extra lard, the solution is extremely simple: Energy expenditure must exceed energy intake for a suitable length of time. Obviously, this message is simple only in principle, but very difficult to put into practice. Indeed, more than half of the adult American population must now be classified as overweight or obese.

Thus, it’s not surprising the market is flooded with hundreds of products that promise to shed extra lard quickly and easily. Unfortunately, it’s not easy to find objective information on these products. Even articles found in the various sports magazines that support the use of herbals and dietary supplements for fat loss are often commercially biased.

With that said, this article reviews the scientific rationale behind the most popular thermogenic (fat-burning) supplements.

Thermogenesis and Extra Lard: A Short Course

There are two types of fat tissue: white fat tissue and brown fat tissue. When we talk about body fat, we refer to white fat tissue (i.e., lard). White fat tissue has a number of functions in the body that include mechanical cushioning (e.g., around some internal organs) and thermal insulation, but its main role is that of storing food energy in the form of triglycerides and releasing it in the form of free fatty acids when it’s needed by other tissues.

However, brown fat tissue has a unique metabolic feature.

Not all the energy in foods is transferred to adenosine triphosphate (ATP; the universal energy carrier in each cell). Instead, a portion of this energy becomes heat. On average, 35 percent of the energy in foods becomes heat during ATP formation. However, in brown fat, sympathetic nervous stimulation (“fight-or-flight” response) causes liberation of large amounts of heat. Brown fat tissue is the major site of heat production (thermogenesis) in the newborn and is especially prominent in the mammalian fetus. The largest accumulation of brown fat tissue envelops the kidneys and adrenal glands. The mass of brown fat tissue peaks at birth and gradually decreases during the early weeks of life.

Brown fat contains a large number of mitochondria (powerhouses of the cell) and many small globules of fat instead of one large fat globule. In these cells, the process of oxidative phosphorylation (formation of ATP by using energy derived from an electron transport to oxygen) in the mitochondria is mainly “uncoupled.” That is, when the cells are stimulated by the sympathetic nerves, the mitochondria produce a large amount of heat but almost no ATP. Therefore, almost all the released oxidative energy immediately becomes heat. The important bottom line is that radiating energy away as heat enables the body to spend, rather than store, energy.

Since the process of uncoupling dissipates metabolic energy, there has been great interest in this process in relation to regulation of body weight: If we could stimulate uncoupling, it would be a wonderful way to burn extra lard. Indeed, a possible link between obesity and deficient brown fat function has been researched. For example, evidence indicates that thermogenesis is defective in instances of obesity.

Two types of external stimuli trigger thermogenesis: 1) the ingestion of food and 2) prolonged exposure to cold temperature, both of which stimulate the tissue via sympathetic innervation via the hormone norepinephrine (noradrenaline). The sympathetic signals increase the size of brown fat tissue. (For a more detailed review on brown fat tissue and thermogenesis, see reference #3).

How Do Scientists Determine the Effectiveness of Thermogenic Supplements?

The gold standard in scientific research design is a prospective, double-blind, randomized, placebo-controlled clinical study. Simply stated, subjects are randomized to either treatment (thermogenic supplementation) or a control group (fake supplementation) and followed from that point.

Obviously, the metabolic rate (i.e., energy expenditure) must be measured. There are two basic approaches. First, scientists can measure directly the heat liberated by the body (direct calorimetry). However, that requires sophisticated equipment, so the alternative approach is that of indirect calorimetry. In this approach, energy expenditure is assessed from measurement of the burning of fuels, which are in turn assessed from the whole-body consumption of oxygen and production of carbon dioxide. An indirect calorimeter can be constructed in the form of a room in which a subject may live a relatively normal life.

If you are still awake, it’s finally time to examine the rationale behind the thermogenic supplements.

Ephedrine Caffeine: Most Popular Thermogenic Stack

Clearly, ephedrine is— or at least was— the most popular thermogenic supplement known to mankind. Ephedrine is classified as a sympathomimetic drug and central nervous system stimulant. In most dietary supplements, ephedrine used to appear as an extract from one of two herbs: ephedra or Ma Huang.

Although ephedra species have a long tradition of use (more than 5,000 years) for respiratory ailments, the FDA recently decided to ban ephedra-containing supplements. The pharmacokinetics (i.e., the characteristic interactions of a drug and the body in terms of its absorption, distribution, metabolism and excretion) of ephedrine following ingestion of supplements formulated as concentrated ephedra extracts is distinguishable from that of synthetic ephedrine found in conventional dosage forms. Nevertheless, the FDA did not ban ephedrine.

Ephedrine has also been coupled with both caffeine and aspirin to further enhance its effectiveness (i.e., ECA). Ephedrine stimulates release of

noradrenaline, which stimulates the synthesis of prostaglandins by the activated tissues. Aspirin inhibits the synthesis of prostaglandins and serves as a prostaglandin blocker, and thereby may prevent inhibition of norepinepherine release.

The history of ephedrine as a weight loss agent is rather interesting. In 1972, Dr. Erikson, a Danish general practitioner in Elsinore, Denmark, noted unintentional weight loss when he prescribed a compound containing ephedrine, caffeine and Phenobarbital to patients he was treating for asthma. By 1977, over 70,000 patients were taking the “Elsinore Pill,” and one Danish pharmaceutical house was producing one million tablets a week!

Early commercial ephedra-caffeine supplements were extremely popular among serious athletes simply because they worked and had few, if any, adverse effects when used as directed. Indeed, numerous well-controlled studies support this contention. For example, Dr. Boozer and colleagues at the New York Obesity Research Center reported that in a six-month placebo-controlled trial, ephedra plus caffeine promoted bodyweight and body fat reduction and improved blood lipids without significant adverse effects.

More recently, a new study by Dr. Greenway and co-workers at the Pennington Biomedical Research Center examined the effect of a supplement containing herbal caffeine and ephedrine on metabolic rate, weight loss, body composition and safety parameters. Results indicated that ephedra plus caffeine promoted more weight and fat loss than placebo (fake supplement) and was well tolerated. According to the authors, “Dietary herbal supplements containing [ephedra and caffeine] should remain available to obese individuals trying to control their weight.”

When it comes to purported adverse effects, Dr. Soni and co-workers concluded that the adverse event reports raise concerns about the risks associated with ephedra usage, but did not establish a direct causal relationship between intake of ephedra and reported injuries. They also pointed out that the published preclinical and clinical studies, and the long history of safe use of ephedra, support the safety-in-use of ephedra when used as directed. According to Dr. Soni et al., the problems associated with the adverse events appear to be the result of overuse, inconsistent potency, individual sensitivity, contaminations, etc.

In summary, ephedrine-caffeine supplementation promotes fat loss and is relatively safe when used as directed. However, ephedrine/ephedra is certainly not for everyone and must be used responsibly. For example, it should be never, under any circumstances, be used by someone with heart disease or high blood pressure. If you decide to use ephedrine/ephedra, it’s very important that you read product labels, warnings and cautions, and follow the directions.

Caffeine Nicotine: The Super Thermogenic Stack?

It’s well established that nicotine replacement therapy limits weight gain after smoking cessation. So, Dr. Anna Jessen and colleague at the Royal Veterinary and Agricultural University in Denmark examined the acute

thermogenic effects of chewing gum containing different doses of nicotine and caffeine. This well-controlled study included 12 healthy, normal-weight men. Energy expenditure was measured with indirect calorimetry before and 2.5 hours after subjects chewed the gum.

The results indicated that one milligram of nicotine has a pronounced thermogenic effect, which is increased by about 100 percent when it’s combined with 100 milligrams of caffeine. Further, no side effects were reported with the gum that contained one milligram of nicotine with 50 or 100 milligrams of caffeine. Nevertheless, if you want to give this stack a try, talk with your doctor first.

Capsiate: The Latest Thermogenic

The capsicum species, native to tropical America, incorporates such peppers as the cayenne, red and chili. Chili is the Aztec name for the cayenne pepper, and it has been used by Native Americans as food and medicine for over 9,000 years.²

The medicinal properties of capsicum are attributable to a compound known as capsaicin, although other capsaicinoids are also available. Capsaicin is regarded as a pain reliever, possibly blocking pain fiber by depleting substance P, the neurotransmitter mediating pain signals to the brain.

Further, capsaicin has been reported to 1) elevate body temperature; 2) stimulate the secretion of catecholamines (noradrenaline, adrenaline); 3) promote energy expenditure; and 4) suppress body fat accumulation in experimental animals. However, capsaicin is strongly pungent and neurotoxic, which largely prohibits its administration to humans.

Dr. S. Yazawa and co-workers reported that CH-19 Sweet, a non-pungent cultivar of Capsicum annuum L, rarely contains pungent capsaicinoids, but contains a large amount of two capsaicinoid-like substances. The chemical structures of these two substances have been identified and named capsiate and dihydrocapsiate by Dr. Kobata and colleagues.

Recently, Dr. Masuda Yoriko and colleagues from Japan examined whether continuous administration of capsiate promotes energy expenditure in mice.⁹ They measured respiratory gas by indirect calorimetry. Results indicated that oxygen consumption (i.e., energy expenditure) was significantly higher in the capsiate group than in the control group. Also, carbohydrate and fat burning was significantly higher in the capsiate group than in the control group. Consequently, the mean bodyweight of mice in the capsiate group was significantly lower than that of mice in the control group.

In summary, continuous administration of capsiate raises oxygen consumption, an index of energy expenditure, suggesting that capsiate-treated mice burned more calories. The authors of this study concluded: “This study suggests that capsiate, a non-pungent capsaicin analog, may be an alternative to capsaicin for the therapeutic treatment of obesity in humans.” However, well-controlled human studies are needed before firm conclusions can be drawn.