Thermogenic Ingredients for Dietary Supplements

At the core, the mechanics of keeping a healthy weight are simple: the number of calories in should equal the number of calories out. Thermogenesis is inherent to this equation.

A naturally occurring bodily function, thermogenesis works as such: as the body raises its energy output (temperature), metabolism increases-and calories are burned and fat cells utilized as an energy source. Lipolysis, the breakdown of fat before it can be burned, is also part of the process.

For research-oriented dietary supplement suppliers targeting thermogenesis, the goal is to provide a product that can safely encourage or increase the body’s own natural thermogenesis and support healthy metabolism. There are a number of ingredients offered to this end, as discussed ahead. (The following is a representative sampling of ingredients. Please consult Nutritional Outlook’s Nutra-Q online supplier database, www.NutritionalOutlook.com/Nutra-Q, for information on others.)

Decaffeinated Green Coffee Bean Extract

Svetol is a standardized decaffeinated green coffee bean extract (Coffea canephora) from Naturex (Avignon, France). It has been featured in weight-loss supplements to help increase the lean mass:fat mass ratio. A 2012 mouse study published in Nutritional Neuroscience (L Ho et al.) proclaims to have specifically uncovered Svetol’s affinity for a particular gene in the brain involved in the metabolic process. As such, “[Svetol] improves mitochondrial energy metabolism and influences the gene involved in metabolism,” summarizes Benjamin Voiry, business manager, NAT life, Naturex.

This recent discovery adds to Svetol’s two previously determined synergic mechanisms of action: decreasing intestinal glucose absorption and inhibiting the enzyme glucose-6-phosphatase, which would otherwise stimulate the liberation of glucose in the blood stream. Instead, as the liver releases less glucose, the body must rely on another source of energy-such as fat.

Additionally supporting Svetol’s weight-loss effects, in 2006, the ingredient was found to significantly help individuals trim up. Compared with placebo, supplementation with 400 mg of Svetol per day for 60 days increased weight loss by 5.7% and increased the lean mass:fat mass ratio by 4% (O Dellalibera et al.).

Green Tea Extract

Popularized in a memorable commercial as a way to “lose stubborn belly fat,” the active constituent in green tea, epigallocatechin gallate (EGCG), has long been shown to accelerate fat burning.

Studies show green tea can aid in boosting metabolism and fat oxidation. An additional boon? Consumers seem to be already somewhat familiar with the link between green tea consumption and health, including weight loss.

Among others, two crossover studies support the positive effects of green tea extract in encouraging fat oxidation and energy expenditure in healthy subjects.

The first crossover study was published in the American Journal of Clinical Nutrition in 2008. Study A tested 12 healthy men who performed 30 minutes of exercise at 60% maximal oxygen consumption before and after supplementation with either green tea extract or placebo. In study B, 11 healthy men took an oral glucose-tolerance test before and after supplementation. The studies revealed that average fat oxidation rates were 17% higher after ingestion of green tea extract than after ingestion of placebo. Moreover, the contribution of fat oxidation to total energy expenditure was also significantly higher, by a similar percentage, after green tea extract supplementation.

This study validates a 1999 study published in the American Journal of Clinical Nutrition (AG Dulloo et al.) on 10 male subjects to determine whether a green tea extract could increase energy expenditure and fat oxidation. On three separate occasions (breakfast, lunch, and dinner), subjects were randomly assigned one of three treatments: green tea extract (50 mg caffeine and 90 mg EGCG), caffeine (50 mg), and placebo. Green tea extract was shown to have thermogenic properties and promote fat oxidation “beyond that explained by its caffeine content per se,” wrote the study authors. They stated that green tea may play a role in the control of body composition via sympathetic activation of thermogenesis, fat oxidation, or both.

Pharmachem Laboratories’ (Kearny, NJ) patented Teavigo green tea extract is derived through a proprietary process that concentrates the benefits of fresh green tea leaves. This process, points out Mitch Skop, director new product development, ensures that Teavigo “is potent and pure,” with a minimum 90% EGCG. 

Chili Pepper

Philip Domenico, PhD, human nutrition scientist for OmniActive Health Technologies (Morristown, NJ), describes the pungent (hot) principal from chili pepper (Capsicum annuum) known as capsaicinoids as being “a preferred thermogenic agent, since it does not adversely affect metabolism or sleep.”

Capsaicinoids have been shown to increase thermogenesis. In a randomized, placebo-controlled, double-blind crossover study published in Lipids in Health and Disease in 2010, subjects ingesting 100 mg of OmniActive’s Capsimax ingredient (2 mg capsaicinoids) showed a significant increase in blood free fatty acids and glycerol (byproducts of lipolysis) at selected times post-ingestion.

Capsimax also produced increased blood catecholamine levels compared to placebo, indicating sympathetic nervous system stimulation. “Capsimax activates the sympathetic nervous system in a limited way, leading to increased secretion of catecholamines,” Domenico explains. “The extent of release of catecholamines is just adequate enough to cause lipolysis in adipose tissue.”

He emphasizes that Capsimax stimulates the sympathetic nervous system in a controlled fashion. “While controlled or limited activation of the sympathetic nervous system could be useful in causing lipolysis, over-activation is not desirable.”

Additionally, no difference was noted in heart rate or blood pressure between placebo and Capsimax, thus supporting its safety, he says.

Another more recent study published in the Journal of the Science of Food and Agriculture in 2011 showed that capsaicinoids help improve fat metabolism by reducing lipogenic enzyme activity and increasing hormone-sensitive lipase activity.

Domenico also observes that although a 2001 report in The Lancet supports an association between capsicum consumption and a lower incidence of obesity, many people can’t tolerate those doses shown to actually produce the desired effects. He says that by contrast, OmniActive’s Capsimax ingredient offers a better-tolerated approach because it encapsulates capsaicinoids in OmniBead beadlets to prevent capsicum from irritating the mouth and stomach.

Another company, Sabinsa Corp. (East Windsor, NJ), launched its Capsallyl ingredient in 2011. Capsallyl contains capsaicin and isothiocyanate from mustard oil, both of which are known to induce thermogenesis, says Anurag Pande, PhD, vice president of scientific affairs.

Pande explains that capsaicin from capsicum improves circulation and boosts metabolism, thus allowing the body to burn more calories. Interestingly, says Pande, several human studies found that capsaicin caused a shift in oxidation from carbohydrate to fat oxidation, which translates into a fat-burning effect.

Bitter Orange

Patented Advantra Z bitter orange extract (Citrus aurantium) and its dominant amine p-synephrine are supported by more than 30 studies showing safety, efficacy-and thermogenesis, says supplier Nutratech (West Caldwell, NJ).

Advantra Z works by increasing thermogenesis primarily by stimulating beta-3 receptors, which are responsible for triggering thermogenesis, the company explains. Moreover, company president Bob Green says that Advantra Z works without exerting negative cardiovascular and central nervous system side effects. The compound does not cross the fatty membranes of the blood-brain barrier because it isn’t very lipophilic, he says. Instead, it prefers retention in peripheral tissue rather than passing into the brain, where central nervous system side effects can occur.

The ingredient also makes minimal contact with alpha-1, -2 and beta-1, -2 (excitatory) receptors, which are responsible for negative cardiovascular side effects. “This is due to p-synephrine, a stable isomer of synephrine, which primarily stimulates beta-3 receptors that increase thermogenesis and lipolysis but does not affect blood pressure,” Green explains.

He also clarifies that p-synephrine should not be confused with m-synephrine, found in nasal decongestants and sprays, which does impact alpha, beta-1, and beta-2 receptors, increasing blood pressure and heart rate.

Finally, Nutratech claims that there are efficacy differences between natural and synthetically derived p-synephrine. The company points to a paper by Sidney J. Stohs, PhD, dean emeritus of the School of Pharmacy and Health Professions, Creighton University Health Sciences Center in Omaha, NE. Stohs is a researcher in performance enhancing/weight management ingredients and has served as a consultant to Nutratech. In a paper published in the Journal of Functional Foods titled “Stereochemical and physiological differences between naturally occurring p-synephrine and synthetic p-synephrine,” Stohs et al. concluded that “The naturally occurring L-form of p-synephrine as is present in Advantra Z (Citrus aurantium extracts) will exhibit at least twice the physiological activity as compared to an equal weight of the synthetic dl mixture of p-synephrine.” The difference, they write, is due to receptor binding. “This difference occurs because the d- or[S-(+)]-form provides little or no binding to adrenergic receptors in contrast to the L-form.”

African Mango

According to Suzanne McNeary, president of ingredients supplier Icon Group LLC (Brattleboro, VT), African mango (Irvingia gabonensis) is effective at promoting thermogenesis via its ability to enhance the function of leptin. Leptin is a hormone produced by the fat cells of white and brown adipose tissue and is said to play a key role in regulating thermogenesis.

According to McNeary, those who are overweight or obese can develop “leptin resistance.” She explains that those individuals may develop increased inflammation via increased C-reactive protein levels. “Studies have shown that C-reactive protein can bind leptin, preventing it from crossing the blood-brain barrier, which reduces its ability to promote thermogenesis,” she says. Icon Group offers what it says is the industry’s sole patented, certified extract of Irvingia gabonensis, called WellTrim iG IGOB131.

A double-blind, placebo-controlled study on WellTrim iG IGOB131 published in Lipids in Health and Disease in 2009 showed that 102 healthy but overweight/obese individuals who took 150 mg of WellTrim iG 30 to 60 minutes before meals twice daily for 10 weeks showed significant improvements not only in body weight and fat but in leptin and adiponectin levels as well as a variety of parameters associated with metabolic syndrome.

Fucoxanthin

Fucoxanthin is a major marine carotenoid found in edible seaweeds such as Undaria pinnatifida, commonly known as wakame. In a study of obese mice, published in the International Journal of Molecular Medicine, fucoxanthin was shown to suppress weight gain of white adipose tissue. Researchers concluded, “Because most body fat is stored in white adipose tissue, decreasing white adipose tissue weight by fucoxanthin might be a very effective approach for preventing and/or alleviating obesity.”

“Fucoxanthin is thought to be a non-stimulant thermogenic, which means it has no effect on the sympathetic nervous system and can be taken without concerns of cardiovascular exhaustion or blood pressure deregulation,” explains Nichole De Block, marketing director for Nutraceuticals International Group (Paramus, NJ), which offers a highly concentrated 10% extract form of fucoxanthin called FucoPure.

Additionally, De Block adds, fucoxanthin extract may also play a role in breaking down fat that accumulates as a result of the body’s storing of unburned protein. By helping to break apart stored coupled proteins within fat cells, fucoxanthin may play a role in turning stored fat back into protein so that it can be used as energy.

7-Keto

7-Keto (3-acetyl-7-oxo-dehydroepiandrosterone) from Nutra Bridge (Shoreview, MN) is a patented, non-stimulant thermogenic ingredient that encourages the body to burn fat more efficiently by increasing the activity of key fat-burning enzymes, the company says.

7-Keto is naturally produced in the human body, but declines dramatically with age. Typically, a person loses about 50% of his/her endogenous 7-Keto levels by age 40, resulting in slower or compromised thermogenic ability. Nutra Bridge says that multiple clinical studies, such as one published in Current Therapeutic Research  in 2002, have shown that 7-Keto supplementation produces 200% greater weight loss than placebo (diet and exercise). This translated to an average additional five pounds of weight lost above that produced by diet and exercise alone. Additionally, the majority of the weight loss was pure body fat. A study published in the Journal of Nutritional Biochemistry in 2007 showed that 7-Keto also increases metabolism by 5.4% compared to placebo, which was a restricted-calorie diet.

Working Together

Some ingredients in combination may offer additional efficacy.

LeptiCore from Icon Group is a patent-pending complex of plant-based polysaccharides, esterified fatty acids, pomegranate extract, beta-carotene, and blue-green algae. According to the company, each ingredient has been clinically proven to reduce C-reactive protein and leptin levels in randomized, double-blind, placebo-controlled clinical trials. Like the company’s aforementioned WellTrim iG ingredient, by reducing serum C-reactive protein, LeptiCore’s ingredients allow leptin to more easily pass the blood-brain barrier and as a result encourage thermogenesis in the body.

LeanGard, Sabinsa’s proprietary blend of branded ingredients-ForsLean Coleus forskohlii, GarCitrin Garcinia cambogia, and BioPerine bioavailability-enhancing Piper nigrum-provides triple action: appetite suppressing, lipolysis, and thermogenesis. Pande describes this as a  “‘Break-Block-Burn’ synergy for managing weight.”

As Pande describes, ForsLean is a direct activator of the enzyme adenylate cyclase, which increases the rate of lipolysis in the adipose tissue and hence is able to accelerate fat breakdown. GarCitrin is a potent inhibitor of citrate lyase, which is implicated in formation of fat in the body. Hydroxy citric acid, present in GarCitrin, also accelerates fat oxidation or fat burning as well as suppresses appetite.

Adipromin from P.L. Thomas (Morristown, NJ) is a formulation of three food-grade herbs (Curcuma longa, Moringa oleifera, and Murraya koenigii) that the company says is clinically proven to inhibit excess adipose tissue formation while also enhancing the breakdown of fatty tissue for energy. Other benefits of this formulation are a positive impact on serum adiponectin, a protein hormone that regulates metabolic processes; and lowering serum ghrelin, an appetite-enhancing hormone.

Weight-Loss Marketing: REsponsible and Realistic

As long as consumers desire to lose weight, there will be a share of “predatory” bad actors seeking to take advantage of the supplements market. These outliers are seeing some enforcement action from the FTC. Earlier this year, the agency announced it had reached a $1.5 million settlement with an Internet company selling acai weight-loss products. The company was accused of making deceptive health claims, advertising fake celebrity product endorsements, and promoting false free-trial offers.

Suzanne McNeary, president of Icon Group LLC, observes that the weight-management category has always endured a higher level of scrutiny than other supplement categories. Responsible companies encourage action against those bad actors, whose unsubstantiated and irresponsible claims mar the integrity of the dietary supplements industry as a whole, including those suppliers and marketers who do market clinically efficacious ingredients. “A few bad apples can negatively impact the rest of us,” McNeary says. “Enforcement to remove unscrupulous weight-loss supplement marketers benefits the industry.”

Anurag Pande, PhD, vice president of scientific affairs for Sabinsa Corp., says that consumers are often “taken for a ride by promotional materials that promise the sky-and deliver little or nothing. Misinterpretation or hiding the facts, improper labeling of supplements, and lack of quality in manufacturing are not only harmful for the end-consumer but also to the industry. Hence, such activities should be ceased.”

Responsible suppliers will also help consumers realistically manage their own weight-loss expectations. Scott Steil, president of Nutra Bridge, believes that in 2012, the industry is far beyond the “If you build it, they will come” school of marketing. “Consumers are now very sophisticated. The first thing marketers of weight-management products must do is break the myth that there is a magic bullet out there for weight loss. To build consumer confidence-and thereby increase sales-our industry must take a responsible stance to weight management and get rid of bloated claims and single-magic-bullet theories. Nobody can sit on the sofa, eat potato chips, and lose weight by taking a supplement.” He and other respondents for this article validate that responsible weight-management marketing must clearly stress the essential complementary components of a healthy diet and exercise.

In addition, the concept of achieving healthy lean body mass is gaining traction over simple “weight loss,” according to Sabinsa’s Pande. Pande adds, “The uniqueness of the product is not in how quick it attains the weight loss; rather, how it helps to attain healthy weight, which is more sustainable.”

We can also now begin to clearly discern that one weight-loss product does not fit all. This is key when formulating, and specifically when marketing. Unlike other condition-specific categories-say, vision health-purchases of weight-control formulas are inspired by diverse personal desires and needs. McNeary sees two distinct consumers: the vanity-driven customer who wants to drop 10 pounds for bathing suit season, and the physician-directed consumer who needs to lose weight for health reasons (e.g., reducing blood pressure, dealing with potential diabetes). She notes that “the physician-directed weight-loss segment is larger than the vanity consumer market.”

Pande adds that there is also an attractive category for athletes who want to maintain their well being and physique.

Meanwhile, Nutra Bridge’s Steil sees three types of consumers in the weight-loss sector. Consumers who want to improve long-term health are committed to the long haul and well educated on the benefits that a long-term, multipronged supplementation plan offers. Good science, realistic claims, and education are essential to reaching this group.

“The second group,” he says, “comprises people who want to maximize results from a weight loss/diet program (average three months) and who are also interested in being educated.”

“The third group contains those who are seeking the magic bullet,” he concludes.

Keep in mind, though, that the expectations of many “magic bullet” consumers can be, and often are, converted-notably when they experience the failure of said bullet not working. Therefore, by continuing to emphasize a responsible and realistic message, the weight-control sector can indeed remain “large and in charge.”