Thermogenic Ingredients and Weight

If, as it is said, age is just a number, then what is weight? An accusation? A badge of shame? A death sentence? Well, maybe not those, but certainly a warning.

More than one-third of the U.S. population is carrying around extra weight, and this increases the risk of a long list of ailments, including hypertension, heart disease, stroke, diabetes, arthritis, gallbladder disease, sleep apnea, and even endometrial, breast, and colon cancers. These risk factors make it critical that people try to control their weight.

Financial Considerations

Financial consequences are also being felt, says Jayant Deshpande, PhD, chief technology officer for OmniActive Health Technologies (Morristown, NJ). He references a 2012 study published by the American Journal of Preventive Medicine in which a research team, led by Eric Finkelstein, PhD, estimated that medical costs associated with treating obesity will rise from $48 billion currently to $66 billion by 2030. At that time, the scientists indicated that 42% of adults will be obese, and the loss in economic productivity may reach $580 billion. Thinking internationally, Deshpande adds, “Obesity has become such a worldwide phenomenon that the World Health Organization (WHO) coined the phrase ‘globesity’ to describe the recent boom in obese and morbidly obese people.”

At Chemi Nutra (White Bear Lake, MN), business development and marketing manager Chase Hagerman points to a Nielsen study that found “60% of the world’s population is struggling with their weight-50% with overweight [and] 10% with underweight issues.” The study reveals that 46% of respondents are choosing to cut down on portions in an attempt to control weight. But if past experience is any guide, counting calories isn’t enough.

Hagerman calls attention to other research, conducted by Marketdata Enterprises, which set the total 2012 U.S. weight-loss market-including not just supplements, but foods, pharmaceuticals, diet “clubs” such as Weight Watchers, and exercise facilities-at $61.1 billion. This year, the value is expected to increase another 2.6% and reach nearly $63 billion.

Statistics like these add up to opportunity for suppliers of nutraceutical ingredients. Citing a report in Nutrition Business JournaI, Scott Steil, president of Nutra Bridge (Shoreview, MN), says, “The 2012 U.S. weight-loss supplement market was estimated at $1.8 billion with a growth rate of 10.4% versus 2011. This makes it one of the fastest-growing categories in the supplement market and continues to drive interest and new product development.”

Supplement ingredient suppliers are responding, and they are usually taking one of three alternative approaches to weight control-accelerating fat burning, also known as thermogenesis, increasing satiety, or lowering glycemic response.

Thermogenesis

Bob Green, president of Nutratech Inc. (West Caldwell, NJ), the supplier of the ingredient Advantra Z, describes thermogenesis as the “production of heat in the body, increasing the resting metabolic rate and the rate at which fat is released from body stores and broken down (lipolysis) to help burn calories and produce more energy.”

Green cites recent research supporting the safety and efficacy of Advantra Z, which is made from Citrus aurantium, more commonly known as bitter orange.

According to Green, a study by Hector Lopez Jr., MD, a board-certified specialist in physical medicine and rehabilitation, found no “adverse effects (of bitter orange) at a dose of up to 98 mg daily.” At the same time, the researchers said, “Significant beneficial changes were observed in body composition-body weight, fat mass, lean mass, waist and hip measurements-as well as energy levels and food cravings.” The bitter orange study was published this past May in Food and Chemistry Toxicology.

Last year alone, says Steil, sales of 7-Keto, a non-stimulant, thermogenic fat burner developed by Humanetics Corp. (Minneapolis) and distributed by Nutra Bridge, grew over 300%. Steil says this strong showing is a result of “solid media exposure and the fact that our clinical trial pedigree is industry-leading.” He cites multiple clinical studies showing that the ingredient, sourced from plants, produces 200% greater weight loss than placebo. According to Steil, this translated into an average additional 5 lbs of weight loss above that produced by diet and exercise alone. And, he stresses, “The majority of the weight loss was pure body fat.”

Hagerman says Chemi Nutra has a novel weight management ingredient called PhosphoLean N-Oleoyl-PE + EGCG (NOPE+EGCG) that comes at weight control from two directions-satiety and thermogenesis. According to Hagerman, when PhosphoLean is taken, it makes its way into the intestinal tract, where Oleoyl ethanolamine (OEA), a lipid messenger involved in feeding regulation, is liberated. The OEA binds to a cell receptor that is responsible for signaling the brain center to decrease appetite.

In addition, he says, “The EGCG (epigallocatechin gallate) polyphenols in PhosphoLean act synergistically with OEA via sympathetic activation of thermogenesis and increased fat oxidation, thus enhancing the compound’s weight-management effects.” By signaling the brain to switch off sensations of hunger and switch on feelings of satiety, this compound may help people stay on their diets. “Without some kind of help, a staggering one out of three people drop off their diets in the crucial first five to seven days,” says Hagerman.

At Pharmachem Laboratories (Kearny, NJ), Mitch Skop, the senior director of new product development, says Teavigo green tea extracts boasting a minimum of 94% pure EGCG are the most important thermogenic offerings. He says there are numerous scientific studies showing that green tea extracts enhance metabolism, increase fat oxidation, and help assist in the reduction of body fat.

In a very recent study, published in the August 2013 issue of Modern Endocrinology, a magazine published by The Endocrine Society, Stanford University researchers Peter J. Malloy and Brian J. Feldman discussed the difference between white adipose tissue and brown adipose tissue. They indicated that the former stores energy in the form of lipids, while the latter expends energy via uncoupled fatty acid oxidation, which leads to the generation of heat.

According to Malloy and Feldman, “Obesity reflects an imbalance between energy storage and energy expenditure and is strongly associated with metabolic and cardiovascular disease. Therefore, there are important medical and biological implications for elucidating the mechanisms that promote energy expenditure in humans.”

Working with human patient samples from individuals with hereditary vitamin D-resistant rickets, the scientists noted that the vitamin D receptor (VDR) directly inhibits the expression of a protein needed for uncoupling fatty acid oxidation in brown fat and burning of energy. Deletion of VDR increases expression of this protein, known as UCP-1, and results in a “browning” of adipocytes.

“Importantly,” said Malloy and Feldman, “we found that this process occurs cell-autonomously and is independent of the physiologic VDR hormone ligand, 1,25-dihydroxyvitamin D. These results identify a mechanism for modulating energy balance in humans.”

Commenting on the study, Skop says, “We believe this study is important in how it reveals biochemical actions that impact healthy thermogenesis. Thermogenesis, to us, is more than just a sexy marketing word. It is the critical essence of how each individual is able to live a healthy life through optimum sustained energy formed by calories consumed and utilized.”

Mangosteen and Pepper

InterHealth Nutraceuticals (Benicia, CA) has two thermogenic items on its ingredients menu: Meratrim and Super CitriMax. InterHealth CEO Paul Dijkstra says Meratrim, sourced from Sphaeranthus indicus flower heads and mangosteen (Garcinia mangostana) fruit rind, can play “a key role in adjusting the way the body forms fat cells and how it breaks down the fat to promote healthy weight loss.”

Dijkstra says study findings published earlier this year by both Obesity and the Journal of Medicinal Food affirm that “Meratrim supplementation for eight weeks resulted in a statistically significant increase in adiponectin levels compared with placebo. It has been shown that the circulating levels of this hormone are inversely proportional to the amount of body visceral fat. These results suggest that Meratrim may influence lipid metabolism, which is consistent with the reduction in waist circumference also seen with Meratrim.”

According to Dijkstra, both studies featured randomized, double-blind, placebo-controlled methodology. On average, he reports, the Meratrim group lost around 11 lbs over eight weeks while the control group only lost around 4 lbs. In addition, the Meratrim group also shaved away 4.75 inches around the waist as opposed to the placebo group’s 2.5 inches.

Dijkstra describes Super CitriMax as an extract from the South Asian fruit Garcinia cambogia that is bound to essential minerals calcium and potassium, and that also supplies hydroxycitric acid (HCA).

In one randomized placebo-controlled study, Dijkstra says the ingredient, taken in beverages for two weeks, significantly decreased daily energy intake by 25% and calories from snacking by 40% compared to placebo. This, in turn, led to reduced body weight.

Sabinsa Corporation (East Windsor, NJ) has a product lineup that features seven weight-control ingredients, says Anurag Pande, PhD, Sabinsa vice president of scientific affairs.

Derived from Garcinia fruit rinds, Citrin comes in three different versions: regular, branded hydroxycitric acid extracts; water-soluble Citrin K; and GarCitrin, containing 5% garcinol, a natural histone acetyltransferase inhibitor, and 50% HCA. According to Pande, the hydroxycitric acid competes with citrate produced in the Krebs cycle to inhibit the synthesis of precursors of fatty acids, thus limiting the formation of new fat.

Pande also says the company’s ForsLean is a direct activator for adenylate cyclase, which is involved in the generation of cAMP (cyclic adenosine mono phosphate), bypassing the adrenergic receptors. An increase in cAMP leads to activation of hormone-sensitive lipase, and this may contribute to the increase in the metabolic rate and thermogenesis, he adds.

But Pande identifies Capsallyl as Sabinsa’s newest entry in this sector. As a thermogenic product that contains beadlets of capsaicin (the active component of chili peppers), Pande says the ingredient “causes the shift in oxidation from carbohydrate to fat, thus creating a fat-burning effect.”

Capsimax, also featuring capsaicin in beadlets, is OmniActive’s leading thermogenetic ingredient, says Jayante Deshpande at OmniActive. He says that while “immense potential” exists for manufacturers to incorporate capsicum and its active capsaicinoids into dietary supplement formulations, some companies are reluctant to do so. Difficulties may occur during formulation and production because individuals exposed to airborne capsaicin-rich particulates may experience varying degrees of physical discomfort and burning, he explains.

Thanks to its patented OmniBead technology, Deshpande says, OmniActive is able to minimize the negative side effects. “Each beadlet provides a standard dosage of capsaicinoids and is designed with high density and superior flow characteristics to facilitate safe and easy handling in high-speed tablet and capsule lines,” he says. “A novel food-grade surface coating envelops the capsaicinoid-rich particles, ensuring minimal irritation in the course of normal product handling during manufacturing.”

Conjugated Linoleic Acid

Laura Troha, industry marketing manager at BASF Nutrition & Health (Florham Park, NJ), says 18 human clinical studies show that her firm’s Tonalin conjugated linoleic acid (CLA) ingredient is effective in body shaping, reducing body fat in the legs, waist, and stomach.

Troha says the ingredient helps maintain lean muscle mass by decreasing muscle protein breakdown. “With more lean muscle mass,” she explains, “you increase your metabolism and burn more calories.”

For support, Troha cites a 2011 study, published in the Journal of the American College of Nutrition. In that trial, a team led by researcher Maria Pfeuffer determined that CLA decreased body weight and did not impair endothelial function, compared with safflower oil, in 85 overweight and obese men aged 45 to 68.

L-Carnitine

Kevin Owen PhD, North American head of technical marketing and scientific affairs at Lonza (Allendale, NJ), describes his company’s Carnipure ingredient as a “premium grade of L-carnitine.”

Owen says there is plenty of documentation that, in order to lose weight, energy expenditure has to be greater than energy intake. “As fatty acids enter the mitochondria to be processed, they are transported via L-carnitine,” he says. “Without L-carnitine, long-chain fatty acids are not broken down by the mitochondria for energy expenditure. Therefore, Carnipure L-carnitine can play an important role as part of a weight-loss program that includes energy restriction and exercise.”

The Lonza executive cites a pilot study published in the February 2013 issue of Food and Nutrition Sciences. The study, conducted by the Japanese clinical research organization Souken, examined how a low dose of Carnipure tartrate L-carnitine affected weight management and energy metabolism in overweight but otherwise healthy human subjects. According to Owen, only subjects in the group receiving a combination of Carnipure and motivation training, showed a statistically significant reduction in body weight after the four-week supplementation period. Owen says there were no significant changes in body weight in any of the other groups. In addition, the supplemented group showed the largest decrease in blood triglyceride levels among all the groups.

Other Approaches

As indicated above, ingredients aimed at increasing satiety and/or lowering glycemic response are also important parts of the weight-control puzzle.

Amélie Pinot, a health platform expert with DuPont Nutrition & Health (Paris), identifies Litesse polydextrose soluble fiber and Xivia xylitol as two of her company’s leading products aimed at achieving these goals.

Pinot cites a number of studies dating all the way back to 1998, showing that food volume, caloric density, and glycemic response all have a measurable impact on satiety.

Today, she says, the latest science on weight management is related to the potential role that gut microbiota may play on weight management and metabolism.

In 2011, says Pinot, Jacques Amar and a team from the Rangueil Hospital in France reported that, even before the onset of diabetes, “after only one week of a high-fat diet, live commensal intestinal bacteria are present in large numbers in the adipose tissue and the blood, where they can induce inflammation.”

The researchers went on to say, however, that this “bacterial translocation process from intestine towards tissue can be reversed by six weeks of treatment with the probiotic strain Bifidobacterium animalis subsp. lactis 420, which improves the [subjects’] overall inflammatory and metabolic status.”

Alex Fink, marketing director for Kemin Health LC (Des Moines, IA), points to Slendesta, a natural protein called Proteinase Inhibitor II (P12), as his company’s leading ingredient for weight control. “This protein is found under the skin of the potato, and it works by enhancing the body’s release of cholecystokinin (CCK),” he says. “This is a natural factor used by the body to signal the brain that food has been eaten, which helps to create feelings of fullness and
satisfaction.”

Earlier this year, Kemin locked horns with the European Food Safety Authority (EFSA) when that body declared there was insufficient scientific substantiation to allow a weight-reduction health claim for Slendesta.

Kemin responded immediately, claiming “a significant body of evidence supporting that Slendesta potato extract contributes to weight loss in overweight individuals.” The company noted that it had submitted proprietary data, including four unpublished, pertinent human studies on weight loss, one unpublished meta-analysis, and 12 supportive published and unpublished human intervention trials-all testifying to the effects of the ingredient on gastric emptying, post-prandial blood glucose concentrations and increases in satiety measurements and cholecystokinin concentrations.

“Notably, EFSA’s negative opinion only addresses the proposed health claims that can be made on labeling of finished products in Europe and does not impact the ingredient’s regulatory status,” said the company. “Slendesta retains its status as a lawful and non-novel food ingredient that can continue to be used by our customers in their food supplements and conventional foods.”

Deanne Dolnick, vice president of Next Pharmaceuticals (Salinas, CA), says her firm’s ingredient Relora, a proprietary raw material derived from a blend of Magnolia officinalis and Phellodendron amurense, “helps curb stress-related eating while lessening cravings for sweet and salty snacks.”

According to Dolnick, Relora works by helping to balance hormones while targeting specific neurotransmitters that effect stress and anxiety. “It helps to calm the HPA (hypothalamic-pituitary-adrenal) axis thereby decreasing the secretion of cortisol,” she says.

Summing up, Dolnick sees clear skies ahead for the marketplace potential of not only her company’s product, but all weight-control ingredients, thermogenic or otherwise. “As long as we have this level of obesity,” says Dolnick, “the category will continue to grow.”