Weight management ingredients : many actives at the forefront

The global weight management market shows strong year-over-year gains, reaching retail value sales of US $14 billion in 2013, with growth projected to continue through 2018 (Euromonitor International data).

The USA is by far the world’s largest weight management market, accounting for approximately one-third of global sales. A few years ago women were the main target of weight-management dietary supplements or functional foods, and more precisely, women aged 25 to 60. Today, with the global increase of overweight or obesity troubles, many people of all ages are interested in losing or maintaining weight: teenagers, adults, and seniors; males and females, etc.

The new and major trend of this growing market is that weight management is now even more aligned with global “health” management. People now take into consideration the fact that being overweight is not only a problem of physical appearance/external beauty, but is also generally linked to serious health problems (among others: cardiovascular, cholesterol, blood pressure, etc,). Ingredients should therefore not only target weight loss, but also offer holistic health features.

 

The French Company Fytexia has developed Sinetrol®, a patented polyphenolic compound mix – including flavonoids (naringin, narirutine, hesperidin…), anthocyanins (cyaniding, 3 glycoside) – extracts of Mediterranean citrus fruit: orange, blood orange and grapefruit. Sinetrol®’s mechanism of action has been studied: adipocyte lipolysis comes from phosphodiesterase inhibition. This results in a significantly higher release of free fatty acids than in the placebo. A double-blind 12-week study showed that 450mg of the XPur grade (more than 90% total polyphenols) consumed twice daily resulted in a significant decrease in abdominal, stomach and hip fat. Another effect: a decrease in the plasma markers of inflammation (CRP and fibrinogen). Another study on the EXP grade (60% polyphenols, 1.4 g/day) revealed, at the end of three months, a significant weight and body fat decrease.

This week, Fytexia announces the launch of a new concept : Fat Shredding Technology. As lipolysis is a catabolic process leading to the breakdown of triglycerides stored in fat cells.
Sinetrol acts through the exclusive mechanism of Fat Shredding Technology to enhance the release of free fatty acids from the adipocytes, leading to a reduction of the fat mass. A new investigation on human adipocytes demonstrates the exclusive mechanism of action from the patented combination of Sinetrol: proven polyphenol synergy.

Sinetrol’s powerful Fat Shredding Technology was proven to efficiently support body weight management in 2 published clinical studies involving 115 subjects.
Although slimming formulas can sometimes be quite obscure – namely with regard to the plants and extracts used, some players have committed to long-term approaches to validate their ingredients’ effects on weight management – by taking part in clinical trials. This approach relies on developing a marketing vision that leads to the creation of brands of ingredients. Following is a review of some of them.

Sabinsa Group was one of the first to propose a brand in the field of slimming ingredients. We are talking about ForsLean®, a Coleus Forskohlii extract launched over 15 years ago. Since then, many ingredients have been standing out through their brands: conjugated linoleic acid (CLA) (Clarinol® and Tonalin® brands from Lipid Nutrition and respectively BASF) is such an example, green coffee extracts(Svetol® from Naturex ), L-carnitine (Carnipure® from Lonza)…

What has led to the development of these brands? Their number is high. In very competitive markets, they are a means of distinguishing between different formulas, especially since in most cases the providers substantiate their brands with efficacy and/or consumer satisfaction studies. Finally, brand development allows communicating more easily with consumers – many of the brands have their own dedicated website.
The importance of chlorogenic acid

Svetol® is a natural extract of decaffeinated green coffee (Robusta) produced by Naturex based on an exclusive processing technology. Hence, its unique composition which provides the benefits of coffee and stimulates weight loss. Naturex controls the entire production chain, from sourcing to extraction, in a US factory registered with the FDA.

Unlike other green coffee extracts sold on the market which focus mainly on the total content of chlorogenic acids, thanks to its specific extraction process Naturex guarantees the production of a unique and balanced chlorogenic acid profile. Studies have shown that these compounds promote weight loss by slowing down the absorption of sugars in the blood and by increasing fat elimination.

SelectSIEVE® Apple PCQ from Principium /Engredea is extracted from apple juice through an eco-sustainable process based on soft conditions. It consists of three main polyphenols: phloridzin, chlorogenic acid and quercetin, which act in synergy according to various metabolic pathways. They are isolated from the fruit in their glycosylated form – which stands as proof of their naturalness and improves their stability, bioavailability and digestibility. Phlorizin is glucose inhibitor – it decreases absorption and thereby calories. The chlorogenic acid controls the release of glucose into the liver. Quercetin is an inhibitor of PPAR gene, which is responsible for the preadipocyte differentiation into adipocytes, thereby reducing fat accumulation.

Together, the SelectSIEVE® Apple PCQ components decrease the intestinal absorption of glucose by modulating SGLT1/GLUT, they regulate the gastrointestinal hormones in the liver and insulin secretion. Finally, they affect the preadipocyte differentiation into mature adipocytes. The dosages of SelectSIEVE® Apple PCQ in formulations vary depending on the product positioning: menopause – 150 mg/day; slimming – 180 mg/day; glycemic control – 250 mg/day.
Nexira offers three ingredients for weight loss, body shaping and decreased caloric intake. Historically, NeOpuntia™ has enabled the group to enter the slimming segment. This lipophilic fibre extracted from cactus leaves (nopal, Opuntia ficus indica) physically interacts with fat. A two-step action: hydrophobic interactions between fat and insoluble fibres; stabilization of these first interactions as the soluble fibres (polysaccharides) form a gel which remains stable in any pH. In vitro tests which simulate the gastrointestinal environment showed that NeOpuntia® reduces the bioavailability of fatty acids with about 28% and its lipohilic action is higher than that of chitosan. A pilot clinical study also suggests that 1.6g NeOpuntia® per meal increases fat excretion by 27% on average, as compared to placebo. Please note that a clinical study showed also that these soluble and insoluble fibres can balance blood lipid levels and reduce cardiovascular risk through its positive effects on HDL cholesterol. Hence, an important role in the regulation of certain parameters related to the metabolic syndrome (not only HDL, but also triglycerides). Also from the cactus, but this time from the fruit, Nexira extracts Cacti-Nea™. Two clinical studies were carried out. The first highlighted the draining effects: a positive effect on the body composition by limiting the fat intake, a significant reduction in body water, after a week of treatment, accompanied by positive effects on the figure, significant weight loss in the Cacti-Nea™ Group (up to -3.3 kg) – no effect in the placebo group; finally, unlike conventional diuretics, Cacti-Nea™ has no negative effect on blood pressure or on the mineral balance – as confirmed by an in vivo study on rats carried out in comparison with hydrochlorotiazide (reference diuretic substance).

Finally, Nexira developed ID-alG ™, a brown seaweed extract which offers a complete slimming action – high levels of polyphenols, minerals and trace elements of marine origin. Nexira showed that the polyphenols contained in ID-alG™ offered a unique slimming property by inhibiting two of the main digestive enzymes, and could therefore be involved in reducing the caloric intake. A preliminary in vitro trial showed that ID-alG™ could reduce the alpha-amylase and lipase activities by 50%. The slimming effect was confirmed by a clinical study on overweight women for a period of two months: weight loss of about 3 kg (corresponding to a body fat loss), thighs and firm buttocks. Finally, 76% of consumers were convinced of the effects ID-alG™ exerts.

 

Dialpha continues to work on MealShape, a natural ingredient positioned in the slimming and blood sugar segments. Extracted from Ceylon Cinnamon, MealShape instantly reduces carbohydrate digestion with over 20%. These new properties of cinnamon were obtained through a proprietary extraction method patented by Dialpha. The extract inhibits the activity of alpha-amylase, a digestive enzyme which divides long-chain carbohydrates into smaller units. Consumed 20-30 minutes before a meal, MealShape lowers the glycemic peak for better control of blood sugar.

Going into the “starchblockers” category, the extract regulates the absorption of carbohydrates and, in addition to a varied and balanced diet, can improve weight loss. Indeed, by reducing the absorption of sugars in the blood, MealShape limits the glucose excess which is later transformed into fat and stores as such. It has also been shown that the reduction of postprandial blood glucose, just like the diets with a low glycemic index, is beneficial for controlling cholesterol, the oxidative stress and ultimately for cardiovascular health.

The ingredient’s effectiveness has been demonstrated in clinical trials in humans. The results, which reveal more than 20% reduction in blood glucose after a standard meal, have just been published in the BMC Alternative and Complementary Medicine scientific journal.
The potato extract developed by Kemin Health under the Slendesta® brand explores a different way to control weight. Indeed, Slendesta® acts on satiety control by amplifying it- which results in lowering the calorie intake by reducing food consumption. The active is a proteinase inhibitor II – PI2: it increases the release of cholescystokinine (CCK) by inhibiting trypsin and chymotrypsin via a feedback regulatory mechanism. CCK is one of the best known hormones regulating satiety by delaying gastric emptying, decreasing appetite, and ultimately, decreasing food consumption (both in animal model and humans). According to Kemin, the right dose is 300mg Slendesta® (5% extract providing 15mg of PI2) consumed one hour before one of the two main daily meals. As many as fifteen studies (1989-2011) were performed. Two examples of food supplements with Slendesta® on the French market: CCK-30 from Fenioux Laboratories, Satieline from Ineldea.
Diana Food has developed Appl’InTM, a patented natural solution to limit the absorption of sugars and the related insulin response, factors regulating fat storage. This apple extract rich in polyphenols, of which phloridzin, has revealed, namely in various clinical trials, a significant reduction in post-prandial glucose (-11.6%) and a glucose peak delayed by 15 minutes.
Phaseolus vulgaris

Beanblock® from Indena is a dry extract of Phaseolus vulgaris white bean characterized by its standardized content of a complex protein inhibitor of alpha-amylase – inhibitory activity of 1,100 U/mg. Several studies have shown its effectiveness and have described its mechanism of action. Consumed as part of a Mediterranean-style diet, it has a positive effect on glucose metabolism. Beanblock® also modulates ghrelin secretion (a hormone which stimulates appetite) and induces a longer period of satiety. According to Indena Group, the effective dose is 100mg taken before each meal.
Also extracted from white bean, StarchLite® from Pharmachem (Ingredia Nutritional ensures distribution in Europe) is part of the very exclusive circle of ingredients which have received positive health claims. Two of them have been validated by the FDA (Food and Drug Administration). The extract acts on reducing carbohydrate digestion and absorption. Formulas containing them are intended for consumers wishing to adopt a low glycemic index diet, to control their blood sugar levels (reducing the impact of glucose) or to manage their weight (decreased caloric impact).

Decoding the mechanisms behind…

Japanese researchers of the Kaneka Group managed to develop a Glycyrrhizaglabra L. standardized licorice extract called Glavonoid™, formulated without Glycyrrhizinic acid and containing 30% polyphenols. The extract is standardized to 3% glabridin, the main active component, and is transported in a matrix of medium-chain triglycerides; all the other harmful phytochemicals were removed. Glavonoid™ was approved for use as a Novel Food Ingredient by the European authorities (food supplements and functional foods).
Several studies in humans and animals have been conducted and methods of innovative measures were used (quantitative RT-PCR, analysis on DNA chips, dual-energy X-ray absorptiometry (DXA), analysis and tomography absorptiometry scanning) to evaluate and justify the effectiveness of Glavonoid™. These studies have shown that body fat (particularly visceral) was reduced with a real proven fat burning effect (as measured by sensors on the skin). 100mg/d Glavonoid™ burn daily an average of 130 kcal body fat. Glavonoid™ has beneficial effects on cholesterol, weight and waist size.

Glavonoid™ has a dual mechanism of action: firstly, the positive regulation of the genes involved in fatty acid oxidation and secondly, the negative regulation of the genes involved in the synthesis of fatty acids.
…including the conventional ones

FinomateTM (EFLA®920) is a green mate leaf extract (Ilexparaguariensis St. Hil.) produced by Frutarom, which has the same effects on health like a green mate traditional preparation but can be used in a more practical way. The mate is a popular refreshing and stimulating infusion widely consumed in South America. For the Guarani Indians in southern Brazil, Paraguay and Argentina, dried or roasted leaves are a multifunctional natural treatment – regulation of appetite, renal excretion of water, physical and mental stimulant.

Research has recently confirmed that mate preparations regulate the appetite, increase energy consumption, reduce body fat and prevent obesity in animal models. In vitro, the mate infusion inhibited the action of pancreatic lipase, an enzyme involved in the release of fatty acids into the digestive tract, resulting in reduced fat absorption, with less fat stored in the body. The effectiveness of FinomateTM was studied in a randomized double-blind study against placebo (60 overweight volunteers, three capsules (330 mg) of FinomateTM/day for six weeks) with the following results: a significantly lower body fat mass and body fat percentage – the latter parameter being statistically different from the placebo. The positive effects of FinomateTM were also observed on the body mass index (BMI), weight and waist size.
Capsaicinoids – such as chilli, pepper – play a role in weight management by acting through multiple mechanisms of action. They stimulate lipolysis, the mobilization of fatty acids in the circulation, releasing hormones which act on the lipase. They stimulate thermogenesis in brown fat – through a protein-decoupling process, and play a role in energy metabolism. OmniActive has developed Capsimax®, controlled-release granules, based on its patented OmniBead™ technology.
AMP-K, one of the keys to activate

5’adenosine monophosphate- activated protein kinase enzyme (AMP-K) is a metabolic “circuit breaker” which determines whether the consumed calories are stored as fat or used immediately. Aerobic exercise generates hypoxia and increases cAMP levels in muscle, thus activating the AMP-K – it stops energy storage and increases energy expenditure. Activation of the AMP-K during aerobic exercise involves the activation of the coding genes for sestrins – normally activated by physical stress.

Extensive research has been conducted to identify plants with sestrin activity/AMP-K. Thus, South Korean researchers have identified the Gynostemma pentaphyllum (a Chinese plant of the gourd family), traditionally used as a tonic. An extract, ActivAMP (Gencor Pacific), whose main components (damulin A and damaulin B) have been standardized, has been subject to a double-blind clinical study versus placebo (80 subjects, BMI 25-30, 3 months). The 450 mg/day consumption of ActivAMP led to a significant decrease in abdominal fat, weight, body fat and BMI.

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