Top Ingredients for Fitness Formulations by Steve Myers Top Ingredients for Fitness Formulations by Steve Myers

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Special Report Top Ingredients for Fitness Formulations by Steve Myers Top Ingredients for Fitness Formulations by Steve Myers

For brands offering top fitness products to consumers, formulation is more complicated and challenging than in the past. New consumer demographics and demands must be considered and more companies are venturing into this space every year with new ingredients, products and delivery formats. Efficacious, safe ingredients are the heart of any good formulation. It is important such ingredients are backed by evidence, especially if there is a need to substantiate claims. Several novel ingredients provide fitness formulators with researched-backed benefits that can beef up product value. These ingredients fall into several categories such as energy-fatigue management, muscle development, cognitive function and recovery dynamics (inflammation, stress and immune).

Energy is produced in the body from the molecule adenosine triphosphate (ATP). Creatine—popular in sports nutrition products for increasing muscle stores of phosphocreatine, which is used to quickly make ATP and fuel short bursts of intense exercise. On performance, creatine supplementation can increase muscle power.1,2 Ribose—a five-carbon carbohydrate that is in the center of the ATP molecule. Supplementation (as Bioenergy®, from Bioenergy) can increase strength and total repetitions before failure.3 Carnitine—helps shuttle fatty acids into the mitochondria, where longer aerobic exercise requires fat oxidation to make ATP for energy. Supplementation with carnitine tartrate (as Carnipure®, from Lonza) was shown to raise muscle carnitine levels and led to higher work output during exercise.4 Medium-Chain Triacylglycerols (MCTs)—dietary fats commonly found in coconut oil. MCTs may help fuel energy production, especially during ketosis, a very low-carb state in which fat oxidation is preferred over glycolysis for ATP production.5

Top Ingredients for Fitness Formulations Top Having adequate energy supply is a popular target for all types of sports nutrition consumers, but adding fatigue-inhibiting ingredients can give a formula a solid one-two punch. Beta-Alanine—a nonessential amino acid that combines with histidine in muscles to make carnosine. During intense exercise, lactic acid is a byproduct of ATP production and can result in a build-up of hydrogen ions in the muscles. Left unchecked, these Natural Products INSIDER | ions can trigger muscle fatigue, but carnosine buffers the hydrogen and preserves

PAGE muscle endurance, namely its ability to contract. Research has demonstrated beta- 2 alanine supplementation (as Carnosyn®, from Natural Alternatives International) not only delays fatigue, but may increase physical work capacity.6 L-Glutamine—a conditionally essential amino acid that can be enzymatically converted into a ketone acid used to drive ATP production via the krebs cycle. A dipeptide of L-alanine and L-glutamine glutamine (as Sustamine®, from Kyowa Hakko) was found to delay fatigue, increase hydration and improve endurance.7,8 Citrulline—a nonessential amino acid central to the urea cycle, in which its role is to recycle ammonia. Large amounts of supplemental branched-chain amino acids (BCAAs) can increase muscle ammonia levels during exercise, promoting fatigue; citrulline supplementation can manage this ammonia fatigue effect.9 Research has shown citrulline malate—malic acid is a key compound in the krebs cycle of energy production—can delay fatigue and increase performance, specifically work and power output.10,11 Citrulline is a precursor to the amino acid arginine, which improves blood flow by increasing levels of the vasodilator nitric oxide (NO). Citrulline combined with the antioxidant glutathione (as Setria®, from Kyowa Hakko) was shown to increase NO levels in resistance-trained men.12 Arginine—in vitro research indicated inositol-stabilized arginine silicate (as Nitrosigine®, from Nutrition 21) significantly increases NO production significantly more than arginine, arginine AKG, citrulline, citrulline malate and agmatine sulfate.13 Nitrosigine increased blood flow to and improved the performance of the muscles and the brain.14,15

Cognitive function is a growing area of sports nutrition. The brain affects fatigue signaling and cognitive functions such as focus, attention, reaction time and processing, all of which are crucial to exercise and performance. Caffeine—a purine alkaloid found naturally in many botanicals, but also made synthetically. Caffeine competes with adenosine, a byproduct of breaking the bond of ATP to produce energy. Adenosine triggers fatigue signaling when taken up by these receptors, so caffeine inhibits fatigue by winning this game of musical chairs in the brain. Low and moderate doses of caffeine can improve performance with few side effects,16 but higher doses of caffeine can overstimulate the central nervous system (CNS) and increase adrenaline and heart rate to unhealthy levels. Theacrine—a purine alkaloid similar in structure to caffeine, but without dangers (addiction and overstimulation). Research confirmed theacrine supplementation (as Teacrine®, from Compound Solutions) in healthy men is safe and not habit-forming.17

Top Ingredients for Fitness Formulations Top Both 200 mg/d and 400 mg/d doses of Teacrine were shown to increase energy, focus and concentration without adverse effects, but only the lower dose associated with increased willingness to exercise, anxiety, motivation to train and libido. Theanine—a non-protein amino acid found in tea (Camellia sinensis) that improves cognitive performance and relaxation (e.g., sleep).18 Several studies on theanine taken

Natural Products INSIDER | with caffeine found delayed fatigue, increased alertness, improved reaction time, better visual information processing and increased speed, accuracy and attention.19,20,21,22 PAGE 3 Choline—a vitamin-esque essential nutrient for cellular energy, brain health and muscle function. Choline factors in NO production and resultant blood flow improvements and helps transport fats from the liver for energy production—it complements carnitine’s role in fat metabolism. Like carnitine, choline plays a role in the production of acetylcholine, a neurotransmitter that affects motor function. Research has found choline influences focus and accuracy.23 Citicoline—also known as cytidine diphosphate choline (CDP), is a source of both choline and cytidine, a a modulator of transmitter glutamate in neurons and glial (neuronal support) cells. Supplemental citicoline (as Cognizin®, from Kyowa Hakko) increases acetylcholine and phosphatidylcholine in the brain and improves brain bioenergetics.24 Further research in healthy adolescents showed Cognizin improved attention and psychomotor speed while reducing impulsivity.25 Spearmint—the leaves of this plant (Mentha spicata) contain rosmarinic acid, as well as numerous other active phenolic compounds. Rosmarinic acid increases BDNF (brain-derived neurotrophic factor), a neurotrophin—such compounds impact the survival, development and function of neurons. Improved overall quality of working memory and spatial working memory accuracy were associated with a proprietary extract of spearmint leaves (as Neumentix™, from Kemin Foods) containing rosmarinic acid and more than 50 phenolic constituents, including salvianolic, lithospermic and caftaric acids.26 The ingredient also was found to improve active reaction time in recreationally active adults in research testing with the Makoto Arena II—a unique device linking cognitive function to active performance.27 Ashwagandha—an adaptogenic herb popular in Ayurveda, the traditional medicine of India. This botanical (Withania somnifera) contains steroidal lactones, called withanolides, and several alkaloids. Supplementation can increase levels of BDNF and glial fibrillary acidic protein (GFAP), which affects neuronal and synaptic activities related to learning and memory.28 A full-spectrum ashwagandha root extract (as KSM-66®, from Ixoreal Biomed) may improve both immediate and general memory, as well as executive function, attention and processing speed.29 Similarly, a root and leaf extract of ashwagandha (as Sensoril®, from Natreon) demonstrated improved cognitive and psychomotor performance, including reaction times.30

Energy, fatigue and brain health all impact the muscles. This is also where sports

Top Ingredients for Fitness Formulations Top nutrition superstar protein shines. The key to building muscle is protein synthesis, which helps rebuild muscles bigger and stronger following exercise. Whey—one of the two primary proteins in milk; casein is the other. Whey is a quick-acting protein, meaning it has faster absorption. Whey supplementation before and after exercise can increase muscle gains and improve agility.31 Whey combined

Natural Products INSIDER | with essential amino acids (EAAs) can increase body mass and strength when used with an exercise program.32 PAGE 4 Casein—a slower-acting protein that may be more beneficial taken later in the day for overnight gains. A combination of casein and the probiotic Bacillus coagulans GBI- 30, 6086 (as Ganeden BC30®, from Ganeden) increased recovery and reduced soreness in recreationally trained men.33 BCAAs—found in whey and casein and includes the amino acids leucine, isoleucine and valine. Muscle protein synthesis (MPS) may depend on reaching a “leucine threshold,” a set muscle level that triggers MPS. Evidence showed BCAAs improved performance in endurance sports, preserved muscle strength in resistance training and reduced immunosuppression often experienced following exercise.34,35,36 HMB—beta-hydroxy-beta-methylbutyrate, is produced in the body from leucine metabolism, but is also found in citrus fruits and fish. HMB appears to limit muscle damage, manage acute immune response and boost muscle mass and strength.37 Supplementation with HMB (as BetaTOR®, from MTI Biotech) and disodium ATP (as Peak ATP, from TSI Inc.) in weightlifters increased muscle strength and power, vertical jump performance and lean body mass.38 Further, a dietary supplement (MaxxTOR™, from Max Muscle) containing HMB, leucine, vitamin D3 and phosphatidic acid (as Mediator®, from Chemi Nutra) increased lean body mass and muscle strength in bodybuilders, compared with exercise alone.39 Fenugreek—the seeds from this botanical (Trigonella foenum-groecum L.) are rich in steroidal phytochemicals including diosgenin, which improves glucose metabolism, and glycosides, which are known to increase testosterone levels. Supplementation with fenugreek (as Testofen®, from Gencor Pacfic) increased both total serum testosterone and free testosterone in healthy men 43 years and older.40 In resistance-trained men, Testofen increased muscle strength and repetitions to failure, as the associated increased free testosterone promoted anabolic and androgenic activity.41 Zinc/Magnesium/Vitamin B6—a proprietary micronutrient combination touted for increasing total and free testosterone levels, as well as insulin growth factor-1 (IGF-1) for muscle strength and power gains. Exercise may decrease muscle levels of zinc and magnesium, resulting in fatigue and endurance decline. B6 is added to this supplement tandem for improved absorption. Research confirmed supplementing with this combination (as ZMA®, from Interhealth, part of Lonza) in football players increased levels of zinc and magnesium, leading to higher levels of free testosterone and IGF-1 as well as increased power and torque.42 Magnesium aspartate and zinc methionine Top Ingredients for Fitness Formulations Top (L-Opti-Zinc®, from Lonza) are the forms used in ZMA.

Inflammation and oxidative stress resulting from exercise can prolong recovery and lessen gains if not adequately managed. Tart Cherry—can address oxidative and inflammatory issues, and may influence

Natural Products INSIDER | aerobic performance. Endurance runners taking Montmorency tart cherry (as CherryPURE™, from Shoreline Fruit) before, during and after a half marathon had PAGE 5 faster race times, more consistent pacing, increased antioxidant activity and lower inflammation, compared to those taking placebo.43 Other research demonstrated Montmorency tart cherry can improve several aspects of recovery—maximal voluntary isometric contraction (MVIC), counter movement jump (CMJ) and agility—in addition to inhibiting delayed onset muscle soreness (DOMS) and acute inflammation.44 Omega-3s—polyunsaturated long-chain fatty acids (PUFAs) including docosahexaenoic acid (DHA) and eicosapentaenoic acid (EPA), known for their role in producing anti-inflammatory compounds including resolvins (Rvs), maresins and protectins. A study of European football (soccer) players found DHA supplementation increased anti-inflammatory compounds, including prostaglandins and resolvins.45 Methlysulfonylmethane—MSM is an anti-inflammatory sulfur ingredient known for its benefit to painful joints, but it also has some promise in muscle health. Athletes taking MSM (as OptiMSM®, from Bergstrom Nutrition) had improved muscle force recovery, reduced delayed onset muscle soreness (DOMS) and limited immunosuppression following exercise.46

The best fitness formulations for the growing market and expanded consumer base will consider these and other ingredients researched for their potential impact on energy, endurance, fatigue, performance, muscle development, cognitive function and recovery. Top Ingredients for Fitness Formulations Top

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Top Ingredients for Fitness Formulations Top Nutr. 2016 Apr 5;13:16. 46. Van der Merwe M and Bloomer RJ. “The Influence of Methylsulfonylmethane on Inflammation-Associated Cytokine Release before and following Strenuous Exercise.” J Sports Med (Hindawi Publ Corp). 2016;7498359. Natural Products INSIDER |

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