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Introduction
Ergogenic aids, or Nutrition supplements 500-400 B.C. Enhance performance Influence by manufacturers
Weight loss and muscle gain Nutritional supplements are used by
40-100% athletes Over 600 nutrition supplements
Ex Nutr c10-Supplement 2Clinical Evaluation of Nutrition Supplements Studies Does the study have a clear hypothesis? Was the study on cell, muscle, animals, or humans? Was the population for which claims are made
comparable to the population in the study? Were external variables controlled? Was the study placebo controlled? Were adequate techniques used? Were the trials randomized? Was a crossover design used? Was it random assignment or was self-section used? Do other studies confirm the findings? Was the study peer reviewed?
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Androstenedione
Claim: increase testosterone, muscle mass, and improve recovery
most popular supplement in USA Used by Mark McGwire when broke MLB single
season HR record 1994 allowed to sell as food supplements No supporting evidence Decrease HDL-C IOC banned, MLB banned in 2006
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New drugs tetrahydrogestrinone ( THG ) 全新的藥物,和已知的類固醇在結構上有很大的不同
直到 2003 年 6 月,一位匿名的教練將一支含有 THG 的針筒寄到美國藥檢局總部
位於舊金山的運動營養品公司- Bay Area Laboratory Co-Operative ( BALCO )提供 THG 給運動員
Jason Giambi, Barry Bonds, Roger Clemens, Marion Jones, Montgomery 等可能使用
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tetrahydrogestrinone ( THG )
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Bee Pollen
Claim: Increase energy level, enhance physical fitness and improve endurance, and boosts immune function
Reduces free-radicals, weight control, longevity, and prevent asthma
No supporting evidence
Ex Nutr c10-Supplement 11Beta-Hydroxy Beta Mtheylbutyrate (HMB) A metabolite of Leucine (Fig 10.2) Synthesis rate 0.2-0.4 g/day Popular among body builders Claimed
Increase LBM, strength and improve recovery Increase immune function, lower cholesterol, stress,
reduce body fat For both endurance and strength athletes
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HMB metabolism
Nissen SL, 1997
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41untrained subjects, 3 wk weight training Control, 1.5 g/day, 3.0 g/day
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Boron 硼 In noncitrus fruits, leafy vegetable, nuts, and
legumes. Improve bone density, muscle mass, and
strength Improve bone mineral density in post-
menopausal women, not in men
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Caffeine Paleolithic time – brew a drink for stimulus properties Stimulate central nervous system Stimulate release of epinephrine Improve high-intensity and endurance exercise, fat oxidation ↑Post-exercise glycogen recovery? Effective dosage 3-15 mg/kg, ~1 hr before exercise
Not a banned substance any more 70 kg male, consume 100 mg, ~1.5 ug/ml urine Safe dosage 8-10 mg/kg (recommend <7, usually 3-5 mg/kg) 100-150 mg in a cup of coffee, 20-50 mg in a cup of tea, 35-55 mg
in a can of coke Individual difference in effect, dosage, excretion
Adaptation, may need to avoid caffeine Purified caffeine in capsule may better than coffee
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Effect of Caffeine in Performance Endurance exercise
Ingested 1 h before exercise Increase FA conc., decrease muscle glycogen utilization
- improve endurance performance Not all studies found performance improved: Dosage,
fitness level, habitual caffeine consumption, and duration of exercise
Maximal exercise 6 mg/kg improve time to exhaustion at 100%VO2max Muscle glycogen still high at exhaustion neuromuscular pathway? muscle ion handling? enhance
anaerobic energy production? 150-200 mg improve 1500 m (4:46-4:50)
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Effects of Caffeine in Performance
Supramaximal Exercise: Uncertain No effect in 15-second sprint, 30 s Wingate test
Cognitive function Caffeine (2-3 mg/kg) + carbohydrate
electrolytes drink Improve cognitive functioning (attention,
psychomotor skills, memory) Improve concentration
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Ex Nutr c10-Supplement 25Meta-analysis of caffeine on endurance performance (vs placebo)
Conger SA, 2011
Ex Nutr c10-Supplement 26Meta-analysis of caffeine on endurance performance (vs CHO)
Conger SA, 2011
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L-Carnitine 肉鹼 from meat and dairy products, popular
among athletes Also endogenous production from
methionine and lysine Synthesis in liver, ~27g stores, 98% in skeletal
muscle and heart muscle Lost from only urine and stool
Claim ↑VO2max, muscle, fat oxidation, spare muscle
glycogen ↓lactate, fat mass
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Carnitine in fat metabolism
Transport long-chain FA across Mitochondrial inner membrane
Maintaining acetyl-CoA/CoA ratio Action on PDH Acetyl-CoA + carnitine –> acetyl-carnitine +
CoA Reduces lactate production, may enhance high
intensity exercise
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Carnitine as a slimmer agent
Regular ingestion of carnitine increases muscle carnitine concentration which may increase fat oxidation?
No effect 6 g/day for 14 days did not increase in muscle
carnitine concentration Human muscle has more than enough free
carnitine for CPTI to maximal activity
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Carnitine in Performance
Endurance exercise theory – increase muscle carnitine concentrations NO effect in fat oxidation and glycogen
breakdown NO effect in performance during prolonged
cycling or running exercise High-intensity exercise
No effect on VO2max, performance and lactate accumulations
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Choline
Acetylcholine precursor Abundant in meat and dairy products,
lecithin, pysophatidylcholine and sphiongomyelin
Strenuous exercise decrease plasma choline Supplementation no effect on performance
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Chromium 鉻 Fat burner and muscle builder Claim: ↑Insulin action, ↑ protein synthesis
Essential for insulin sensitivity Evans 1989 – 40-42 days weight training +
200 ug/day Chromium Subsequent data did no confirm the results May cause chromosome damage
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Coenzyme Q10
ETC in mitochondria Used in CVD patients for recovery Functions – improve oxidative metabolism
Exercise capacity Antioxidant – free radical
NO effects on VO2max, performance, lactate conc.
Free radicals?
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Creatine Popular after 1992 Olympic game
Linford Christie (100 m), Sally Gunnell (400 m hurdle) 1996 Atlanta – 80% athletes used creatine 3,000,000 kg/year Ingestion 2g/day, breakdown 2g/day into creatinine
and excreted in the urine Primary source in fish and red meat Vegan depends on endogenous synthesis 70 kg man – 120g creatine, 95% in muscle Creatine synthesis in liver and kidney Type II has 30% more than type I
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Creatine in the metabolic process Phosphocreatine (PCr) + ADP + H+ Creatine
(Cr) + ATP Muscle 30% ATP falls – muscle fatigue PCr stores can be depleted in 5 s ↑creatine conc creatine kinase
↑ PCr synthesis Safety: generally safe, minor side effects
Gastrointestinal, cardiovascular and muscular problems Nausea, vomiting, diarrhea Alterations in kidney and liver function Muscle cramps Elevated blood pressure
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Creatine supplementation
Harris et al. 1992 5 g creatine 4-6 times/day 30% increase in PCr
Greenhaff 1993 20 g/day for 5 days improve 6% repeated bout maximal knee ex.
In 1999 – 62 studies, 42 positive results
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Creatine Loading Regimens
Loading + maintenance 20 g/day (5g for 4 times) 6 days increases
muscle creatine by 25 mmol/kg, ~20% Follow up by 2 g/day maintain for 35 days 3 g/day for 28 days = rapid loading Initial muscle concentration 160 mmol/kg dw – maximal conc. Ingest with simple carbohydrate solution
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Creatine and Weight Gain
20 g for 6 days – 0.5-3.5 kg weight gain Increase intracellular water Increase protein synthesis Decrease protein breakdown
10 wks weight training + creatine 20-25% increase in maximal strength 60% fat free mass increased
Allow more repetitions – better training quality Negative effect on weight bearing activities?
Running, Gymnastics
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Creatine and performance
High-intensity exercise, repeated exercise 70% of all studies – improve in strength, force
production or torque 25 g for 6 days, 10X6s sprints 20 g for 5 days, 2X30s
Endurance exercise: No effect
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Mechanism of Creatine Action
Increased PCr stores – especially in type II Increased PCr resynthesis Increased use of PCr, reduced anaerobic
glycolysis and lactic acid formation Buffer of hydrogen ion
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ATP shuttling Creatine important in
shuttling high-energy phosphate from mitochondria to myofibrils
Potential mechanism for Cr in improving endurance exercise performance Endurance performance
NOT affected
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Dehydroepiandrosterone (DHEA)
DHEA, DHEAS Stimulate muscle growth Olympic Committee banned
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Fish Oil
No effects on performance Need further study
May benefit health Cardiovascular disease Fat/cholesterol metabolism inflammation
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Ginseng
Improve VO2max? Running performance in rats!!
Inconsistent results
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Glycerol
A substrate as glyconeogenesis Convert into glucose in the liver as fuel As hyperhydrating agent
Act like a sponge Increase plasma osmolarity 1g/kg bw in 1-2 L water
Banned by WADA
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Inosine, Lecithin
Inosine: Nucleoside, ATP structure Claim: ↑ ATP stores, ↑ muscle strength, ↑
oxygen delivery, ↑ endurance No evidence
Lecithin: phosphotidylcholine Claim effects: similar to choline No effect on performance
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Lactate Salts and Polylactate
Lactate – energy source for heart Lactate salt – sodium or potassium lactate
10 g without any gastrointestinal problem Polylactate – low in bioavailability No effect on performance
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Medium Chain Triacylglycerol MCT FA contain 8-10 carbons May elevated plasma FA and spared muscle
glycogen – improve performance CHO, CHO+MCT, MCT 57% VO2max, 180 min Contribute to total energy expenditure is small
MCT rapid emptied from stomach Ingest 20 g MCT does not affect muscle
glycogen breakdown Probably no positive effect on performance
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Pangamic Acid
Vit B15 Increase VO2max, reduce lactate formation,
improve performance No effect Not Vitamin Synthetic pangamic acid is harmful – FDA
forbid the sale as dietary supplement or as a drug
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Phosphatidylserine, Phosphorus
Phosphatidylserine Soy bean Decrease in stress Inconclusive in exercise performance
Phosphorus Phosphate loading – 4 g/day ↑VO2max?, ↓lactate ? Inconsistent findings, need further confirmation
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Pyruvate (and dihydroxyacetone)
Claim:↑ fat oxidation, ↑ muscle glycogen storage, ↑ endurance capacity, ↓ fat mass
Stanko et al. 1990 – 75 g DHA+25g pyruvate ↑ VO2max and endurance time
Morrison et al. 2000 – 7 g/day, 7 days No change
More studies are needed
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Sodium Bicarbonate / citrate
Maximal exercise ↑acidity ↓performance Alkalizers may buffer the acidity
sodium bicarbonate, sodium citrate ↑lactate efflux from muscle cell, ↑plasma lactate Fitness and skill performance?
H++HCO3- <-> H2CO3 <-> H2O+CO2
200-300 mg/kg 1-2 h before exercise improve performance
Side effects Diarrhea, GI discomfort, Bloating, cramp
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Vanadium / Wheat Germ Oil
Vanadium Trace elements Insulin-like effects –↑glucose uptake, but only in
type II diabetes or glucose intolerance subjects No evidence support in healthy subjects
Wheat Germ Oil Claim: increase endurance, stamina, and vigor No effect
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Contamination of Supplement
Banned products in nutritional supplements Nandrolone, 19-Norandrostenedione, 19-
norandrostenediol ephedrine, DHEA
94 in 634 (15%) dietary supplements tested positive in IOC-accredited lab in Cologne Contain enough anabolics to cause positive result
on drug test ~20% in 240 US-made supplements
contained prohormones
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Erythropoietin (EPO)
First generation of erythropoietin: Epoetins recombinant human erythropoietins that have
the same amino acid sequence as endogenous EPO.
glycosylation varies 3 currently commercially available types of
epoetin (alpha, beta and omega) contain a higher proportion of sialylated, acidic carbohydrate residues than endogenous EPO.
injected 2-3 times/week
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Erythropoietin (EPO)
Second generation: darbepoetin alfa (Aranesp), glycoengineering of EPO differs from endogenous erythropoietin by containing
two more N-linked oligosaccharide chains Injected every 1-2 weeks
Third generation: CERA (Continuous Erythropoiesis Receptor Activator) methoxy polyethylene glycol-epoetin beta, addition of
polyethylne glycol molecule longer duration of action, injection every 3-4 weeks,
WADA started to detect in Tour de France 2008 and 2008 Olympics
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Beullens M, Blood 2006
Possible false-positive in urine EPO test
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Human growth hormone
GH increases plasma free FA and glycerol Decrease protein oxidation during exercise Increase protein synthesis, decrease fat mass in
untrained men Probably ineffective in athletes
no evidence that GH enhances muscle strength, power, or aerobic capacity in trained adult athletes
GH increase anaerobic exercise capacity accelerating recovery from soft-tissue injury,
increase collagen synthesis
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Growth hormone in ex performance
Birzniece, 2011
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Punishment to reduce cheating
Incentive to winning in big events is too high Athletes are willing to take risk in health,
punishment Increased punishment in bigger events may
reduce athlete’s incentive to cheat