ESPEN Congress Lisbon 2015 PUTTING ON DIET A LARGE … · Ephedra has a long and distinguished...
Transcript of ESPEN Congress Lisbon 2015 PUTTING ON DIET A LARGE … · Ephedra has a long and distinguished...
ESPEN Congress Lisbon 2015
Does the magic pill exist?E.M. Williamson (UK)
PUTTING ON DIET A LARGE PLANET:OPPORTUNITIES AND CHALLENGES
Is there a magic pill for weight loss ?Liz Williamson
University of Reading, School of [email protected]
Outline of talk• What type of products are being used?• The main mechanisms claimed for them• The most hyped products and an examination of their claims and safety issues
• A conclusion – is there a magic herbal pill?!
What is being used? A selection….
Natural• Acai berry• Bitter orange• Chilli pepper• Ephedra• Garcinia • Guarana• Hoodia• Kelp• Thunder god vine• Green tea• Green coffee• Prickly pear• Raspberry ketones• White Kidney Bean Extract• Chitosan
Synthetic• Dinitrophenol• Prescription drugs (phentermine, orlistat etc)• Illegal drugs (cocaine, amfetamine)• Mixtures of herbal and synthetic drugs
The focus of this talk is on natural supplements which consumers buy , usually without expert advice – but with the influence of advertising…..
Mechanisms relevant to natural supplements
Reducing calorie intake• Appetite suppression• Inhibition of fat and/or carbohydrate absorption and/or inhibition of metabolism to prevent absorption
• Use of fibre for both purposes
Increasing energy output• Induce thermogenesis• Increase lipolysis• Increase thyroid activity• Increase effects of leptin
Others (not currently involving herbal products)• Inhibit pancreatic lipase• Attenuation of effects of
ghrelin, glucagon‐like peptides and incretins
Thermogenic products = ‘increase or improve metabolism’
• Caffeine‐containing: very many ‐ e.g. guarana, green tea, green coffee
• Raspberry ketones • Garcinia cambogia (hydroxycitric acid), • Bitter orange peel (synephrine) • Ephedra (ephedrine)• Chilli pepper (capsaicin) • Thyroid ‘support’ (iodine)
Calorie‐intake reducers
• Appetite suppression via sympathomimetic activity/release of catecholamines (ephedrine)
• Use of fibre to induce sense of satiety • Inhibiting fat absorption with ‘binders’
(chitosan) or prickly pear extract (fibre complex)• Inhibition of carbohydrate breakdown to
prevent absorption (white kidney bean extract)
‘Green Tea Extract by Nutravita ‐ 100% Pure High Strength Weight Loss Supplement’
‘12 weeks of treatment resulted in significant weight loss, reduced waist circumference, and a consistent decrease in total cholesterol and LDL plasma levels without any adverse effects in women with central obesity. The mechanism of green tea extract might be associated in part with ghrelin secretion inhibition, leading to increased adiponectin levels’. Chen et al Clin Nutr. 2015. pii: S0261‐5614(15)00134‐X.
Green tea preparations appear to induce a small, statistically non‐significant weight loss in overweight or obese adults. Green tea had no significant effect on the maintenance of weight loss. Jurgens et al Cochrane Database Syst Rev. 2012 Dec 12;12:CD008650.
‘NatureWise Green Coffee Bean Extract 800 Fat Burner with GCA, 1600 mg Per Daily Serving, THE highest available on the market’
‘The result reveals a significant difference in body weight in GCE compared with placebo (mean difference: −2.47 kg; 95%CI: −4.23, −0.72). The magnitude is moderate. It is concluded that the results from these trials are promising, but the studies are all of poor methodological quality’.Onakpoya et al 2015Gastroenterol Res Pract. 2011; 2011: 382852.The Use of Green Coffee Extract as a Weight Loss Supplement: A Systematic Review and Meta‐Analysis of Randomised Clinical Trials
Green coffee bean contains chlorogenic acid and caffeine
‘GBSci Raspberry Ketones 2000mg| High Strength | Fruit Extract | Natural Health and Weight Loss Supplement | Proven Results | Effectively Speeds Up Metabolism | Reduces Fat Build‐Up | Suppresses Appetite’
1kg of raspberries 1‐4 mg of raspberry ketones (0.0001‐0.0004% ! The raspberry ketones in supplements are synthetically made.
Unfortunately, there is not a single study on raspberry ketones in humans.
Raspberry ketone: 4‐(4‐hydroxyphenyl)‐2‐butanone); p‐hydroxybenzyl acetone; frambinone.
“Kate claims Garcina GCB and Radiant Detox combo were the key factors in losing 12 kilos in just 4 weeks”.
http://co‐life‐facts.com/kate‐mirror‐garcinia/ accessed Aug 2015
“Celebs have been raving aboutGarcina GCB and Radiant Detox. They confess that it's the secret to their incredible figures”.
‘Most studies in humans have been conducted on small samples and mainly in the short term. None have shown whether effects persist beyond 12 weeks of intervention.
At the doses usually administered, no differences have been reported in terms of side effects or adverse events (those studied) in humans between individuals treated with G. cambogia and controls.’Crit Rev Food Sci Nutr. 2012;52(7):585‐94. Márquez F, Babio N, Bulló M, Salas‐Salvadó J
Garcinia cambogia
G. cambogiamay increase the levels of serotonin, possible interacting with medicines that increase serotonin levels such as SSRIs. Extracts exhibited anti‐obesity activity including reduced food intake and body fat gain by regulating serotonin levels related to satiety, increased fat oxidation and decreased de novo lipogenesis.
Fitoterapia. 2015;102:134‐48. A comprehensive scientific overview of Garcinia cambogia. Semwal RB, SemwalDK, Vermaak I, Viljoen A
Chilli, cayenne, hot pepper
‘In energy balance, addition of capsaicin to the diet increases satiety and fullness, and tends to prevent overeating when food intake is ad libitum. After dinner, capsaicin prevents the effects of the negative energy balance on desire to eat’.Janssens et al. Appetite. 2014;77:44‐9
‘Capsaicin activation of TRPV1 promotes lipolysis in both in vitro and in vivo. TRPV1 activation by dietary capsaicin improves visceral fat remodelling.’Chen et al Cardiovasc Diabetol. 2015 13;14:22.
‘Capsinoids –non‐pungent capsaicin analogs – increase energy expenditure through activation of brown adipose tissue in humans.Yonishiro et al Am J Clin Nutr. 2012 95(4):845‐50.
6 mg/d capsinoids orally appeared to be safe and was associated with abdominal fat loss.Snitker et al Am J Clin Nutr. 2009 89(1):45‐50.
Chilli peppers contain pungent substances –capsaicins – which are thermogenic ‐ butthey also contain non‐pungent analogues called capsinoids which are currently of interest for weight loss
"Capsinoids structure" by Sheldon Handler Ph.D., M.D.; David Rorvik ‐ PDR for Nutritional Supplements Second Edition.. Licensed under Attribution via Commons ‐https://commons.wikimedia.org/wiki/File:Capsinoids_structure.png#/media/File:Capsinoids_structure.png
Ephedra, Ma Huang, Ephedra sinica
Contains the sympathomimetic amines ephedrine and pseudoephedrine
Ephedra has a long and distinguished history in Chinese and Western medicine as a treatment for asthma and bronchitis, due to its decongestant and bronchodilatoryeffects. Ephedrine is still used for this purpose.
It used in much higher doses for weight loss or as a performance enhancer in sport.
It has caused hypertension, stroke, cardiac arrhythmia, and death.
The FDA prohibited its sale in the US in 2004.It is also a banned substance in sport.You can still buy it over the Internet.
Norspeudoephedrine = cathine (in khat, Catha edulis)Norephedrine = phenylpropanolamine (in cold remedies)
Bitter orange‘Citrus aurantium (bitter orange) extract and its constituent p‐synephrine are widely used in weight loss products. The potential dangers associated with the use of products containing C. aurantiumextract are frequently touted…
….millions of people consume on a daily basis various juices and food products from Citrus species that contain p‐synephrine.
The data indicate that based on current knowledge, the use of bitter orange extract and p‐synephrine appears to be exceedingly safe’The safety of Citrus aurantium (bitter orange) and its primary protoalkaloid p‐synephrine.Shohs et al , Phytother Res. 2011 (10):1421‐8.
p‐Synephrine is a phenylethanolamine derivative with the hydroxy group in the paraposition on the benzene ring of the molecule Much confusion exists because there is also m‐synephrine, which is also known as phenylephrine. This is approved in some countries for nasal decongestants and sprays.Shohs et al , Phytother Res. 2011 (10):1421‐8.
Enhancing the effects of leptin
Celastrol suppressed food intake, leading to up to 45% weight loss in hyperleptinemicdiet‐induced obese mice, by increasing leptin sensitivity. (It was ineffective in leptin‐deficient (ob/ob) and leptin receptor‐deficient (db/db) mouse models.) These results indicate that Celastrol is a leptin sensitizer and a promising agent for the pharmacological treatment of obesity.
Cell, 161, 5, 21 2015, 999‐1011 Liu J, Lee J, Hernandez MAS, Mazitschek R, Ozcan U.
Thunder god vine, Tripterygium wilfordii
Why would a patch work when the active ingredient (called p57) is a peptide?!
Claim: ‘Increase metabolism , block fat and suppress appetite, halt the creation of fat cells; release anti‐oxidants to attack free radicals which build fat cells’
‘We conclude that although Hoodia gordonii seems to have an effect on appetite and weight loss, this may at least in part be a symptom of the serious adverse effects that are associated with consumption of the high doses required to achieve therapeutic clinical effect.’ Hoodia gordonii: To eat, or not to eat’. Smith C, Krygsman A. J. Ethnopharmacology 155 (2014) 987–991
Hoodia
Antioxidants e.g. AcaiEuterpe oleacea
Contains polyphenolics e.g. orientin, isoorientin and anthocyanins cyanidin‐3‐glucoside and cyanidin‐3‐rutinoside.
No clinical evidence for weight loss at all.(Some beneficial effects reported in athletes).
A review of six clinical trials of white kidney bean extracts did find a statistically significant reduction in body fat (averaging about 4 pounds) when compared to placebo, although there was insufficient evidence to demonstrate weight loss (Onakpoya, Br J Nutr 2011).
‘Phaseolamin’ inhibits alpha‐amylase (which otherwise turns starch into absorbable sugar), supposedly reducing absorption . This approach is not validated!
White kidney bean extract
‘The fat trapped was clinically insignificant. For men, it would take more than 7 months to lose 1 pound of body fat. For women, no fat was trapped’. Gades et al. J Am Diet Assoc. 2005 105(1):72‐7. Chitosan supplementation and fat absorption in men and women.
There is some evidence that chitosan is more effective than placebo in the short‐term treatment of overweight and obesity. Results obtained from high quality trials indicate that the effect of chitosan on body weight is minimal and unlikely to be of clinical significance. Jull et al. Cochrane Database Syst Rev.2008 Jul 16;(3):CD003892.
Not suitable for those with allergies to sea‐food
Chitosan
Compared with placebo, Litramine showed a greater reduction in BMI, body fat composition and waist circumference. The natural fibre complex Litramine represents an effective non‐pharmacological intervention to induce weight loss. Grube et al Obesity 2013: 21(1):58‐64.
Prickly pear extract – fibre is not a drug apparently!
Evidence from four RCTs showed that 3g daily of Litramine IQP‐G‐002AS over 7 days increased faecal fat excretion compared with placebo (15.8% (SD 5.8%) v. 4.6% (SD 3.1%); P < 0.001). In a 12‐week study, weight loss (3.8 kg (SD 1.8 kg) v 1.4 kg (SD 2.6 kg); P < 0.001) was observed in overweight and obese subjects. No relevant GI side effects were reported at the dosages studied. Chong et al Evid Based Complement Alternat.Med. 2014;2014:943713.
‘ULTRA Strong Weight Loss Diet PillsFat Burners For Men & Women
(Work Quicker Than Raspberry Ketones, Colon Cleanse, T5, T6, Detox Tablets)’
Bitter Orange Peel Powder 200mg, Trimethylxanthine (pure caffeine) 220mg, Green tea Extracts (45% EGCG) 150mg, Maral Root (Rhaponticum carthamoides)50mg, L‐Tyrosine 50mg, Guarana Seed 12mg
Green Tea ‐ 40% EGCG (1,380mg), L‐Carnitine (900mg), Caffeine, N‐methylglycine, L‐Tyrosine, Bitter Orange Peel, Green Coffee Bean 15:1 (450mg equivalent), ALA, Vitamin B6, Zinc, Biotin, Chromium
‘T5 Xtreme (180 Capsules)Thermogenic Fat Burner ‐ Intense weight loss supplement ’
Combinations – a bit of everything, with lots of caffeine…
‘BELLY FAT REDUCER ‐ The Number 1 Tummy FAT BUSTER Worldwide ! Specially Formulated to target that hard to shift STOMACH FAT !
This product contains trimethylxanthine which is the bitter component found in coffee beans and research has shown when combined with other weight Loss products like GREEN TEA and GUARANA EXTRACT it burns through FAT like WILDFIRE ! Lose Up 5 Kilos In 12 Weeks ! AMAZING Strong Fat Burner’
NB: trimethylxanthine = caffeine. Green tea contains caffeine. Guarana contains caffeine (= ‘guaranine’)
Caffeine overload?
‘To Improve Thyroid Function to Support a healthy metabolism, reduce fatigue, promote weight loss and increase energy’
‘With Kelp (Iodine), Bladderwrack and Tyrosine which play critical roles in the natural support of thyroid hormones and Ashwaganda and Schizandra for thyroid function support’.
No clinical evidence available. Not much pre‐clinical evidence. Weak rationale!
Aristolochia fangchi‐ a cautionary tale
In the 1990's, >100 Belgian patients developed aristolochic acid (AA) nephropathy . 70% evolved into end‐stage renal disease, requiring dialysis or renal transplantation. Nachtergael A et al. J. Ethnopharmacol. doi: 10.1016/j.jep. 2015.07.045.
The preparation contained fenfluramine, diethylproprion, cascara, belladonna, acetazolamide, Stephania tetrandra and Magnolia officinalis. The kidney failure and urinary cancer were attributed to the substitution of Aristolochia fangchi (Guang Fang Ji) for Stephania. Han Fang Ji). It can be difficult to visually differentiate the two herbs and because their names in Chinese are similar .
Conclusion and acknowledgements• Some products may be promising but most rely on stimulants
(caffeine, also a diuretic) as ‘thermogenic’ agents• Fibre is a healthy addition to the diet but over‐rated as an aid
to weight loss• Celastrol as a leptin‐sensitiser is a very interesting lead • Non‐pungent capsinoids from chilli look promising• But sorry, no, there is no magic pill….• …but anyway, thanks for inviting me and thanks for listening!