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Lecture 24 Weight Loss Supplements
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Supplements for Weight Loss
Lecture 24
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Overview of Gastrointestinal System
Esophagus
Stomach
Small intestine
Large intestine
Absorption
Cells
Blood streamnutrients
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First, where in the process from digestion tostorage would a weight loss supplement act
!ncreasing adipose tissue lipol"sis #and use$%caffeine & ephedra, con'ugated linoleic acid
Bloc(s fatt" acid s"nthesis%h"dro)"citric acid #*CA$
+educe fat absorption from the small intestine%chitosan
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an" of the common actions of epinephrine#adrenaline$ are mediated b" the cA- s"stem.
!n response to a sudden stress #fear, surprise$epinephrine is released from the adrenal medullaand binds to target cells in the heart, arteriole
smooth muscle, adipose tissue, muscle and li/er.+ise in cA- and acti/ation of protein (inasescause ↑ *+, ↑ B-, mobili0ation of fatt" acids from
1, brea(down of gl"cogen to glucose.
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Effects of epinephrine do not last more than 5minutes or so.
Ephedrine #s"nthetic or e)tracted from ephedraplant as a component of ma huang$ mimicsthe action of epinephrine but with a more
sustained response.% non6drows" cold medicines% diet drugs, herbal ecstas"
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7o dietar" supplement illustrates the promise andperils of dietar" supplement use, #lac( of$
regulation, and manufacturing more than ephedra.
!n 2888, sales of ephedra were 9.85 billion, upfrom 9:88 million in ;;; #according to 7utr. Bus.
<.$.
!n their natural form, some species of ephedraplants contain a mi)ture of al(aloid compounds
including ephedrine, pseudoephedrine, etc.ma huang= powdered e)tract
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enerall" mar(eted to increase energ", burn fat,increase metabolic rate #thermogenesis$, lose
weight, ele/ate mood.
Some claim enhanced athletic performance.
E/er" careful stud" in which the effects of mahuang or ephedrine alone on athleticperformance #time to e)haustion, strength,power, lactate, fat>carboh"drate o)idation$ has
shown no effect.
Caffeine ? ephedrine impro/ed c"cling time toe)haustion #E<A-$
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-roducts reputed to contain ma huang include+ipped Fuel, Energel, @iet Fuel, @iet6*erb,
etabolife 5, ltimate Drange, *erbalEcstas", herbal -hen6Fen, @iet -ep, @iet-hen, Escalation, E)cel ..
suall" claim to contain about 58658 gramsof ephedra herb or ma huang per dosage andoften recommend 26 doses>da".
ost do not ma(e a label claim for ephedrinecontent. ost also contain 886488mg ofcaffeine, usuall" in the form of guarana.
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Metabolife International, one of the largest distributors of
ephedra in the United States, says many of the people in
the FDA reports who died may have been taking the
supplement, but it didn't kill them
!"here are reports where someone was shot and killed in a
gro#ery store, and they happened to be taking ephedra,!
said Metabolife's Dr $andy Smith
Still, University of Arkansas pharma#ologist %ill &urley said
he is worried about people who take ephedra for many
weeks or who take more than the re#ommended dosage
!ou have to reali(e that these things are potent #ardia#
stimulants, and when you are e)er#ising and lifting heavy
weights, you are already ta)ing your #ardiovas#ular
system, and ephedra makes it work harder*
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urle" anal"0ed appro)imatel" 28 ephedraproducts and found great /ariabilit" in the
amount of acti/e ingredient, not onl" betweenproducts but often within the same brand.
!f a con/entional pharmaceutical compan" hadthis (ind of 3ualit" control, the F@A would shutthem down in a heartbeat, urle" said.
1hough it did not appear on the label, the F@Arecommended that pregnant women, peoplewith high blood pressure, heart conditions or
neurological disorders a/oid ephedra products.
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urle" et al. studied the actual al(aloidcontent of popular ephedra6containing products
and compared it with product labels.
1he" found that=
. most products contained ephedra al(aloids inmar(edl" different 3uantities than labels indicate.
e.g. GEphedraH label indicates I5mg ephedra but
contains onl" 5.84mg total al(aloids.
2. man" products did not contain GnaturalH ephedra.
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7atural ephedra sources contain a mi)ture of allthe al(aloids. an" products contain onl"
ephedrine and pseudoephedrine.
e.g. *erbal Ecstas", @iet -ep, @iet -hen,Energel, *erbal -hen6Fen #onl" E-*$.
Suggests products are spi(ed with s"ntheticsources of E-*, -E-*.
Few products report E-* content on label e/enwhen the" contain substantial 3uantities.
e.g. @iet -ep ma(es no E-* claim but containsJmg>tablet
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Sin#e +-, the FDA has had more than .// reports of side
effe#ts from ephedrine, in#luding heart palpitations,
psy#hosis, heart atta#ks and strokes %ut the &A0 said the
FDA needed to provide better eviden#e to support the
proposed restri#tions
!FDA needs to provide stronger eviden#e on the
relationship between the intake of dietary supplements#ontaining ephedrine alkaloids and the o##urren#e of
adverse rea#tions,! the &A0 said
FDA relied heavily on Adverse 1vents $eports without
providing its usual follow2up investigation, the &A0 said
"he &A0 report is #onsidered a vi#tory for dietary
supplements
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*ow strong is the e/idence that ephedra productswere dangerous
;;6;;;, F@A collected more than 488 reportsof ad/erse e/ents, :8 fatal, that were GassociatedHwith use of ephedra.
!ndustr" claimed association does not pro/ecause6and6effect. !f use of ephedra productsreduces obesit" #which causes prematuredeath$, what if it sa/es more li/es than it causes
1his is a reasonable point so the F@A GhiredH*aller and Benowit0 to re/iew 48 ad/erse e/entreports submitted to the F@A ;;I6;;
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1he" found that of those cases, K weredefinitel" or probabl" related to ephedra, Kwere possibl" related, and IK were unrelated#2K no wa" to 'udge$.
Found that common theme in most seriousad/erse e/ents was combination of ephedra,caffeine and e)ercise.
ost e/ents were cardio/ascular and usuall"
in/ol/ed cerebral hemorrhage, stro(e, or !.
1"pical culprit was ele/ated blood pressure.
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E/idence has also shown ephedra plus caffeine to besomewhat effecti/e and #ma"be$ safe for promoting weightloss in clinical trials.
Boo0er et al.= : wee(s of E?C supplementation promoted2.K loss in bod" fat with minor side effects.
Boo0er et al.= also reported a 6month clinical trial with nosignificant ad/erse e/ents.
olnar et al.= o/erweight children, 28 wee(s with E?C
obser/ed .K decrease in bod" fat with no side effects.
reenwa" et al.= E?C was more cost effecti/e treatmentfor reducing weight, cardiac ris(, and L@L cholesterolthan se/eral weight loss drugs.
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!n 2888, college football pla"ers died undercircumstances that suggested a lin( with ephedra.
1he most highl"6publici0ed casewas death of Baltimore pitcherSte/e Bechler in spring training
2882. !t sto(ed the fires in call forbanning of ephedra6containingproducts.
Ephedra was banned inminor6league baseball
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1)perts, Senator 3riti#i(e 1phedra, 8>;>82
WAS*!71D7 #A-$ 66 A senator chided the F@A for
not ta(ing some action to bloc( the sales of dietsupplements containing ephedra, an herb that hasbeen lin(ed in man" reports with heart attac(s, highblood pressure and e/en death.
Sen. +ichard @urbin, @6!ll., chairing a Senatesubcommittee hearing, said 1uesda" that e/enthough there ha/e been thousands of reports lin(ing
ephedra with serious medical complications,companies continue to sell it to children and theF@A has ta(en little action.
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!n the spring of 2884, the F@A #finall"$ bannedthe sale of ephedra6containing dietar"supplements in the .S. mar(et.
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So caffeine ? ephedra has some efficac" but safet" isan issue. E)ercise ? EC is potentiall" lethal.
What other supplements promote fat reduction
Stimulates lipol"sis% caffeine, ephedra and con'ugated linoleic acid
Bloc(s fatt" acid s"nthesis%h"dro)"citric acid #*CA$
+educe fat absorption from the small intestine
%chitosan
Also grouped into the fat reduction categor" ischromium #!!!$ picolinate, a supplement in/ol/ed in
glucose control.
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Con'ugated linoleic acid #CLA$= !somers of linoleicacid that contain con'ugated double bonds
-rimaril" meat and dair" products #and /egetable oil$
ar(eted as a weight6loss and muscle buildingsupplement.
CLA seems to reduce bod" fat in mice #-ar( et al.$
% a" be through a reduction in energ" inta(eMhowe/er the results were also correlated with a
reduction in growth rate and total bod" protein.
% Dn the other hand a different stud" #@elan" et al.$found fat accumulation and higher protein content
with CLA supplementation.
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!n humans...CLA=
1here are few studies, the" ha/e not been
published in peer6re/iewed 'ournals.
Some studies ha/e shown CLA ma" modestl"increase lean bod" mass and promote fat loss
Dthers show that CLA has no effect on bod"composition in trained or untrained indi/iduals
Suggested that the discrepanc" in the findings isdue to the differences in purit" and ratio ofisomers... Call for more research.
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%4ydro)y#itri# a#id 543A67 Bloc(s fatt" acids"nthesis N ma" suppress appetite
"heory7 N Con/ersion of C*D to fat re3uires p"ru/ate to be
con/erted to acet"l6CoA #inside the mitochondria$
N Fatt" acid s"nthesis re3uires the acet"l group to
be transported from mitochondria to c"tosol N Acet"l group is transported as citrate
N A1-6citrate l"ase clea/es citrate into acet"l6CoAand o)aloacetate #acet"l group enters s"nthesis
pathwa"$
*CA inhibits A1-6citrate l"ase= pre/ents the
con/ersion of C*D to fatt" acids
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*CA is obtained from e)tracts of the herbs arcinia
cambogia and Garcina indica, both nati/e to !ndia.
Animal studies= *CA administered orall" orintra/enousl" inhibits fatt" acid s"nthesis in the li/erand significantl" reduced total bod" fat.
Also lowered food inta(e #appetite suppressant$.
*uman studies= well controlled studies are lac(ing...
Studies ha/e been done with *CA in con'unctionwith other ingredients, which could be acti/eingredients.
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%3hitosan7 @ecreases fat absorption from theintestine
!s a fiber supplement in the form of chitin=e)tracted from the shells of crustaceans.
Functions in one of two wa"s=
N B" binding to bile acids and reducing their
rec"cling bac( to li/er N Binding to the fat in the small intestine anddela"ing digestion>absorption
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Chitosan...contOd.
Animal studies= !n se/en studies conducted inrats, all se/en report that chitosan reduced bloodcholesterol le/els.
– Yet to be determined if there is an effect on body fat
Dne human stud"= irola et al. #;;$ di/idedobese sub'ects into treatment #chitosan, *CA andchromium$ or placebo and had them consume a
h"pocaloric diet #888 (cal$
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irola et al. found that the treatment group lostmore weight than the placebo and that the effectwas dose dependent. Sub'ects also saw a
reduction in total cholesterol and L@L.
When fat absorption is inhibited, fat is eliminated inthe feces.
N @iarrhea N +eduction in calcium absorption and fat soluble
/itamins #especiall" /itamin E$
N +ecommend supplementation of nutrients lost infeces.
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3hromium 5III6 pi#olinate
Acti/e ingredient in o/er 55 supplements #as of
288$... !t is the second largest6selling mineral#Calcium is P$ in the SA. N 7umerous claims ha/e been made that chromium
aids in bod" de/elopment #for athletes$ and in
losing weight #obese indi/iduals$ N Studies ha/e failed to demonstrate chromium helps
with muscle growth or fat loss.
Chromium deficienc" is lin(ed to improper glucosemetabolism b" ma(ing insulin less effecti/e. 1huschromium supplementation AQ help with glucosecontrol in people with 1"pe62 diabetes
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3hromium 5III6 pi##olinate
eta6Anal"sis in 2882 found no association
between chromium and glucose>insulinconcentrations for non6diabetics and inconclusi/eresults in diabetics.
1his stud" was challenged b" Ralman in 288 thatit did not include some significant positi/e findings.
!n addition, chromium #!!!$ piccolinate ma" cause
@7A mutations. !t has also been associated withdecreased iron transport in the blood, (idne" failureand when combined with /itamin C the ris( forad/erse side effects ma" be greater.
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Summar"
Weight loss is dependent on creating an energ"
deficit. 1his can be done two wa"s=. +estricting calories2. E)ercise
Supplements are designed to mimic e)ercise#increase metabolism, promote fat use$ as well asrestrict nutrients from entering the cell for storage.
1he old adage of Gno pain, no gainH usuall" appliesto weight loss strategies with the most effecti/e onebeing a modest reduction in total energ" inta(e incon'unction with e)ercise #aerobic ? resistance$