TAG Metabolism

A) Overview

    1) Fatty Acids (FA) are the principle source of energy for vertebrates.
     a) glycogen supplies glucose for 1 day
     b) protein can metabolized to glucose for 1 week.
     c) Tri acyl glycerol (TAG) can provide FA for energy for 3 months.
    2) Adipose is the primary site of TAG storage
    3) In response to glucagon or adrenaline, TAG is broken into glycerol and FA.
     a) FA provide energy for gluconeogenesis
     b) FA can be metabolized to ketone bodies in place of glucose
     c) glycerol is used as a substrate for the synthesis of glucose.

B) TAG metabolism
    1) Glucagon or adrenalin increases and binds to adipocytes and PK is activated
     a) Hormone Sensitive Lipase (HSL) is phosphorylated
     a1) phosphorylation activates HSL
     a2) HSL activation is the rate limiting step in TAG breakdown
     a3) phosphorylated HSL moves from cytosol to lipid droplet
     b) perilipins (membrane proteins enclosing TAG in lipid bodies) are phosphorylated
     b1) phosphorylation of perilipins disrupts the perilipin shell
     b2) TAG redistributes and becomes accesible to HSL
    2) Activated HSL breaks down TAG

TAG --> FA + Glycerol

     a) glycerol is released to liver because it is not used by adipocytes directly (see 3 below)

    3) FA are retained or released to blood stream based on cellular glucose status
     a) adipocytes require glucose for FA synthesis
     a1) Glycerol 3 phosphate (GlOH 3P) is a key intermediate for FA synthesis
     a2) adipocytes cannot directly phosphorylate glycerol to GlOH 3P
     a3) adipocytes can convert dihydroxy acetone (DHAP) to GlOH 3P
     a4) DHAP is formed in glycolysis so glucose level inside adipocytes is indirectly sensed by the level of GlOH 3P
     c) if GlOH 3P is high
     c1) glucose is high
     c2) FA are reesterified to TAG
     d) if GlOH 3P is low
     d1) glucose is low
     d2) FA arereleased to blood stream

Fatty Acid Oxidation
A) Overview
    1) beta oxidation in occurs in mitochondrial matrix and the peroxisome
    2) FA oxidation generates energy
     a) FADH2
     b) NADH
     c) acetyl CoA
     c1) citric acid cycle
     c2) ketone body synthesis
    3) the Carnitine Cycle transports FA to the mitochondrial matrix and attatches CoA to the chain
     a) Long chain FA and higher (12-20 C) must be transported to mitochondrial matrix using carnitine as a carrier
     b) FA oxidation requires that the FA be linked to CoA before than can be metabolized.
     c) Carnitine is not required for short (1-3C) or medium (4-12C) chain acyl-CoA intermediates entry to matrix
    2) Fatty acid oxidation can occur in several ways
     a) Saturated Even Chain beta oxidation
     a1) 2 carbons removed each cycle as acetyl CoA
     b) Saturated Odd chain beta oxidation
     b1) 2 carbons removed each cycle as acetyl CoA
     b2) terminal 3C chain converted to methylmalonyl CoA which can be converted to succinyl CoA for use in gluconeogenesis
     c) Unsaturated FA beta oxidation
     c1) B-oxidation occurs until unsaturated bond interferes
     c1) double bond is reduced and isomerized
     c2) b oxidation continues
     d) very long chain b-oxidation
     d1) occurs in peroxisomes
     d2) oxidation similar to saturated even chain beta oxidation except O2 is reduced to H2O2 so no FADH2 produced
     d3) Oxidation continues until octanoyl (8C)
     d4) octanoyl enters mitochondria for normal beta oxidation
     e) Branched Chain beta oxidation
     e1) alpha oxidation removes terminal COOH in peroxisomes
     e2) normal beta oxidation resumes
     f) omega oxidation
     f1) occurs in ER
     f2) NADPH and O2 used to form dicarboxylic acid

B) Carnitine Cycle
    1) Acyl CoA sythetase (FA thiokinase) attaches CoA to the FA that will be oxidized
     a) occurs on the outer mitochondrial membrane on the inter mitochondrial space side
     b) two step reaction
     b1) FA is reacted with ATP to form an acyl adenylate intermediate

FA + ATP --> acyl-AM + Ppi

     b2) acyl adenylate intermediate reacts with high energy SH of CoA to form acyl CoA with a high energy thioester bond

Acyl-AMP + CoA --> Acyl-CoA + AMP

     b3) High energy bond required for reaction with carnitine or any FA oxidation
     c) short (1-3C) or medium (4-12C) chain acyl-CoA intermediates do not require Carnitine carrier for entry to matrix

    2) Carnitine Acyl Transferase I (CAT I)- attatches a carnitine to long chain acyl CoA intemediates

AcylCoA + Carnitine --> Acyl-Carnitine + CoA

     a) Oxidation occurs in matrix
     b) long chain FA are transported to matrix by a carnitine carrier
     c) CAT I is inhibited by the key intermediate in FA synthesis: malonyl CoA. If synthesis is on, oxidation needs to be off and visa versa.

    3) Carnitine/Acyl-Carnitine Translocase: transfers Acyl-Carnitine to matrix
     a) Acyl-Carnitine enters matrix and simultaneously
     b) Free carnitine is transported out of matrix

    4) Carnitine acyl transferase II (CAT II): frees FA from carnitine and adds CoA back to FA
     a) on matrix side of inner mitochondrial membrane

Acyl-Carnitine + CoA --> acyl-CoA + carnitine

     b) oxidation requires that CoA is complexed to FA chain
     c) free carnitine is recycled back to inner mitochondrial space for use on CAT I by Carnitine/Acyl-Carnitine Translocase (3 above)

C) Saturated Even Chain Beta Oxidation
    1) 2 carbon units are removed from each acyl-CoA chain as acetyl CoA with each cycle
     a) 1 FADH2 and 1 NADH2 is produced by each cycle
     b) acetyl CoA can enter TCA for metabolism (1FADH2, 3NADH, 1GTP)
     c) Net ATP per Cycle:
     c1) 2xFADH2   4 ATP
     c2) 4xNADH    12ATP
     c3) 1xGTP 1ATP
     c4) Total 17 ATP
     d) for palmityl (C16), 7 cycles (last 4C broken into 2xacetyl CoA so 8 cycles do not occur) occur to produce 8 acetyl CoA

C16 --> 8 acetyl CoA + 7 FADH2 + 7 NADH

     d1) 130 net ATP per C16

    2) There are four general reactions per cycle
     a) Oxidation producing FADH2
     b) Hydration
     c) Oxidation producing NADH
     d) Thiolyis releasing acetyl CoA

    3) Enzymes catalyzing each of the general reactions are specific for chain length and are named with the appropriate prefix.
     a) long (C12-C18)
     b) medium (C4-C12)
     c) short (C4-C6)

    4) FA oxidation is not a significant fuel for all tissues
     a) Since RBCs do not have mitochondria they do not use FA for energy
     b) Brain and nervous tissue do not use FA as significant fuel source

    5) Specific Reactions
     a) acyl CoA dehydrogenase (CAD)- oxidation

acyl-CoA + FAD --> enoyl-CoA + FADH2

     a1) generation of FADH2
     a2) double bond created between alpha and beta carbon
     a3) double bond must be trans to proceed
     a4) defficiency in medium chain length CAD decreases FA oxidation, causes severe hypoglycemia and is the cause of up to 10% of SIDS
     b) enoyl CoA hydratase: hydration

enoyl-CoA + H2O --> beta hydroxy-acyl CoA

     b1) water added across double bond to create alcohol on beta
     c) beta hydroxy acyl CoA dehydrognase: oxidation

beta hydroxy-acyl-CoA + NAD --> beta keto-acyl-CoA + NADH

     c1) NADH generated
     c2) alcohol on beta carbon is converted to a ketone
     d) Acyl CoA acyltransferase: thiolysis

beta keto-acyl-CoA + CoA --> Acyl-CoA (-2C) + acetyl CoA

     d1) acetyl CoA released and new acyl CoA intermediate formed
     d2) final cycle (#7 for C16, 4C step), generates 2 acetyl CoA

D) Saturated Odd Chain beta oxidation
    1) identical to sturated even chain beta oxidation until last cycle
     a) last cycle (#7 for C15) generates a 3 carbon intermediate: propionyl CoA (ProCoA)
     b) ProCoA is converted to Methyl Malonyl CoA (MM CoA)
     c) MM CoA forms Succinyl CoA

    2) the reactions
     a) propionyl CoA Carboxylase: MM CoA formed

ProCoA + HCO3 + ATP --> MM CoA + ADP

     a1) ATP used to add CO2
     b) methyl malononyl CoA mutase

MM CoA --> Succinyl CoA

     b1) requires B12
     b2) because succinyl CoA is part of the citric acid cycle, it can be used for gluconeogenesis
     b3) Net Metabolism in TCA
1 GTP +1ATP
1FADH2   2ATP
1NADH    +3ATP
-1ATP (Formation) -1ATP
total     5ATP
     b4) Net Metabolism of 2 acetyl CoA (even chain)
2GTP 2ATP
6NADH    18ATP
2FADH2   4ATP
     24ATP
     b5) 1 odd chain C less cost 19 ATP

E) Unsaturated FA beta oxidation
    1) identical to beta oxidation of saturated FA until a double bond at C4-C5 occurs
     a) double bond must be eliminated to proceed
     b) double bond is reduced and then isomerized

    2) the reactions
     a) acyl CoA dehydrogenase (CAD)- oxidation

acyl-CoA + FAD --> 2,4 dienoyl-CoA + FADH2

     a1) This is identical to step 1 of saturated FA beta oxidation above except a double bond is also between C4-C5 because the FA was unsaturated
     a2) generation of FADH2
     a3) double bond created between alpha and beta carbon
     b) 2,4 dienoyl reductase: reduction

2,4 dienoyl-CoA + NADPH --> cis-delta3-enoyl CoA + NADP

     b1) NADPH is consumed
     b3) C2-C3 double bond and C4-C5 double bond reduced to form a cis C3 C4 double bond
     c) cis delta3 enoyl isomerase: isomerize

cis delta3-enoylCoA --> trans delta2-enoyl CoA

     c1) cis C3-C4 double bond is isomerized to trans C2-C3 double bond
     c2) this is the identical intermediate to that generated in step 1 (CAD) of sturated b oxidation.
     d) Hydratase, Dehydrogenase, and Thiolysis cycle resumes identical to that in saturated FA beta oxidation (above)

F) Very Long Chain FA beta oxidation
    1) very long (C14-C20)
    2) occurs in peroxisomes
    3) similar to saturated beta oxidation except:
     a) no FADH2 is produced in first step because e- are transfered to molecular O2 to generate H2O2
     b) peroxisomal beta oxidation continues until octanoyl (8C),     c) after oxidation to octanoyl, the 8C molecule is transported to mitochondria to complete oxidation there
    4) the reactions
     a) acyl CoA oxidase: oxidation

acyl-CoA + O2 --> enoyl-CoA + H2O2

     a1) No FADH2 produced so ATP yield is reduced by 2 for every cycle until 8C compared to mitochondrial beta oxidation. In addition, reducing equivalents (NADH)must be transported into the mitochondria by the glycerol 3 phosphate or malate/aspartate shuttle.
     a2) e- transfered directly to molecular oxygen to form H2O2
     a3) C2-C3 double bond created
     b) enoyl CoA Hydratase: hydration
     b1) similar to mitochondrial beta oxidation
     c) hydroxy enoyl dehydrogenase: oxidation
     c1) similar to mitochondrial beta oxidation
     c2) NADH produced
     d) ketoacyl CoA thiolase: thiol cleavage
     d1) similar to mitochondrial beta oxidation
     e) cycle continues until 8C (octanoyl reached) and 8C is transported to mitochondria to complete beta oxidation

G) Branched chain beta oxidation
    1) Branched chain FA (ie phytanic acid from Chloryphyll) can be metabolized by a slight alteration of very long chain beta oxidation.
     a) "branched" means methyl groups come off of main chain FA, and these methyl groups block beta oxidation
     b) also occurs in peroxisome
     c) Acyl CoA is attatched to long chain by ligase
     d) alpha oxidation removes C terminal COOH
     e) peroxisomal beta oxidation then occurs, so first step is acyl CoA oxidase and no FADH2 is produced.
     f) last step of each cycle releases propionyl CoA not Acetyl CoA
    2) the reactions
     a) long chain FA acyl CoA ligase: attatches CoA to phytanic acid

phytanic acid + CoA + ATP --> phytanoyl CoA + AMP + Ppi

     b) SCP2: alpha oxidation remoces C terminal COOH group
     b1) step 1

phytanoyl CoA + 1/2 O2 --> pristanal + formyl CoA

     b2) step 2

pristanal --> pristanic acid

     b3) Refsums disease: alpha oxidation step does not occur, phytanic acid accumulates causing neurological complications.

     c) pristanic acid undergoes peroxisomal beta oxidation. Enzymes carry out similar reactions, their names are different to reflect the substrate they work on.
     c1) pristanoyl CoA oxidase: oxidation no FADH2
     c2) pristenoyl CoA hydratase: hydration
     c3) 3-hydroxy pristanoyl CoA dehydrogenase: oxidation and NADH produced
     c4) 3-ketopristanoyl CoA thiolase: thiol cleavage -Last step eleases propionyl CoA not Acetyl CoA
     -propionyl CoA can be converted to Succinyl CoA as shown for odd chain FA beta oxidation.
    

H) Omega Oxidation
    1) Occurs in ER
    2) cytochrome p450 catalyzes the formation of COOH group addition to the omega carbon using molecular oxygen and NADPH.
     --See NADPH usage in hexose monophosphate shunt under glycolysis
    3) dicarboxylic acid formed
    4) omega oxidation of keratins prevents H2O leakage from skin.

Ketone Body metabolism
A) Overview
    1) there are 3 ketone bodies we are concerned with
     a) acetoacetate (AcAc)
     b) beta hydroxy butyrate (B-HB)
     c) acetone
    2) Ketone bodies are made in liver mitochondria
     a) Ketone are normal fuels of respiration
     a1) heart and renal Cortex use AcAc in preference to glucose
     a2) brain can adapt to use AcAc during starvation: 75% of fuel during starvation
     b) liver makes, but cannot utilize ketone bodies because it lacks ketoacid transferase
    3) Ketone body usage
     a) heart and renal cortex prefer AcAc: gluconeogenesis usage in liver decreased, protein utilization spared
     b) brain utilizes AcAc during starvation: gluconeogenesis usage in liver decreased, protein utilization spared

B) Synthesis of Ketone Bodies
    1) When fasting or eating a high fat low carbohydrate diet, liver is synthesizing glucose and metabolizing FA
     a) increased FA in blood stream, increases beta oxidation, which increases acetyl CoA, NADH and ATP
     b) gluconeogenesis converts lactate or alanine to pyruvate and then converts pyruvate to oxaloacetate (OA)
     c) OA can only leave mitochondria as malate or aspartate to enter cytosol.
     d) excess NADH, due to FA metabolism, shunts large levels of OA into malate

OA + NADH --> malate + NAD

     e) OA is depleted in matrix
     f) TCA stops because citrate synthetase can't form citrate without OA and because NADH is still accumulating
     g) Slowed TCA while FA oxidation still making acetyl CoA causes acetyl CoA and NADH to accumulate further
     h) high concentration of acetylCoA and NADH triggers ketone bony synthesis

    2) thiolase: combines 2 acetyl CoA to form acetoacetyl CoA

acetyl CoA + acetyl CoA --> acetoacetyl CoA + CoA

    3) HMG CoA Synthetase generates HMG CoA

Acetyl CoA + acetoacetyl CoA --> HMG-CoA + CoA

     a) HMG = 3 hydroxy 3 methyl Glutaryl
     b) fasting induces the synthesis of HMG CoA synthetase
     c) HMG CoA can lead to steroid metabolism through HMG CoA reductase
    4) HMG CoA Lyase: converts HMG CoA to acetoacetate (AcAc)

HMG CoA --> acetyl CoA + AcAc

    5) AcAc has three different metabolic fates
     a) AcAc enters blood stream
     b) AcAc is reduced to beta hydroxybutyrate (B-HB) by 3 hydroxybutyrate dehdrogenase and enters blood

AcAc + NADH --> B-HB + NAD

     b1) Overall level of NADH/NAD determines the relative amounts of AcAc and B-HB produced (ie high NADH, low NAD, regenerate NAD by forming B-HB)
     b2) humans tend to produce more B-HB than AcAc
     c) AcAc spontaneously decomposes to acetone which enters blood stream

AcAc ---> Acetone + CO2

C) Ketone Body Oxidation
    1) Occurs in cell mitochondria except for liver
    2) KetoAcid transferase (succinyl CoA:AcAc CoA transferase): forms acetoacetyl CoA from succinyl CoA

AcAc + succinyl CoA --> acetoacetyl CoA + succinate

     a) ketoacid transferase is missing in liver so ketone body oxidation does not occur in the liver
    3) Acetoacetyl CoA thiolase: reforms acetyl CoA for use in the TCA

acetoacetyl CoA + CoA --> 2 Acetyl CoA

    4) beta hydroxy butyrate dehydrogenase converts B-HB to AcAc

B-HB + NAD --> AcAc + NADH

     a) AcAc is metabolized through KetoAcid transferase (#2 above)
     b) the production of NADH makes the metabolism of B-HB yield more energy than the metabolism of AcAc.