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[6,30], these analyses were only carried out over the time frame prior to the formation of significant levels of lipid and protein oxidation products i.e.. Minor increases in electrophore

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Glycation and glycoxidation of low-density lipoproteins by glucose and low-molecular mass aldehydes

Formation of modified and oxidized particles

Heather M Knott*, Bronwyn E Brown, Michael J Davies and Roger T Dean†

The Heart Research Institute, Camperdown, Australia

Patients with diabetes mellitus suffer from an increased

incidence of complications including cardiovascular disease

and cataracts; the mechanisms responsible for this are not

fully understood One characteristic of such complications

is an accumulation of advanced glycation end-products

formed by the adduction of glucose or species derived from

glucose, such as low-molecular mass aldehydes, to proteins

These reactions can be nonoxidative (glycation)or oxidative

(glycoxidation)and result in the conversion of low-density

lipoproteins (LDL)to a form that is recognized by the

scavenger receptors of macrophages This results in the

accumulation of cholesterol and cholesteryl esters within

macrophages and the formation of foam cells, a hallmark of

atherosclerosis The nature of the LDL modifications

required for cellular recognition and unregulated uptake are

poorly understood We have therefore examined the nature,

time course, and extent of LDL modifications induced by

glucose and two aldehydes, methylglyoxal and

glycolalde-hyde It has been shown that these agents modify Arg, Lys

and Trp residues of the apoB protein of LDL, with the extent

of modification induced by the two aldehydes being more rapid than with glucose These processes are rapid and unaffected by low concentrations of copper ions In contrast, lipid and protein oxidation are slow processes and occur to a limited extent in the absence of added copper ions No evi-dence was obtained for the stimulation of lipid or protein oxidation by glucose or methylglyoxal in the presence of copper ions, whereas glycolaldehyde stimulated such reac-tions to a modest extent These results suggest that the earliest significant events in this system are metal ion-independent glycation (modification)of the protein component of LDL, whilst oxidative events (glycoxidation or direct oxidation of lipid or proteins)only occur to any significant extent at later time points This carbonyl-stress may facilitate the forma-tion of foam cells and the vascular complicaforma-tions of diabetes Keywords: AGE; atherosclerosis; glycolaldehyde; methyl-glyoxal; protein modification

The correlation between diabetes and cardiovascular disease

(CVD)has been well established [1], although the precise

mechanisms that facilitate the many complications

associ-ated with diabetes, including CVD and cataracts, are poorly

understood Uncontrolled plasma glucose concentrations and the ability of glucose to either oxidatively or nonoxid-atively (covalently)modify proteins have been proposed to

be instrumental in the development of CVD in both the insulin-deficient and insulin-resistant forms of diabetes [2–4] Both free and protein-bound glucose are known to undergo nonenzymatic and enzymatic modifications which can result in the formation of low molecular mass aldehydes such as methylglyoxal (MG), glyoxal, and glycolaldehyde (GA) These aldehydes form adducts with Lys and Arg residues resulting in Schiff base formation, Amadori rearrangements, and the formation of advanced glycation end products (AGEs)[5–9] Thus, reaction of GA with Lys results in the formation of the well characterized AGE carboxymethyllysine whilst reaction of MG with Lys gives carboxyethyllysine [10,11] The levels of these small reactive a-dicarbonyls are known to be elevated in diabetics [12–14] and the accumulation of AGEs has been implicated in the pathogenesis of diabetes and ageing [4,7]

Modification of low-density lipoprotein (LDL)can lead

to alteration of the apoB protein to the extent that it is no longer recognized by the regulated cholesterol-feedback receptors [15] Instead, this modified LDL is taken up via scavenger receptors leading to cholesterol and cholesteryl ester loading of macrophages [16]; this is believed to be the primary step in foam cell formation and the development of

Correspondence to Heather M Knott, Centenary Institute of Cancer

Medicine and Cell Biology, Locked Bag Number 6, Newtown,

Sydney, NSW 2042, Australia.

Fax: +61 2 9565 6101, Tel.: +61 2 9565 6156,

E-mail: h.knott@centenary.usyd.edu.au

Abbreviations: CVD, cardiovascular disease; AGE, advanced

gly-cation end-products; GA, glycolaldehyde; MG, methylglyoxal; LDL,

low-density lipoprotein; DOPA, 3,4-dihydroxyphenylalanine;

m-Tyr, m-tyrosine (3-hydroxyphenylalanine); o-Tyr, o-tyrosine

(2-hydroxyphenylalanine); PTQ, phenanthrenequinone; TOH,

a-tocopherol; FC, free cholesterol; CA, cholesteryl arachidonate;

CL, cholesteryl linoleate; 7K, 7-ketocholesterol; apoB, apolipoprotein

B100; CEO(O)H, cholesteryl ester hydro(pero)xides; REM,

relative electrophoretic mobility.

*Present address: Centenary Institute of Cancer Medicine and Cell

Biology, Newtown, Sydney, Australia.

Present address: University of Canberra ACT 2601 Australia.

(Received 17 February 2003, revised 19 June 2003,

accepted 8 July 2003)

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atherosclerosis [17] Furthermore, the two- to threefold

increase in nonenzymatic glycosylation of serum albumin in

hyperglycaemia has been suggested to alter the antioxidant

(radical scavenging)role of this protein which may, in

concert with increased levels of redox-active copper and iron

levels [18], contribute to the complications of diabetes [19]

In this study the nature, time course, and extent of the

covalent and oxidative changes that occur on LDL particles

exposed to glucose, GA, and MG have been quantified in

order to determine the significance of glycation and

glycoxidation to the pathogenesis of atherogenic

complica-tions related to diabetes

Materials and methods

Materials

All solutions were prepared with nanopure water (Milli Q

system, Millipore-Waters)and treated with washed

Chelex-100 (Bio-Rad)to remove transition metals prior to use [20]

PD-10 columns (Sephadex G-25M)were from Amersham

Biosciences Pre-cast 1% agarose gels were from Helena

Laboratories (Mt Waverly, VIC, Australia) Fatty

acid-free BSA, fluorescamine, MG, GA, glucose, arginine, and

lysine were all from Sigma-Aldrich All other chemicals

were of analytical grade and all solvents were of HPLC

grade

Isolation of LDL

LDL (density 1.019–1.063 gÆmL)1)was prepared from

plasma of fasted, healthy volunteers by density gradient

ultracentrifugation as described previously [21] After

iso-lation, LDL was dialysed against four to five 1 L changes of

degassed NaCl/Pi containing 0.1 mgÆmL)1

chlorampheni-col, filter sterilized, and used immediately in most cases

When necessary, dialysis buffers were supplemented with

1 mgÆmL)1EDTA and the LDL stored until required In

the latter case, EDTA was removed immediately prior to

use by either dialysis (as above)or by passage of LDL

(<2 mL)through two PD-10 columns as per the

manu-facturer’s instructions; NaCl/Pi was used as both the

equilibration and elution buffer Removal of the EDTA

was confirmed by carrying out a small-scale oxidation of

0.4 mgÆmL)1LDL with 10 lMCuSO4for 2–3 h at 37C

After this incubation, a wavelength difference spectrum was

acquired using the control (no copper ion)sample as a

blank Gross changes in the spectrum, particularly the loss

of the carotenoid peak at 450 nm and changes in the

absorbance at 234 nm, were accepted as indicative of

susceptibility to oxidation [22] If such changes were not

observed, the LDL was subject to further dialysis or

rechromatographed Oxidation assays were only performed

using LDL tested in this manner

Data analysis

For the lipid and protein oxidation data, the variation in

absolute data obtained from LDL extracted from different

donors, containing different levels of antioxidants and

pre-existing lipid peroxides and hence different lag phases [22],

made collation of all data impractical This variation results

in differing absolute kinetics, though the trends with each donor were the same Therefore, although all data were analysed, we present here that from a single experiment representative of all with each data point representing the average of two samples and the error bars representing standard deviation (half-range) The protein modification data are presented as mean ± SEM of data from four samples and normalized to the control (no added modifier)

at each time point after initial assessment indicated minimal variation in the zero time raw data Statistics were performed by one-way analysis of variance (ANOVA)with Tukey’s multiple comparison post-test analysis using

GRAPHPAD PRISM (version 3.0a for MacIntosh, GraphPad Software, San Diego, California, USA) For each compar-ison, statistical significance was set at P < 0.05 unless stated otherwise For each of the protein modification assays, control experiments were performed to exclude the possibility that direct interference between the fluorescamine

or phenanthrequinone and either aldehyde contributed to the changes in fluorescence observed

Protein assays LDL protein concentration was measured by the bicin-choninic acid (BCA; Pierce)method using 0.4 mgÆmL)1 BSA as a standard, with incubations performed at 60C for 45–60 min

Glycoxidation of LDL Glucose, MG, and GA stock solutions were prepared immediately prior to use and filter-sterilized EDTA-free LDL was diluted to 350–450 lgÆmL)1 in filter-sterilized NaCl/Picontaining the required concentration of aldehyde and/or copper ions and incubated at 37C under 5% (v/v)

CO2 The screw caps on the incubation vials were loosely fastened to enable oxygen ingress without compromising the sterility of the sample

Lipid extraction and analysis

At the required times, 0.1 mL samples were collected aseptically into tubes containing 10 lL 20 mM EDTA,

10 lL 0.2 mM butylated hydroxytoluene (BHT), and

400 lL nanopure water (or alternatively 0.2 mL sample/

20 lL EDTA/20 lL BHT/300 lL water)and the samples mixed immediately One mL methanol and 5 mL hexane were added and the samples were mixed thoroughly Extracts were stored at )20 C until use Samples were centrifuged at 2060 g for 5–10 min, 4 mL of the hexane layer was removed and evaporated to dryness and the residue was resuspended in 200 lL of isopropanol Lipid content was analysed by reversed-phase HPLC on a Shimadzu system with a Supelco ODS LC 18 column (25· 0.46 cm, 5 lm particle size)and a 2 cm Pelliguard guard column The mobile phase, ethanol/methanol/iso-propanol at 19.7 : 6 : 1 (v/v/v), was degassed immediately prior to use Lipophilic components were separated iso-cratically at 1 mLÆmin)1 over 30 min with the eluent monitored using a diode array UV detector (PDA-M10AVP)set at 205 and 234 nm and a RF-10AXL fluorescence detector (for TOH; k 290 nm and k

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330 nm) Metabolites were quantified by comparison with

standards and expressed as nmolÆmg)1apoB protein

Protein isolation and analysis

Samples (0.5 mL)of the LDL incubations were collected

aseptically into 50 lL 20 mM EDTA and 50 lL 0.2 mM

BHT and mixed thoroughly Samples were subsequently

stored at)20 C before further processing Protein samples

were reduced by addition of 10 lL 10 mgÆmL)1NaBH4and

incubation at room temperature for >30 min The samples

were delipidated by the addition of 100 lL 0.3% (w/v)

sodium deoxycholate, precipitated using 50 lL 50% (w/v)

trichloroacetic acid, and centrifuged at 4000 g for 2 min

After removal of the supernatant, the protein pellet was

washed twice with ice-cold acetone and once with diethyl

ether, with the samples centrifuged (6610 g, 1 min)and the

supernatant discarded after each addition The samples

were then evaporated to dryness and subjected to gas-phase

hydrolysis in Pico-Tag vessels (Waters)containing 1 mL

6MHCl and 50 lL 2-mercaptoacetic acid The vessels were

sealed under vacuum and incubated at 110C overnight

After hydrolysis, the samples were dried, resuspended in

200 lL nanopure water, filtered through 0.22 or 0.45 lm

membranes, and analysed by HPLC

Analysis of oxidized amino acids was performed by

reversed-phase HPLC using UV and fluorescence

detec-tion as described previously [23] Quantificadetec-tion was

performed by integration of peak areas and comparison

with standards Oxidized amino acid levels are expressed

as lmol per mol parent amino acid to account for any

losses during sample preparation o-Tyr data was

con-verted from lmolÆmol)1Tyr to lmolÆmol)1Phe using the

abundance of these amino acids in the apoB100 molecule

(152 Tyr/223 Phe) Preliminary experiments that

quanti-fied the consumption of Tyr under the incubation

conditions used indicated that the (low)loss of Tyr had

negligible impact on this calculation (data not shown)

Previous studies using this methodology have demonstrated

minimal artefactual oxidation during such sample

hand-ling and analysis [23,24]

Relative electrophoretic mobility gels

Samples (10–15 lL)were removed from the LDL

incuba-tions and loaded onto precast 1% (w/v)agarose gels Native

and acetylated LDL (Ac-LDL, prepared as described

previously [25])were loaded as negative and positive

controls, respectively, and the samples were run at 90 V

for 45 min Gels were fixed in 100% methanol (1 min),

stained for 5–10 min with Fat Red 7B (Sigma-Aldrich),

destained for 5–10 min with 70% methanol, and dried at

60C The relative electrophoretic mobility (REM)is

defined as the ratio of the distances travelled by modified

LDL and native LDL

Tryptophan consumption

Samples (0.2 ml)were removed from the LDL incubations,

0.1 vol each of 20 mM EDTA and 0.2 mM BHT were

added, and the volume adjusted to 1 mL with NaCl/Pi Trp

fluorescence was measured on a Perkin Elmer

Lumines-cence LS50B Spectrometer with kex 280 nm and kem

335 nm

Lysine consumption Samples (80 lL)were removed from the LDL incubations and 0.1 vol each of 20 mMEDTA and 0.2 mM BHT and

670 lL borate buffer (pH > 8)were added During vortex mixing, 250 lL 0.15 mgÆmL)1fluorescamine dissolved in acetone was added The fluorescence of these samples, representative of free amine groups, was measured using kex

390 nm and kem475 nm and expressed as a percentage of the zero time value for the control (no added aldehyde/ glucose)samples [26]

Arginine consumption One-tenth vol each of 20 mM EDTA and 0.2 mM BHT were added to 0.25–0.50 mL of the LDL incubation and the volume adjusted to 1 mL with NaCl/Pi Three millilitres

120 lM 9,10-phenanthrenequinone (PTQ; in absolute eth-anol)was added and the reaction initiated by addition of 0.5 mL 2M NaOH with the samples then incubated at

60C for 3 h At both t ¼ 0 and t ¼ 3 h, 0.5 mL samples were removed and the reaction stopped by addition of an equal volume of 1.2MHCl The fluorescence was recorded using kex312 nm and kem392 nm with the Arg-dependent fluorescence calculated as the difference between the t¼ 0 and t¼ 3 h samples [27]

Results

Glucose-mediated oxidation of LDL Lipid oxidation Six different parameters of lipid peroxi-dation were measured (Fig 1A–F) Three concentrations

of glucose representing normal (5 mM), pathological (25 mM), and suprapathological (100 mM)levels with

1 lMCu2+were examined, as well as samples containing

1 lMCu2+alone, 100 mMglucose only, and no additions The zero time levels of all lipids and products correlate well with published plasma data (e.g [28])and are not statistically different between experiments The oxidation

of the lipid moieties of LDL in the presence of glucose and 1 lM Cu2+proceeded slowly with complete destruc-tion of a-tocopherol (TOH; Fig 1A)occurring between

1 and 2 w These results correlate with loss of free cholesterol (Fig 1B, FC), cholesteryl arachidonate (Fig 1C, CA), and cholesteryl linoleate (Fig 1D, CL)

by 2 weeks as well as the accumulation of the cholesterol oxidation product, 7-ketocholesterol (Fig 1E, 7K), to a maximum of 200 nmolÆmg)1 apoB at 4 w Cholesteryl ester hydroxide and hydroperoxide accumulation (Fig 1F, CEO(O)H) was not detected for the Cu2+-containing samples; this presumably reflects the production and subsequent rapid degradation of these unstable products With 100 mM glucose alone and with the incubated control (no addition)samples, oxidation proceeded more slowly than in any of the samples containing 1 lMCu2+

A small acceleration of the rate of oxidation was detected

in the 100 mM glucose samples compared with the controls at 2 and 4 weeks in all the parameters measured,

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with the exception of FC and 7K In these samples, no

conversion of FC to 7K was detected, whilst TOH was

not fully depleted until 7 weeks in the presence of 100 mM

glucose, with a corresponding 84% loss in the control

Due to the lower rate of oxidation of these samples,

accumulation of CEO(O)H was detected and reached a

maximum (170 nmolÆmg)1 apoB)by 4 weeks The small

increases in the rate of oxidation observed in the presence

of 100 mM glucose compared with the controls is

consistent with a very low rate of radical formation in

the absence of added metal ions such as Cu2+ No additive effect of the various glucose concentrations over the rate of oxidation induced by Cu2+ alone was discernible

Protein oxidation and modification The formation of the Tyr and Phe oxidation products, DOPA and o-Tyr, were examined in identical incubations to those described above The levels of these products are shown in Fig 1G and H Zero time levels of DOPA (900 lmolÆmol)1Tyr)and o-Tyr (550 lmolÆmol)1Phe)are in accord with literature data for plasma [23] and not statistically different between prepara-tions By week 2, accumulation of both DOPA (Fig 1G, four- to sixfold increase)and o-Tyr (Fig 1H, seven- to eightfold increase)was evident in all samples containing added Cu2+, independent of the glucose concentration with

no statistically significant change in the two controls The levels of DOPA detected tended towards a decrease at longer incubation times, consistent with the further oxida-tion of this material to undetected indolic materials [29]

To complement the above markers of oxidative damage

to apoB, analysis of the potential loss of other amino acid side chains (Trp, Lys and Arg), that would be expected to be targets of glycation reactions (i.e covalent modification), was quantified The loss of each of these side chains was examined using fluorescence spectroscopy and in each case changes were measured relative to control (no addition) samples Care was taken to eliminate any possible inter-ference from the added reagents As previous data has suggested that glycation reactions are rapid (e.g [6,30]), these analyses were only carried out over the time frame prior to the formation of significant levels of lipid and protein oxidation products (i.e up to 2 weeks, see above)

No evidence was obtained for significant consumption of Trp or Lys residues under any of the incubation conditions studied (data not shown)indicating that neither glucose nor low levels of Cu2+induce significant Trp or Lys modifica-tion Furthermore the absence of any peak shifts in the Trp fluorescence spectra imply only minor, if any, structural changes in the vicinity of these residues, as the fluorescence

of this residue is environment dependent Changes in the level of Arg were detected with high, but not low, concentrations of glucose with this being independent of the presence of added Cu2+ Thus a loss of 67% of Arg residues was detected after 14 days’ incubation with

100 mMglucose when compared with incubated controls;

no significant loss of Trp or Lys residues was detected under these conditions (data not shown)

The relative electrophoretic mobility of the modified LDL particles was also examined using agarose gels, as this technique yields information on the overall net positive charge on the particle (i.e the total contribution of Arg, Lys, and protonated His residues together with the N terminus, relative to Glu, Asp, and the C terminus) Minor increases

in electrophoretic mobility were evident for the samples incubated with low concentrations of glucose (data not shown), though these were only 1.2–1.3-fold greater than native (nonincubated)LDL, and similar changes were detected with the incubated controls These minor changes were Cu2+-independent and consistent with minor extents

of modification of Lys and Arg residues With samples incubated with 100 m glucose for 14 days a small increase

Fig 1 Glucose-mediated oxidation of the lipid and protein moieties of

LDL LDL ( 0.4 mg proteinÆmL)1)was incubated with varying

concentrations of glucose and/or copper ions At the indicated times,

0.2 mL samples were removed and extracted with 1 mL methanol and

5 mL hexane Four millilitres of the hexane fraction was then dried to

completion, resuspended in 200 lL isopropanol, and the levels

(expressed as nmolÆmg LDL protein)1)of TOH (A) , FC (B) , CA (C) ,

CL (D), 7-KC (E), and CEO(O)H (F) were determined by HPLC (see

Materials and methods) Concurrently, 0.5 mL samples were removed,

delipidated, hydrolysed, and the resulting oxidized and parent amino

acids quantified by reversed-phase HPLC The levels of the oxidized

amino acids DOPA (G)and o-Tyr (H)are expressed relative to their

parent amino acids, Tyr and Phe, respectively Each data point

rep-resents the mean (± SD)of two replicates from a single experiment

representative of several Black bars, 100 m M glucose + 1 l M Cu 2+ ;

horizontal striped bars, 25 m M glucose + 1 l M Cu2+; dark stippled

bars, 5 m M glucose + 1 l M Cu 2+ ; light stippled bars, 100 m M glucose

only; white bars, 1 l M Cu 2+ only; diagonal striped bars, control (no

addition)incubations Asterisks indicate the first time point at which

the data becomes statistically different when compared with the t ¼ 0

value.

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in REM was detected but this was not significantly different

from the incubated controls (data not shown) Acetylated

LDL samples run under identical conditions as positive

controls gave REM values of 3–4

MG-mediated oxidation of LDL

Lipid oxidation LDL was incubated with a wide range of

MG concentrations (10 lM)100 mM)in both the absence

and presence of low concentrations of added Cu2+(1 lM)

No evidence for lipid oxidation was obtained up to the

longest time period studied (17 days, data not shown) That

is, there was no change in the level of TOH, no loss of

cholesterol or the cholesteryl esters examined (CA, CL), and

no accumulation of CEO(O)H or 7K (data not shown)

Protein oxidation and modification As the above lipid

data was negative, the generation of DOPA and o-Tyr,

which are radical-mediated products [31,32], was not

examined Protein modification by MG was examined by

quantifying the loss of Trp, Lys, and Arg residues and the

changes in REM using the same incubation conditions as

described above Fig 2 shows the data obtained, expressed

as a percentage of control incubations (no added MG) At

the initial time point there was a significant decrease in the

measurable level of Trp in the presence of 100 mM MG

(P < 0.001)while there was no statistical difference

between any of the other conditions No statistically

significant changes in Trp levels were detected with low

concentrations of MG (10 and 100 lM) With higher

concentrations (10 and 100 mMMG)a significant decrease

in the level of this residue was observed by day 5 (Fig 2A);

this decrease occurred in the absence of added Cu2+but

was dependent on the MG concentration (by 1 day the

difference between 100 mM and 10 mM is significant to

P< 0.01) The concentration of Lys residues was not

significantly different at zero time Significant Lys loss

(Fig 2B)was detected by 1 day in the samples containing

either 100 or 10 mMMG (P < 0.001 relative to all other

samples)and at this time has occurred to a greater extent in

the 100 mMthan in the 10 mMMG samples (P < 0.001),

indicating that that the loss of this residue is dependent on

the concentration of MG In the experiments using 100 lM

MG, loss of lysine was only seen in the samples containing

1 lMCu2+(P < 0.05 relative to other samples)and not

until day 14 (P < 0.01 relative to previous time points)

Whilst this is suggestive of a copper-ion dependence it is not

supported by any of the other data

Modification of Arg residues by MG has also been

quantified and the data obtained is presented in Fig 2C

(expressed relative to control samples at each time point,

with the latter set to 100%) With low concentrations of

MG (10 lM or 100 lM)no significant changes were

observed in the presence or absence of added copper ions,

except with 100 lMMG in the absence of Cu2+from day 5

onwards With higher (millimolar)concentrations, rapid

concentration-dependent loss of this side-chain was detected

even in the absence of Cu2+(P < 0.05 by 1 day for both 10

and 100 mMMG); this is in accord with a previous report

[33] Loss of Arg was particularly rapid, with significant

losses observed immediately after mixing (i.e in the t¼ 0

samples)with the 100 m MG samples (P < 0.01 relative

to other samples at time zero) No additional loss of Arg was observed at later time points For the samples containing 10 mM MG, a significant (P < 0.01)loss of arginine was seen at 1 day with, again, no further losses during the remainder of the time course

As expected on the basis of the above data, changes in the REM of LDL incubated with MG (conditions as above) were detected (Fig 2D) For the sake of clarity, data for native LDL (REM set to 1)and AcLDL (REM > 3)are not shown With 10 lMMG, minor changes occurred after

5 days of incubation and increased at subsequent time points (approximately twofold relative to native LDL by

14 days) More pronounced and more rapid changes were detected with higher concentrations of MG in the absence of added Cu2+

GA-mediated oxidation of LDL Lipid oxidation LDL was incubated with 0, 0.1, or 1 mM

GA with and without added 1 lMcopper ions Fig 3 shows typical data; similar trends were observed with other

Fig 2 MG-mediated modification of apoB LDL ( 0.4 mg proteinÆmL)1)was incubated with 10 or 100 l M MG with and without added 1 l M Cu2+or LDL ( 1 mg proteinÆmL)1)was incubated with

10 or 100 m M MG in the absence of Cu 2+ Trp residues (A)were quantified by fluorescence (k ex 280 nm, k em 335 nm)after dilution in NaCl/P i Lys residues (B)were quantified by fluorescence (k ex 390 nm,

k em 475 nm)after dilution in borate buffer (pH > 8)and derivatiza-tion with fluorescamine Arg residues (C)were quantified by fluores-cence (k ex 312 nm, k em 392 nm)after derivitization with 9,10-phenanethrequinone For further details see Materials and methods Data are means (n ¼ 4)± SEM For REM analysis (D), 10–15 lL samples were loaded onto precast 1% (w/v)agarose gels, subjected to electrophoresis, and the distance migrated relative to native LDL (REM set to 1)calculated Data are expressed as a per-centage of control incubations with no added MG Black bars,

100 m M MG; horizontal striped bars, 10 m M MG; dark stippled bars,

100 l M MG + 1 l M Cu 2+ ; light stippled bars, 100 l M MG; white bars, 10 l M MG + 1 l M Cu2+; diagonal striped bars, 10 l M MG Asterisks indicate the first time point at which the data becomes statistically different when compared with the t ¼ 0 value.

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concentrations of GA (data not shown) No significant

differences were seen for any of the lipid peroxidation

parameters between treated and nontreated samples at the

zero time point By 15 days, the most rapid lipid

peroxi-dation occurred in those samples containing 1 mM GA

supplemented with 1 lM copper ions In this case, TOH

(Fig 1A)and CA (Fig 1C)were completely consumed and

CL (Fig 1D)partly consumed ( 70% and  20%,

respectively)with a concomitant accumulation of

CEO(O)H (Fig 1E) (loss of TOH significant at 7 days,

loss of CA and accumulation of CEO(O)H significant at

12 days, and loss of CL significant at 15 days The two

other Cu2+-containing conditions showed significant

changes in these parameters at day 15, except in the case

of consumption of CL which did not decline at any time

point In no case was there any statistically significant

change in the level of FC (Fig 1B)nor any accumulation of

7K (data not shown) No statistically significant changes

were observed with the Cu2+-free conditions, suggesting

that Cu2+ acts as a catalyst for GA-mediated LDL

oxidation Experiments were performed to exclude the

possibility of GA and Cu2+competing for the same sites on

LDL and therefore interfering with the ability of each agent

to initiate oxidation In these experiments, incubations were

carried out as normal but either the GA or Cu2+were left

out initially and then added after 1 h (an arbitrary time

frame anticipated to enable binding of either oxidant to the

surface of the LDL) In these experiments, the order of preincubation had no impact on the rate or extent of oxidation (data not shown)suggesting that competition for particular sites on the LDL particle was not affecting the extent of lipid oxidation

Protein oxidation and modification As the above experi-ments demonstrated little lipid oxidation at short incuba-tion times, it was expected that protein oxidaincuba-tion might also

be modest This was confirmed by the examination of DOPA and o-Tyr formation as a result of the incubation of LDL with either 0.1 or 1 mMGA with and without added

Cu2+ over 4 days; no significant generation of either material was detected under these conditions (data not shown)

Protein modification was examined in LDL samples incubated with 1, 10, and 100 mM GA alone (with

1 mgÆmL)1 LDL)and 1 mM GA with added Cu2+ (1 lM) The data obtained are presented in Fig 4 and expressed as percentage of control samples (no added GA)

A rapid and extensive loss of Trp fluorescence was detected with high concentrations of GA that was time- and concentration-dependent (Fig 4A)and these changes occurred in the absence of Cu2+; for 10 and 100 mMGA loss of Trp was significant at 1 day, with higher loss of Trp

at this time point occurring in the presence of 100 mMGA For the lower concentrations of GA, losses did not become significant until 7 days when compared with time zero

Fig 3 GA-mediated oxidation of LDL lipids and alpha-tocopherol.

LDL ( 0.4 mgÆmL protein)1)was incubated with 0, 0.1 or 1 m M GA

with and without 1 l M Cu 2+ ; control samples were incubated with

1 l M Cu2+alone At the indicated time points, 0.2 mL samples were

removed and the levels of TOH (A) , FC (B) , CA (C) , CL (D) , and

CEO(O)H (E) quantified as indicated in the legend to Fig 1 Each data

point represents the mean (± SD)of two replicates from a single

experiment representative of several Black bars, 1 m M GA + 1 l M

Cu 2+ ; horizontal striped bars, 1 m M GA; dark stippled bars, 0.1 m M

GA + 1 l M Cu2+; light stippled bars, 0.1 m M GA; white bars,

1 l M Cu2+ Asterisks indicate the first time point at which the data

becomes statistically different when compared with the t ¼ 0 value.

0 1 7 14

Time (days)

0 20 40 60 80 100 120

0 1 7 14

Time (days)

0 20 40 60 80 100 120

0 1 7 14

Time (days)

0 20 40 60 80 100 120

140

0 1 7 14

Time (days)

0 1 2 3 4

5 6 140

A

*

*

*

C

*

B

D

*

*

*

*

*

Fig 4 GA-mediated modification of apoB LDL ( 0.4 mg proteinÆ

mL)1)was incubated with 1 m M GA ± 1 l M copper ions or LDL ( 1 mg proteinÆmL)1)was incubated with 1, 10 and 100 m M GA Quantification of Trp (A), Lys (B)and Arg (C)residues was carried out as described in the legend to Fig 2 The data are mean (n ¼ 4)± SEM REM analysis (D)was carried out as described in the legend to Fig 2 Black bars, 1 mg LDL proteinÆmL)1with 100 m M

GA; horizontal striped bars, 1 mg LDL proteinÆmL)1with 10 m M

GA; dark stippled bars, 1 mg LDL proteinÆmL)1with 1 m M GA; light stippled bars, 0.4 mg LDL proteinÆmL)1 with 1 m M GA + 1 l M

Cu 2+ ; white bars, 0.4 mg LDL proteinÆmL)1with 1 m M GA only Asterisks indicate the first time point at which the data becomes sta-tistically different when compared with the t ¼ 0 value.

Trang 7

Similar behaviour was observed for Lys (Fig 4B) In this

case, an effect of Cu2+could be seen) the high

concentra-tion GA samples, and those containing Cu2+, each showed

statistically significant (relative to zero time)loss of Lys

residues by day 1, while those samples containing 1 mMGA

with no added Cu2+did not show significant loss of Lys

until day 7 The effect of GA on the Arg residues of apoB

is shown in Fig 4C; these data are expressed relative to the

controls at each time point and zero time values of all

samples (data not shown)were compared to exclude the

possibility of interference by GA with the assay In the

presence of 100 mMGA, 50% of the Arg residues were

observed to be lost in the samples examined immediately

after mixing (t¼ 0 samples)and no further loss was

observed at longer time points In none of the other samples

was any statistically significant loss of Arg residues detected

Fig 4D shows the changes in REM for analogous LDL

incubations Native LDL and AcLDL were also examined

but these data are not shown for reasons of clarity; the

values obtained for these materials were within the expected

range (see above) Incubations with 10 or 100 mM GA

showed maximal changes in REM as early as 24 h (up to

4.8-fold increase), with little increase after this time, while

the lower concentrations of GA facilitated small increases

by 24 h ( 1.8-fold)increasing to  2.7-fold by 14 days

These changes in LDL mobility also occurred in the absence

of added copper ions

Discussion

Although there is a direct parallel between increased

blood sugar and the clinical state of diabetes, and

extensive support for the theory that increased oxidative

stress is involved in this pathology [4,7], detailed studies

on the processes of glycation and glycoxidation have not

provided a conclusive causative mechanism (or

mech-anisms)for the damage induced by high glucose

concen-trations It has been clearly established that products of

metal ion catalysed oxidation of glucose and

protein-bound glucose (i.e glycoxidation)can accumulate at

elevated levels on proteins from diabetic patients, as do

products of direct covalent modification (glycation)

[3,4,7] Whether one or both of these processes is

causative in the development of the complications of

diabetes, such as atherosclerosis, is less well established

[4] It is therefore pertinent to establish the relative roles

of both oxidative processes and direct glycation (covalent,

nonoxidative)reactions in the development of

atheroscle-rosis, in particular the modification of LDL which might

promote the formation of lipid-laden (foam)cells in the

artery wall; a hallmark of early atherogenesis Several

studies have reported elevated levels of oxidized- and/or

AGE-modified LDL in diabetic subjects [34–36] and in

human atherosclerotic lesions [37] It has also been

reported that glycoxidized and peroxidized LDL

colocal-ize with the macrophage scavenger receptor [38]

indicat-ing a plausible involvement of the accumulation of AGEs

and increased oxidative stress in this pathology

Further-more, protein-bound sugars have been demonstrated to

generate free radicals (particularly in the presence of

metal ions [39]), which could potentiate further damage,

including lipid peroxidation [40–42], while the

suscepti-bility of LDL to Cu2+-induced oxidation has been shown

to increase in the presence of glucose [43,44]

In addition to the hyperglycaemia seen in poorly controlled diabetic patients, and its potential involvement

in the accumulation of AGEs, a number of studies have examined the role of low molecular mass aldehydes such as glyoxal, MG, and GA These materials are formed both as a consequence of oxidative processes and AGE modifications

of proteins as well as by a variety of nonrelated metabolic processes [45,46] Evidence has been presented for an elevated level of these materials (or products arising from them)in diabetics [47,48] and the presence of antibodies to MG-derivatized proteins in corneal collagen and plasma proteins [49] We have therefore carried out a comprehen-sive analysis of the relative efficacies of glucose and two aldehydes (MG and GA)in inducing lipid and protein oxidation and antioxidant depletion of LDL particles as well as glycation of the apoB protein by measuring specific parameters of these processes As previous workers [44,50,51] have presented data demonstrating that lipid peroxidation and protein modification of LDL by glucose can be dependent on the presence of transition metal ions, studies were also carried out in the presence of low levels of

Cu2+ This transition metal ion dependence may indicate a cooperative effect of glucose and Cu2+as glucose has been reported to increase Cu2+-induced LDL oxidation without affecting oxidation by aqueous peroxyl radicals [52] Glu-cose- and transition metal ion-dependent protein oxidation has also been detected in studies on rat tail collagen as measured by accumulation of the specific protein side chain oxidation products DOPA, m-Tyr, di-Tyr, and Leu and Val alcohols [53]

In the current study it has been shown that the time course of oxidation of antioxidants, lipids, and protein side chains in LDL is slow in the presence of glucose alone, though marginally faster than in control samples with no additions The time course of oxidation was much more rapid in the presence of low concentrations of Cu2+, compared with its absence, but there were no significant differences between the samples treated with Cu2+alone compared with those containing Cu2+ plus any of the glucose concentrations This suggests that the observed reactions are primarily due to oxidation catalysed by Cu2+ alone and that glucose does not play a major role in these reactions over the concentration range studied, the highest

of which is well in excess of that observed even in very poorly controlled diabetics It has been shown that the oxidation of LDL by Cu2+is saturable, due to the limited number of high-affinity Cu2+-binding sites on the LDL particle [54], but the experiments performed here were carried out with Cu2+: LDL ratios ( 1.2 : 1)that are well below the lower threshold of 5–6 postulated by the these workers, and hence the absence of any stimulatory effect of glucose cannot be ascribed to a saturation effect This marginal effect of glucose is in accord with some previous reports which have shown that elevated levels of glucose failed to potentiate the accumulation of the protein oxidation product o-Tyr in skin collagen [55] and urine [56] from diabetics compared with nondiabetics, suggesting that the accumulation of this oxidation product is

unaffect-ed by the level of hyperglycaemia The absence of any effect

of glucose on Cu2+-stimulated oxidation is, however, in

Trang 8

contrast to another recent study which has reported a

stimulatory effect of glucose on Cu2+-mediated LDL

oxidation [44] The latter study used Cu2+: LDL ratios

which were higher that those used in the current study (3 : 1

and 31 : 1)which may account for the observed differences

in behaviour; the lower ratios used in the current study are

likely to be the more physiologically relevant

A similar absence of any stimulatory effect on the

oxidation of the lipid, protein, and antioxidants of LDL,

above that seen with Cu2+alone, was observed with MG

Within this system, even the presence of Cu2+ alone

induced only very limited oxidation In contrast GA, which

is more chemically reactive than either glucose or MG, did

induce the oxidation of lipids and consumption of

a-tocopherol in LDL with this process being GA

concen-tration-dependent although GA in the absence of Cu2+had

little effect No protein oxidation was detected in the Cu2+

plus GA system, suggesting that such oxidation occurs after

the induction of lipid oxidation and potentially as a result of

damage transfer from the oxidized lipids to the protein

component; this possibility was not investigated further

Overall, the oxidation of lipids and protein side chains in

LDL and the depletion of a-tocopherol by glucose and the

two aldehydes examined appears to proceed slowly, even in

the presence of low concentrations of Cu2+

In contrast with the above processes, covalent

modifica-tion (glycamodifica-tion)of LDL has been shown to occur rapidly

with the aldehydes, occur in the absence of added metal

ions, and depend on both the structure of the compound

and its concentration Of the two aldehydes examined,

modification of Trp and Lys was more rapid with GA than

with MG and the loss of Lys appears to occur earlier than

that of Trp in the MG system With GA the loss of these

two amino acids occured too rapidly to determine an order

of reaction Loss of Arg occurred prior to either of these

other amino acids as evidenced by the significant loss of this

residue in the time zero samples that were analysed

immediately after mixing A more extensive loss of Arg

was detected with GA compared with MG at this time point

but again the reactions were too rapid to analyse

statisti-cally Thus with MG the order of depletion of these residues

is Arg > Lys > Trp which is in accord with previous

studies on the reaction of MG with LDL [33], and GA and

MG with Lys and Arg residues on other proteins [6,9,57–

59] Adducts formed with both residues have been identified

on plasma proteins [10,58]

The mechanisms of modification of the Lys and Arg

residues, and the products formed, have not been examined;

it is likely that these reactions proceed by the pathways

outlined previously (e.g [6,9]) The loss of Trp fluorescence

was observed to occur in the absence of added Cu2+

Whether this reflects conversion of Trp to products (e.g via

the kynurenine pathway)or alteration in the local

environ-ment of these (hydrophobic)residues cannot be clearly

differentiated from the current data [60] The observed

alteration of Lys and Arg residues, which are major

contributors (with protonated His side-chains)to the overall

charge of the LDL particle, are mirrored in the observed

changes in the relative electrophoretic mobility of the

modified particles

In contrast with the behaviour of GA and MG, no

modification of either Trp or Lys residues was detected even

with the highest levels of glucose used (100 mM)in either the absence or presence of Cu2+ Limited modification of Arg residues was however detected with high concentrations of glucose with and without added Cu2+ These observations are in accord with a more rapid rate of modification of Arg residues over Lys residues, particularly given the higher concentration of Lys residues over Arg in apoB (356 Lys vs

148 Arg; Swiss-Prot file P04114, residues 28–4563) Fur-thermore, the absence of significant levels of Lys and Trp modification in systems where Cu2+was added, and where significant levels of lipid oxidation were detected (cf the data obtained after 2 weeks of incubation in Fig 1), suggests that modification of these residues by lipid oxidation products does not occur to any significant extent under the conditions used This is in contrast to previous reports which have suggested that lipid oxidation is a major route to the modification of protein side chains such as Lys residues on LDL [50] In accordance with these measure-ments, only small changes were detected in the REM of the glucose-treated LDL particles except with both supra-pathological levels of glucose and long incubation times

It has been established that neither glucose nor MG are effective catalysts of oxidation of the major components of LDL particles in either the presence or absence of added

Cu2+; this inability of MG to initiate LDL oxidation agrees with a previous report [33] In contrast, GA can facilitate lipid peroxidation induced by Cu2+ but is relatively ineffective in the absence of such metal ions These results indicate that the glycoxidation of LDL, as has been suggested previously [52], is transition metal ion-dependent Interestingly, GA, but not MG, can promote oxidation and this is likely to be due to the oxidizable b-hydroxyaldehyde function [– CH(OH)-C(O)-] on this molecule which is not present in MG which contains the corresponding oxidized a,b-dicarbonyl function [i.e (– C(O)-C(O)-)] Reaction of the b-hydroxyaldehyde function with Cu2+is believed to result in the formation of the reduced metal ion Cu+and a radical anion species from the GA (e.g [61]) Further reactions of one or both of these species may give rise to the observed induction of lipid peroxidation Similar reactions cannot occur with MG but are likely to occur, albeit at a much lower rate, with the open-chain form of glucose; the low concentration of this latter species in equilibrium mixtures of glucose anomers is likely to be at least partially responsible for the slow reaction kinetics detected when compared with equimolar amounts of GA [61] In contrast with such oxidative reactions, covalent modification (gly-cation)appears to be a much more rapid and potentially more significant process, particularly as there is controversy regarding the presence of significant concentrations of reactive transition metal ions in the artery wall and in developing atherosclerotic lesions [62–64]

The loss (derivatization, covalent modification)of Lys and Arg residues may be highly pertinent to the biological effects

of modified LDL particles as it has been shown that modification of Lys residues promotes recognition of LDL

by the macrophage scavenger receptor [65,66] The effect of specific modification of Arg residues on LDL particle recog-nition is less well established Preliminary data (B E Brown,

H M Knott, R T Dean and M J Davies, unpublished results)on the uptake of LDL particles modified by GA,

MG, and glucose prepared under similar conditions to

Trang 9

those used in the studies reported here are consistent with the

recognition of GA- (and possibly MG-)modified LDL

particles, but not glucose-modified species, by receptors

present on mouse macrophage-like cells (cf data with other

modified proteins [59,67])and the subsequent accumulation

of lipids (cholesterol and cholesteryl esters, as measured by

HPLC)within these cells These data support a previous

suggestion [68] that covalent modification (glycation), in the

absence of lipid or protein oxidation or antioxidant

consumption, is sufficient for the formation of foam

cells Such carbonyl stress may play a significant role in

the modification of LDL particles both in plasma and in the

intima of the artery wall and may therefore contribute to the

elevated (two- to threefold)levels of atherogenesis observed

in diabetic patients compared with nondiabetic patients

Acknowledgements

This work was supported by the National Health and Medical

Research Council, the Australian Research Council, the Juvenile

Diabetes Foundation International, Diabetes Australia Research Trust,

and the Wellcome Trust B.E Brown gratefully acknowledges receipt

of an Australian Postgraduate Award, administered through The

University of Sydney.

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