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Tài liệu Báo cáo khoa học: Analysis of oxidative events induced by expanded polyglutamine huntingtin exon 1 that are differentially restored by expression of heat shock proteins or treatment with an antioxidant ppt

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Tiêu đề Analysis of oxidative events induced by expanded polyglutamine huntingtin exon 1 that are differentially restored by expression of heat shock proteins or treatment with an antioxidant
Tác giả Wance J. J. Firdaus, Andreas Wyttenbach, Chantal Diaz-Latoud, R. W. Currie, André-Patrick Arrigo
Trường học Université Claude Bernard Lyon 1
Chuyên ngành Molecular biology
Thể loại Research article
Năm xuất bản 2006
Thành phố Villeurbanne
Định dạng
Số trang 18
Dung lượng 468,89 KB

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Nội dung

The effects mediated by Hsp overexpression on the formation of inclusion bod-ies were assessed by transient transfection of COS-7 cells with httEx1-72Q-EGFP or httEx1-103Q-EGFP vectors i

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polyglutamine huntingtin exon 1 that are differentially

restored by expression of heat shock proteins or treatment with an antioxidant

Wance J J Firdaus1, Andreas Wyttenbach2, Chantal Diaz-Latoud1, R W Currie1,3

and Andre´-Patrick Arrigo1

1 Laboratoire Stress Oxydant, Chaperons et Apoptose, Centre de Ge´ne´tique Mole´culaire et Cellulaire, Universite´ Claude Bernard Lyon-1, Villeurbanne, France

2 Southampton Neuroscience Group, School of Biological Sciences, University of Southampton, UK

3 Department of Anatomy and Neurobiology, Dalhousie University, Halifax, Canada

Neuronal selective loss and formation of

intraneuron-al protein aggregates are characteristics of

Hunting-ton’s disease (HD), which is one of more than 10

known neurodegenerative disorders caused by

abnor-mally expanded polyglutamine polyQ tracts in the

diseased protein [1] HD is a progressive, autosomal

dominant and hereditary neurodegenerative disorder

that induces a relatively selective loss of neurons in striatum and cortex The mutated gene involved in

HD encodes the 350 kDa huntingtin protein, an iron-regulated neuronal protein implicated in vesicle traf-ficking [2,3] that, if inactivated, results in impairment

of basic cellular processes [4] The mutation is charac-terized by the expansion of CAG triplets 17 codons

Keywords

heat shock proteins; huntingtin polyQ

inclusion bodies; oxidized proteins;

proteasome; reactive oxygen species

Correspondence

A.-P Arrigo, Laboratoire Stress Oxydant,

Chaperons et Apoptose, CNRS UMR 5534,

Centre de Ge´ne´tique Mole´culaire et

Cellulaire, Universite´ Claude Bernard Lyon-1,

43 Blvd du 11 Novembre, 69622

Villeurbanne Ce´dex, France

Fax: +33 472 440555

Tel: +33 472 432685

E-mail: arrigo@univ-lyon1.fr

(Received 16 February 2006, revised

20 April 2006, accepted 12 May 2006)

doi:10.1111/j.1742-4658.2006.05318.x

We recently reported that the transient expression of polyglutamine tracts

of various size in exon 1 of the huntingtin polypeptide (httEx1) generated abnormally high levels of intracellular reactive oxygen species that directly contributed to cell death Here, we compared the protection generated by heat shock proteins to that provided by the antioxidant agent N-acetyl-l-cysteine In cells expressing httEx1 with 72 glutamine repeats (httEx1-72Q), the overexpression of Hsp27 or Hsp70 plus Hdj-1(Hsp40) or treatment of the cells with N-acetyl-l-cysteine inhibited not only mitochondrial mem-brane potential disruption but also the increase in reactive oxygen species, nitric oxide and protein oxidation However, only heat shock proteins and not N-acetyl-l-cysteine reduced the size of the inclusion bodies formed by httEx1-72Q In cells expressing httEx1 polypeptide with 103 glutamine repeats (httEx1-103Q), heat shock proteins neither decreased oxidative damage nor reduced the size of the inclusions In contrast, N-acetyl-l-cys-teine still efficiently decreased the oxidative damage induced by httEx1-103Q polypeptide without altering the inclusions N-Acetyl-l-cysteine was inactive with regard to proteasome inhibition, whereas heat shock proteins partially restored the caspase-like activity of this protease These observa-tions suggest some relaobserva-tionships between the presence of inclusion bodies and the oxidative damage induced by httEx1-polyQ

Abbreviations

DCFH-DA, 2¢,7¢-dichlorofluorescein diacetate; 2,4-DNPH, 2,4-dinitrophenyl hydrazine; EGFP, enhanced green fluorescent protein; FCCP, p-trifluoromethoxy carbonyl cyanide phenylhydrazone; HA, hemagglutinin; HD, Huntington’s disease; HE, dihydroethidine; Hsp, heat shock protein; NAC, N-acetyl- L -cysteine; polyQ, polyglutamine tract; ROS, reactive oxygen species.

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downstream of the initiator ATG in exon 1 (Ex1) of

the 67 exon-containing htt gene [5] Pathogenesis in

HD correlates with the cleavage of mutated htt and

the release of an N-terminal fragment bearing the

mutation that is capable of nuclear localization [6,7]

HttEx1-polyQ N-terminal fragments with repeats of

fewer than 38 glutamine residues are soluble and

harmless, but those with more repeats are toxic and

precipitate as insoluble fibers in affected neurons [8]

In human and HD transgenic mice, the disease

corre-lates with the appearance of intraneuronal,

intranu-clear and perinuintranu-clear aggregates⁄ inclusions containing

the abnormal N-terminal htt fragment [1,9,10]

How-ever, the role of the inclusion bodies is controversial

[8,11,12], since experiments performed in Drosophila

and mouse models have revealed that polyQ proteins

can be toxic even in the absence of detectable

forma-tion of aggregates [13,14] Experiments performed in

tissue culture cell models have revealed that the

pres-ence of inclusion bodies containing polyQ expanded

httEx1 correlates with the toxicity [15,16] but not

with the cell death induced by this polypeptide [17]

This suggests that inclusion bodies may decrease the

risk of cell death and could have a protective role

More recent observations support the hypothesis that

inclusion formation is part of a mechanism that

pro-motes the clearance of mutant protein by activating

autophagy [18,19]

Intracellular aggregates containing ubiquitylated

proteins are a prominent cytopathologic feature of

most neurodegenerative disorders For example,

aggre-gated htt-polyQ in neuronal inclusions of HD mice

and HD patients appears to be ubiquitylated [20] The

accumulation of ubiquitylated abnormal proteins

results in the formation of pathologic aggregates that

perturb the normal physiology of neurons and lead to

proteotoxicity The ubiquitin-26S proteasome system

(UPS), which normally degrades short-lived and

abnormal proteins, is probably recruited to eliminate

the pathologic aggregates formed by ubiquitylated

htt-polyQ [21,22] However, this degradation is likely to

be far from complete [23], because the proteasome

can-not digest polyglutamine sequences and release them

during degradation of polyglutamine-containing

pro-teins [24] This may interfere with proteasome function

and help explain why long polyQ expansions promote

early disease onset

Elevated levels of oxidative damage at the level of

DNA, lipids and proteins are evident in numerous

neu-rodegenerative disorders, including Alzheimer’s disease

and HD, suggesting that oxidative stress is inherent to

these neuronal degenerations [25–29] Recently, we and

others reported that the expression of the expanded

httEx1-polyQ gene product generated mitochondrial complex IV deficiency, elevated reactive oxygen species (ROS) levels and elevated nitric oxide [15,30] levels that directly contributed to cell death It is of interest that the increase in ROS levels was found to correlate with the number of CAG repeats in the httEx1-polyQ polypeptide [15] The mechanism responsible for the appearance of an oxidative stress in response to the presence of aggregated proteins including expanded polyQ peptides is unclear [31,32] Mitochondrial dys-function may participate in this phenomenon, since expression of proteins containing glutamine repeats usually correlates with mitochondrial depolarization [33,34] and impaired clearance of oxidized proteins [35]

Heat shock or stress proteins (Hsps) are expressed in neurons of polyQ diseased brains and have recently been identified as potent inhibitors of polyQ toxicity [16,36–38] In cell models, Hsp70 and Hdj-1(Hsp40) can inhibit self-assembly of polyglutamine proteins into amyloid-like fibrils [39] and are associated with aggre-gates in the brains of HD transgenic mice [40] Hsp70 and Hdj-1 can inhibit polyQ aggregation and reduce the size of htt-polyQ inclusion bodies [15,36,37] and therefore protect against their cytotoxicity Hsp27 is less effective than Hsp70⁄ Hdj-1 in suppressing polyQ aggregation [15] Nevertheless, Hsp27 protects neuronal cells against apoptosis [41,42], oxidative stress [43,44] and polyQ-expanded httEx1-mediated oxidative stress [15]

Several links exist between the proteasome and oxidative stress First, the intracellular redox status is

an important parameter that either upregulates (oxi-dative stress conditions) [45] or downregulates (anti-oxidant conditions) [46] the chymotrypsin-like activity

of the 20S proteasome Second, the 20S proteasome appears to be responsible for the degradation of oxidized proteins [47–51], probably without the need for a ubiquitylation step [52,53] Indeed, relatively mild oxidative stress rapidly (but reversibly) inacti-vates both the ubiquitin-activating⁄ conjugating system and 26S proteasome activity but does not affect 20S proteasome activity [52,54,55] Third, it has been observed that proteasome inhibitors can mimic the effects of oxidative stressors on mitochondrial mem-brane potential and increase cell vulnerability to oxi-dative injury [32] Moreover, Hsps can confer resistance to oxidative stress by preserving some function and attenuating the toxicity of protea-some inhibition [31] It is, however, not yet known if the oxidative stress generated by polyglutamine-con-taining httEx1 polypeptides is due to alterations in proteasome activities

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The analysis presented here was performed in

COS-7 cells because of their very high transfection

efficiency Using transiently transfected COS cells

expressing mutated Ex1 of htt (httEx1-polyQ), we have

compared the protective activity provided by Hsps and

the antioxidant agent N-acetyl-l-cysteine (NAC)

For-mation of inclusion bodies, mitochondrial membrane

potential (DYm), ROS, protein oxidation, iron and

nitric oxide levels as well as proteasome activities were

examined

Results

Hsp overexpression impedes

HttEx1-polyQ-mediated inclusion body formation whereas

treat-ment with the antioxidant agent NAC does not

To compare the oxidative effects induced by

httEx1-polyQ expression, we used monkey kidney COS-7 cells,

which are characterized by a very high yield of

trans-fection efficiency (more than 80%; Fig 1B)

Transfec-tions were performed with either a control vector

(pCIneo-EGFP) expressing enhanced green fluorescent

protein (EGFP) alone, or vectors expressing polyQ

mutants of httEx1 (25 repeats, 25Q; 72 repeats, 72Q;

and 103 repeats, 103Q) fused to EGFP Two days after

transfection, the corresponding polypeptides (denoted

EGFP, 25Q-EGFP, 72Q-EGFP and 103Q-EGFP) were

analyzed in immunoblots probed with anti-EGFP

Figure 1A shows comparable levels of accumulation of

these polypeptides

Two days after transfection, COS-7 cells were also

analyzed by confocal microscopy as described in

Experimental procedures As we previously reported

[15], httEx1-25Q-EGFP polypeptide had a diffuse

cytoplasmic distribution and did not form inclusion

bodies (Fig 1B,Ca) In contrast, httEx1-72Q-EGFP

polypeptide expression resulted in the formation of

perinuclear inclusion bodies in about 55% of the cells

(Fig 1B,Cb,D) The percentage of cells that

dis-played inclusion bodies was up to 80%

follow-ing transfection with httEx1-103Q-EGFP polypeptide

(Fig 1B,Cc,D) In both cases (72Q and 103Q), a

broad distribution of the size of the inclusions was

noticed Moreover, the percentage of cells presenting

inclusions as well as the distribution of the size of the

inclusions were dependent on when the analysis was

performed after transfection Therefore, all the

follow-ing analyses were performed 2 days after transfection

At that time point, the size of the inclusions formed

by either httEx1-72Q-EGFP or httEx1-103Q-EGFP

polypeptide was heterogeneous but averaged around

10 lm

We and others have already reported that the expression of either Hsp70⁄ Hdj-1 or Hsp27 induces protection against httEx1-polyQ-induced cell death [15,56] The Hsp70⁄ Hdj-1 chaperone machine acts by decreasing htt aggregation [39,40], whereas Hsp27, which is less effective than Hsp70⁄ Hdj-1 at reducing aggregation, appears to interfere with cell death through its antioxidant-related properties [15] Hsp overexpression in COS-7 cells was assessed by transient transfection using vectors encoding either Hsp70,

Hdj-1, Hdj-2 or Hsp27 Hdj-2 is an isoform of Hdj-1 that has been previously shown not to decrease htt inclu-sion body formation in COS-7 cells [39] Immunoblot analysis of the intracellular level of Hsps revealed an apparent large increase in the level of 1 and

Hdj-2, whereas the upregulation of Hsp27 and Hsp70 levels was more modest (Fig 1E) The effects mediated by Hsp overexpression on the formation of inclusion bod-ies were assessed by transient transfection of COS-7 cells with httEx1-72Q-EGFP or httEx1-103Q-EGFP vectors in combination with vectors encoding for either Hsp70⁄ Hdj-1 or Hsp27 Forty-eight hours after trans-fection, confocal analysis was performed to analyze the EGFP-containing inclusions Figure 1F shows that the expression of Hsp70 together with Hdj-1 (Hsp40) did decrease the average size of the EGFP-containing inclusion bodies (average size of 10 lm reduced to about 2 lm) formed by httEx1-72Q-EGFP This find-ing is consistent with previous studies that showed a decrease of aggregate⁄ inclusion body formation by these chaperones [39,40,57] Hsp27 overexpression also decreased the size of the inclusions but the effect was less intense (average size of 10 lm reduced to about 4–5 lm) In contrast, the size of the inclusions was not significantly altered by the presence of the antioxidant NAC Concerning the inclusions formed by httEx1-103Q-EGFP, it can be seen in Fig 1F that the overexpression of either Hsp70 + Hsp40 or Hsp27, or treatment with NAC, did not significantly alter their size Similar observations were made when cells were treated with another antioxidant drug, glutathione ethyl ester, instead of NAC (not shown) These results indicate that in COS-7 cells, Hsps are not effective in reducing the size of the inclusions if httEx1 polypep-tide contains 103 CAG repeats

NAC treatment reverses mitochondrial membrane potential (DYm) disruption induced

by httEx1-polyQ but Hsps are only active towards httEx1-72Q

The expression of httEx1-polyQ is known to alter mitochondrial activity, leading to mitochondrial

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membrane potential (DYm) disruption and ROS

production [15,58] The phenomenon was measured in

our cell system to compare the protective effects

medi-ated by Hsps and NAC Analysis of DYm was per-formed in COS-7 cells transiently transfected as described above Forty-eight hours after transfection,

Fig 1 (A–D) Characterization of httEx1-polyQ-EGFP expression in COS-7 cells (A) Immunoblot analysis performed 48 h after transfection of total protein extracts of COS-7 cells transfected with either the pCIneo-EGFP control vector (denoted EGFP) or the same vector bearing either the httEx1-25Q-EGFP (denoted 25Q-EGFP), httEx1-72Q-EGFP (denoted 72Q-EGFP) or httEx1-103Q-EGFP (denoted 103Q-EGFP) coding sequence The immunoblots were probed with anti-EGFP and visualized with ECL as described in Experimental procedures (B) Confocal immunofluorescence analysis of transfected cell population COS-7 cells were transfected with vectors encoding either (a) httEx1-25Q-EGFP, (b) httEx1-72Q-EGFP) or (c) httEx1-103Q-EGFP Forty-eight hours after transfection, cells were fixed and analyzed by confocal microscopy as described in Experimental procedures Bar, 100 lm (C) As (B) but enlarged fields are shown Note the presence of the granules in the cyto-plasm of the cells Bar, 20 lm (D) The percentage of EGFP-containing cells displaying granules is shown The average percentages, including standard deviations calculated from three independent experiments, are shown (E,F) Heat shock proteins (Hsps), but not

N-acetyl-L -cysteine (NAC), decrease the size of httEx1-72Q-EGFP inclusion bodies but are not efficient in decreasing the size of those containing httEx1-103Q-EGFP (E) Immunoblot analysis performed 48 h after transfection of total protein extracts of COS-7 cells transfected with either (a) control vector (pCIneo) or (b) vectors bearing the Hsp70 ⁄ Hdj-1, Hdj-2 or Hsp27 coding sequence The immunoblots were probed with the corresponding antibodies Control of gel loading was performed with anti-actin Immunoblots were visualized by ECL as des-cribed in Experimental procedures (F) Confocal immunofluorescence analysis of COS-7 cells transfected with vectors encoding either httEx1-72Q-EGFP (72Q-EGFP) or httEx1-103Q-EGFP (103Q-EGFP) together with pCIneo vector or vectors bearing the Hsp70 ⁄ Hdj-1 (+ Hsp40 + Hsp70) or Hsp27 (+ Hsp27) coding sequence NAC (2 m M ) was added (+ NAC) to the culture medium 24 h after transfection

of the cells Two days after transfection, cells were fixed and analyzed by confocal microscopy as described in Experimental procedures Bar, 20 lm.

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cells were incubated with the fluorescent probe

MitoTrackertm

Red (CM-H2XRos), and the resulting

red fluorescence was analyzed in a FACS calibur

Cytometer (see Experimental procedures) As seen in Fig 2A, CM-H2XRos fluorescence was not altered

in cells transfected with httEx1-25Q-EGFP vector,

25Q

B

FL2-H

25Q +NAC

72Q

72Q+NAC

103Q

103Q+NAC

FL2-H

FL2-H

Fig 2 Analysis of mitochondrial membrane potential (DYm) and morphology (A) DYm analysis COS-7 cells were transiently transfected with vectors encoding either httEx1-25Q-EGFP (25Q), httEx1-72Q-EGFP (72Q) or httEx1-103Q-EGFP (103Q) Twenty-four hours after trans-fection, cells were treated or not treated with 2 m M N-acetyl- L -cysteine (NAC) Forty-eight hours after transfection, cells were incubated with MitoTracker TM Red CM-H 2 XRos and analyzed by cytometry as described in Experimental procedures The intensity of MitoTracker TM Red fluorescence is shown on the FL2-H axis Black curve, untreated cells; light curve, NAC-treated cells (B) Quantitative analysis of the protect-ive effect of heat shock proteins (Hsps) and NAC against httEx1-polyQ-mediated DYm disruption Transfections were performed with a com-bination of either httEx1-72Q-EGFP or httEx1-103Q-EGFP vectors with those encoding Hsp70 ⁄ Hdj-1 and Hsp27 As in (A), httEx1-103Q-EGFP-expressing cells were treated or not treated with 2 m M NAC COS-7 cells transiently transfected with pCIneo-EGFP vector were also treated for 15 min with 10 l M of the mitochondria uncoupler p-trifluoromethoxy carbonyl cyanide phenylhydrazone (FCCP) before being ana-lyzed Analysis was performed with MitoTracker TM Red CM-H 2 XRos and cytometry was performed as described in (A) The percentage of the cell population with an FL2-H fluorescence greater than 2 · 10 1

was recorded during the FACS analysis The percentage of decrease of DYm was calculated as the ratio of the percentage of cells with FL2-H fluorescence greater than 2 · 10 1 in the samples to that observed in control cells (transfected with pCIneo-EGFP) A representative experiment is presented The data from three independent experiments were used to perform statistical analysis (see Experimental procedures) (C) Electron microscopy analysis of mitochondrial morphology of COS-7 cells transfected with either pCIneo-EGFP vector (pCIneo), httEx1-72Q-EGFP vector (72Q) or httEx1-103Q-EGFP vector (103Q) Transfections were performed with a combination of those encoding Hsp70 ⁄ Hdj-1 (Hsp70 + Hdj-1) and Hsp27 (Hsp27) Cells transfected with httEx1-103Q-EGFP vector were also exposed to 2 m M NAC before being analyzed (as described in the previous figures) Bar, 1 lm.

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whereas it was slightly decreased by the transfection of

httEx1-72Q-EGFP vector This suggests an alteration

of DYm as a consequence of the expression of

httEx1-72Q-EGFP polypeptide A similar effect was noticed

when the experiment was carried out with

httEx1-polyQ-HA vectors [15] encoding httEx1 polypeptides

with 23 or 74 glutamine repeats not fused to EGFP,

but to a hemagglutinin (HA) tag (data not shown)

This control experiment suggests that no significant

green fluorescent spillover or cytotoxicity was induced

by EGFP expression The mitochondrial

depolariza-tion mediated by httEx1-103Q-EGFP expression was

more drastic and was roughly similar to that induced

by a 15 min incubation of control cells with a 10 lm

solution of the mitochondrial depolarizer

p-trifluoro-methoxy carbonyl cyanide phenylhydrazone (FCCP)

(Fig 2B) These observations confirm that, in our cell

system, httEx1-polyQ expression decreases and can

even abolish DYm in a polyQ repeat-dependent

man-ner If, after transfection, cells were treated with NAC

before being analyzed, the fluorescence of

MitoTrack-ertm

Red was almost normal, suggesting that DYm

was not altered Similar observations were made when

cells were treated with glutathione ethyl ester (not

shown) To analyze the effects mediated by Hsp

over-expression on DYm disruption induced by

httEx1-polyQ, COS-7 cells were transiently transfected with

vectors encoding httEx1-72Q-EGFP or

httEx1-103Q-EGFP and either Hsp70⁄ Hdj-1 or Hsp27 As shown in

Fig 2B, in cells expressing httEx1-72Q-EGFP, an

almost complete reversal of the 15% decrease in DYm

was induced by Hsp27 or Hsp70⁄ Hdj-1 expression In

contrast, in cells expressing httEx1-103Q-EGFP, no

significant protective effect of Hsps was detected

against the 65% loss in MitoTrackertm

Red fluores-cence Electron microscopy analysis (see Experimental

procedures) was performed as a control This

experi-ment confirms that COS-7 cells transiently transfected

with vectors encoding either httEx1-72Q-EGFP or

httEx1-103Q-EGFP have mitochondria with damaged

morphology (Fig 2C), a phenomenon not observed in

the presence of NAC In this respect, Hsps were active

only in the case of cells transfected with

httEx1-72Q-EGFP vector In cells expressing httEx1-103Q-httEx1-72Q-EGFP,

the presence of Hsps did not restore normal

morphol-ogy of the mitochondria (Fig 2C)

This suggests that ROS are probably responsible for

the DYm disruption and damage to mitochondrial

morphology in httEx1-72Q-EGFP-expressing or

httEx1-103Q-EGFP-expressing cells In contrast,

httEx1-25Q-EGFP expression did not alter DYm

(Fig 2A) or the morphology of mitochondria (not

shown)

Comparative analysis of the protective effect of NAC and Hsps against ROS, protein oxidation, iron and nitric oxide level upregulation caused

by expanded httEx1 expression DYm disruption usually causes an intracellular burst

of ROS [58] that induce oxidative damage, such as that observed in cells expressing expanded httEx1 [15] Recently, we showed, using different cell lines, inclu-ding COS-7 cells, incubated with the fluorescent probe DCFH-DA, that peroxide production was induced by the expression of httEx1-polyQ-HA polypeptides [15]

An increase in the number of CAG repeats from 23 to

74 correlated with an increase in the oxidation process Here, we have performed similar experiments using the httEx1-polyQ-EGFP vectors described above that con-tain a broader range of polyQ repeats: 25, 72 and 103

As seen in Fig 3A, 48 h after transfection, the fluores-cence of DCFH-DA (see Experimental procedures) increased by 30% in cells expressing httEx1-25Q-EGFP compared to the value observed in cells expres-sing EGFP only An almost two-fold increase (P < 0.001) was then observed in httEx1-72Q-EGFP-expressing cells compared to httEx1-25Q-EGFP-expressing cells The fluorescence index was further increased by about 17% in cells expressing the httEx1-103Q-EGFP polypeptides As shown in Fig 2, cells were treated with NAC before being analyzed to deter-mine if the increase in fluorescence described above was indeed due to ROS accumulation In the presence

of the antioxidant, the fluorescence of httEx1-103Q-EGFP-expressing cells decreased and was roughly similar to that observed in cells expressing httEx1-25Q-EGFP Immunoblot analysis revealed a constant level of expression of httEx1-polyQ-EGFP polypep-tides in the presence of NAC (not shown) and, as shown in Fig 1, NAC did not change the size and EGFP fluorescence of inclusion bodies Similar obser-vations were made in cells treated with glutathione ethyl ester (not shown) We also tested the effects mediated by the pan-caspase inhibitor z-VAD-fmk to verify that the increase in ROS did not arise from the low percentage (about 20%) of cells that underwent apoptosis in response to 48 h of expression of httEx1-polyQ-EGFP polypeptides We have previously reported that z-VAD-fmk completely suppressed httEx1-polyQ-induced death in COS-7 cells [39] As seen in Fig 3A, z-VAD-fmk did not significantly modify the increased fluorescent signal in cells transiently expres-sing httEx1-103Q-EGFP A similar observation was made in the case of cells expressing httEx1-72Q-EGFP (not shown) Hence, upregulation of ROS levels appears to be an intrinsic property of living COS-7

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cells expressing httEx1-72Q or httEx1-103Q

polypep-tides Similar to the use of DCFH-DA, upregulated

fluorescence was detected using dihydroethidine (HE),

a probe that is preferentially oxidized to ethidium bro-mide by superoxide anions O2•–(data not shown) and has a different fluorescent emission wavelength from EGFP (EGFP, 510 lm; HE, 590 lm) Hence, despite the fact that EGFP and DCFH-DA have quite sim-ilar emission wavelengths, it is possible to detect an NAC-sensitive increase in fluorescence that reflects accumulation of intracellular ROS levels in COS-7 cells transiently transfected with httEx1-polyQ-EGFP vectors

To analyze the effects on ROS mediated by Hsp over-expression, COS-7 cells were transiently transfected with vectors encoding httEx1-72Q-EGFP and either Hsp70⁄ Hdj-1 or Hsp27 In control cells transfected with the EGFP vector, the overexpression of Hsp70⁄ Hdj-1 decreased ROS levels slightly but not significantly (Fig 3B) In contrast, overexpression of Hsp27 was more efficient and induced a significant decrease (P < 0.001; Fig 3B) Similar observations were made

by analyzing cells expressing httEx1-25Q-EGFP (not shown), confirming our previous observations that, even

in unstressed cells, Hsp27 transient overexpression can decrease intracellular ROS levels [15,59] We also show here that the effect is specific to Hsp27, since it is not observed in the case of Hsp70⁄ Hsp40(Hdj-1) overex-pression In cells expressing httEx1-72Q-EGFP, the coexpression of Hsp70⁄ Hdj-1 inhibited the mutant htt-induced increase in ROS levels by 65% (P < 0.001) (Fig 3B) Coexpression of Hsp27 also significantly reduced the httEx1-72Q-EGFP-mediated increase in ROS levels (about 35%, P < 0.001) Coexpression of Hsp70⁄ Hdj-1 and Hsp27 together in httEx1-72Q-EGFP-expressing COS-7 cells significantly decreased ROS level upregulation by about 80% (P < 0.001, compared to the cells expressing httEx1-72Q-EGFP)

We also analyzed the activity of the Hsp70⁄ Hdj-1 reconformation machine by cotransfecting COS-7 cells with vectors encoding Hsp70 and the nonactive isoform of Hsp40, Hdj-2 In the presence of Hsp70⁄ Hdj-2, no significant decrease (P > 0.05) in ROS levels was observed However, under these conditions, Hsp27 was still able to decrease ROS levels (30% decrease; P < 0.001) Similarly, coexpression of the Hsp27(C137A) mutant with either Hsp70⁄ Hdj-1 or Hsp70⁄ Hdj-2 was less effective at reducing the ROS levels as compared to wild-type Hsp27 This means that

in httEx1-72Q-EGFP-transfected COS-7 cells, both Hsp70⁄ Hdj-1 and Hsp27 are efficient in buffering the ROS burst generated by httEx1-72Q-EGFP expression, and when all three Hsps were overexpressed, a more intense decrease (P < 0.001) in ROS levels was observed, an effect that was reversed if Hsp27(C137A) mutant was overexpressed instead of wild-type Hsp27

Fig 3 httEx1-polyQ expression enhances reactive oxygen species

(ROS) levels (A) Analysis of ROS induced by httEx1-polyQ

expres-sion COS-7 cells were transfected with either control pCIneo-EGFP

vector (EGFP vector), or vectors encoding httEx1-25Q-EGFP (25Q

EGFP), httEx1-72Q EGFP (72Q EGFP) or httEx1-103Q EGFP (103Q

EGFP) Forty-eight hours after transfection, cells were washed with

NaCl ⁄ P i , and incubated with 2¢,7¢-dichlorofluorescein (DCFH-DA),

and fluorescence was monitored by FACS cytometry as described

in Experimental procedures The fluorescence index was

determined as the ratio of the fluorescence of cells expressing

httEx1-polyQ polypeptides to that of control pCIneo-EGFP

vector-transfected cells A representative experiment is presented As

control, 36 h after transfection, cells transfected with

httEx1-103Q-EGFP were exposed or not exposed to 20 l M z-VAD-fmk before

being analyzed Treatment with 2 m M N-acetyl- L -cysteine (NAC)

was as previously described (B) ROS induced by httEx1-72Q-EGFP

expression in COS-7 cells expressing different sets of heat shock

proteins (Hsps) COS-7 cells were transfected with either control

pCIneoEGFP vector (EGFP vector) or the vector encoding

httEx1-72Q EGFP (httEx1-72Q EGFP) In addition, cotransfections were

per-formed using vectors encoding Hsp70 ⁄ Hdj-1, Hsp70 ⁄ Hdj-2, Hsp27

or mutant Hsp27(C137A) (C) Same as (B), except that cells were

transfected with httEx1-103Q-EGFP vector (103Q EGFP) and that

Hsp27 C137A and Hdj-2 mutants were not analyzed The data from

four independent experiments were used to perform statistical

ana-lysis (see Experimental procedures) In (A) and (B) the asterisks

denote statistical significance when compared with respective

con-trols: *P < 0.05; **P < 0.001.

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The Hsp27(C137A) mutant is characterized by the

sub-stitution of the unique cysteine residue of Hsp27 by an

alanine residue, and is unable to protect against cell

death induced by different agents, including oxidative

stress [15,44,60]

In cells expressing httEx1-103Q-EGFP, the efficiency

of Hsps was less marked, since Hsp70 + Hdj-1

decreased ROS production by 37% and Hsp27 by only

18% (Fig 3C) In contrast, NAC completely abolished

ROS production (Fig 3A)

Hence, these observations support the hypothesis

that the expression of expanded httEx1 and the

pres-ence of httEx1 aggregates⁄ inclusion bodies correlate

with elevated ROS levels, and that NAC and Hsps

have different abilities to counteract this phenomenon

One of the most potent ROS that oxidize

macromol-ecules inside the cell is the hydroxyl radical (OH•),

which originates from the Harber–Weiss⁄ Fenton

reac-tions [61–63] One of the major and easily detectable

oxidative modifications mainly induced by OH• is the

formation of carbonyl residues on amino acid side

chains of proteins [43,64] In order to explore the

abil-ity of httEx1-polyQ to oxidize cellular proteins, we

performed immunoblot detection of protein carbonyl

residues in 2,4-dinitrophenylhydrazine

(2,4-DNPH)-treated extracts of COS-7 cells expressing the different

httEx1-polyQ-EGFP polypeptides (see Experimental

procedures) (Fig 4A) Quantitative analysis of the

oxyblots (in the 10–40 kDa molecular mass range) is

presented in Fig 4B,C As seen in Fig 4A,

httEx1-polyQ-EGFP expression increased the detection of

protein carbonyl residues in cellular polypeptides in a

polyQ expansion size-dependent manner No specific

oxidized protein bands corresponding to the gel

migra-tion of httEx1-polyQ-EGFP polypeptides were

detec-ted, suggesting that httEx1-polyQ-EGFP expression

mainly enhances the oxidation of cellular proteins

(particularly in the 10–40 kDa molecular mass range)

that already display a basal level of oxidation in

con-trol cells Expression of Hsp70⁄ Hdj-1 or Hsp27 did

not significantly change the pattern and level of

oxid-ized proteins in control cells, whereas the

overexpres-sion of these chaperones correlated with a decreased

level of oxidized proteins in response to

httEx1-72Q-EGFP expression (Fig 4A) Analysis of

httEx1-103Q-EGFP-expressing cells revealed that in this case

Hsp70⁄ Hdj-1 or Hsp27 were not efficient in

counter-acting the increased level of protein oxidation In

con-trast, NAC efficiently interfered with the accumulation

of oxidized proteins in httEx1-103Q-EGFP-expressing

cells These observations suggest that elevated levels of

OH• are produced in cells expressing

httEx1-polyQ-EGFP polypeptides

Iron regulates huntingtin polypeptide [2] and cata-lyzes OH• formation through Fenton reactions [61– 63] Since elevated levels of OH• appear to be pro-duced in cells expressing httEx1-polyQ-EGFP poly-peptides, we have analyzed whether the phenomenon correlated with increased levels of Fe(II) The intra-cellular level of Fe(II) was determined (see Experi-mental procedures) in COS-7 cells transfected as described above As seen in Fig 5, the expression of httEx1-25Q-EGFP and httEx1-72Q-EGFP polypep-tides induced only a weak increase in the absorbance

of the ferrozine–Fe(II) complex In contrast, expres-sion of httEx1-103Q-EGFP polypeptide resulted in a 1.7-fold increase in absorbance, which was abolished when cells were cotransfected with vectors encoding either Hsp70⁄ Hdj-1 or Hsp27 or were treated with NAC These observations suggest that the increase in Fe(II) levels observed in cells transiently expressing httEx1-103Q-EGFP polypeptide is a consequence rather than a cause of the deleterious effect generated

by the oxidative stress

Another important parameter of oxidative stress is nitric oxide (NO•) Indeed, elevated levels of NO•have been observed in HD [65] and transgenic HD mice (R6⁄ 2 and R6 ⁄ 1 model) that may contribute to patho-genesis and precede neuronal cell death [66,67] The pathology of NO• results from its reaction with O2•–

to form peroxynitrite (ONOO•–), which can diffuse for several micrometers before decomposing to form the powerful and cytotoxic oxidants OH• and nitrogen dioxide [68] These observations prompted us to ana-lyze NO• levels in COS-7 cells expressing httEx1-polyQ-EGFP polypeptides and to test whether Hsps or NAC could modulate NO•levels

A comparison of NO• levels in COS-7 cells trans-fected with either control or httEx1-polyQ-EGFP vec-tors was performed Figure 6 shows that the transient expression of httEx1-25Q-EGFP did not much change the intracellular level of NO• In contrast, httEx1-72Q-EGFP expression increased the intracellular level of

NO•by about 38% (P < 0.001) The increase was up 52% (P < 0.001) in the case of httEx1-103Q-EGFP expression When the vectors encoding either Hsp70⁄ Hdj-1 or Hsp27 were cotransfected, a small but signifi-cant decrease in the basal level of NO• was observed (P < 0.001) compared to the level observed in COS-7 cells transfected with control EGFP and httEx1-25Q-EGFP vectors When the Hsp-encoding vectors were transfected together with that encoding httEx1-72Q-EGFP, the level of NO• was the same as in control cells (P < 0.001) Under these conditions, both Hsp70⁄ Hdj-1 and Hsp27 expression abolished the increase in NO• level generated by httEx1-72Q-EGFP

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expression Concerning the elevation of NO• induced

by httEx1-103Q-EGFP polypeptide, Hsp70⁄ Hdj-1

overexpression had no significant effects, whereas

Hsp27 reduced the increase in NO•level by more than

50% (P < 0.001) It is of interest that NAC

com-pletely abolished the increase in NO• level generated

by httEx1-103Q-EGFP expression

Analysis of httEx1-polyQ expression with regard

to the three major proteolytic activities of 20S proteasome, a phenomenon partially restored

by Hsp expression but not by NAC Proteasome inhibition is known to induce intracellular protein aggregation and increased carbonyl formation

EGFP vector

A

Control Hsp70/Hdj-1 Hsp27 Control Hsp70/Hdj-1 Hsp27 Control Hsp70/Hdj-1 Hsp27 Control Hsp70/Hdj-1 Hsp27 NA

kDa 54 37

29

20

25Q EGFP vector

72Q EGFP vector

103Q EGFP vector

Fig 4 (A) Oxyblot analysis COS-7 cells were transfected with either control pCIneo-EGFP vector (EGFP vector) or the vector encoding httEx1-25Q-EGFP (25Q EGFP vector), httEx1-72Q-EGFP (72Q EGFP vector) or httEx1-103Q-EGFP (103Q EGFP vector) Cotransfections were performed using the vectors encoding Hsp70 ⁄ Hdj-1 or Hsp27 Forty-eight hours after transfection, cells were lysed and the carbonyl content present in proteins was determined using 2¢,4¢-dinitrophenyl hydrazine (2,4-DNPH) as described under Experimental procedures Quantita-tively equivalent amounts of each fraction were analyzed The immunoblots were probed with anti-DNPH, and gel loading was verified by immunological detection of actin (not shown) Immunoblots were visualized by ECL as described in Experimental procedures The samples from the derivation-control solution (negative controls, see Experimental procedures) were devoid of any signals and are not presented in the figure As a control, 24 h after transfection, cells transfected with httEx1-103Q-EGFP were exposed to 2 m M N-acetyl- L -cysteine (NAC) before being analyzed The arrow indicates the position of the more intensively oxidized polypeptide in the assay The bracket underlines the domain (molecular mass range 10–40 kDa) of the oxyblots that contains the greatest changes in protein oxidation (B) Quantitative analysis

of the oxyblots presented in (A) (see Experimental procedures) The domains of the blots indicated by a bracket (see Fig 4A) were scanned and the signals quantified (see Experimental procedures) This approach was used to avoid the major oxidized protein (about 45 kDa), which shows a rather unaltered signal throughout the experiment The level of protein oxidation (arbitrary units) is presented (C) Protein oxidation index The values in (B) were divided by the value determined for the control cells transfected with the EGFP vector The results from a rep-resentative experiment are shown.

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in proteins [31,69] Hence, we first investigated the

pos-sibility that proteasome inhibition could be responsible

for the oxidative stress mediated by the expression of

httEx1-polyQ-EGFP polypeptides Control

pCIneo-EGFP-transfected COS-7 cells were exposed for 1 h to

10 lm of the proteasome inhibitor lactacystin In these

cells, 80% inhibition of proteasome activities

correla-ted with a 50% increase in ROS levels and with a

1.7-fold increase in the level of oxidized proteins (ranging

between 10 and 40 kDa, as defined above in Fig 4)

(not shown) The oxidative stress induced by

protea-some inhibition therefore seems to be less intense than

that induced by the expression of httEx1-72Q-EGFP

and httEx1-103Q-EGFP polypeptides (see above;

Figs 3 and 4)

We next analyzed the effects mediated by the

expres-sion of the different httEx1-polyQ-EGFP polypeptides

and Hsps as well as those induced by NAC treatment

on the three major proteolytic activities of the 20S

pro-teasome Indeed, Hsps (particularly, Hdj-1⁄ Hsp40) can

confer resistance to oxidative stress by preserving

proteasome function and by attenuating the toxicity

induced by proteasome inhibition [31] To perform this

analysis, COS-7 cells were transiently transfected with

the different vectors encoding httEx1-polyQ-EGFP or

Hsps as described above Forty-eight hours after trans-fection, the chymotrypsin-like activity of the 20S proteasome was determined in cell extracts with fluoro-peptide suc-LLVY-MCA, and the trypsin-like and caspase-like activities were determined using N-boc-LSTR-MCA and N-Cbz-LLEb-NA fluoropeptides, respectively (Fig 7; see Experimental procedures) No alteration of the chymotrypsin-like activity was induced by httEx1-25Q-EGFP expression, and only a slight decrease (about 10%) was induced by httEx1-72Q-EGFP and httEx1-103Q-EGFP expression (Fig 7A) No significant effects were induced by either Hsp70⁄ Hdj-1 or Hsp27 overexpression or NAC treat-ment The trypsin-like activity of 20S proteasome was more altered than the chymotrypsin-like activity, since

a 30% decrease was noticed in httEx1-103Q-EGFP-expressing cells (P < 0.01) Despite a small increase in the trypsin-like activity mediated by Hsp70⁄ Hdj-1 and Hsp27 in control EGFP cells, these chaperones were not effective in restoring the inhibition mediated by

Fig 5 Analysis of intracellular level of iron [Fe(II)] Forty-eight hours

after transfection using the vectors described in Fig 4A, COS-7

cells were washed and scraped off the culture dish in NaCl ⁄ P i

Fol-lowing centrifugation, pelleted cells were used to determine the

Fe(II) level as described in Experimental procedures All samples

contained similar amounts of protein Absorbance of the ferrozine–

Fe(II) complex (AU, arbitrary units) was read at 562 nm The results

for cells treated, as described in the previous figures, with 2 m M

N-acetyl- L -cysteine (NAC) is presented The data from three

inde-pendent experiments were used to performed statistical analysis

(see Experimental procedures) *P < 0.05.

Fig 6 Nitric oxide level determination COS-7 cells were transfected with either control pCIneo-EGFP vector (EGFP vector), or the same vector encoding httEx1-25Q-EGFP (25Q EGFP), httEx1-72Q-EGFP (72Q EGFP) or httEx1-103Q-EGFP (103Q EGFP) Cotransfections were performed using the vectors encoding Hsp70 ⁄ Hdj-1 or Hsp27 Forty-eight hours after transfection, cells were processed for nitric oxide level determination as described in Experimental procedures Cells transfected with httEx1-103Q-EGFP were also exposed to

2 m M N-acetyl- L -cysteine (NAC) before being analyzed (as described

in the previous figures) The data from three independent experi-ments were used to performed statistical analysis (see Experimental procedures) The asterisks denote statistical significance when compared with respective controls: *P < 0.05; **P < 0.001.

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