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Enhancement of oxidative stress-induced apoptosis by Hsp105ain mouse embryonal F9 cells Nobuyuki Yamagishi, Youhei Saito, Keiichi Ishihara and Takumi Hatayama Department of Biochemistry,

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Enhancement of oxidative stress-induced apoptosis by Hsp105a

in mouse embryonal F9 cells

Nobuyuki Yamagishi, Youhei Saito, Keiichi Ishihara and Takumi Hatayama

Department of Biochemistry, Kyoto Pharmaceutical University, Japan

Hsp105a is one of the major mammalian heat shock proteins

that belongs to the HSP105/110 family, and is expressed at

especially high levels in the brain as compared with other

tissues in mammals Previously, we showed that Hsp105a

prevents stress-induced apoptosis in neuronal PC12 cells,

and is a novel anti-apoptotic neuroprotective factor in

the mammalian brain On the other hand, we have also

demonstrated that Hsp105a is expressed transiently at

high levels during mouse embryogenesis and is found not

only in various tissues but also in apoptotic cells In the

present study, to elucidate the role of Hsp105a during

mouse embryogenesis, we established mouse embryonal F9

cell lines that constitutively over-express Hsp105a

Over-expression of Hsp105a enhanced hydrogen

peroxide-induced apoptosis by enhancing the activation of caspase-3, poly(ADP-ribose)polymerasecleavage,cytochrome crelease and activation of p38 mitogen-activated protein kinase (p38) Furthermore, oxidative stress-induced apoptosis was suppressed by SB202190, a potent inhibitor of p38, in F9 cells These findings indicated that the activation of p38 is an essential step for apoptosis in F9 cells and that Hsp105a enhances activation of p38, release of cytochrome c and caspase activation Hsp105a may play important roles in organogenesis, during which marked apoptosis occurs, by enhancing apoptosis during mouse embryogenesis Keywords: apoptosis; F9 cells; Hsp105; p38 MAPK; oxida-tive stress

Cell death is classified into two major morphologically and

biochemically distinct modes, necrosis and apoptosis [1]

Necrosis is characterized by swelling of organelles and cells,

followed by lysis of the plasma membrane and random

DNA degradation In contrast, apoptosis is a process that is

characterized by cell shrinkage, plasma membrane blebbing,

nuclear condensation and endonucleolytic cleavage of DNA

into fragments of oligonucleosomal length, and is a

funda-mental and indispensable process during normal embryonic

development, tissue homeostasis and regulation of the

immune system [2–4] In addition, environmental stresses

such as heat shock, radiation, chemical agents and oxidative

stress can also induce apoptosis

Heat shock proteins (Hsps) are a set of highly conserved

proteins that are induced in response to physiological and

environmental stress, and are classified into several families

on the basis of their apparent molecular weights, such as

HSP105/110, HSP90, HSP70, HSP60, HSP40 and HSP27

[5,6] Several studies have shown that Hsp70, Hsp90 and

Hsp27 protect against cell death through apoptosis by a

variety of stressors, such as heat shock, oxidative stress and

chemotherapeutic agents [7–9] In addition, recent studies

have demonstrated that Hsp70, Hsp90, Hsp60 and Hsp27

can modulate the functions of several major components of apoptotic processes, including the caspase cascade and the c-Jun N-terminal kinase (JNK) signalling pathway [10–19]

We have previously characterized two heat shock pro-teins, Hsp105a and Hsp105b, which belong to the HSP105/

110 family and are expressed in various mammals including human, mouse and rat [20–22] Hsp105a is a constitutively expressed 105-kDa stress protein and is induced by a variety

of stressors, whereas Hsp105b is an alternatively spliced form of Hsp105a that is specifically induced by heat shock at

42C These proteins exist as complexes associated with Hsp70/Hsc70 [23,24], and negatively regulate Hsp70/Hsc70 chaperone activity [25] In addition, our recent study demon-strated that Hsp105a protects neuronal cells against the apoptosis induced by various stresses [26] On the other hand, we have shown previously that the level of Hsp105a increases transiently in most tissues of mouse embryos from gestational day 9–11, and that Hsp105a is localized not only

in various tissues, but also in apoptotic cells and apoptotic bodies at the interdigital regions of limbs, suggesting that Hsp105a may play important roles in apoptosis dur-ing mouse embryogenesis [27]

In the present study, to examine the role of Hsp105a during mouse embryogenesis, we established mouse embry-onal F9 cells that constitutively express Hsp105a, and showed that Hsp105a enhanced the oxidative stress-induced apoptosis at or upstream of p38 mitogen-activated protein kinase (p38) activation

E X P E R I M E N T A L P R O C E D U R E S

Cell culture Mouse teratocarcinoma F9 cells were obtained from the Japanese Cancer Research Resources Bank and maintained

Correspondence to T Hatayama, Department of Biochemistry,

Kyoto Pharmaceutical University, 5 Nakauchi-cho, Misasagi,

Yamashina-ku, Kyoto 607-8414, Japan.

Fax: + 81 75 595 4758, Tel.: + 81 75 595 4653,

E-mail: hatayama@mb.kyoto-phu.ac.jp

Abbreviations: HSP, heat shock protein; JNK, c-Jun N-terminal

kinase; PARP, poly (ADP-ribose) polymerase; Ac-DEVD-pNA,

N-acetyl-Asp-Glu-Val-Asp-p-nitroanilide.

(Received 19 March 2002, revised 19 June 2002,

accepted 11 July 2002)

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in Dulbecco’s modified Eagle’s minimal essential medium

(Nissui Pharmaceutical) supplemented with 10% foetal

bovine serum (Life Technologies) in a humidified

atmo-sphere of 5% CO2in air at 37C To induce cell

differen-tiation, cells grown on collagen-coated culture dishes were

incubated in the presence of 100 nMretinoic acid or 1 mM

dibutyryl-cAMP/100 nMretinoic acid at 37C for 6 days

Cell morphology was examined using a difference

interfer-ence contrast microscope

Construction of mouse Hsp105a expression plasmid

and isolation of Hsp105a-over-expressing cells

Plasmid pcDNA105a was u sed to express mou se Hsp105a

in F9 cells To construct this plasmid, the mouse Hsp105a

cDNA derived from pB105-1 plasmid [21] was subcloned

into EcoRV–XbaI sites of the mammalian expression vector

pcDNA3 (Invitrogen)

F9 cells were transfected with pcDNA105a or pcDNA3

empty vector by lipofection using Superfect reagent (Qiagen)

according to the manufacturer’s instructions Forty-eight

hours after transfection, the cells were maintained in

complete medium containing 400 lgÆmL)1 geneticin (Life

Technologies) for 3 weeks to select geneticin-resistant cells

The surviving cell clones were isolated, grown in complete

medium containing 200 lgÆmL)1geneticin, and the

expres-sion levels of Hsp105a were analysed by Western blotting

using anti-mouse Hsp105 Ig [28]

Oxidative stress treatment

Cells were grown exponentially on culture dishes at 37C

for 24 h and then treated with 0.25–2 mM hydrogen

peroxide in NaCl/Picontaining 0.9 mMCaCl2and 0.5 mM

MgCl2at 37C for 30–60 min, washed with NaCl/Piand

further incubated in fresh medium at 37C for 24 h

Cell viability assay

After stress treatment, cells were incubated in medium

containing 50 lgÆmL)1neutral red at 37C for 3 h, then

fixed with 1% formaldehyde containing 1% CaCl2 for

1 min The dye incorporated into viable cells was extracted

with 50% ethanol containing 1% acetic acid, and

absorb-ance at 540 nm was measured

DNA fragmentation analysis

DNA fragmentation was analysed essentially as described

by Ishizawa et al [29] Cells were lysed at 37C for 30 min

in 200 lL lysis bu ffer (10 mM Tris/HCl pH 8.0, 150 mM

NaCl, 10 mM EDTA, 0.1% SDS, 0.5 mgÆmL)1

ribonuc-lease A, 0.5 mgÆmL)1 proteinase K), and the cell lysates

were mixed with 300 lL NaI solu tion (6M NaI, 10 mM

Tris/HCl pH 8.0, 13 mMEDTA, 0.5% sodium

N-lauroyl-sarcosine, 30 lgÆmL)1glycogen) and incubated at 60C for

15 min An equal volume of isopropanol was added to the

mixtures, which were shaken vigorously and kept for

15 min at room temperature After centrifugation at

15 000 g for 15 min, the precipitate was washed successively

with 50% and 100% isopropanol, dried in air, and resolved

in Tris/HCl/EDTA buffer (10 mMTris/HCl pH 8.0, 1 mM

EDTA) Aliquots of 5 lg of DNA were electrophoresed on

2% agarose gels and stained with 1 lgÆmL)1 ethidium bromide

Morphological examination of apoptotic cells Cells were plated onto coverslips at a density of 1· 105 cellsÆcm)2and grown at 37C for 24 h After treatment, cells were washed with NaCl/Pi, fixed with 3.7% formalde-hyde for 30 min at room temperature, and stained with

10 lMHoechst 33342 for 10 min in the dark After washing with NaCl/Pi, the stained cells were observed using a fluorescence microscope (Zeiss) Cells were scored as apoptotic if they displayed nuclear fragmentation and/or chromatin condensation

Assay for poly (ADP-ribose) polymerase (PARP) cleavage Cells (1· 106 cells) were lysed with 200 lL lysis bu ffer (50 mMTris/HCl pH 8.0, 150 mMNaCl, 1% NP-40, 0.1% SDS, 5 lgÆmL)1aprotinin, 5 lgÆmL)1leupeptin, 2 lgÆmL)1 pepstatin A, 1 mMphenylmethanesulfonyl fluoride) on ice for 1 h The lysate was then sonicated for 10 s and centrifuged at 20 000 g for 15 min at 4C The supernatant was recoverd as the cell extract Aliquots (20 lg protein) of cell extracts in SDS sample buffer containing urea (62.5 mM Tris/HCl pH 6.8, 6Murea, 10% glycerol, 2% SDS, 5% 2-mercaptoethanol, 0.00125% Bromophenol blue) were sub-jected to 7.5% SDS/PAGE, then transferred onto nitrocel-lulose membranes by electrotransfer The membranes were blocked with 10% skim milk in NaCl/Tris (20 mMTris/HCl

pH 7.6, 137 mMNaCl) containing 0.1% Tween 20 (NaCl/ Tris/Tween), and incubated with anti-PARP Ig (Santa Cruz) Then, the membranes were incubated with horse-radish peroxidase-conjugated anti-rabbit IgG, and the antibody–antigen complexes were detected using the ECL-Western blot detection system (Amersham Pharmacia Biotech)

Measurement of caspase-3 activity Caspase-3 activity was measured using the colorimetric CaspACE assay system according to the manufacturer’s instructions (Promega) Briefly, cells (1· 106 cells) were suspended in 50 lL cell lysis buffer on ice for 10 min, and lysed by freezing and thawing After centrifugation at

20 000 g for 20 min at 4C, the supernatants were recov-ered as cell extracts Cell extracts (50 lg protein) were incubated in caspase assay buffer (100 mMHepes pH 7.5,

10 mM sucrose, 0.1% Chaps, 10 mM dithiothreitol) con-taining 200 lM N-acetyl-Asp-Glu-Val-Asp-p-nitroanilide (Ac-DEVD-pNA) at 25C for 2 h, and then absorbance

at 405 nm was measured using a microplate reader Release of cytochromec from mitochondria Release of cytochrome c was analysed essentially as des-cribed by Yano et al [30] Briefly, cell suspensions were mixed with an equal volume of 100 lgÆmL)1digitonin in NaCl/Pi, and incubated at 25C for 5 min After centrif-ugation at 15 000 g for 2 min, supernatants were recovered

as cytosolic fractions Pellets were dissolved in NaCl/Pi containing 0.5% Triton X-100, and centrifuged, then supernatants were recovered as mitochondrial fractions

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Both fractions were subjected to 15% SDS/PAGE, and

analysed by Western blotting using anti-cytochrome c Ig

(Santa Cruz)

Activation of JNK and p38

Phosphoryled JNK and p38 were detected by Western

blotting using PhosphoPlus JNK (Thr183/Tyr185) and

PhosphoPlus p38 (Thr180/Tyr182) antibody kits (Cell

Signaling Technology, Inc.), respectively Cell extracts

(20 lg protein) were separated by SDS/PAGE (10%

polyacrylamide), and analysed by Western blotting using

phosphorylation state-specific anti-JNK Ig or anti-p38 Ig

Then, the membranes were incubated at 50C for 30 min in

stripping buffer (62.5 mM Tris/HCl pH 6.7, 2% SDS,

100 mM2-mercaptoethanol), and total JNK or p38 on the

same membranes were detected using JNK Ig or

anti-p38 Ig, respectively

Kinase activity of p38 was assayed by its ability to

phosphorylate MAPKAPK-2 Cell extracts (20 lg protein)

were separated by SDS/PAGE (10% polyacrylamide), and

analysed by Western blotting using phosphorylation

state-specific anti-(MAPKAPK-2) Ig (Cell Signaling Technology,

Inc.)

R E S U L T S

Characterization of stable transfectants over-expressing

Hsp105a

To determine the role of Hsp105a in embryonal cells, we

established mouse embryonal F9 cell clones that express

Hsp105a at high levels In this study, we used two Hsp105a over-expressing F9 cell lines, S3 and S23, in which the expression levels of Hsp105a were about two-and threefold higher than that in parental F9 cells or controls transfected with empty pcDNA3 vector (V1), respectively (Fig 1A) The growth rates of S3 and S23 cells were not significantly different from those of F9 and V1 cells (Fig 1B) F9 cells can be differentiated toward primitive like and parietal endoderm-like cells by exposure to retinoic acid and dibutyryl-cAMP/retinoic acid, respectively [31,32] Upon exposure

to retinoic acid, S3 and S23 cells showed an enlarged and flattened morphology as seen in F9 or V1 cells, which is characteristic of primitive endoderm-like cells (Fig 1C, e–h) In addition, the Hsp105a over-expressing cells were also induced to differentiate toward parietal endo-derm-like cells by treatment with retinoic acid and dibutyryl-cAMP; they also showed the typical changes

in morphology (Fig 1C, i–l) Thus, over-expression of Hsp105a did not affect cell growth and differentiation toward primitive like and parietal endoderm-like phenotypes in F9 cells

Enhancement of oxidative stress-induced apoptosis

by over-expression of Hsp105a in F9 cells

As Hsp105a is expressed transiently at high levels during mouse embryogenesis and is localized in apop-totic cells [27], we next examined the effects of over-expression of Hsp105a on stress-induced cell death in embryonal F9 cells When F9, V1, S3 and S23 cells were treated with 0.25–1 m hydrogen peroxide for 1 h,

Fig 1 Over-expression of Hsp105a in F9 cells and its effects on growth and differentiation (A) Cell extracts (20 lg protein) from parental F9 cells (F9) and cell clones stably transfected with either pcDNA3 vector (V1) or pcDNA105a (S3 and S23) were separated by SDS/PAGE, and the levels

of Hsp105a were determined by Western blotting using anti-mouse Hsp105 Ig (B) F9 V1, S3 and S23 cells were plated into 35 mm culture dishes at

a density of 1 · 10 4

cells per dish, and cultured for 6 days at 37 C At the indicated times, cell numbers were counted (C) Cells (1 · 10 5

cells per dish) were cultured in the presence of 100 n M retinoic acid (+ RA) or 1 m M dibutyryl-cAMP/100 n M retinoic acid (+ RA/cAMP) at 37 C for

6 days Cell morphology was observed using a difference interference contrast microscope Scale bars ¼ 10 lm.

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S3 and S23 cells were more sensitive to the oxidative

stress than F9 or V1 cells (Fig 2A) Therefore, we

further analysed the hydrogen peroxide-induced cell

death of F9 cells

Cell death is classified into two morphologically and

biochemical distinct modes, apoptosis and necrosis [1]

To characterize the hydrogen peroxide-induced cell

death in F9 cells, we examined whether DNA

fragmen-tation, characteristic of apoptosis, occurred in these cells

As shown in Fig 2B, nucleosomal-length DNA

frag-mentation was observed in the hydrogen

peroxide-treated F9 cells, and the amounts of fragmented DNA

caused by low doses of hydrogen peroxide were

increased in the Hsp105a over-expressing cells as

compared with those in S3 and S23 cells In addition,

apoptotic morphology such as nuclear condensation and

chromatin fragmentation was also prominently observed

by Hoechst 33342 staining in these cells (Fig 3A), and

the rate of apoptotic cells was approximately threefold

higher in the Hsp105a over-expressing cells than in F9

or V1 cells (Fig 3B) However, these morphological

changes were suppressed by treatment with a

cell-permeable caspase inhibitor zVAD-fmk Thus, Hsp105a

was demonstrated to enhance oxidative stress-induced

apoptosis in F9 cells

Over-expression of Hsp105a enhances caspase-3 activity and PARP cleavage after treatment with hydrogen peroxide

A common event in the apoptotic pathway is the activation of caspases These enzymes participate in a cascade that is triggered in response to pro-apoptotic signals and results in cleavage of a set of proteins, resulting in disassembly of the cells Caspase-3 is a major effector caspase, and induces cleavage of several substrate proteins and is responsible for several apoptotic processes

We next assayed caspase-3 activity in extracts from cells treated with oxidative stress As shown in Fig 4A, although caspase-3 activity increased slightly in F9 and V1 cells treated with hydrogen peroxide, its activity was increased markedly in S3 and S23 cells by this treatment

In addition, the activation of caspase-3 was suppressed by the treatment with a cell-permeable caspase inhibitor zVAD-fmk

PARP, a DNA repair-related enzyme, is an important substrate of caspase-3, and is cleaved from a 116-kDa protein to an 85-kDa fragment and inactivated during apoptosis [33,34] Western blotting analysis clearly revealed cleavage of PARP in F9 cells treated with hydrogen peroxide (Fig 4B) Furthermore, in accordance with the

Fig 2 Effects of Hsp105a over-expression on the sensitivityof F9 cells to hydrogen peroxide F9, V1, S3 and S23 cells were exposed to 0.1–1 m M hydrogen peroxide for 1 h, and further incubated for 24 h at 37 C (A) Cell viability was then determined by neutral red assay Experiments were repeated at least three times and essentially the same results were obtained each time (B) DNA was extracted from the cells treated with hydrogen peroxide, and aliquots (5 lg each) of DNA were electrophoresed on a 2% agarose gel and visualized by staining with ethidium bromide.

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enhancement of caspase-3 activity, the cleavage of PARP

by hydrogen peroxide was more intense in S3 and S23 cells than in F9 or V1 cells Thus, over-expression of Hsp105a was shown to markedly enhance the activation

of procaspase-3 during apoptosis induced by hydrogen peroxide

Over-expression of Hsp105a enhances release

of cytochromec from mitochondria after treatment with hydrogen peroxide

In mammalian cells, one of the main pathways that activates caspase-3 is via mitochondria When mitochondria receive appropriate signals from a variety of stresses or are damaged irreversibly, pro-apoptotic molecules such as cytochrome c are released from mitochondria into the cytosol [35–37] In the cytosol, cytochrome c forms a complex with Apaf-1 and procaspase-9, and activates caspase-9, which in turn converts procaspase-3 into its active form, resulting in apoptosis [38–40] We next analysed whether cytochrome c is released from mitochondria in F9 cells by oxidative stress When F9 cells were fractionated into mitochondrial and cytosolic fractions and cytochrome c was examined by Western blotting, a large amount of cytochrome c was found in mitochondria with only a small amount in the cytosolic fraction of control cells under these experimental conditions (Fig 5A) However, although the amounts of cytochrome c released by hydrogen peroxide increased slightly in F9 or V1 cells, the release was increased

to a greater extent in S3 and S23 cells than in control and V1 cells (Fig 5B) Thus, over-expression of Hsp105a seemed to enhance the release of cytochrome c from mitochondria in F9 cells by hydrogen peroxide

Fig 3 Enhancement of oxidative stress-induced apoptosis byover-expression of Hsp105a (A) F9, V1, S3 and S23 cells were grown on coverslips, exposed to 1 m M hydrogen peroxide for 1 h, and further incubated at 37 C for 24 h Ten l M z-VAD-fmk was added to the medium 1 h before treatment Cells were washed with NaCl/P i , fixed with 3.7% formaldehyde, and stained with 10 l M Hoechst 33342 Nuclear morphology of cells was observed using a fluorescence microscope (B) Rates of apoptotic cells were obtained from at least 200 cells in each experiment Data are shown

as the means ± SD of three independent experiments The significance of differences was assessed by unpaired Student’t t-test.

Fig 4 Effects of over-expression of Hsp105a on caspase-3 activity F9,

V1, S3 and S23 cells were exposed to 1 m M hydrogen peroxide for 1 h,

and further incubated for 24 h at 37 C (A) Caspase-3 activity in cell

extracts was measured with caspase-3 substrate, Ac-DEVD-pNA.

Data represent the means ± SD of three independent experiments (B)

Aliquots (20 lg protein) of cell extracts were separated by SDS/

PAGE, and PARP (116 kDa) and the cleaved fragment (85 kDa) were

detected by Western blotting using anti-PARP Ig.

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Over-expression of Hsp105a enhances activation

of p38 after treatment with hydrogen peroxide JNK and p38 pathways are activated by cellular stresses and inflammatory cytokines, resulting in growth arrest and apoptosis, and have been implicated as key regulators of stress-induced apoptosis in many cell types [41,42] Fur-thermore, mitochondria are influenced by proapoptotic signals through the JNK pathway [43] To determine the effects of Hsp105a on JNK and p38 signalling pathways, we examined the activation of JNK and p38 in F9 cells by oxidative stress As shown in Fig 6A, JNK was not activated in control F9 or V1 cells by treatment with hydrogen peroxide In contrast, hydrogen peroxide-treat-ment induced marked activation of JNK within 30 min in S23 cells, but not in S3 cells Therefore, the enhancement of the oxidative stress-induced JNK-activation seemed not to

be solely due to the over-expression of Hsp105a in F9 cells

On the other hand, p38 was activated at low levels within 1–2 h in F9 and V1 cells after treatment with hydrogen peroxide, and the activation of p38 by hydrogen peroxide was enhanced in both S3 and S23 cells compared with F9 and V1 cells (Fig 6B) Thus, over-expression of Hsp105a seemed to enhance the oxidative stress-induced activation of p38 but not JNK in F9 cells

As Hsp105a enhances the activation of p38 induced by oxidative stress, we further examined whether its activation

is responsible for the induction of apoptosis in F9 cells using SB202190, a potent inhibitor of p38 As shown in Fig 7A, although hydrogen peroxide-treatment induced apoptosis in F9 cells as described above, the apoptosis was significantly suppressed by SB202190 Under these conditions, although phosporylation of MAPKAPK-2, a substrate of p38, was enhanced by the hydrogen peroxide treatment, it was suppressed to basal level by treatment with 10 lMSB202190 (Fig 7B) These findings indicate that the activation of p38

is an essential step for induction of apoptosis by hydrogen peroxide, and Hsp105a is suggested to enhance the

oxida-Fig 6 Effects of Hsp105a on activation of JNK and p38 byoxidative stress F9, V1, S3 and S23 cells were exposed to 1 m M hydrogen peroxide for 30 min and further incubated for 0.5, 1 or 2 h at 37 C Aliquots (20 lg protein)

of cell extracts were separated by SDS/PAGE Activated and total JNK or p38 were detected

by Western blotting, as described in Experi-mental procedures (A) JNK, (B) p38 Upper and lower panels represent activated and total JNK or p38, respectively.

Fig 5 Effects of Hsp105a over-expression on release of cytochrome c

from mitochondria F9, V1, S3 and S23 cells were exposed to 1 m M

hydrogen peroxide for 45 min, and further incubated for 24 h at

37 C Cells were then fractionated into cytosolic and mitochondrial

fractions, as described in Experimental procedures (A) Both fractions

were subjected to 15% SDS/PAGE, and analysed by Western blotting

using anti-cytochrome c Ig C, cytosolic fraction; M, mitochondrial

fraction (B) The densities the cytochrome c bands were quantified by

densitometry, and the rates release into the cytosol are shown Data

represent the means ± SD of three independent experiments Filled

bars, untreated cells; open bars, hydrogen peroxide-treated cells.

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tive stress-induced apoptosis at or upstream of p38

activa-tion in F9 cells

D I S C U S S I O N

Hsp105a is expressed in most tissues, but its levels are

especially high in the brain of adult mammals such as rats,

mice and humans [21–23] We have shown that Hsp105a

plays an important role in protection of neuronal cells

against stress-induced apoptosis [26] In accordance with

these findings, ischemia/reperfusion in the rat forebrain

induces the expression of HSP105/110 family proteins,

Hsp105a, APG-1 (testis-specific homologue of Hsp105) and

APG-2 [44,45], and Hsp110 (hamster homologue of

Hsp105a) confers heat resistance on rat fibroblasts and

human epithelial carcinoma cells [46] On the other hand, we

have also shown that the levels of Hsp105a increase

transiently in embryonic tissues during mouse

embryogen-esis, and this protein is localized not only in various tissues,

but also in apoptotic cells and apoptotic bodies at the

interdigital regions of limbs [27] In the present study, to

explore the function of Hsp105a in embryogenesis, we

established mouse embryonal F9 cell lines that constitutively

express Hsp105a Although growth rate and differentiation

of F9 cells were not affected by the over-expression of

Hsp105a, the sensitivity of cells to oxidative stress was

enhanced by the over-expression of Hsp105a, and these

findings were in clear contrast with those in neuronal PC12

cells However, as sensitivity of F9 cells to stresses such as heat shock, etoposide, actinomycin D and serum depriva-tion was also enhanced by over-expression of Hsp105a (unpublished data), the enhancement of cell death by Hsp105a seemed to be a general phenomenon in embryonal F9 cells The present findings together with previous observations in neuronal PC12 cells suggested that Hsp105a has a pro-apoptotic effect in embryonal cells and an anti-apoptotic effect in neuronal cells Thus, these observations provide the first evidence that Hsp105a can function as an enhancer or suppressor of apoptosis depending on the cell type in mammals

Apoptosis is an active process resulting in characteristic morphological changes such as cell shrinkage, condensation

of chromatin and membrane blebbing [2–4] The common pathway of apoptosis involves a family of proteases known

as the caspases, which are activated in a proteolytic cascade

to cleave specific substrates The release of cytochrome c from mitochondria triggers the formation of apoptosome complex with Apaf-1 and pro-caspase-9, and activates caspase-9, which then in turn activates downstream effector caspases such as caspase-3 [38–40] Active caspase-3 cleaves several substrates such as PARP [33,34], and activates death effector molecules or triggers the structural changes char-acteristic of apoptotic cells Here, we showed that over-expression of Hsp105a enhances PARP cleavage, caspase-3 activation and release of cytochrome c from mitochondria

in F9 cells exposed to hydrogen peroxide, and our results

Fig 7 Suppression of oxidative stress-induced

apoptosis in F9 cells bya potent p38 inhibitor.

F9, V1, S3 and S23 cells were grown on

coverslips, treated with or without 10 l M

SB202190 for 1 h before and during the

1 h-treatment with 1 m M hydrogen peroxide,

and further incubated at 37 C for 24 h (A) or

2 h (B) (A) Cells were then washed with

NaCl/P i , fixed with 3.7% formaldehyde, and

stained with 10 l M Hoechst 33342 Nuclear

morphology of cells was observed using a

fluorescence microscope Rates of apoptotic

cells were obtained from at least 300 cells in

each experiment Data are shown as the means

± SD of at least three independent

experi-ments The significance of differences was

assessed by unpaired Student’t t-test (B) Cell

extracts (20 lg proteins) of S23 cells were

separated by SDS/PAGE, and

phosphory-lated MAPKAPK-2 was detected by Western

blotting using anti-phospho-MAPKAPK-2

Ig.

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suggested that Hsp105a enhances the apoptosis at or

upstream of cytochrome c release from mitochondria

Furthermore, the transmission of signals from external

stresses is accompanied by the activation of a family of

stress-activated protein kinases, JNK and p38 Activation of

these signalling pathways leads to apoptosis [41,42], and

mitochondria is influenced by proapoptotic signal

trans-duction through the JNK pathway [43] As the activation of

p38 is an essential step for apoptosis induced by hydrogen

peroxide in F9 cells as shown in Fig 7, Hsp105a was

suggested to enhance the oxidative stress-induced apoptosis

directly or indirectly at or upstream of activation of p38 In

contrast, although Hsp105a prevents the apoptosis induced

by several stresses including hydrogen peroxide in neuronal

PC12 cells, p38 is not activated by these stresses in neuronal

cells [26] The p38 signalling pathway may be a possible

target at which Hsp105a enhances the apoptosis induced by

hydrogen peroxide in embryonal cells

Several Hsps have been shown to modulate the pathway

of apoptosis positively or negatively Hsp60 with or without

Hsp10 directly stimulates apoptosis by promoting the

proteolytic maturation of caspase-3 [17,18] In contrast,

Hsp70, Hsp90 and Hsp27 exert negative influences on

apoptotic signalling In particular, Hsp70 has been shown to

protect against apoptosis by a variety of stressors through

suppression of JNK activation [10–13] and apoptosome

formation [14,15] Interestingly, a recent study

demonstra-ted that the chaperone activity of Hsp70 is required for

protection against heat-induced apoptosis [47] In contrast,

we cannot detect the chaperone activity of Hsp105a, but the

protein exists as complexes associated with Hsp70/Hsc70

[23,24] and suppresses the Hsc70 chaperone activity [25]

Therefore, it is possible that Hsp105a may stimulate

stress-induced apoptosis by negative regulation of Hsp70/Hsc70

chaperone that is required for suppression of apoptosis

In conclusion, we showed here that Hsp105a enhances

apoptosis at or upstream of p38 activation The

apoptosis-enhancing activity of Hsp105a may play important roles in

organogenesis, in which marked apoptosis occurs during

mouse embryogenesis, although further studies are

neces-sary to understand the precise mechanism by which Hsp105a

enhances stress-induced apoptosis

A C K N O W L E D G M E N T S

This study was supported in part by grant from the Ministry of

Education, Science, Sports and Culture of Japan (T H.).

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