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Tiêu đề Hepatic stimulator substance mitigates hepatic cell injury through suppression of the mitochondrial permeability transition
Tác giả Yuan Wu, Jing Zhang, Lingyue Dong, Wen Li, Jidong Jia, Wei An
Trường học Capital Medical University
Chuyên ngành Cell biology
Thể loại Research article
Năm xuất bản 2010
Thành phố Beijing
Định dạng
Số trang 13
Dung lượng 617,6 KB

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The mitochondrial membrane transition and cytochrome c leakage were significantly inhibited in the HSS-expressing cells as compared with the untransfected cells, and, as a consequence, th

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through suppression of the mitochondrial permeability

transition

Yuan Wu1,*, Jing Zhang1,*, Lingyue Dong1, Wen Li1, Jidong Jia2and Wei An1

1 Department of Cell Biology and Municipal Key Laboratory for Liver Protection and Regulation of Regeneration, Capital Medical University, Beijing, China

2 Liver Unit, Beijing Friendship Hospital, Capital Medical University, Beijing, China

Introduction

Hepatic stimulator substance (HSS) is expressed in the

liver cytosol of weanling or partially hepatectomized

adult rats, and was first described by LaBrecque and

Pesch [1] A major function of this protein is to pro-mote hepatocyte proliferation and liver regeneration after partial hepatectomy [1–3] The HSS-mediated

Keywords

apoptosis; hepatic stimulator substance;

mitochondria; mitochondrial membrane

potential; mitochondrial permeability

transition

Correspondence

W An, Department of Cell Biology,

Municipal Key Laboratory for Liver

Protection and Regulation of Regeneration,

Capital Medical University, Beijing 100069,

China

Fax: +86 10 83911480

Tel: +86 10 83911480

E-mail: anwei@ccmu.edu.cn

*These authors contributed equally to this

work

(Received 12 October 2009, revised 18

December 2009, accepted 23 December

2009)

doi:10.1111/j.1742-4658.2010.07560.x

Hepatic stimulator substance (HSS) has been shown to protect liver cells from various toxins However, the mechanism by which HSS protects hepatocytes remains unclear In this study, we established BEL-7402 cells that stably express HSS and analyzed the protective ability of HSS on cells through mitochondrial permeability (MP) After administration of carbonyl cyanide m-chlorophenylhydrazone (CCCP), a specific agent that leads to depolarization of the mitochondrial transmembrane potential, the apoptosis rate of HSS-expressing cells was significantly reduced, as measured using Hoechst staining and flow cytometry The mitochondrial membrane transition and cytochrome c leakage were significantly inhibited

in the HSS-expressing cells as compared with the untransfected cells, and,

as a consequence, the cellular ATP content in the HSS-expressing cells was relatively preserved Additionally, decreased caspase-3 activity was observed in the HSS-expressing cells treated with CCCP as compared with the vector-transfected cells and cells expressing mutant HSS Furthermore, silencing of HSS expression using small interfering RNA accelerated CCCP-induced apoptosis In isolated mitochondria, recombinant HSS reduced the release of cytochrome c induced by CCCP, indicating a possi-ble role for HSS in regulation of mitochondrial permeability transition (MPT) HSS-expressing BEL-7402 cells are resistant to CCCP injury, and HSS protection is identical to that observed with cyclosporin A, an inhibi-tor of MPT Therefore, we propose that the protective effect of HSS may

be associated with blockade of MPT

Abbreviations

ALR, augmenter of liver regeneration; CCCP, carbonyl cyanide m-chlorophenylhydrazone; COX IV, cytochrome c oxidase subunit IV; CsA, cyclosporin A; HSS, hepatic stimulator substance; IM, inner membrane; JC-1,

5,5¢,6,6¢-tetrachloro-1,1¢,3,3¢-tetraethylbenzimidazolocarbocyanine iodide; MP, mitochondrial permeability; MPT, mitochondrial permeability transition;

PTP, permeabilization transition pore; rHSS, recombinant hepatic stimulator substance; siRNA, small interfering RNA; w m , inner

transmembrane potential.

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promotion of liver regeneration has been demonstrated

to be related to its inhibition of hepatic natural killer

cell activity in an acute liver injury model [4] HSS

expression has also been reported to be increased in

cirrhotic human livers, and the mRNA level of HSS

was elevated in tissue samples of hepatocellular

carci-noma and cholangiocellular carcinoma [5] This

increased expression of HSS in liver tumors may due

to its ability to stimulate DNA synthesis [6–8] In

addi-tion to its ability to promote liver regeneraaddi-tion, HSS

has been shown to protect the liver from acute injury

caused by several compounds, including CCl4 [9],

d-galactosamine [10], ethanol [11], H2O2 [12], and

cad-mium [13] HSS has also been shown to have clinical

potential, as exogenous HSS administration to rats

with thioacetamide-induced liver fibrosis⁄ cirrhosis is

able to significantly decrease fibrosis and to suppress

the onset of cirrhosis [14]

Several in vitro studies have demonstrated that

although HSS promotes cell growth in dividing

hepatocytes, it is unable to stimulate cell division of

primary cultured or mature hepatocytes When added

to cultures of primary hepatocytes, HSS had minimal

effects on cell growth; instead, it augmented the

mito-genic effects of other growth factors, such as

epider-mal growth factor [15] Thereafter, HSS crude extract

was further purified, and a fraction (· 830 000) that

was responsible for the growth-augmenting activity

was referred to as augmenter of liver regeneration

(ALR) [16] In 1996, the cDNA sequence of ALR

was reported by Giorda et al [17] Unlike complete

mitogens such as hepatic growth factor or

transform-ing growth factor-a, ALR alone showed little effect

on hepatocyte proliferation in vitro, suggesting that

hepatocytes might not contain surface receptors

spe-cific for ALR This hypothesis has now been refuted,

as high-affinity receptors for ALR have been found

on the surface of hepatic cells [18] Although current

data suggest that HSS and ALR are very similar

mol-ecules with regard to their cDNA and protein

sequences, there are a few disagreements For

exam-ple, HSS was present only in the liver, but ALR was

found to be expressed in many tissues [19,20], with

different subcellular localizations [21], and seems to

have remarkably diverse functions related not only to

liver regeneration [22] More recent publications have

demonstrated that HSS has diverse functions For

example, it regulates FAD-linked disulfide bridges in

proteins, the biogenesis of cytosolic Fe–S proteins,

and electron transfer via FAD to cytochrome c [23]

Most recently, Thirunavukkarasu et al have reported

that HSS is an important intracellular survival factor

for hepatocytes [24]

In 2001, Lisowsky et al [25] first reported that mammalian HSS is an FAD-linked sulfhydryl oxidase with a CXXC active motif in the C-terminal domain Yeast Erv1p (essential for respiration and vegetative growth) has about 42% amino acid homology with mammalian HSS in the C-terminal domain [26] Yeast ERV1, the mouse [17], rat [27] and human [26] HSS genes, and some orthologous genes that have been identified in dsDNA viruses [28] have together been defined as the ERV⁄ HSS gene family [29] Members of this family have a highly conserved C-terminal domain, and this conserved C-terminus is functionally interchangeable between yeast and human Like Erv1p, HSS is located in the mitochondrial intermembrane space, and they both help with the maturation of Fe–S proteins outside of the mitochondria [23] Additionally, HSS has been shown to induce mitochondrial gene expression and enhance the oxidative phosphorylation capacity of liver mitochondria [30] Studies that have focused on HSS and the mitochondria have indicated that HSS not only affects the activity of P450 via gene repression [31], but also interacts with the respiratory chain via the modification of cytochrome c [32]

It is widely accepted that mitochondria play a criti-cal role in the regulation of cell death [33–35], and mitochondrial permeability transition (MPT) is consi-dered to be the pivotal event of mitochondria-mediated cell death [36] MPT leads to loss of the inner trans-membrane potential (wm) [37], reduction of the intra-cellular ATP level, matrix swelling, and the release of proapoptotic proteins such as cytochrome c

As mitochondria play an essential role during cell death, we aimed to determine the relationship between HSS expression and mitochondrial protection, and whether mitochondrial permeability (MP) would be targeted by HSS In this study, we established a BEL-7402 cell line that stably expresses HSS and iden-tified the mitochondrial location of HSS After a mito-chondrial lesion specifically caused by carbonyl cyanide m-chlorophenylhydrazone (CCCP), a classic protonophore-type uncoupling agent [38], we analyzed

Dwm, the intracellular ATP level, and the leakage of cytochrome c HSS demonstrated a protective effect against CCCP-induced apoptosis, inhibiting MPT The protective effect of HSS was compared, in parallel, with that of another known MPT inhibitor, cyclospo-rin A (CsA), and its analog NIM811 CsA and NIM811 displayed inhibitory effects on MPT, in a dose–response manner; similarly, HSS also inhibited MPT, further supporting our hypothesis that HSS pro-tection is strongly associated with the mitochondrial membrane pore Knockdown of HSS expression by RNA interference destroyed MP, leading to a great

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increase in the ability of CCCP to damage the

mitochondria In conclusion, HSS protects liver cells

from CCCP-induced apoptosis From this result, we

propose that the potential mechanism by which HSS

mediates its antiapoptotic effect is related to regulation

of MPT

Results

HSS expression in the cells

Real-time RT-PCR demonstrated that HSS was

signif-icantly expressed in transfected cells as compared with

vector-transfected cells (pcDNA3.0 alone) or wild-type

cells (Fig 1A) Protein expression of HSS in the three

cell lines (untransfected cells, vector-transfected cells,

and HSS-expressing cells) was detected using western

blot As shown in Fig 1B, a 15 kDa band was

detected after hybridization with the antibody against HSS in the cells transfected with the HSS expression construct By contrast, HSS expression in wild-type and vector-transfected cells was minimal

Morphological evidence of the antiapoptotic effect of HSS

As shown in Fig 2A,B, the treatment of cells with

50 lm CCCP induced profound changes in the nuclear morphology of hepatoma cells, with chromatin con-densation and fragmentation being observable using fluorescence microscopy As detected using Hoechst 33342 staining, vector-transfected cells and cells expressing mutant HSS underwent typical apopto-tic changes [39], including shrinkage, membrane bleb-bing, chromatin condensation, and the formation of apoptotic bodies, after being treated with CCCP How-ever, in cells expressing HSS, the apoptotic rate was significantly decreased following treatment with CCCP

To verify this putative protective effect by HSS, we set

up a parallel control using 10 lm CsA, which is a potent inhibitor of MPT Both CsA treatment and the expression of HSS decreased the number of apoptotic cells, and CsA alone was able to greatly alleviate CCCP-induced apoptosis

Apoptosis evaluated by flow cytometry

As shown in Fig 2C,D, the proportions of apoptotic vector-transfected cells and cells expressing mutant HSS treated with 50 lm CCCP were comparatively high (74.24% ± 3.32% and 75.11% ± 4.40%, respec-tively) However, the proportion of apoptotic cells fol-lowing treatment with CCCP was significantly reduced

in HSS-expressing cells (52.4% ± 3.90%) Thus, the apoptotic rate in HSS-expressing cells was decreased

by about 30% as compared with vector-transfected cells and mutant HSS-expressing cells Similarly, CCCP-induced apoptosis was also inhibited by CsA

Effect of HSS on alteration of wm Alteration of wm is known to be an early event in the apoptotic signaling cascade [40] As it has been shown that HSS is localized to the mitochondria of hepatoma cells [12], we explored whether HSS plays an important role in protecting the mitochondria from CCCP-induced damage and apoptosis As shown in Fig 3A,B, the addition of 30 lm CCCP to the isolated mitochondria induced MPT-dependent swelling, as shown by a large decrease in the fluorescence intensity

in cells CsA, NIM811 and HSS induced a

dose-depen-Fig 1 (A) The level of HSS RNA in the three types of cells was

quantified by real-time RT-PCR, and is expressed as genomic

equiv-alents per culture The expression of HSS in cells stably transfected

(Tr) with the HSS expression construct is significantly greater than

that in wild-type cells and vector-transfected cells (B) The

differen-tial expression of HSS in the three cell lines Mitochondrial protein

extracts (25 lg) from each of the cell cultures were analyzed using

western blot and an antibody against HSS.

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dent increase in wm At the maximal dose of HSS

(10 lgÆmL)1), however, addition of CsA to the

mito-chondria did not increase wm further, indicating that

HSS protection against MPT could not be enhanced

by CsA (Fig 3A) In order to determine whether HSS

can augment the protective effect of CsA against

MPT, we added various doses of CsA to the isolated

mitochondria subjected to CCCP injury Both CsA

and its analog NIM811 showed potent protection

against MPT; however, similar to the finding shown in

Fig 3A, the protection provided by CsA and NIM811,

if obtained at the maximal doses, could not be further

enhanced by HSS These results imply that HSS

pro-tection of mitochondria might be due to inhibition of

the MP disruption, and the inhibition of MPT,

although not fully clarified yet, could be due to a

mechanism similar to that responsible for the effect of

CsA or NIM811 In addition, we investigated whether

HSS protection could be obtained in the isolated

mito-chondria of HSS-expressing cells As seen in Fig 3C,

MP in the mitochondria of HSS-transfected cells was

affected less by CCCP than that of vector-transfected

cells CsA could rescue MP effectively in HSS-expressing cells, indicating that HSS transfection could alleviate mitochondrial damage through inhibition of

MP collapse Moreover, damage to the mitochondrial membrane pores following treatment with CCCP led

to a remarkable amount of leakage of cytochrome c, whereas in HSS-expressing cells, the leakage of cyto-chrome c was inhibited Exposure of cells to CCCP resulted in substantial loss of wm, and, as a consequence, the mitochondrial membranes were easily damaged and there was massive leakage of cyto-chrome c (Fig 4)

Effect of HSS on alteration of cytochrome c leakage

As shown in Fig 4, treatment of cells with CCCP (50 lm) led to serious damage to the mitochondrial membrane, resulting in the leakage of cytochrome c from the mitochondria in vector-transfected cells (Fig 4A, lane 4) However, the cytochrome c content was significantly preserved in cells expressing HSS

Fig 2 Assessment of apoptosis by Hoechst 33342 (A) Wild-type cells, vector-transfected cells and HSS-expressing cells were analyzed after Hoechst 33342 staining The cells treated with CCCP have undergone chromatin condensation and margination (B) The number of apoptotic cells decreased as compared with the control (ctrl) group and cells treated with CsA (C) Apoptosis was analyzed using flow cytometry The CCCP treatment significantly increased the apoptotic rate in vector-transfected and mutant HSS-expressing cells However, apoptosis was markedly inhibited in HSS-expressing cells (D) Statistical evaluation of the apoptotic rate from three independent experi-ments.

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(Fig 4A, lane 5); the cytochrome c leakage was

reduced by approximately 75% in HSS-expressing cells

as compared with vector-transfected cells (P < 0.05)

The preservation of mitochondrial cytochrome c was

not observed in cells expressing mutant HSS (Fig 4A,

lane 4) Treatment with CsA decreased cytochrome c

leakage in both vector-transfected and HSS-expressing

cells, but CsA appeared to have more of an effect in

HSS-expressing cells (Fig 4A, lanes 6 and 7) A densi-tometric analysis of the cytochrome c content is shown

in Fig 4B,D

Effect of HSS on the intracellular ATP level

To examine the energy production of mitochondria in CCCP-treated cells, the intracellular ATP level was measured The intracellular ATP level in vector-trans-fected cells and HSS-expressing cells was greatly reduced after treatment with CCCP (Fig 5A) Although the ATP level of HSS-expressing cells fell to

a low level, the relative amount of ATP in HSS-expressing cells was about 45% higher than that in vector-transfected cells, suggesting that HSS-expressing cells were less affected by the impaired energy produc-tion After addition of CsA, the ATP level in HSS-expressing cells was more readily restored than that in vector-transfected cells Moreover, we examined the effects of CsA and NIM811 on the restoration of intracellular ATP level Figure 5B shows that both agents were able to increase the ATP levels in HSS-expressing cells, with a dose-dependent pattern The maximal effects of CsA and NIM811 could be obtained

Effect of HSS on CCCP-induced apoptosis Caspase activation is a key step in DNA damage-induced apoptosis To further understand the protec-tive effect of HSS against CCCP-induced apoptosis, the activation of caspase-3 was examined using the enzymatic Caspase-Glo 3⁄ 7 assay After CCCP treat-ment, caspase-3 activity increased markedly in vector-transfected cells, and this increase was inhibited in HSS-expressing cells (P < 0.05; Fig 6), but not in cells expressing mutant HSS Similarly, CsA showed a potent inhibitory effect on cell apoptosis by decreasing the activity of caspase-3 in the three cell lines

Effect of HSS knockdown on CCCP-induced apoptosis

To further elucidate the functional role of HSS in CCCP-induced apoptosis, the expression of HSS was inhibited at the post-transcriptional level by using a gene silencing strategy [small interfering RNAs (siRNAs)] As demonstrated by western blot, the HSS level in cells transfected with the HSS-specific siRNA was much lower than that in cells transfected with a scrambled siRNA (data not shown) Using these trans-fected cells, we investigated the intracellular ATP level, caspase-3 activity, and cytochrome c level As shown

Fig 3 Effect of CCCP on MPT (A, B) Equal cell numbers from

dif-ferent cultures were treated with CCCP (30 l M ) for 1 h The

mito-chondria were then isolated HSS, CsA and its analog NIM811

were added to the mitochondria, and their effects on MPT were

analyzed In (A) and (B), MPT was increased in a dose-dependent

pattern; **P < 0.05 versus treatment with CCCP (C) Dwm

follow-ing treatment with CCCP and CsA Dwm in HSS-expressing cells

was less severe than in vector-transfected cells; **P < 0.05 as

compared with vector-transfected cells ctrl, control.

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in Fig 7A, following treatment with 15 lm CCCP, the

intracellular ATP level in HSS siRNA-transfected cells

was significantly reduced as compared with that in

scrambled siRNA-transfected cells (about 40%

reduc-tion) In addition, caspase-3 activity was greatly

increased in HSS siRNA-transfected cells (Fig 7B),

suggesting that knockdown of HSS expression increases cellular susceptibility to CCCP damage As a result, the cytochrome c content markedly declined in the mitochondrial compartment in CCCP-treated cells transfected with the HSS siRNA as compared with controls (Fig 7C) This indicates that there was an impairment of the permeabilization transition pore (PTP) of the mitochondrial membrane and that HSS expression is a critical factor that protects cells from CCCP-induced apoptosis

Effect of recombinant HSS (rHSS) on CCCP-induced cytochrome c release

Having demonstrated that HSS expression can inhibit apoptosis, we next aimed to determine whether the

Fig 4 Western blot of mitochondrial cyto-chrome c (Cyt c) Mitochondria were iso-lated from wild-type cells, vector-transfected cells, HSS-expressing cells, and mutant HSS-expressing cells, and analyzed using western blot with an antibody against cyto-chrome c All blots were blotted with an antibody against COX IV to control for equal loading *P < 0.001 and **P < 0.05, respec-tively, as compared with vector-transfected cells (A, B); **P < 0.05 as compared with mutant HSS-expressing cells (C, D) ctrl, control.

Fig 5 Intracellular ATP level (A) HSS-transfected or

vector-trans-fected cells were treated with CCCP and CsA, and the intracellular

ATP level was measured **P < 0.05 as compared with the ATP

level in vector-transfected cells (B) Effect of CsA and its analog

NIM811 on ATP in HSS-transfected cells **P < 0.05 versus CCCP

treatment ctrl, control.

Fig 6 Caspase-3 activity Following treatment with CCCP and CsA, caspase-3 activities were analyzed in wild-type cells, vector-transfected cells, and HSS-expressing cells **P < 0.05 as com-pared with vector-transfected cells and mutant HSS-expressing cells ctrl, control.

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addition of rHSS to isolated mitochondria would

pre-vent impairment of the PTP rHSS and mutant rHSS

(Cys62fi Ser, Cys65 fi Ser) were expressed in and

purified from prokaryotic cells The resulting protein

had a molecular mass of 15 kDa, as determined using

SDS⁄ PAGE (data not shown) As shown in Fig 8, incubation of isolated mitochondria with CCCP (300 lm at 4C) for 4 h resulted in substantial cyto-chrome c release as compared with the control (lane 2) The administration of rHSS reduced cyto-chrome c release (Fig 8, lane 4), suggesting that HSS protects the mitochondria from CCCP-induced injury However, the mutant protein and a mock protein were both incapable of protecting the mitochondria (Fig 8, lanes 3 and 5, respectively) These results suggest a possible role for HSS in the regulation of MPT This protective role in mitochondria may be dependent upon the intact form of HSS, and if the CXXC motif

at the C-terminus, which is essential for its enzymatic activity [34], is mutated, then HSS loses its protective effect (Fig 8, lane 5)

Discussion

Mitochondria are the energy producers of the cell, and are essential for the maintenance of cell life However,

in the last 10 years, it has also become apparent that mitochondria are the control centers for cell death In healthy cells, the mitochondrial inner membrane (IM), which is the boundary between the intermembrane⁄ intercristae space and the matrix, is nearly

imperme-Fig 7 Silencing HSS expression accelerates CCCP-induced

apop-tosis Cells were transfected with an HSS-specific siRNA or a

scrambled siRNA as a control Forty-eight hours post-transfection,

the cells were treated with 15 l M CCCP for 24 h and harvested for

determination of the intracellular ATP level, the caspase-3 activity,

and the cytochrome c (Cyt c) level (A) Intracellular ATP level The

ATP level was measured as described in Experimental procedures.

The data are presented as the mean value from three independent

experiments; **P < 0.05 as compared with control

siRNA-trans-fected cells (B) Caspase-3 activity was determined as described in

Experimental procedures The data are presented as the mean of

triplicate determinations from three independent experiments;

**P < 0.05 as compared with scrambled siRNA-transfected cells.

(C) The cytochrome c level in the mitochondrial pellet was

mea-sured using western blot The blots were reprobed for the

mito-chondrial marker COX IV to confirm equal protein loading ctrl,

control.

Fig 8 rHSS inhibits CCCP-induced cytochrome c (Cyt c) release from isolated mitochondria The cytochrome c and COX IV levels were analyzed using western blot The control is untreated mito-chondria **P < 0.05 as compared with the other panels.

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able to all ions, including protons The charge

imbal-ance that results from the generation of an

electro-chemical gradient across the IM forms the basis of the

IM wm During cell death, MP often increases,

allow-ing for the release of soluble proteins The only

mechanism underlying mitochondrial membrane

per-meabilization that has been described to date is MPT,

which is generally studied in isolated mitochondria and

compromises the normal integrity of the mitochondrial

IM This results in the IM becoming freely permeable

to protons, leading to the uncoupling of oxidative

phosphorylation MPT is caused by the opening of the

nonselective, highly conductive PTP in the

mitochon-drial IM [39] The exact molecular composition of the

PTP remains unclear When MPT occurs, MP

collapses, leading to the failure of oxidative

phosphor-ylation and necrotic cell death [41–43] In addition,

MPT causes large-amplitude swelling, outer membrane

rupture, and release of cytochrome c from the

inter-membrane space, triggering activation of caspases and

apoptosis [41,44]

Apoptosis is a genetically predetermined mechanism

that may be activated by several molecular pathways

The best characterized and the most prominent

path-ways are the extrinsic and intrinsic pathpath-ways In the

intrinsic pathway (also known as the ‘mitochondrial

pathway’), apoptosis results from an intracellular

cas-cade of events in which mitochondrial permeabilization

plays a crucial role During apoptosis, MPT generally

precedes apoptotic cell death, both in vitro and in vivo

[41] The release of cytochrome c as a consequence of

MPT is one of the key events in

mitochondria-depen-dent apoptosis [45] Of the released mitochondrial

pro-teins, cytochrome c is considered to be the most

important, because it can trigger a critical step in the

activation of mitochondria-dependent apoptosis [12],

the assembly of the apoptosome Upon formation of

this complex, caspase-9 acquires the ability to trigger

the processing and activation of the downstream

cas-pase cascade, which ultimately culminates in apoptotic

cell death

CCCP is a protonophore that renders the

mito-chondrial IM permeable to protons and causes

dissi-pation of the proton gradient across the IM CCCP

also uncouples the transfer of electrons through the

electron transfer chain from ATP production

CCCP-induced apoptosis has been reported in many cell

lines, such as Jurkatneo, FL5.12, HL-60, and ST486

[46–49]

To test the hypothesis that HSS overexpression

pro-tects cells from apoptosis, the present in vitro study

used CCCP to explore the influence of mitochondrial

uncoupling on hepatocytes The mitochondria of

hepatocytes became depolarized 24 h after exposure to CCCP Uncoupling may further lead to an impairment

in mitochondrial ATP formation and the hydrolysis of ATP by the uncoupler-stimulated ATPase [50] There-fore, as seen in Fig 5, ATP levels may drop substan-tially after CCCP treatment

The results of the current experiments provide evi-dence that mitochondrial uncoupling in hepatocytes leads to PTP opening and cell swelling, an event that

is probably reduced in extent by CsA CsA specifically inhibits PTP opening by binding to cyclophilin D in the matrix and on the inner surface of the IM [51–54] Growing evidence has implicated MPT in the necrotic and apoptotic death of hepatocytes [42,43,55] In a previous report, HSS was considered to be an impor-tant intracellular survival factor for hepatocytes [24]; however, the mechanism by which HSS protects hepatocytes remains unclear It has recently been dem-onstrated that HSS is a novel component of the mito-chondrial intermembrane space that is specifically required for maturation of Fe–S-binding proteins [23] Subsequently, we found that the overexpression of HSS protects hepatic cells from H2O2-mediated injury [12] Therefore, in this study, we investigated whether HSS could function as an MPT inhibitor, thereby alle-viating hepatic injury and promoting the survival of hepatocytes, after transfection of HSS into the cells or the administration of HSS to isolated mitochondria

in vitro

HSS exerts a potent hepatocyte protective effect

by a hitherto unknown mechanism [56,57] As a fol-low-up to our initial report [12], in this article we demonstrate that HSS represses the onset of MPT, substantially decreasing mitochondrial depolari-zation (Fig 3), alleviating cellular ATP level (Fig 5), and therefore enhancing cell survival (Fig 2) Fur-thermore, HSS-deficient hepatocytes were sensitive to CCCP-mediated damage (Figs 2–6) A similar phe-nomenon was observed with H2O2-mediated injury (data not shown), indicating that endogenous HSS has an important role in the protection of hepatocytes from apoptotic death resulting from MPT

Our results suggest that MPT probably plays a critical role in the damage induced by CCCP HSS

is able to protect the hepatocytes, probably by inhib-iting MPT resulting from the mitochondrial PTP However, more precise investigations of the protein– protein interactions of HSS within the mitochondria will be required to elucidate the molecular mecha-nism underlying HSS-mediated liver protection and

to identify candidate HSS-binding molecules Never-theless, in this study, we provide the first evidence

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that HSS is equivalent to CsA in inhibiting the onset

of MPT

Experimental procedures

Reagents

DMEM and TRIzol were purchased from Gibco BRL

(Paisley, UK), and fetal bovine serum was purchased

from Hyclone (Victoria, Australia) Both

Lipofecta-mine 2000 and the SuperScript III First-Strand Synthesis

System were purchased from Invitrogen (Carlsbad, CA,

USA) The gentamicin analog G418 was purchased from

Gibco BRL The power SYBR Green PCR Master Mix

was purchased from Applied Biosystems (Warrington,

UK) The CellTiter-Glo Luminescent Cell Viability Kit

and the Caspase-Glo 3⁄ 7 Assay were purchased from

Promega (Madison, WI, USA) Fluorescein

isothiocya-nate-conjugated annexin V was purchased from Biosea

(Beijing, China) The Mitochondria⁄ Cytosol Isolation Kit

was purchased from Applygen Technologies (Beijing,

China) The siRNA and nontargeting control (scrambled)

siRNA were purchased from Dharmacon RNA

Technolo-gies (Shanghai, China) The QuikChange Site-Directed

Mutagenesis Kit was purchased from Stratagene (La

Jolla, CA, USA) The His-tag vector pET-15b and the

Escherichia coli strain Origami (DE3) were purchased

from Novagen (Darmstadt, Germany) The His

Gravi-Trap Kit was purchased from Phamarcia (Little Chalfont,

UK) The bicinchoninic acid kit was purchased from

Pierce (Rockford, IL, USA) The antibody against HSS,

the antibody against cytochrome c and the enhanced

chemiluminescence kit were purchased from Santa Cruz

Biotechnology (Santa Cruz, CA, USA) The horseradish

peroxidase-conjugated goat anti-(mouse IgG) was

pur-chased from Cell Signaling Technology (Beverly, MA,

USA) Bisbenzimide Hoechst 33342, CCCP, CsA,

5,5¢,6,6¢-tetrachloro-1,1¢,3,3¢-tetraethylbenzimidazolocarbo-cyanine iodide (JC-1), dimethylsulfoxide and other

chemi-cal reagents were all purchased from Sigma Aldrich (St

Louis, MO, USA) The CsA analog NIM811 was kindly

provided by Novartis (Basel, Switzerland)

Cell culture and plasmid DNA transfection

BEL-7402 hepatoma cells were cultured at 37C in DMEM

supplemented with 10% fetal bovine serum, 100 UÆmL)1

penicillin and 100 lgÆmL)1 streptomycin in a 5% CO2

humidified atmosphere incubator A total of 2· 106

BEL-7402 cells were seeded and allowed to grow to 50–

70% confluence The cells were transfected with 5 lg of

either HSS–pcDNA 3.0 or pcDNA 3.0 vector with

Lipofec-tamine 2000, following the manufacturer’s

recommenda-tions Eight hours post-transfection, the cells were selected

using G418 (400 lgÆmL)1) for 14 days The cells resistant

to G418 were used for further study

RNA extraction and real-time PCR

Total RNA from HSS-expressing cells, vector-transfected cells and wild-type cells was extracted using the QIAamp RNA Purification Kit The extracted RNA was reverse-transcribed into cDNA, using the SuperScript III First-Strand Synthesis System cDNA was synthesized from 3 lg

of total RNA in 20 lL of reaction mixture Real-time PCR was performed using the Power SYBR Green Master Mix,

as recommended by the manufacturer The HSS gene was amplified using the ABI Prism 7300 Sequence Detection System (Applied Biosystems, Foster City, CA, USA) with specific primers The 18S rRNA was amplified as an inter-nal standard Primers were designed using the primer design software primer express (Applied Biosystems)

Microscopic observation of cellular morphology

The cells were plated in 24-well plates at 105cellsÆmL)1 Sixteen hours after plating, the cells were treated with either

50 lm CCCP or 50 lm CCCP and 10 lm CsA for 24 h After

24 h, 1.5 lL of 10 mgÆmL)1Hoechst 33342, a DNA-specific fluorescent dye, was added to each well, and the plates were incubated for 10 min at 37C The stained cells were then observed using a Leica DMILH fluorescence microscope

Flow cytometric analysis

Cells were seeded in 100 mm culture dishes After attach-ment, the cells were incubated with either 50 lm CCCP or

50 lm CCCP and 10 lm CsA for 24 h After being washed twice with NaCl⁄ Pi, the cells were resuspended in binding buffer [10 mm Hepes⁄ NaOH (pH 7.4), 140 mm NaCl, 2.5 mm CaCl2] Fluorescein isothiocyanate-conjugated ann-exin V was added to a final concentration of 1 mgÆmL)1 The mixture was incubated for 10 min in the dark at room temperature The cells were then resuspended in propidium iodide solution, and incubated again in the dark for another 30 min at room temperature The stained cells were analyzed using a FACScan flow cytometer (Becton Dickin-son, Franklin Lakes, NJ, USA) The data were analyzed using cellquest software (Becton Dickinson)

Isolation of mitochondria

The isolation of mitochondria was performed according to the instructions for the Mitochondria⁄ Cytosol Isolation Kit for Cultured Cells The cells were harvested and homoge-nized in 1.5 mL of ice-cold Mito-Cyto Buffer with a Dounce homogenizer After centrifugation twice at 800 g for 5 min at 4C, the supernatant was collected,

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trans-ferred to a fresh microcentrifuge tube, and centrifuged at

12 000 g for 10 min at 4C The pellet, which contained

the mitochondria, was resuspended in 30 lL of Mito-Cyto

Buffer The protein concentration was determined using the

bicinchoninic acid method [58], with BSA as a standard

The isolated mitochondria were stored on ice prior to the

experiments, and all experiments were performed up to

1–5 h after preparation

Measurement of wmin isolated mitochondria

JC-1 is a mitochondrion-specific dye that can be used to

determine wm Mitochondria with high wm will form JC-1

aggregates and fluoresce red ( 590 nm); consequently,

mitochondrial depolarization is indicated by a decrease in

the red fluorescence intensity [59] The cells were grown to

80–90% confluence After pretreatment with a gradient of

either CsA (0.1, 1.0, 10 or 15 lm) or its analog NIM811

(0.1, 1.0, 10 or 15 lm) for 15 min, the cells were incubated

with CCCP (30 lm) for 1 h, and the mitochondria were

then isolated as mentioned above.The wm was measured

after JC-1 staining, mainly as described by van der Toorn

M et al [60] The wmwas obtained with 485 nm excitation,

using a 590 nm bandpass filter in SPECTRA max M2

(Molecular Devices, Sunnyvale, CA, USA)

Determination of the intracellular ATP level

The intracellular ATP level was measured using the

Cell-Titer-Glo Luminescent Cell Viability Assay Kit The

HSS-expressing cells were plated in 96-well plates at

2.5· 104cells per well The cells were treated with CCCP

(30 lm) for 1 h, and subsequently lysed with 100 lL of lysis

buffer The ATP concentration was immediately measured

using a Glomax 96 Microplate Luminometer (Promega)

Caspase-3⁄ 7 activity

Caspase activity was detected by using the Caspase-Glo 3⁄ 7

Assay Kit Briefly, the cells were seeded in a 96-well plate

and incubated for 24 h at 37C The cells were treated with

either 50 lm CCCP or 50 lm CCCP and 100 lm CsA for

24 h The caspase-3⁄ 7 reagent (100 lL) was then added to

each well, and the plate was incubated on a rotary shaker

for 30 min at room temperature Luminescence was

recorded for each well The caspase-3⁄ 7 activity is presented

as the mean of results from three experiments

Small interfering RNA-mediated gene silencing

BEL-7402 cells were transfected with an HSS-specific siRNA

or nontargeting control (scrambled) siRNA, according to

standard protocols Briefly, confluent BEL-7402 cells were

replated in six-well plates (3· 105

cells per well) and grown

in 10% fetal bovine serum⁄ DMEM without antibiotics for

24 h to 70–80% confluence To prepare the transfection com-plex, DharmaFECT-4 transfection reagent (4 lL per well) was incubated with the HSS-specific siRNA or the scrambled siRNA in antibiotic-free and serum-free medium for 30 min

at room temperature The cells were then incubated with the siRNA–DharmaFECT-4 complexes for 24 h at 37C For recovery, the cells were cultured in 10% fetal bovine serum⁄ DMEM (antibiotic-free) for another 24 h Before the CCCP treatment, BEL-7402 cells were serum-deprived over-night in antibiotic-free 0.1% fetal bovine serum⁄ DMEM, and the cells were then treated with 15 lm CCCP or dimeth-ylsulfoxide for 24 h and harvested to determine the ATP content, caspase-3 activity, and the cytochrome c level as described above

Preparation of recombinant protein

The HSS cDNA (375 bp) was amplified by PCR The Cys62fi Ser and Cys65 fi Ser mutants of HSS were con-structed using the QuikChange Site-Directed Mutagenesis Kit All constructs were verified by DNA sequencing The NdeI and BamHI restriction sites were used for cloning the PCR fragments into the His-tag vector, pET-15b The recombinant proteins were generated in the E coli strain Origami (DE3), and the N-terminal His-tagged proteins were purified using a His GraviTrap kit according to the manufacturer’s protocols Purification to homogeneity was verified using SDS⁄ PAGE gels and by antibody tests The pure proteins were desalted, concentrated, and stored at –

80C until further use The concentration of the protein was estimated using the bicinchoninic acid assay

Cytochrome c release in CCCP-treated mitochondria

Mitochondria were isolated from BEL-7402 cells by differ-ential centrifugation as described above To determine the effect of rHSS protein on the release of cytochrome c, mito-chondria (50 lg) were incubated with protein (rHSS, mutant rHSS, or mock protein; 100 lgÆmL)1 each) in

25 lL of buffer for 1 h at 4C CCCP (300 lm) was then added to the mitochondria, and the CCCP-treated mito-chondria were incubated at 4C for 4 h The mitochondrial suspension was then centrifuged at 12 000 g for 5 min, and the resulting supernatants were analyzed for the release of cytochrome c with western blot The mitochondrial pellets were probed with the cytochrome c oxidase subunit IV (COX IV) antibody to normalize for loading

Statistical analysis

All values are expressed as mean ± standard deviation Statistical significance was determined using a one-way

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