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Báo cáo khoa học: TRB3, upregulated by ox-LDL, mediates human monocyte-derived macrophage apoptosis pot

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The aim of this study was to investigate the role of the TRB3 gene in macrophage apoptosis induced by oxidized low-density lipoprotein ox-LDL.. Furthermore, TRB3-silenced macrophages sho

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monocyte-derived macrophage apoptosis

Yuan-yuan Shang1,*, Zhi-hao Wang1,*, Li-ping Zhang2, Ming Zhong1, Yun Zhang1, Jing-ti Deng2 and Wei Zhang1

1 Key Laboratory of Cardiovascular Remodeling and Function Research, Chinese Ministry of Education and Chinese Ministry of Public Health, Department of Cardiology, Qilu Hospital of Shandong University, Ji’nan, China

2 Department of Anatomy, School of Medicine, Shandong University, Ji’nan, China

Acute coronary syndrome is the consequence of rupture

or erosion of pre-existing atherosclerotic plaques, with

subsequent formation of local thrombus, leading to

crit-ical occlusion of coronary arteries The principal

patho-logical basis of acute coronary syndrome is vulnerable

plaques [1] Macrophage apoptosis contributes

signifi-cantly to the development of vulnerable atherosclerotic

plaques [2–4] A possible mechanism linking

macro-phage apoptosis to vulnerable plaque progression is that

the reduced level of macrophages fails to clear apoptotic

smooth muscle cells and macrophages, which leads to secondary necrosis of these cells and facilitates forma-tion of an atheromatous core within plaques In addi-tion, apoptotic macrophages can release cholesterol, which results in accumulation of acicular cholesterol crystals in the lipid core, thus injuring the fibrous cap of plaques In addition, apoptotic macrophages may be a source of tissue factor, a procoagulant molecule that is considered to play an important role in coagulation and thrombosis associated with advanced plaques [3]

Keywords

apoptosis; atherosclerosis; macrophage;

ox-LDL; TRB3

Correspondence

W Zhang, Department of Cardiology, Qilu

Hospital of Shandong University, Ji’nan

250012, China

Fax: +86 531 86169356

Tel: +86 531 82169339

E-mail: zhangweisdu@gmail.com

J.-t Deng, Department of Anatomy, School

of Medicine of Shandong University, Ji’nan

250012, China

Fax: +86 531 86169356

Tel: +86 531 88382093

E-mail: jingtideng@hotmail.com

*These authors contributed equally to this

paper

(Received 16 January 2009, revised 4 March

2009, accepted 9 March 2009)

doi:10.1111/j.1742-4658.2009.06998.x

Tribble3 (TRB3), a mammalian homolog of Drosophila tribbles, slows cell-cycle progression, and its expression is increased in response to various stresses The aim of this study was to investigate the role of the TRB3 gene

in macrophage apoptosis induced by oxidized low-density lipoprotein (ox-LDL) We found that, in human monocyte-derived macrophages, TRB3 is upregulated by ox-LDL in a dose- and time-dependent manner The cell viability of TRB3-overexpressing macrophages was decreased, but apoptosis was increased and the level of activated caspase-3 increased Fac-torial analyses revealed no significant interaction between TRB3 overex-pression and ox-LDL stimulation with respect to macrophage apoptosis Furthermore, TRB3-silenced macrophages showed decreased apoptosis, and TRB3-silenced cells treated with ox-LDL showed significantly increased apoptosis Silencing of TRB3 and ox-LDL stimulation showed significant interaction for macrophage apoptosis, suggesting that TRB3 knockdown resisted the macrophage apoptosis induced by ox-LDL There-fore, TRB3 in part mediates the macrophage apoptosis induced by ox-LDL, which suggests that TRB3 might be involved in vulnerable atherosclerotic plaque progression

Abbreviations

MAPK, mitogen-activated protein kinase; MTT, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide; ox-LDL, oxidized low-density lipoprotein; siRNA, small interfering RNA; SiTRB3, siRNA targeting TRB3; ssDNA, single-stranded DNA; TRB3, Tribble3.

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Signal transduction of apoptosis in macrophages

involves a complex network system Various risk

fac-tors, such as an increased level of oxidized low-density

lipoprotein (ox-LDL), can induce macrophage

apopto-sis through multiple apoptotic signaling pathways, such

as Akt/protein kinase B (PKB) and mitogen-activated

protein kinase (MAPK) [5–7] However, the mechanism

of macrophage apoptosis remains to be elucidated

Tribbles, a Drosophila protein, slows progression

through the G2 stage of the cell cycle [8] Three

mam-malian orthologs, TRB1, TRB2 and TRB3, all contain

a consensus serine⁄ threonine kinase catalytic core but

lack an ATP-binding pocket and so do not possess

kinase activity Recently, TRBs have been shown to be

expressed in unstable regions of carotid plaques [9]

TRB3, also named neuronal cell death-inducible

puta-tive protein kinase, is expressed in the liver, thymus,

prostate and heart [10], and may have broad biological

activity TRB3 has been reported to be an important

regulatory protein involved in signal pathways, and

works at least through CDC25⁄ String, Akt and

MAPK [11–13] Activation of MAPK and inhibition

of Akt kinase activity result in macrophage apoptosis

[5–7], which is implicated in the development of

vul-nerable atherosclerotic plaques [2–4] TRB3 may be

involved in macrophage apoptosis induced by ox-LDL,

and could play an essential role in the progression of

vulnerable plaques

We investigated whether TRB3 is implicated in

ox-LDL-induced apoptosis by stimulating human

monocyte-derived macrophages with ox-LDL, then

transfecting them with a recombinant adenoviral

TRB3 construct or a small interfering RNA (siRNA)

targeting TRB3

Results

TRBs mRNA expression in human macrophages

To determine whether the TRB genes TRB1, TRB2

and TRB3 were expressed in human monocyte-derived

macrophages, monocytes were first allowed to

differen-tiate naturally into macrophages Quantitative

real-time PCR performed on days 1, 3, 5, 7, 9 and 11

showed that all three genes were expressed in

mono-cyte-derived macrophages Macrophages

predomi-nantly expressed TRB3 (Fig 1), and the level of TRB3

mRNA increased on day 3 and peaked on day 7

TRB3 expression upregulated by ox-LDL

To examine whether TRB3 mRNA expression in

mac-rophages was regulated by ox-LDL, macmac-rophages were

treated with various concentrations of ox-LDL or LDL for 24 h Quantitative real-time PCR showed that expression of TRB3 mRNA was significantly upregulated by ox-LDL but not by LDL (Fig 2A) The mRNA expression increased with increasing ox-LDL concentration; a statistical difference between ox-LDL and LDL treatments was observed at a con-centration of 50 lgÆmL)1 (4.72 ± 2.72 versus 1.04 ± 0.42, P < 0.01)

Fig 1 TRBs mRNA expression in macrophages.

LDL

A

B

C

ox-LDL

LDL ox-LDL

4 5

6

*

1 2 3 4

0 1

8 10

2 4 6

0

TRB3 GAPDH

Fig 2 TRB3 mRNA and protein expression are upregulated by ox-LDL (A) Quantitative real-time PCR analysis of macrophages in serum-free medium treated with various concentrations of ox-LDL or LDL for 24 h (B) Quantitative real-time PCR analysis of macrophages treated with 50 lgÆmL)1 ox-LDL or LDL for various durations (C) Western blot analysis of macrophages treated with 50 lgÆmL)1 ox-LDL or LDL for 24 h For (A) and (B), expression was normalized

to that of GAPDH *P < 0.05, **P < 0.01 versus LDL-treated cells.

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Macrophages treated with 50 lgÆmL)1 ox-LDL or

LDL for various durations showed increased TRB3

mRNA expression with increasing time (Fig 2B)

Expression of TRB3 mRNA was significantly higher

after a 24 h treatment with 50 lgÆmL)1 ox-LDL than

with LDL treatment (3.32 ± 2.63 versus 1.14 ± 0.50,

P< 0.05) and was further increased after 48 h of

ox-LDL treatment (8.55 ± 4.78 versus 1.32 ± 0.46,

P< 0.01) The TRB3 protein level was also

signifi-cantly increased after treatment with 50 lgÆmL)1

ox-LDL for 24 h (Fig 2C)

Ox-LDL induces macrophage apoptosis

Macrophages were treated with various concentrations

of ox-LDL or LDL for 24 h, and then cell viability

was determined by MTT assay Cell viability was

sig-nificantly reduced in cells treated with ox-LDL but not

those treated with LDL (Fig 3A) Cell viability was

significantly lower with 50 lgÆmL)1 ox-LDL treatment

than with 50 lgÆmL)1 LDL treatment (42.5 ± 1.0%

versus 106.5 ± 16.3%, P < 0.05) However, at lower

concentrations, the reduction in cell viability with

ox-LDL was not significantly different from that with

LDL

Macrophages were treated with 50 lgÆmL)1ox-LDL

or LDL for various durations Incubation for 24 h

with ox-LDL resulted in a lower cell viability than with LDL (42.5 ± 1.0% versus 89.6 ± 19.0%,

P < 0.01), and was further decreased after 48 h treatment (16.8 ± 17.1% versus 106.5 ± 16.3%, P < 0.01) (Fig 3B) Therefore, we selected 50 lgÆmL)1 ox-LDL treatment for 24 h as the optimal stimulus in subsequent experiments

Macrophages treated with 50 lgÆmL)1 ox-LDL for

24 h were subjected to western blot analysis to determine the level of activated caspase-3 with 17 and 19 kDa, a marker of apoptosis, and showed an increased level of activated caspase-3 (see Fig 8A below)

TRB3 mediates macrophage apoptosis induced

by ox-LDL

We were able to express the cloned TRB3 protein suc-cessfully in mammalian cells using the adenoviral expression system only, because of the lack of effec-tiveness of other transfection techniques in this case The level of TRB3 protein was increased with increas-ing multiplicities of infection with adenovirus (Fig 4) Endogenous TRB3 protein could not be detected in nuclear extracts except when 100 lg total protein was used for western blot analysis, which indicates that the endogenous TRB3 protein is barely detectable and that the protein is present at low abundance in human mac-rophages

As cell apoptosis increased with increased TRB3 expression, we investigated the role of TRB3 in ox-LDL-induced macrophage apoptosis by determina-tion of cell viability Macrophages were transfected with adeno-TRB3 or empty vector and incubated for

an additional 24 h with or without ox-LDL MTT assay results revealed a reduced cell viability of macro-phages treated with 50 lgÆmL)1 ox-LDL for 24 h compared with vector controls (59.6 ± 8.5% versus

100 ± 0.2%, P < 0.01) (Fig 5A), and in TRB3-over-expressing macrophages compared with vector controls (67.1 ± 18.2% versus 100 ± 0.2%, P < 0.01)

140

160

60

80

100

120

LDL

A

B

ox-LDL

LDL

ox-LDL

*

0

20

40

Control 2.5 µg·mL –1

5 µg·mL–110 µg·mL–125 µg·mL–150 µg·mL–1

120

140

40

60

80

100

*

0

20

40

0 h 4 h 8 h 12 h 24 h 48 h

*

Fig 3 Effect of ox-LDL and LDL on macrophage cell viability by

MTT assay (A) Macrophages were treated with various

concentra-tions of ox-LDL or LDL for 24 h (B) Macrophages were treated

with 50 lgÆmL)1 ox-LDL or LDL for various durations *P < 0.05,

**P < 0.01 versus LDL-treated cells.

TRB3 GAPDH

Vector 50IFU 100IFU 200IFU

50 kDa

37 kDa

Fig 4 Western blot analysis of TRB3 protein expression in vitro Macrophages were transfected with purified recombinant adeno-TRB3 at multiplicities of infection of 50, 100 and 200 inclusion-forming units (IFU) or with vector (control), and the TRB3 level was analyzed 24 h later.

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Treatment of TRB3-overexpressing macrophages with

ox-LDL markedly reduced cell viability further

com-pared with vector control cells (46.0 ± 12.8% versus

100 ± 0.2%, P < 0.01) and with cells overexpressing

TRB3 alone (46.0 ± 12.8% versus 67.1 ± 18.2%,

P< 0.05), but no statistical difference was found

compared with ox-LDL-treated vector control cells

(46.0 ± 12.8% versus 59.6 ± 8.5%, P > 0.05)

Factorial analyses revealed a significantly lower cell

viability in macrophages treated with ox-LDL

com-pared to those that were not treated with ox-LDL

(50.4 ± 15.9% versus 69.0 ± 18.6%, P < 0.01), and

significantly lower cell viability in

TRB3-overexpress-ing cells than in non-TRB3-overexpressing cells

(46.9 ± 10.6% versus 73.5 ± 18.6%, P< 0.01) (Table 1) However, overexpression of TRB3 and stim-ulation with ox-LDL did not show a significant inter-action for cell viability (P = 0.206) Thus, overexpression of TRB3 compromises cell viability, with further reduction caused by ox-LDL; however, overexpression of TRB3 has no effect on cell viability already reduced by ox-LDL, which indicates that TRB3 is involved in part in macrophage survival With regard to apoptosis, the single-stranded DNA (ssDNA) absorbance of macrophages treated with ox-LDL was significantly higher than that in vector control cells (0.57 ± 0.02 versus 0.38 ± 0.04,

P < 0.01), and that of TRB3-overexpressing macro-phages was also significantly increased (0.52 ± 0.12 versus 0.38 ± 0.04, P < 0.05) (Fig 5B) In addition, TRB3-overexpressing macrophages treated with ox-LDL showed a significant increase in apoptosis compared with vector control cells (0.77 ± 0.15 versus 0.38 ± 0.04, P < 0.01), ox-LDL-treated vector con-trols (0.77 ± 0.15 versus 0.57 ± 0.02, P < 0.01) or cells with TRB3 overexpression alone (0.77 ± 0.15 versus 0.52 ± 0.12, P < 0.01)

Factorial analyses revealed no significant interaction between overexpressed TRB3 and ox-LDL stimulation with respect to apoptosis (Table 1) Apoptosis was significantly higher in TRB3-overexpressing than non-TRB3-overexpressing cells (0.67 ± 0.14 versus 0.46 ± 0.10, P < 0.01) and higher in cells treated with ox-LDL compared to those that were not treated with ox-LDL (0.64 ± 0.18 versus 0.48 ± 0.10, P < 0.01) Western blot analysis (see Fig 8B below) showed an increased activated caspase-3 protein level in TRB3-overexpressing cells compared with vector control cells,

an increased level in ox-LDL-treated TRB3-overex-pressing cells compared with ox-LDL-treated vector controls, and an increased level compared with TRB3 overexpression alone

To clarify the role of TRB3 in macrophage apopto-sis, siTRB3 was transfected into macrophages to silence TRB3 gene expression The expression of TRB3 mRNA was significantly reduced after siTRB3 trans-fection (Fig 6) MTT assay results showed that the cell

1

0

20

40

60

80

100

120

140

160

A

B

0.6

0.8

Vector

P < 0.01

P < 0.05

P < 0.01

P < 0.05

P < 0.05

P < 0.01

P < 0.01 P < 0.01

0

0.2

0.4

TRB3

Vector TRB3

Fig 5 Influence of TRB3 overexpression on macrophage

apop-tosis Macrophages were transfected with adeno-TRB3 or empty

vector before incubation for an additional 24 h with or without

ox-LDL (A) Cell viability evaluated by the MTT assay (B) Apoptosis

detected by ELISA.

Table 1 Parameters of apoptosis for the various treatment groups comprising overexpression of TRB3 and ⁄ or stimulation with ox-LDL Data are means ± SD TRB3, overexpression of TRB3; ox-LDL, oxidized low-density lipoprotein.

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viability of macrophages transfected with siTRB3 was

higher than in those transfected with control siRNA

(100 ± 1.7% versus 78.8 ± 2.6%, P < 0.01), and the

cell viabilities of cells treated with ox-LDL

(47.8 ± 1.8% versus 78.8 ± 2.6%, P< 0.01) or

silenced TRB3 followed by treatment with ox-LDL

(57.5 ± 5.3% versus 78.8 ± 2.6%, P < 0.01) were

both markedly decreased compared to that of

macro-phages transfected with siTRB3 With ox-LDL

treat-ment, cell viability of TRB3-silenced cells was

significantly higher than for cells transfected with

con-trol siRNA (57.5 ± 5.3% versus 47.8 ± 1.8%,

P< 0.05) (Fig 7A)

Factorial analyses revealed a significant interaction

between silenced TRB3 and ox-LDL stimulation with

respect to macrophage viability (P = 0.048) Cell

viability was significantly lower in macrophages treated

with ox-LDL compared to those that were not treated

with ox-LDL (52.2 ± 0.2% versus 89.4 ± 13.3%,

P< 0.01) and higher in TRB3-silenced cells than in

non-TRB3-silenced cells (73.5 ± 18.6 versus 46.9 ±

10.6, P < 0.01) (Table 2)

ELISA results showed that apoptosis of

TRB3-silenced macrophages was lower than that for control

siRNA-transfected cells (0.29 ± 0.01 versus

0.38 ± 0.05, P < 0.05) (Fig 7B), but apoptosis of

ox-LDL-treated cells was significantly higher

(0.75 ± 0.09 versus 0.38 ± 0.05, P < 0.01) as was

that of TRB3-silenced cells (0.48 ± 0.02 versus

0.38 ± 0.05, P < 0.01) Apoptosis of TRB3-silenced

cells treated with ox-LDL was significantly lower than

that for control siRNA-transfected cells (0.48 ± 0.02

versus 0.75 ± 0.09, P < 0.01)

Factorial analyses showed that apoptosis of

macro-phages was significantly higher in cells treated with

ox-LDL compared to those that were not treated with

ox-LDL (0.56 ± 0.21 versus 0.39 ± 0.10, P < 0.01)

and was lower in TRB3-silenced cells than in

non-TRB3-silenced cells (0.33 ± 0.06 versus 0.62 ± 0.15, P < 0.01) (Table 2) The interaction between silenced TRB3 and stimulation of ox-LDL was significant with respect to macrophage apoptosis (P = 0.001) Taken together, the results indicate that TRB3 resists macrophage apoptosis induced by ox-LDL Therefore, TRB3 was confirmed to mediate

in part the macrophage apoptosis induced by ox-LDL The level of activated caspase-3 protein was decreased upon siTRB3 transfection, but this reduction was attenuated with subsequent ox-LDL treatment (Fig 8C) The level of activated caspase-3 in the TRB3-silenced cells treated with ox-LDL was higher than that for control siRNA-transfected cells treated with ox-LDL

Discussion

As regulatory proteins, TRBs play an important role

in signal regulation of apoptosis As ox-LDL-induced macrophage apoptosis is implicated in the formation

of vulnerable atherosclerotic plaques, we investigated the role of the TRB3 gene in macrophage apoptosis induced by ox-LDL Human monocyte-derived macro-phages expressed TRB1, TRB2 and especially TRB3

1.6

0.8

1

1.2

1.4

0

0.2

0.4

0.6

**

Fig 6 Expression of TRB3 mRNA after treatment with siRNA.

Macrophages were transfected with siTRB3 or control siRNA for

24 h, then quantitative real-time PCR was performed to analyze

TRB3 mRNA expression **P < 0.01 versus control siRNA.

0 20 40 60 80 100 120 140

A

Control siRNA siTRB3

Control siRNA

P < 0.01

P < 0.01

P < 0.01

P < 0.05

P < 0.01

P < 0.01

P < 0.01

P < 0.05

siTRB3

0.5 0.4 0.6 0.7 0.8 0.9

0 0.1 0.2

0.3

B

Fig 7 Influence of TRB3 silencing on macrophage apoptosis Mac-rophages were transfected with siTRB3 or control siRNA for 24 h before incubation for an additional 24 h with or without ox-LDL (A) Cell viability evaluated by MTT assay (B) Apoptosis detected by ELISA.

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In addition, TRB3 mRNA expression was upregulated

in macrophages in a dose- and time-dependent manner

upon stimulation with ox-LDL Moreover, TRB3

promoted macrophage apoptosis and is involved in

ox-LDL-dependent macrophage apoptosis

The ox-LDL level is considered a risk factor for

ath-erosclerosis Ox-LDL is taken up by macrophages in a

rapid and uncontrolled manner, which accelerates the

formation of foam cells, the major cellular component

of fatty streaks Ox-LDL may also mediate

atherogen-esis by inducing macrophage apoptosis [14,15]

Although a high concentration of ox-LDL is cytotoxic

for cells, a low concentration can protect cells and

attenuate apoptosis in monocytic cells [16] We also

found that low concentrations of ox-LDL in human

monocyte-derived macrophages had no effect on

apop-tosis and high concentrations induced apoptosis

Apoptosis was markedly increased in mouse peritoneal

macrophages after stimulation with ox-LDL, and

increased macrophage apoptosis increased the size and

number of aortic atheromatous plaques and

phage infiltration of plaques [5], indicating that

macro-phage apoptosis promotes atherosclerosis progression

TRBs, the regulation of which is cell type-specific

[17], are expressed in many types of cells, such as

vas-cular smooth muscle cells, human umbilical cord

endo-thelial cells, and HeLa and HepG2 cells We found

that naturally differentiated macrophages expressed all

three TRB genes but predominantly TRB3 The

expression of TRB3 was significantly increased on

day 3 of differentiation into macrophages We also

found that endogenous TRB3 protein was barely

detected in untreated macrophages as reported previ-ously in untreated 293 cell [18]

TRB3 expression has been shown to be augmented

by multiple cellular stressors, including endoplasmic reticulum stress, hypoxia, oxidative stress, high glucose levels and advanced glycation end products [18–22], but few reports exist of the regulation of TRB3 expres-sion by ox-LDL in human primary macrophages We found that both mRNA and protein expression of TRB3 was upregulated by ox-LDL in human macro-phages in a dose- and time-dependent manner, in agreement with previous results [9] Moreover, the apoptosis of macrophages increased with increasing expression of TRB3 mRNA and protein

TRB3 inhibits cell mitosis and coordinates cell mor-phogenesis and migration in Drosophila by regulating String⁄ CDC25 proteolysis and promoting the degrada-tion of slbo [8,11] As a feedback regulator of the activating transcription factor 4– C⁄ EBP homologous protein (CHOP) pathway, TRB3 is involved in endo-plasmic reticulum stress-induced apoptosis of HepG2 and COS-7 cells [19,23,24] In addition, TRB3 expres-sion in lymphocytes induces G2 cell-cycle delay and cellular depletion [25] However, whether TRB3 is involved in the apoptosis of human monocyte-derived macrophages was unknown Caspase-3, a key molecule

in the classical apoptotic pathway, plays an important role in apoptosis induced by ox-LDL; ox-LDL induces macrophage apoptosis through activation of caspase-3 [26], so expression of activated caspase-3 is used as the primary measure of macrophage apoptosis We found that overexpression of TRB3 in human macrophages

Table 2 Parameters of apoptosis for the various treatment groups comprising silencing of the TRB3 gene and ⁄ or stimulation by ox-LDL Data are means ± SD siTRB3, siRNA targeting TRB3; ox-LDL, oxidized low-density lipoprotein.

Activated caspase-3

GAPDH

TRB3

ox-LDL siTRB3

19 kDa

17 kDa

Fig 8 Western blot analysis of expression of activated caspase-3 protein (A) Macrophages were treated with 50 lgÆmL)1ox-LDL for 24 h (B) Macrophages were transfected with recombinant adeno-TRB3 or empty vector for 24 h, then incubated for an additional 24 h with or without ox-LDL (C) Macrophages were transfected with siTRB3 or control siRNA for 24 h, then incubated for an additional 24 h with or without ox-LDL Expression was normalized to that of GAPDH.

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reduced cell viability, increased apoptosis and

aug-mented activated caspase-3 expression, which suggests

a role in increased macrophage apoptosis Apoptosis

was further increased in TRB3-overexpressing

macro-phages treated with ox-LDL Thus, TRB3 is involved

in ox-LDL-dependent macrophage apoptosis, possibly

through caspase-3

We found decreased cell viability of

TRB3-over-expressing macrophages treated with ox-LDL compared

with ox-LDL-treated control cells, but the differences

were not significant This finding could be explained by

the higher level of TRB3 in macrophages treated with

ox-LDL than in cells treated by transfection alone,

which would compromise the effect of overexpressed

TRB3 In addition, our experiment required that

macro-phages with overexpressed TRB3 be incubated with

ox-LDL; as overexpression of TRB3 promoted

phage apoptosis, many TRB3-overexpressing

macro-phages may have died before incubation with ox-LDL,

which would compromise the effect of ox-LDL

Fur-thermore, the MTT assay and ELISA results differed

ELISA showed higher apoptosis in

TRB3-overexpress-ing macrophages treated with ox-LDL than in control

cells treated with ox-LDL, but the MTT assay revealed

no significant difference The ELISA results may have

been more accurate than MTT results in detecting cell

apoptosis, or many macrophages may have died, to

indi-cate higher apoptosis Furthermore, the MTT assay

measures the net rate of apoptosis and proliferation,

and therefore TRB3 may influence macrophage

prolifer-ation rates just as TRB1 does [27]

Factorial analyses revealed that overexpression of

TRB3 and stimulation of ox-LDL can induce

macro-phage apoptosis, leading to reduced cell viability,

increased apoptosis and an increased level of activated

caspase-3 Ox-LDL aggravated the apoptosis of

TRB3-overexpressing macrophages, but overexpression

of TRB3 did not affect the apoptosis induced by

ox-LDL The interaction of TRB3 overexpression and

stimulation by ox-LDL was not significant, indicating

that TRB3 is involved only in part in macrophage

apoptosis induced by ox-LDL

To further clarify the function of TRB3, transfection

of siTRB3 into macrophages to silence TRB3 gene

expression resulted in increased macrophage viability,

decreased apoptosis and a reduced level of activated

caspase-3, which suggests decreased apoptosis of

mac-rophages Combined with the results above, this

dem-onstrates that TRB3 alone promotes macrophage

apoptosis However, ox-LDL treatment increased the

apoptosis of TRB3-silenced macrophages Further

analysis showed that TRB3 knockdown and

stimula-tion with ox-LDL affect macrophage apoptosis, with

significant interaction between the treatments In addi-tion, TRB3 knockdown attenuated the macrophage apoptosis, as indicated by the high level of activated caspase-3, induced by ox-LDL, which further confirms that TRB3 mediates ox-LDL-induced macrophage apoptosis through caspase-3 Although TRB3 bridges the gap between macrophage apoptosis and stimula-tion with ox-LDL, the specific cellular signal transduc-tion mechanism is still unclear Recently, TRB2 was shown to regulate the inflammatory activation of monocytes by the MAPK pathway [28] Furthermore, the TRB family has been reported to interact and modify the activity of the MAPK system [24] There-fore, TRB3 may mediates macrophage apoptosis via the MAPK pathway, which requires further study Macrophage apoptosis promotes vulnerable athero-sclerotic plaque progression As we found that TRB3

is implicated in macrophage apoptosis induced by ox-LDL and that TRB3 knockdown can attenuate ox-LDL-induced apoptosis, TRB3 may play a crucial role in the development of vulnerable atherosclerotic plaques by regulating apoptosis However, more stud-ies are necessary to elucidate the mechanism Our pre-liminary findings strongly suggest that TRB3 contributes to destabilization of atherosclerotic plaques through its effect on macrophage apoptosis

The signal regulation of macrophages involves a very complex network system ox-LDL has been found to induce macrophage apoptosis through activation of mul-tiple signaling pathways such as Akt and MAPK, and now TRB3 These findings provide a basis for further investigation of TRB3’s role in macrophage apoptosis and formation of vulnerable atherosclerotic plaques

In summary, expression of the regulatory protein TRB3, which is upregulated by ox-LDL in a dose- and time-dependent manner, exceeds that of other TRBs in naturally differentiated human macrophages TRB3 in part mediates macrophage apoptosis induced by ox-LDL, which suggests that TRB3 might be involved

in vulnerable atherosclerotic plaque progression

Experimental procedures

Isolation and culture of human monocyte-derived macrophages

Peripheral blood mononuclear cells were isolated under sterile conditions using endotoxin-free Histopaque-1077 medium (Sigma, St Louis, MO, USA) with a density gradi-ent cgradi-entrifugation technique [29] Cells were plated in 12- or 6-well plates at 3· 105

cellsÆmL)1and cultured in complete culture medium [RPMI-1640 containing 5% human serum (Sigma), 100 IUÆmL)1 penicillin and 100 lgÆmL)1

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streptomycin (both Gibco, Grand Island, NY, USA)] for

2 weeks for differentiation into macrophages Macrophages

were treated or transfected after 2–4 weeks, and exposed for

4–48 h to various concentrations of ox-LDL (Intracel,

Fred-erick, MD, USA) in serum-free medium Human natural

LDL was used as a negative control The study protocol

was approved by the local ethics committee and conformed

to the principles outlined in the Declaration of Helsinki

Quantitative real-time PCR

Total RNA was extracted from cells using an RNeasy mini

kit (Qiagen, Hamburg, Germany) Single-stranded cDNA

was synthesized using hexamer primers and the Superscript

first-strand synthesis system (Invitrogen, Carlsbad, CA,

USA) Quantitative real-time PCR was performed using an

Applied Biosystems TaqMan 7900HT detection system

(Applied Biosystems, Hitchin, UK) with specific primers as

follows (gene symbols and Applied Biosystems primer set

numbers in parentheses): TRB1 (Hs00179769_m1); TRB2

(Hs00222224_m1); TRB3 (Hs00221754_m1) Reactions were

performed in a MicroAmp Optical 96-well reaction plate,

with each reaction mixture containing 1· Master Mix,

200 lm forward and reverse primers and 100 lm probe in a

total volume of 25 lL PCR conditions were 50C for

2 min, 95C for 10 min, then 40 cycles of 95 C for 15 min

followed by 60C for 1 min The relative changes in gene

expression were analyzed by the 2()DDCT) method [30], and

normalized to the expression of GAPDH, as determined

using forward primer 5¢-GCCTTCCGTGTCCCCACT-3¢

and reverse primer 5¢-TGAGGGGGCCCTCCGACG-3¢

cDNA cloning and construction of recombinant

adenoviral TRB3

Human TRB3 open reading frames (ORF) were amplified

by PCR using primers 5¢-GAAGTTATCAGTCGACAT

GCGAGCCACCCCTCTGGCT-3¢ (forward) and 5¢-AT

GGTCTAGAAAGCTTCCATACAGACCACTT-3¢ (reverse)

(restriction sites are underlined) The forward primer was

designed with a unique SalI site, and the reverse primer

with a unique HindIII site PCR was performed using Pfu

Turbo DNA polymerase (Stratagene, La Jolla, CA, USA)

under the following conditions: initial denaturation at 95C

for 15 min, followed by 35 amplification cycles of

denatur-ation at 92C for 15 s, annealing at 55 C for 30 s, and

extension at 72C for 1 min, with a final extension step at

72C for 10 min A BD In-Fusion Dry-Down PCR cloning

kit (BD Biosciences, Franklin Lakes, NJ, USA) was used to

connect the TRB3 cDNA with a linearized pDNR-Dual

donor vector (BD Biosciences) at the unique SalI and

Hin-dIII sites to construct the plasmid pDNR-Dual⁄ TRB3,

which was transformed into Escherichia coli strain TOP10

(Invitrogen) After culturing of the transformed cells

over-night on LB-ampicillin medium (100 lg LB-agar mediumÆmL

ampicillin), the plasmid was amplified and isolated from PCR-screened positive clones DNA sequencing was performed to verify the fidelity of the PCR amplification Adenoviral constructs were prepared using a BD

Adeno-X Expression System 2 (BD Biosciences) according to the manufacturer’s protocol Briefly, the TRB3 gene was trans-ferred from the pDNR-Dual⁄ TRB3 construct (donor vec-tor) to pLP-Adeno-X viral DNA (acceptor vecvec-tor) After digestion with PacI, the recombinant adenoviral plasmid was used to transfect HEK293 cells (Perkin Elmer, Waltham, MA, USA) The adenovirus was isolated by the freeze–thaw method, and purified by use of an Adeno-X virus purification kit (BD Biosciences), and the virus titer was determined using a BD Adeno-X Rapid Titer kit (BD Biosciences)

Transfection of macrophages with recombinant adenoviral TRB3 and siRNA

Macrophages were plated in six-well plates at 3· 105 cell-sÆmL)1, and incubated at 37C in a 5% CO2 atmosphere Cells at 50–70% confluence were transfected with the puri-fied recombinant adenoviral TRB3 construct (adeno-TRB3)

at multiplicities of infection of 50, 100 and 200 inclusion-forming units using Lipofectamine 2000 reagent (Invitro-gen) Cells were incubated for 24 h post-transfection before treatment with ox-LDL or LDL

Double-stranded RNA duplexes targeting human TRB3 (5¢-GGUGUACCCCGUCCAGGAA-3¢) and control siRNA (purchased from Invitrogen) were transfected into macrophages using Lipofectamine 2000 reagent

Western blot analysis Macrophages were lysed to prepare total cell extracts Nuclear and cytoplasmic extracts were prepared according to the manufacturer’s instructions (Nuclear Extra Kit; Active Motif, Carlsbad, CA, USA) Proteins were separated on NuPAGE 4–12% Bis⁄ Tris gels (Invitrogen), transferred to nitrocellulose membranes, and incubated with antibody against TRB3 (IMGENEX, San Diego, CA, USA), antibody against caspase-3 or antibody against GAPDH (Abcam, Cambridge, UK), then horseradish peroxidase-conjugated secondary antibody (Abcam) Blots were developed using Supersignal West Dura extended duration substrate (Perbio, Tattenhall, UK) Images were captured using a Chemigenius imaging system (Syngene, Cambridge, UK)

Detection of cell viability (MTT assay) and apoptosis (ssDNA ELISA)

Macrophages cultured on 96-well plates were treated with ox-LDL or LDL or transfected with adeno-TRB3 or TRB3-targeting siRNA (siTRB3) At various time points,

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5 mgÆmL)1

3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazo-lium bromide (MTT) was added to each well to measure

cell viability [31] After a 4 h incubation at 37C, 100 lL

of dimethylsulfoxide was added to the wells to dissolve

any precipitate The absorbance was read at a wavelength

of 562 nm

Detection of apoptotic macrophages was achieved using

an ApoStrand ELISA apoptosis detection kit (BIOMOL

International, Plymouth Meeting, PA, USA), which

mea-sures ssDNA absorbance, according to the manufacturer’s

instructions

Statistical analysis

All experiments were performed in triplicate and repeated

at least three times Data are presented as means ± SD

Comparisons among groups were performed using one-way

ANOVA Interaction effects were tested by a general linear

model with a 2· 2 factorial design spss 16.0 (SPSS Inc.,

Chicago, IL, USA) was used for analysis A P-value

< 0.05 was considered statistically significant

Acknowledgements

This work was supported by the research grants from

the Key Technologies R & D Program of Shandong

Province (2006GG2202020), the National Natural

Sci-ence Foundation of China (30670874, 30570748 and

30871038) and the National Basic Research Program

of China (973 Program, grant number 2009CB521904)

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