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Among these factors, prostaglandin PG F2a, one of the primary prostanoids Keywords activating transcription factor-1; myocyte enhancer factor 2; NADPH oxidase; NOX1; vascular smooth musc

Trang 1

expression of NOX1 ⁄ NADPH oxidase, a vascular

superoxide-producing enzyme

Masato Katsuyama*, Muhammer Ozgur Cevik*, Noriaki Arakawa, Tomoko Kakehi, Toru Nishinaka, Kazumi Iwata, Masakazu Ibi, Kuniharu Matsuno and Chihiro Yabe-Nishimura

Department of Pharmacology, Kyoto Prefectural University of Medicine, Japan

Reactive oxygen species including hydrogen peroxide,

hydroxyl radical, singlet oxygen, peroxynitrite, and

superoxide (O2 ) have been documented as intrinsic

signaling molecules that modulate multiple cellular

responses The major source of O2 in vascular cells

and cardiac myocytes is the NADPH oxidase family

[1–3] NADPH oxidase catalyzes the reduction of

molecular oxygen to O2 using NADPH as an electron

donor A wealth of data has been collected on the

phagocyte NADPH oxidase, an essential component of

the host antimicrobial defense system [4] The

phago-cyte oxidase consists of the catalytic subunit gp91phox

(NOX2), the regulatory subunits p22phox, p47phox, p40phox and p67phox, and the small GTPase Rac Recent studies in nonphagocytic cells identified several homologs of the catalytic subunit NOX2 NOX1 is one of these homologs predominantly expressed in colon epithelial cells (CEC) and in vascular smooth muscle cells (VSMC)

The expression of NOX1 in VSMC is induced by various vasoactive factors, such as angiotensin II, platelet-derived growth factor (PDGF), phorbol ester, and fetal bovine serum [5,6] Among these factors, prostaglandin (PG) F2a, one of the primary prostanoids

Keywords

activating transcription factor-1; myocyte

enhancer factor 2; NADPH oxidase; NOX1;

vascular smooth muscle cells

Correspondence

C Yabe-Nishimura, Department of

Pharmacology, Kyoto Prefectural University

of Medicine, Kyoto 602–8566, Japan

Fax: +81 75 251 5348

Tel: +81 75 251 5333

E-mail: nchihiro@koto.kpu-m.ac.jp

*These authors contributed equally to this

work

(Received 2 June 2007, revised 26 July

2007, accepted 7 August 2007)

doi:10.1111/j.1742-4658.2007.06034.x

NADPH oxidase is a major source of the superoxide produced in cardio-vascular tissues Expression of NOX1, a catalytic subunit of NADPH oxi-dase, is induced by various vasoactive factors, including angiotensin II, prostaglandin (PG) F2a and platelet-derived growth factor (PDGF) To clarify the molecular basis of this transcriptional activation, we delineated the promoter region of the NOX1 gene RT-PCR and 5¢-rapid amplifica-tion of cDNA ends-based analyses revealed a novel 5¢-terminal exon of the rat NOX1 gene located approximately 28 kb upstream of the exon contain-ing the start codon Both PGF2a and PDGF enhanced the transcriptional activity of the ) 3.6 kb 5¢-flanking region of the NOX1 gene in A7r5 cells,

a rat vascular smooth muscle cell line A PGF2a-response element was located between )146 and )125 in the 5¢-flanking region containing a consensus binding site for myocyte enhancer factor 2 (MEF2), to which binding of MEF2 was augmented by PGF2a Gene silencing of MEF2B

by RNA interference significantly suppressed the expression of NOX1, while silencing of activating transcription factor (ATF)-1, previously impli-cated in up-regulation of NOX1, abolished the PGF2a- or PDGF-induced expression of MEF2B These results indicate that superoxide production in vascular smooth muscle cells is regulated by the ATF-1–MEF2B cascade

by induction of the expression of the NOX1 gene

Abbreviations

ATF, activating transcription factor; CEC, colon epithelial cells; CRE, cAMP response element; CREB, cAMP response element-binding protein; dsRNA, double-stranded RNA; EMSA, electrophoresis mobility shift assay; MEF, myocyte enhancer factor; PDGF, platelet-derived growth factor; PG, prostaglandin; PI3, phosphoinositide 3; VSMC, vascular smooth muscle cells.

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generated in the vascular tissue, was also shown to

induce the expression of NOX1 mRNA and cause

hypertrophy of VSMC through increased generation of

O2 [7] In PGF2a-induced as well as PDGF-induced

NOX1 expression, transactivation of the epidermal

growth factor receptor, which depends on protein

kinase C d, elicits activation of extracellular

signal-regulated kinase 1⁄ 2 as well as of phosphoinositide 3

(PI3) kinase Downstream of PI3 kinase, a

transcrip-tion factor of the cAMP response element

(CRE)-binding protein (CREB)⁄ activating transcription factor

(ATF) family, ATF-1, was suggested to take part in the

induction of NOX1 expression [8–10]

Except for the involvement of ATF-1, the entire

picture of the transcriptional regulation of the NOX1

gene has not been clarified yet In the upstream

region of the human NOX1 gene, an

interferon-c-responsive element was recently identified, which

reg-ulates the expression of NOX1 in CEC [11] On the

other hand, we recently depicted novel transcripts of

the mouse NOX1 gene that were induced to express

under phenotypic modulation of VSMC Of particular

interest is that these transcripts were governed by

promoters different from the one utilized for

expres-sion of the NOX1 transcript in CEC [12] To clarify

the molecular basis of the transcriptional activation

of NOX1 in vascular tissue, we delineated the

pro-moter region implicated in the up-regulation of

NOX1 gene expression We report here the

predomi-nant role of the ATF-1-myocyte enhancer factor 2B

(MEF2B) cascade in superoxide production in

vascu-lar smooth muscle cells by inducing the expression of

the NOX1 gene

Results

Determination of the 5¢-end of the NOX1 mRNA expressed in VSMC

We reported the expression of novel NOX1 transcripts (c- and f-types) in mouse VSMC, which encoded an extended N-terminal peptide sequence upstream of the form expressed in CEC (a-type) [12] We searched the rat genomic database and found the counterpart of the mouse NOX1 exon 1c, the 5¢-terminal exon of the c-type mRNA RT-PCR was then performed in primary VSMC or PGF2a-stimulated A7r5 cells, a rat vascular smooth muscle cell line, using a forward primer for the rat counterpart (ex1c2F in Fig 1A), and a reverse primer covering the start codon of the NOX1 mRNA (NR3 in Fig 1A) Amplified products were sequenced and the 5¢-terminus of the NOX1 transcript was determined by 5¢-RACE The 5¢-terminus encoded

433 bp of exon 1c, and it was placed upstream of exon 1a containing the start codon (Fig 1B) Unlike the mouse c-type mRNA, however, the rat c-type-like NOX1 mRNA neither contained the counterpart of the mouse exon 1b nor encoded an additional N-terminal peptide Although the counterpart of the mouse exon 1f was found in the genomic database, an f-type-like transcript was not detected by RT-PCR in A7r5 cells

PGF2a- and PDGF-induced transcriptional activation of the NOX1 promoter

To examine whether the promoter region of the rat NOX1 gene contains elements responsive to vasoactive

NOX1 mRNA

1a 2

chrX

3 k

28 k

433

ATG

Intron Exon

A

B

Fig 1 Structure of the rat NOX1 gene and

mRNA (A) 5¢-Nucleotide sequences of the

rat NOX1 cDNA and deduced amino acid

sequences at the beginning of the open

reading frame Primers used for RT-PCR

and 5¢-RACE are indicated with arrows.

(B) The exon ⁄ intron structure of the NOX1

gene and its splicing pathway Open boxes

indicate exons Numbers in the box denote

the size of each exon (bp) The size of the

intron is indicated under the broken lines

(bp) Closed boxes show the open reading

frame of the transcript.

Trang 3

factors, approximately 3.6 kb of the 5¢-flanking region

of exon 1c was isolated and subcloned into a luciferase

vector As demonstrated in Fig 2A, the transcriptional

activity of the NOX1 promoter, r3642Luc, in A7r5

cells was significantly enhanced when cells were treated

with PGF2a or PDGF These findings suggest that the

3.6 kb of the 5¢-flanking region contains sequences

responsible for PGF2a-induced as well as

PDGF-induced transcriptional activation As the activation by

PGF2a was more prominent than that by PDGF,

PGF2awas used for the subsequent promoter analyses

MEF2-binding site was essential for transcriptional

activation of the NOX1 promoter

To identify the region responsible for the

transcrip-tional activation, a series of deletion mutants of the

NOX1 promoter-luciferase chimera plasmids were con-structed As shown in Fig 2B, deletion up to)489, but not to )930, reduced PGF2a-induced transcriptional activation, suggesting the existence of an enhancer binding site between )930 and )489 Deletion up to )125, but not to )146, completely abolished the PGF2a-induced transcriptional activation Between )146 and )125, a consensus sequence of the MEF2-binding site, 5¢-CTA(A ⁄ T)4TAG⁄ A-3¢, was located (Fig 3A) The introduction of mutations at this site (5¢-CTATAAATAG-3¢ to 5¢-CTATAgccAG-3¢) abolished PGF2a-induced transcriptional activation (Fig 3B) These findings clearly indicate that the MEF2-binding site between )139 and )130 is essential for PGF2a-induced activation of the NOX1 promoter

Binding of MEF2 to the consensus sequence in the NOX1 promoter

To verify whether the transcription factor MEF2 actu-ally binds to the consensus sequence in the NOX1 pro-moter, an electrophoretic mobility shift assay (EMSA) was carried out using nuclear extracts obtained from A7r5 cells (Fig 4) With the probe containing the con-sensus MEF2-binding site of the NOX1 promoter, several bands were observed (lane 1, Fig 4A) Among these bands, those indicated by arrowheads were mark-edly diminished when the mutated probe was utilized (lane 5) Stimulation of A7r5 cells with PGF2aincreased the intensity of these bands (lane 2), whereas the bands were undetectable in the presence of an excess amount

of the unlabeled wild-type probe (lane 3) By contrast, the bands persisted in the presence of an excess amount

of the mutated probe (lane 4) As shown in Fig 4B, pre-incubation of the nuclear extract with an anti-MEF2 IgG generated supershifted bands as indicated

by arrowheads (lane 3) On the other hand, pre-incuba-tion with an anti-ATF-1 IgG did not affect the mobility

of the specific bands (lane 4, Fig 4B) These results suggest that PGF2a increases the binding of MEF2

to the consensus-binding site located between )139 and)130 of the NOX1 promoter

Gene silencing of MEF2B attenuated PGF2a- or PDGF-induced NOX1 expression

There are four types of MEF2 – MEF2A, MEF2B, MEF2C, and MEF2D – and these subtypes are enco-ded by distinct genes [13] In A7r5 cells, MEF2A, MEF2C and MEF2D were constitutively highly expressed, whereas the expression level of MEF2B was very low (see Fig 5A, Cycles of PCR) Upon stimula-tion with PGF2a or PDGF, however, the expression of

Relative Luciferase Activity

–91 –125 –146 –235 –323

–489

–930

pGL3basic

–3642

AP TA

Relative Luciferase Activity

PGF 2α

A

B

PGDF

*

*

*

*

*

*

*

*

Fig 2 Analyses of the NOX1 promoter activity in A7r5 cells.

(A) PGF2a- or PDGF-induced transcriptional activation of the NOX1

promoter The 3.6 kb of the 5¢-flanking region of exon 1c was

cloned into pGL3-basic and the reporter construct was transfected

into A7r5 cells The b-galactosidase-expression vector was

cotrans-fected as an internal control Serum-starved cells were incubated

with 100 n M PGF2aor 20 ngÆmL)1PDGF-BB for 24 h The relative

luciferase activity is denoted as the fold-increase induced by PGF 2a

or PDGF Bars represent means ±SE of three experiments.

Open bar, pGL3-basic; closed bar, r3642Luc *P < 0.01 versus

pGL3-basic (B) Deletion of the MEF2-binding site abolished

PGF2a-induced transcriptional activation A schematic diagram of

the promoter-luciferase fusion plasmids is shown on the left,

where the 5¢ ⁄ 3¢ ends of the construct relative to the transcription

initiation site are indicated The relative luciferase activity is

denoted as the fold-increase induced by PGF2a Bars represent

means ±SE of three experiments *P < 0.01 versus pGL3-basic.

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MEF2B was markedly augmented (Fig 6A, mock).

We therefore focused on the role of MEF2B in the

PGF2a- or PDGF-induced up-regulation of NOX1

gene expression An expression vector coding a

dou-ble-stranded RNA (dsRNA) targeting nucleotides 470–

494 of the rat MEF2B mRNA sequence was

intro-duced into A7r5 cells Following single cell cloning of

the transfectants, two clones stably expressing the

dsRNA, MEF2B-RNAi-1 and MEF2B-RNAi-2, were

isolated In these clones, mRNA levels of MEF2B, but

not those of other types of MEF2, were reduced

com-pared to levels in the mock-transfected cells (Fig 5A)

As shown in Fig 5B, induction of NOX1 mRNA

expression by PGF2aor PDGF was almost completely

abolished in MEF2B knocked-down cells In addition,

a PGF2a-induced increase in O2 production as well as

the basal level of cellular O2 was reduced in these

clones compared with the mock-transfected cells

(Fig 5C) These results highlight the pivotal role of

MEF2B in the PGF2a- or PDGF-induced

up-regula-tion of NOX1 expression

Gene silencing of ATF-1 attenuated PGF2a- or

PDGF-induced MEF2B expression

We previously reported the involvement of ATF-1, a

transcription factor of the CREB⁄ ATF family, in the

up-regulation of NOX1 expression in VSMC [8] ATF-1 elicits transcriptional activation by binding to the cAMP response element (CRE) As CRE was not found in the promoter region of the NOX1 gene, ATF-1 was assumed to indirectly regulate the expres-sion of the NOX1 mRNA We therefore elucidated the role of ATF-1 in the MEF2B-dependent activation of NOX1 expression As shown in Fig 6, the expression

of MEF2B mRNA induced by PGF2a or PDGF was almost completely abolished in ATF-1 knocked-down clones that we previously isolated [8] These findings provide a clear link between ATF-1 and MEF2B, in that expression of MEF2B in VSMC is governed by ATF-1 itself

Discussion The major lines of evidence provided by this study are

as follows: (a) the 5¢-terminus of the rat NOX1 mRNA expressed in VSMC was a counterpart of the mouse c-type mRNA induced under phenotypic modulation

of VSMC; (b) the promoter region of the NOX1 gene contained a consensus MEF2-binding site that confers the responsiveness to PGF2a; (c) stimulation with PGF2aenhanced the binding of MEF2 to its consensus binding site in the NOX1 promoter; (d) RNA interfer-ence targeted at MEF2B abolished expression of the

Relative Luciferase Activity

–125

–146

luc

pGL3basic –146mut

1c

B

A

A T

*

Fig 3 PGF 2a -induced transcriptional activation of the NOX1 promoter was dependent on the MEF2-binding site (A) A consensus sequence

of the MEF2-binding site and the AP-1 site, and a TATA-like sequence located upstream of the transcription initiation site (B) Introduction of mutations at the MEF2-binding site (5¢-CTATAAATAG-3¢ to 5¢-CTATAgccAG-3¢) abolished PGF 2a -induced transcriptional activation A sche-matic diagram of the promoter-luciferase fusion plasmids is shown on the left, where the 5¢ ⁄ 3¢ ends of the construct relative to the tran-scription initiation site are indicated The relative luciferase activity is denoted as the fold-increase induced by PGF 2a Bars represent means

±SE of three experiments *P < 0.01 versus pGL3-basic.

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NOX1 mRNA induced by PGF2a or PDGF; (e) RNA

interference targeted at ATF-1 attenuated the

induc-tion of MEF2B expression by PGF2aor PDGF Based

on these findings and those of our earlier studies

[8–10], it is reasonable to conclude that the

ATF-1-MEF2B cascade constitutes the major signaling

path-way that leads to the up-regulation of NOX1 gene

expression in VSMC

The 5¢-terminus of the NOX1 mRNA identified in rat VSMC was a counterpart of the mouse c-type mRNA which was expressed in dedifferentiated

origin

probe

MEF2

PGF 2αα

PGF 2α

– + + + +

supershift

lane

A

B

1 2 3 4 5

anti ATF-1 Ab

origin

MEF2

– + + +

– –

– +

free

probes

Fig 4 PGF 2a increased binding of MEF2 to the consensus

sequence (A) Specific bands detected by EMSA Nuclear extracts

were prepared from A7r5 cells incubated with 100 n M PGF2a for

8 h Binding specificity was evaluated with a 100-fold excess of

unlabeled oligonucleotide (lane 3), and with a mutated

oligonucleo-tide probe (lane 5) (B) Supershift bands demonstrated in the

presence of an anti-MEF2 IgG Nuclear extracts were pre-incubated

in the presence or absence of an anti-MEF2 IgG or an anti-ATF-1

IgG.

0 2 4 6

NOX1 GAPDH

mock

MEF2B RNAi-1

MEF2B RNAi-2

Control PGF 2αα

PGF

PGF

2α Control Control

Cycles of PCR

mock RNAi-1 RNAi-2 anti-MEF2B

A

B

C

dsRNA

GAPDH

MEF2B MEF2A MEF2C MEF2D

(40) (40) (25) (25) (25) (25)

mock MEF2BRNAi-1 MEF2BRNAi-2

0 50 60 70 80

90 *

*

*

Fig 5 Gene silencing of MEF2B attenuated PGF2a- or PDGF-induced NOX1 expression (A) Expression of anti-MEF2B dsRNA precursors and silencing of MEF2B expression in the MEF2B RNAi-1 and RNAi-2 clones Total RNA was reverse-transcribed and the cDNA fragments were amplified by PCR (B) Induction of the NOX1 mRNA expression by PGF2a or PDGF was suppressed in RNAi-1 and RNAi-2 A representative northern blot is shown Bars represent the mean ±SE of three experiments *P < 0.01 versus mock control (C) Ethidium fluorescence in the cells untreated (control; open bar) or treated with 100 n M PGF2a(closed bar) for

24 h Mean values of ethidium fluorescence were calculated from four samples *P < 0.05 versus control mock-transfected cells P < 0.05 versus mock-transfected cells treated with PGF2a.

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VSMC The rat NOX1 mRNA, however, did not

con-tain the counterpart of the mouse exon 1b, which

encoded an additional N-terminal peptide upstream of

exon 1a Unlike the NOX1 mRNA expressed in

VSMC, the transcript identified in rat colon or intact

aorta did not contain exon 1c at the 5¢-terminus (data

not shown) The transcript expressed in VSMC

con-tained an extended 5¢-untranslated region that differed

from the colon-type NOX1 mRNA Accordingly, the

5¢-flanking region of exon 1c appears to contain

ele-ments essential for the specific expression of the NOX1

mRNA in dedifferentiated VSMC In the aorta or in a

vascular smooth muscle cell line (T⁄ G HA-VSMC) of

human origin, the c-type-like mRNA has not been

identified so far (data not shown) Thus there seems to

be considerable species–specific differences in the

regu-lation of the NOX gene expression in VSMC It should

be noted that another catalytic subunit of NADPH

oxidase, NOX5, is expressed in human VSMC [14],

but not in rodents

The MEF2-binding site in the promoter region was

shown to be elemental for induction of NOX1

expres-sion in VSMC This site was also conserved in the

mouse NOX1 gene To date the functional role of

MEF2 documented in VSMC has been somewhat

con-troversial MEF2A was reported to be involved in an

angiotensin II-induced vascular hypertrophy [15], and

in inducing the expression of monocyte

chemo-attractant protein-1 [16], which plays a key role in the

development of atherosclerosis and restenosis after

angioplasty Conversely, MEF2B was reported to bind

to the promoter region of the smooth muscle myosin

heavy chain gene to regulate the transcription of the

smooth muscle-specific gene expression [17]

Intrigu-ingly, MEF2B was documented to be highly expressed

in neointima of balloon-injured carotid artery [18], which suggests that the expression of MEF2B is up-regulated under phenotypic modulation of VSMC Among four types of MEF2, MEF2A, MEF2C and MEF2D were constitutively expressed in A7r5 cells, and the levels of these transcripts were relatively high

By contrast, the basal level of the MEF2B mRNA was very low, but expression of MEF2B was increased upon stimulation with PGF2a or PDGF In MEF2B knocked-down cells, the induction of NOX1 mRNA expression by PGF2a or PDGF was almost completely abolished, whereas it was unaffected in MEF2A knocked-down clones (data not shown) Accordingly, inducible expression of MEF2B appears to up-regulate the NOX1 gene expression in VSMC

Previously, the involvement of ATF-1, a transcrip-tion factor of the CREB⁄ ATF family, was suggested in the up-regulation of NOX1 expression by various vasoactive factors [8] ATF-1 is known to activate transcription of genes by binding to CRE In the 3.6 kb promoter region of the rat NOX1 gene, how-ever, a canonical CRE was not found This suggests

an indirect involvement of ATF-1 in the NOX1 tran-scription, though there might be other ATF-1 binding sites elsewhere in the NOX1 gene We also observed that phosphorylation of ATF-1 occurred within 5 min

of stimulation with PGF2a [8], whereas expression of the NOX1 mRNA was not observed until 3 h after the stimulation [7] These findings support the view that ATF-1 indirectly regulates the NOX1 gene expression, possibly by up-regulating the expression of the genes encoding other transcription factors It should be pointed out that a consensus CRE sequence was located approximately 2.6 kb upstream of the tran-scription start site of the rat MEF2B gene (rat MEF2B mRNA, GenBank BC079361; genomic sequence, rat chromosome 16) In accord with this observation, the PGF2a- or PDGF-induced increase in MEF2B mRNA was almost completely abolished in ATF-1 knocked-down clones These results strongly suggest the involvement of the ATF-1-MEF2B cascade in the reg-ulation of vascular NOX1 gene expression

We previously reported the pathophysiological significance of NOX1-derived reactive oxygen species

in angiotensin II-induced chronic hypertension using NOX1-deficient mice [19] The basal level of the NOX1 transcript is much lower than the levels of other NOX isoforms expressed in vascular tissue, whereas inducible expression of NOX1 has been docu-mented in association with various vascular disorders

In this context, identification of the ATF-1-MEF2B cascade involved in the up-regulation of NOX1

MEF2B

GAPDH

mock

ATF-1 RNAi-5

ATF-1 RNAi-16

ControlPGF

2αα

Control PG

F 2α

Control PGF

2α

0

1

2

3

4

5

*

Fig 6 Gene silencing of ATF-1 attenuated PGF 2a - or PDGF-induced

MEF2B expression Expression of the MEF2B transcript was

exam-ined by RT-PCR in the ATF-1 RNAi-5 and RNAi-16 clones Bars

rep-resent the mean ±SE of three experiments *P < 0.05 versus

mock control.

Trang 7

gene expression may lead to a better understanding

of regulatory mechanisms in vascular superoxide

production

Experimental procedures

Materials

PGF2awas purchased from Nacalai Tesque (Kyoto, Japan)

Antibodies against MEF2 and ATF-1 were obtained from

Santa Cruz Biotechnology (Santa Cruz, CA) PDGF-BB

was obtained from PEPROTECH (London, UK) [c-32

P]-ATP, [a-32P]-UTP, and [a-32P]-dCTP were from ICN

Bio-medicals (Costa Mesa, CA)

Cell culture

The A7r5 cell line, obtained from American Type Culture

Collection (Rockville, MD), was cultured in Dulbecco’s

modified Eagle’s medium (DMEM) supplemented with

10% fetal bovine serum Primary VSMC were isolated from

Sprague-Dawley rats by a migration method [20]

5¢-RACE

5¢-RACE was carried out using a-3¢ ⁄ 5¢-RACE kit (Roche,

Basel, Switzerland) Total RNA isolated from either A7r5

cells or primary VSMC was reverse transcribed with the

primer NR1, which is complementary to nucleotides 207–

231 of the rat NOX1 mRNA (GenBank AF152963;

Fig 1A) The cDNAs were tagged with dATP using

termi-nal deoxytransferase The first round of amplification was

carried out using the oligo dT-anchor primer and the

sec-ond primer NR2, complementary to nucleotides 182–206 of

the rat NOX1 mRNA The resulting PCR products served

as templates for the subsequent nested amplification of

cDNAs specific for NOX1 For this amplification, the

anchor primer and the primer cup1R or cup2R,

comple-mentary to the sequence in exon 1c, were utilized (Fig 1A)

Based on the sequencing analyses, the 5¢-end of the longest

cDNA clones was regarded as the transcriptional start site

and denoted as +1

Reporter constructs and luciferase assay

The rat genomic DNA was isolated from A7r5 cells with a

PUREGENE DNA Isolation Kit (Gentra SYSTEMS,

Min-neapolis, MN) The 5¢-flanking region of the rat NOX1

gene was amplified by PCR and cloned into the vector

pGL3-basic (Promega, Madison, WI) The 3.6 kb

5¢-flank-ing region was cloned into the HindIII site of pGL3-basic

A series of 5¢-deletion constructs were made by cleavage

with restriction enzymes or amplification by PCR All

con-structs were subjected to sequencing analyses to verify the

orientation and fidelity of the insert Luciferase plasmids (0.75 lgÆwell)1) and a pSV-b-galactosidase control vector (0.25 lgÆwell)1; Promega) were cotransfected into A7r5 cells with FuGENE 6 Transfection Reagent (Roche) The cells were then cultured for 24 h, and a further 24 h in serum-free DMEM They were subsequently incubated for 24 h in the presence or absence of 100 nm PGF2a or 20 ngÆmL)1 PDGF-BB Luciferase activity in cell lysates was deter-mined and normalized with b-galactosidase activity as described previously [21]

EMSA The EMSA was performed essentially as described previously [22] A double-stranded probe containing an MEF2-binding site was prepared by annealing complemen-tary synthetic oligonucleotides The sense sequence was 5¢-GATTCTTCTATAAATAGGTACTTTCCCTCA-3¢ The sequence of the mutated probe was 5¢-GATTCTTCT ATAgccAGGTACTTTCCCTCA-3¢ Probes were labeled at the 5¢-end with [c-32

P]-ATP and T4 polynucleotide kinase Nuclear extracts of A7r5 cells were prepared as described previously [8] The nuclear extracts and the labeled probe were incubated at 25C for 30 min, resolved in a 4% polyacrylamide gel, and analyzed using a Fujix BAS 2000 Bio-imaging Analyzer (Fuji Film, Tokyo, Japan)

Gene silencing of MEF2B The anti-MEF2B dsRNA was designed against nucleotides 470–494 of the rat MEF2B mRNA sequence (GenBank BC079361) Sense and antisense oligonucleotides containing the hairpin sequence, the terminator sequence, and hanging sequences were synthesized By annealing over-hanging sequences of the synthetic oligonucleotides, PCR was performed to amplify the sequence encoding the dsRNA, which was inserted into pPUR-KE harboring a tRNAValpromoter A7r5 clones stably expressing the anti-MEF2B dsRNA were obtained as described previously [7] Cells incubated for 48 h in DMEM containing 0.5% fetal bovine serum were exposed to 100 nm PGF2a or

20 ngÆmL)1 PDGF-BB for 24 h, and used for the subse-quent isolation of total RNA Northern blot analysis and measurement of intracellular O2 production using a flow cytometer were performed as described previously [7,8] The geometric mean of ethidium fluorescence intensity was used for analysis

Statistical analysis Values were expressed as the mean ± SE The statistical analysis was performed with Student’s t-test For multiple treatment groups, a one-way anova followed by Bonferroni’s t-test was applied

Trang 8

This work was supported in part by Grant-in-Aid for

Young Scientists (B) 17790173 from The Ministry of

Education, Culture, Sports, Science and Technology of

Japan (MK) The nucleotide sequences reported in this

paper have been submitted to DDBJ⁄ EMBL ⁄ GenBank

with accession number AB258525 We thank Dr

S Tsuchiya, Graduate School of Pharmaceutical

Sciences, Kyoto University, for valuable discussions

and advice

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