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Moreover, ectopic expres-sion of miR-203 promoted the apoptosis of human bladder cancer cell lines and inhibited cell proliferation, whereas its depletion increased cell growth.. We demo

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repressing bcl-w expression

Juanjie Bo, Guoliang Yang, Kailing Huo, Haifeng Jiang, Lianhua Zhang, Dongming Liu and

Yiran Huang

Department of Urology, Renji Hospital, Shanghai Jiaotong University, China

Introduction

Human bladder cancer is the fourth most common

malignancy in men, and the tenth most common in

women [1] Molecular and pathological studies suggest

that bladder cancers comprise at least two major

groups The majority of malignant bladder tumors are

urothelial cell carcinomas evolved from the epithelial

lining of the bladder wall [2] The urothelial

carcino-mas are noninvasive papillary tumors that commonly

recur, but rarely progress [3] Patients with tumors in

this group require long-term monitoring Invasive

bladder tumors are more aggressive, presenting with

penetration of the basement membrane or invasion

into muscle Patients with invasive disease have a

much worse prognosis, with a 5-year survival rate of

50% [4] The high frequency of recurrence of

noninva-sive urothelial carcinoma and the poor prognosis of

invasive bladder tumors highlight the necessity for

development of effective targeted therapies [5] How-ever, the lack of effective therapies for advanced blad-der cancer is related to poor unblad-derstanding of the molecular mechanisms underlying the progression of this disease [6]

Apoptosis is believed to be the major mechanism of chemotherapy⁄ radiotherapy-induced cell death in blad-der cancer [7] Unfortunately, many tumor cells evade drug-induced death signals, and certain oncogenes such

as bcl-2 and bcl-w can become overexpressed, resulting

in chemotherapy⁄ radiotherapy resistance [8] Bcl-2 family proteins are essential regulators of apoptosis, and bcl-w is anti-apoptotic member of this family Bcl-w maintains cell viability by preventing mitochon-dria-mediated apoptosis [9,10] Overexpression of bcl-w can prevent cell death, and is a potential mediator of resistance to several chemotherapeutic drugs [11]

Keywords

apoptosis; bcl-w; bladder cancer; miR-203;

proliferation

Correspondence

D Liu, Department of Urology, Renji

Hospital, School of Medicine Shanghai

Jiaotong University, No 145 Shan Dong

Middle Road, Shanghai 200001, China

Fax: +86 21 6373 0455

Tel: +86 21 6373 0455

E-mail: dmliu@hotmail.com

(Received 16 November 2010, revised 13

December 2010, accepted 22 December

2010)

doi:10.1111/j.1742-4658.2010.07997.x

It is increasingly clear that microRNAs (miRNAs) play an important role

in many diseases, including tumorigenesis However, the mechanisms by which miRNAs regulate bladder cancer development remain poorly under-stood Here, we evaluated the expression of microRNA-203 (miR-203) in bladder cancer tissues using real-time PCR, and defined the target genes and biologically functional effect using luciferase reporter assay, flow cytometry and western blot analysis We first verified that the expression of miR-203 was decreased in bladder cancer tissues Moreover, ectopic expres-sion of miR-203 promoted the apoptosis of human bladder cancer cell lines and inhibited cell proliferation, whereas its depletion increased cell growth

We further verified that miR-203 directly targeted 3¢-untranslated region of the bcl-w gene, and decreased its expression in vitro and in vivo Western blot analysis also showed that the expression level of miR-203 was nega-tively correlated with bcl-w level in tumor tissues These data suggest an important role for miR-203 in the molecular etiology of bladder cancer and implicate the potential application of miR-203 in bladder cancer therapy

Abbreviations

miRNA, microRNA; miR-203, microRNA-203; UTR, untranslated region.

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However, the regulation of endogenous bcl-w

expres-sion is complex For example, Michela et al showed

the role of Akt in apoptosis resistance by interacting

with bcl-w [12] They demonstrated that Akt interacted

with the N- and C-terminal sequences of the bcl-w

protein, and phosphorylated bcl-w both in vitro and in

the intact cell Lapham et al [13] demonstrated that

TCF4 and beta-catenin interacted with the bcl-w

pro-moter, and the activity of the bcl-w promoter was

increased or decreased, respectively, by overexpression

of beta-catenin or dominant negative TCF4 Lin et al

[14] showed that bcl-w is a direct target of miR-122

that functions as an endogenous apoptosis regulator in

these HCC-derived cell lines

There is increasing evidence that post-transcriptional

regulation of gene expression, mediated by

micro-RNAs (mimicro-RNAs), plays an important role in the

con-trol of cells proliferation, apoptosis and tumorigenesis

[15–17] miRNAs are noncoding RNAs that have been

highly conserved during evolution and have emerged

recently as potent regulators of gene expression

Over-expression of oncogenic miRNAs and underOver-expression

of tumor suppressor miRNAs play pivotal roles

in tumorigenesis Gottardo et al [18] compared the

miRNA profile of bladder cancers and noncancer

blad-der tissues, and found that 10 miRNAs were

upregu-lated MicroRNA-203 (miR-203), possessing a tumor

suppressive activity, was also downregulated in bladder

cancer tissues [19,20] However, the relationship

between miR-203 and bladder cancer is remains

unknown

In this study, we investigated the role of miR-203 in

bladder cancer development We demonstrated that

expression of miR-203 was downregulated in bladder

cancer tissues, and decreased expression of miR-203

contributed to cells proliferation Finally, we confirmed

that bcl-w is the direct target of miR-203

Results

Expression of miR-203 is significantly

downregulated in bladder cancer

In order to assess the role of miR-203 in bladder

can-cer development, we first evaluated the different

expression of miR-203 in bladder cancer tissues and

normal bladder tissues by using quantitative real-time

PCR Figure 1 shows that miR-203 was expressed at

low levels in bladder cancer tissue, and miR-203 levels

were increased in normal bladder tissue The mean

level of miR-203 expressed in normal bladder tissues

was 2.7, whereas the mean level of miR-203 expressed

in bladder cancer tissues was 1.4 (Fig 1) These data

indicate that down-regulation of miR-203 may be related to bladder cancer development

miR-203 promotes cells apoptosis in vitro

To study the physiological role of miR-203 in cell growth, bladder cancer cell lines treated with miR-203,

or microRNA control, were analyzed Figure 2A shows that overexpression of miR-203 promoted cell apoptosis in T24 cells, a bladder cancer cell line More-over, compared with the nonspecific microRNA con-trol (NC), miR-203 inhibited T24 cells proliferation (Fig 2B), whereas its depletion promoted cell growth (Fig 2C) These data suggest that miR-203 negatively regulates the growth of bladder cancer cells

bcl-w is a target gene of miR-203

In order to identify the target genes of miR-203 in regu-lating bladder cancer cell apoptosis, we searched for candidate genes using TargetScan 5.1 (http://www targetscan.org/) and miRBase (http://www.mirbase org/) microRNA databases The bcl-w gene is one of predicted target genes of miR-203 (Fig 3A), and is an important member of the bcl-2 family described as one

of the anti-apoptotic protein So, we constructed a

fire-fly luciferase reporter containing the 3¢-untranslated region (UTR) of bcl-w We then cotransfected HEK293 cells with the pGL3-promoter–bcl-w–3¢-UTR and miR-203 The reporter assay showed that miR-203 was

0.0

Normal Tumor

*

0.5 1.0 1.5 2.0 2.5 3.0 3.5 4.0 5.0

4.5

Fig 1 miR-203 was downregulated in bladder tumor tissues Analy-sis of miR-203 expression level was performed in bladder tumor tissues (n = 13) or normal bladder tissues (n = 9) Total RNA was subjected to real-time RT-PCR to analyze the expression level of miR-203 in each sample U6 was used as reference for miRNAs Each sample was analyzed in triplicate The 2)DDCtmethod was used

to determine the relative quantization of gene expression levels.

*P < 0.05.

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able to significantly repress luciferase expression

of pGL3-promoter–bcl-w–3¢-UTR (Fig 3B), and

mutation of four nucleotides in the miR-203 target

sequence led to complete abrogation of the suppressive

effect (Fig 3B) Moreover, we observed that ectopic

expression of miR-203 decreased the bcl-w protein

content in a time-dependent manner in T24 cells

(Fig 3C) These observations confirm that miR-203

inhibits endogenous bcl-w in bladder cancer cells

miR-203 expression is inversely related to bcl-w

expression in bladder cancer

To further examine the relationship between miR-203

and bcl-w in bladder cancer tissues, the expression of

miR-203 and bcl-w were detected Our data showed

that miR-203 levels were decreased in bladder cancer

samples bcl-w expression in bladder cancer samples

was analyzed by western bloting The bcl-w levels in

bladder cancer samples were significantly higher than

in normal tissue samples (Fig 4) Importantly, Fig 4 shows that bcl-w expression was increased in bladder cancer tissues that showed significantly decreased

miR-203 expression

miR-203 suppresses bladder cancer progression

by repressing bcl-w Bcl-w is an important determinant of cells prolifera-tion or apoptosis in cancer development, and ele-vated expression of the bcl-w resulted in abnormal cell growth with reduced capability for apoptosis in many cancer types Therefore, we thought that the role of miR-203 in bladder cancer cells growth was mediated by modulating bcl-w expression Figure 5 shows that T24 cell proliferation was restored when bcl-w was re-expressed in cells treated with miR-203 These data confirm that miR-203, at least in part, inhibited bladder cancer progression by repressing bcl-w

0

0

0

0.5

1

1.5

2

2.5

3

3.5

5

10

15

NC miR-203

*

*

*

*

*

NC

NC

miR-203

miR-203-inhibitor

12 0 0.1

0.2

0.3 0.4 0.5

0 0.1 0.2 0.3 0.4 0.5

0.6

0.6 0.7

miR-203

1.32 14.35 4.94

miR-203-inhibitor T24 cells no-specific inhibitor

NC

T24 cells

24 48 60 72

h

h

5

Annexin V-FITC

15

A

B

C

Fig 2 miR-203 inhibited bladder tumor cells proliferation (A) T24 cells were treated with mature miR-203 and apoptosis induc-ers, and apoptosis was detected using the flow cytometry Overexpression of miR-203 promoted cell apoptosis in T24 cells (B) T24 cells were transiently transfected with miR-203 mimics, and at the indicated time points, the numbers of cells per well were measured by the absorbance (450 nm) of reduced WST-8 (C) T24 cells were tran-siently treated with miR-203 inhibitor, and the number of cells per well was measured

by the absorbance (450 nm) of reduced 2-(2-methoxy-4-nitrophenyl)-3-(4-nitrophenyl)-5-(2,4-isulfophenyl)-2H-tetrazolium The results show data from at least three independent experiments, expressed as the mean ± SD *P < 0.05.

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miRNAs have been reported to be involved in several

important biological events, such as tumorigenesis, cell

differentiation, proliferation and apoptosis miRNAs

are also known to act as regulators in bladder cancer

cell growth, and have recently been reported to

regu-late bladder cancer progression [21,22] Some

miRNAs, including miR-145, miR-133a and miR-203,

were markedly downregulated in bladder cancer, and

miR-145 and miR-133a are involved in the regulation

of FSCN1 expression and possibly in the development

of bladder cancer [19,22] However, the relationship

between miR-203 and bladder cancer is still unknown

Here we found that miR-203 suppresses bladder cancer

development by repressing bcl-w expression

Bcl-2 family proteins regulate mitochondrial

apopto-sis downstream of diverse stressors Bcl-w is an

impor-tant anti-apoptotic member of the bcl-2 family

Depletion of bcl-w has been proven to sensitize cells to

apoptosis [23,24] Increased bcl-w protein levels are

commonly observed in various types of cancers,

including colonic, cervical and breast cancer cells [9]

In gastric adenocarcinomas, bcl-w suppresses cancer

cell death by blocking SAPK⁄ JNK activation [25]

Bcl-w expression is modulated by a Met⁄ HGF receptor (c-met) in human colorectal cancers Downregulation

of bcl-w by miR-122 resulted in a decrease in the Bcl-w⁄ Bax ratio, ultimately leading to apoptosis in HCC-derived cell lines [14] However, the regulation of bcl-w expression is complex, and its in-depth research con-tributes to cancer treatment

The function of miR-203 was recently reported Wijnhoven et al [26] showed that levels of miR-203

0 bcl-w Actin T1 T2 T3 T4

*

*

*

*

N1 N2 N3 N4 0.5

1 1.5 2 2.5

3 3.5 4 4.5 5

Fig 4 miR-203 expression is inversely related to bcl-w expression

in bladder tissues Bcl-w was decreased in normal bladder tissues that showed increased miR-203 expression, whereas bcl-w was increased in bladder tumor tissues that showed decreased miR-203 expression T, tumor tissues; N, normal tissues b-Actin was used

as reference for RNAs *P < 0.05.

0

h

miR-203 miR-203 + pcDNA bcl-w

* * NC

0.1 0.2 0.3

0.4 0.5 0.6 0.7

Fig 5 miR-203 suppresses bladder cancer progression by bcl-w modulation Bcl-w was re-expressed in T24 cells treated with miR-203, and the numbers of cells per well were measured by the absorbance (450 nm) of reduced 2-(2-methoxy-4-nitrophenyl)-3-(4-nitrophenyl)-5-(2,4-isulfophenyl)-2H-tetrazolium at 12, 24, 48, 60 and 72 h, respectively The results show data from at least three independent experiments, expressed as the mean ± SD *P < 0.05.

Bcl-w 3′-UTR

A

B

C

CCCAAUUUUUAAAUCCAUUUCAU

CCCAAUUUUUAAAUCCAAAAGAU

GAUCACCAGGAUUUGUAAAGUG 5′

5′

3′

Bcl-w 3′-UTR-mut

hsa-miR-203

0

NC miR-203

Hek293 cells

5

10

15

20

1.2 1 0.8 0.6 0.4 0.2 0 Wildtype Mutation

NC miR-203

bcl-w

Actin

bcl-w Actin

Fig 3 miR-203 inhibits bcl-w expression (A) Schematic

representa-tion of the miR-203 site in bcl-w 3¢-UTR (B) The 3¢-UTR reporter

assay was carried out in HEK293 cells that overexpressed miR-203.

PGL3-promoter–bcl-w–3¢-UTR–WT or PGL3-promoter–bcl-w–3¢-UTR–

MUT was cotransfected with pRL-TK using Lipofectamine 2000.

Luciferase assays were performed 24 h after transfection using the

Dual-Luciferase Reporter Assay System (Promega) Firefly luciferase

activity was standardized to Renilla luciferase control An asterisk

indicates significantly different from the NC (P < 0.05) (C) Western

blot analysis for endogenous bcl-w protein level using antibodies

against bcl-w b-Actin was used as reference for RNAs.

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were high in normal squamous epithelium and low in

columnar epithelia, and dysregulation of miR-203

could contribute to metaplastic and neoplastic

pro-cesses in the oesophageal mucosa Mathe et al [27]

demonstrated that miR-203 expression was reduced in

cancerous compared with noncancerous tissue, and

was potentially clinically useful for developing

prog-nostic biomarkers and identifying novel drug targets

and therapies However, the relationship between

miR-203 and bladder cancer is unknown Our results

showed that miR-203 levels were decreased in bladder

cancer tissues Overexpression of miR-203 promoted

bladder cancer cell apoptosis and inhibited cells

prolif-eration We identified that miR-203 targeted the bcl-w

gene The reporter assay showed that miR-203 was

able to significantly repress luciferase-contained bcl-w–

3¢-UTR expression Western blot analysis also showed

that miR-203 significantly inhibited the bcl-w protein

level in T24 cells

In conclusion, our data demonstrate that miR-203

suppresses bladder cancer cell proliferation by

target-ing bcl-w Thus, miR-203 is an important regulator in

the development of bladder cancer and implicates the

potential application of miR-203 in bladder cancer

therapy

Materials and methods

Tissue samples

Human bladder tissues were obtained with informed

con-sent from Renji Hospital affiliated to School of Medicine

Shanghai Jiaotong University Normal and pathologically

diagnosed biopsy specimens were obtained from patients

with bladder tumors who underwent radical cystectomy or

endoscopic resection for primary or recurrent TCC

Cell culture

Human bladder cancer cells T24 were obtained from the

American Type Culture Collection and were maintained in

RPMI 1640 with 10% fetal bovine serum (Gibco, New

York, USA), and were cultured at 37C with 5% CO2

The human embryonic kidney epithelial cell HEK-293 was

maintained in DMEM with 10% FBS and were cultured at

37C with 5% CO2

Real-time PCR

Total RNA was extracted using Trizol reagent (Invitrogen,

New York, USA), and the reverse-transcription reactions

were carried out using an M-MLV Reverse Transcriptase

kit (Invitrogen) The gene-specific stem–loop RT primers for

miRNAs released by the Sanger Institute were designed according to Chen et al [28] Real-time PCR was performed using a standard SYBR Green PCR kit (Toyobo, Osaka, Japan) protocol on Rotor-Gene RG-3000A (Corbett Life Science, Sidney, Australia) U6 and b-actin were used as ref-erences for miRNAs and RNAs, respectively Each sample was analyzed in triplicate The 2)DDCtmethod was used to determine the relative quantitation of gene expression levels

Luciferase reporter assay

For luciferase reporter assay, HEK293 cells (1–3· 104 cellsÆwell)1) were plated in a 24-well plate and then cotrans-fected with 20 mm of either miR-203 or microRNA control (NC), 40 ng of either pGL3-promoter–bcl-w–3¢-UTR–WT

or pGL3-promoter–bcl-w–3¢-UTR–MUT and 4 ng of

pRL-TK (Promega, Wisconsin, USA), using Lipofectamine

2000 HEK293 cells were collected 24 h after transfection and analyzed using the Dual-Luciferase Reporter Assay Sys-tem (Promega) The pRL-TK vector that provided the con-stitutive expression of Renilla luciferase was cotransfected as

an internal control to correct the differences in both trans-fection and harvest efficiencies Transtrans-fections were done in triplicate and repeated at least three times in independent experiments

Western blot analysis and antibodies

Western blot analysis to assess bcl-w and b-actin expression was performed as previously described [29] The anti-(bcl-w) primary Ig and anti-(b-actin) primary Ig were purchased from Santa Cruz Biotechnology (Santa Cruz, CA, USA)

Flow cytometric analysis

T24 cells transfected with miR-203 (4· 105) were plated in six-well plates and apoptosis inducers A (Apopisa) and B (Apobid) (1 : 1000; Beyotime, Jiangsu, China) were added

to the culture After a 24-h incubation, the cultures were stained with annexin V-fluorescein isothiocyanate and apoptosis rates were analyzed using a flow cytometer (FACSCalibur, BD Biosciences, CA, USA)

Cell proliferation assay

Cell proliferation assays were performed with a Cell Count-ing Kit-8 (Dojindo, Kumamoto, Japan) [30] Cells were pla-ted in 24-well plates in triplicate at 1–2 · 105

cellsÆwell)1 and cultured in the growth medium Then cells were treated with mature miR-203 (miR-203 mimics, MIMAT0000264; Qiagen, Germany) or with miR-203 inhibitor

(anti-miR-203, MIN0000236; Qiagen, Hilden, Germany), the numbers

of cells per well were measured by the absorbance (450 nm)

of reduced

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2-(2-methoxy-4-nitrophenyl)-3-(4-nitrophenyl)-5-(2,4-isulfophenyl)-2H-tetrazolium (monosodium salt) at the

indicated time points

Plasmid pcDNA–bcl-w was constructed by introducing a

BamHI–EcoRI fragment containing the bcl-w cDNA into

the same sites in pcDNA3.1

Statistical analysis

All data are expressed as mean ± SD from at least three

separate experiments The differences between groups were

analyzed using Student’s t-test The difference was deemed

statistically significant at P < 0.05

Acknowledgements

This work was supported by Shanghai Municipal

Nat-ural Science Foundation (09ZR1418000)

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