Inhibitory effects of a selective prostaglandin E2 receptor antagonist RQ-15986 on inflammation-related colon tumorigenesis in APC-mutant rats.

Prostaglandin E2 receptor EP4 is involved in inflammation and related tumorigenesis in the colorectum. This study aimed to investigate the chemopreventive ability of RQ-15986, a selective EP4 antagonist, in colitis-related colorectal tumorigenesis. Male Kyoto APC delta rats, which have APC mutations...

Full description

Saved in:
Bibliographic Details
Main Authors: Yohei Shirakami, Takayuki Nakanishi, Noritaka Ozawa, Takayasu Ideta, Takahiro Kochi, Masaya Kubota, Hiroyasu Sakai, Takashi Ibuka, Takuji Tanaka, Masahito Shimizu
Format: Article
Language:English
Published: Public Library of Science (PLoS) 2021-01-01
Series:PLoS ONE
Online Access:https://journals.plos.org/plosone/article/file?id=10.1371/journal.pone.0251942&type=printable
Tags: Add Tag
No Tags, Be the first to tag this record!
_version_ 1850239921766268928
author Yohei Shirakami
Takayuki Nakanishi
Noritaka Ozawa
Takayasu Ideta
Takahiro Kochi
Masaya Kubota
Hiroyasu Sakai
Takashi Ibuka
Takuji Tanaka
Masahito Shimizu
author_facet Yohei Shirakami
Takayuki Nakanishi
Noritaka Ozawa
Takayasu Ideta
Takahiro Kochi
Masaya Kubota
Hiroyasu Sakai
Takashi Ibuka
Takuji Tanaka
Masahito Shimizu
author_sort Yohei Shirakami
collection DOAJ
description Prostaglandin E2 receptor EP4 is involved in inflammation and related tumorigenesis in the colorectum. This study aimed to investigate the chemopreventive ability of RQ-15986, a selective EP4 antagonist, in colitis-related colorectal tumorigenesis. Male Kyoto APC delta rats, which have APC mutations, were treated with azoxymethane and dextran sulfate sodium and subsequently administered RQ-15986 for eight weeks. At the end of the experiment, the development of colorectal tumor was significantly inhibited in the RQ-15986-treated group. The cell proliferation of the crypts and tumors in the colorectum was decreased following RQ-15986 treatment. RQ-15986 also suppressed the expression of pro-inflammatory cytokines, including tumor necrosis factor-α, interleukin-6, interleukin-18, and monocyte chemotactic protein-1, in the colon mucosa. In addition, the expression levels of indoleamine 2,3-dioxygenase, which is involved in immune tolerance, were decreased in the colorectal epithelium and tumors of the RQ-15986-treated group. These findings indicate that RQ-15986 inhibits colitis-associated colorectal tumorigenesis by attenuating inflammation, suppressing cell proliferation, and modulating the expression of indoleamine 2,3-dioxygenase. Targeting prostaglandin E2/EP4 signaling might be a useful strategy for chemoprevention of inflammation-related colorectal cancer.
format Article
id doaj-art-632ca27268e34ffbae3aa9cd0de6aa1e
institution OA Journals
issn 1932-6203
language English
publishDate 2021-01-01
publisher Public Library of Science (PLoS)
record_format Article
series PLoS ONE
spelling doaj-art-632ca27268e34ffbae3aa9cd0de6aa1e2025-08-20T02:01:00ZengPublic Library of Science (PLoS)PLoS ONE1932-62032021-01-01165e025194210.1371/journal.pone.0251942Inhibitory effects of a selective prostaglandin E2 receptor antagonist RQ-15986 on inflammation-related colon tumorigenesis in APC-mutant rats.Yohei ShirakamiTakayuki NakanishiNoritaka OzawaTakayasu IdetaTakahiro KochiMasaya KubotaHiroyasu SakaiTakashi IbukaTakuji TanakaMasahito ShimizuProstaglandin E2 receptor EP4 is involved in inflammation and related tumorigenesis in the colorectum. This study aimed to investigate the chemopreventive ability of RQ-15986, a selective EP4 antagonist, in colitis-related colorectal tumorigenesis. Male Kyoto APC delta rats, which have APC mutations, were treated with azoxymethane and dextran sulfate sodium and subsequently administered RQ-15986 for eight weeks. At the end of the experiment, the development of colorectal tumor was significantly inhibited in the RQ-15986-treated group. The cell proliferation of the crypts and tumors in the colorectum was decreased following RQ-15986 treatment. RQ-15986 also suppressed the expression of pro-inflammatory cytokines, including tumor necrosis factor-α, interleukin-6, interleukin-18, and monocyte chemotactic protein-1, in the colon mucosa. In addition, the expression levels of indoleamine 2,3-dioxygenase, which is involved in immune tolerance, were decreased in the colorectal epithelium and tumors of the RQ-15986-treated group. These findings indicate that RQ-15986 inhibits colitis-associated colorectal tumorigenesis by attenuating inflammation, suppressing cell proliferation, and modulating the expression of indoleamine 2,3-dioxygenase. Targeting prostaglandin E2/EP4 signaling might be a useful strategy for chemoprevention of inflammation-related colorectal cancer.https://journals.plos.org/plosone/article/file?id=10.1371/journal.pone.0251942&type=printable
spellingShingle Yohei Shirakami
Takayuki Nakanishi
Noritaka Ozawa
Takayasu Ideta
Takahiro Kochi
Masaya Kubota
Hiroyasu Sakai
Takashi Ibuka
Takuji Tanaka
Masahito Shimizu
Inhibitory effects of a selective prostaglandin E2 receptor antagonist RQ-15986 on inflammation-related colon tumorigenesis in APC-mutant rats.
PLoS ONE
title Inhibitory effects of a selective prostaglandin E2 receptor antagonist RQ-15986 on inflammation-related colon tumorigenesis in APC-mutant rats.
title_full Inhibitory effects of a selective prostaglandin E2 receptor antagonist RQ-15986 on inflammation-related colon tumorigenesis in APC-mutant rats.
title_fullStr Inhibitory effects of a selective prostaglandin E2 receptor antagonist RQ-15986 on inflammation-related colon tumorigenesis in APC-mutant rats.
title_full_unstemmed Inhibitory effects of a selective prostaglandin E2 receptor antagonist RQ-15986 on inflammation-related colon tumorigenesis in APC-mutant rats.
title_short Inhibitory effects of a selective prostaglandin E2 receptor antagonist RQ-15986 on inflammation-related colon tumorigenesis in APC-mutant rats.
title_sort inhibitory effects of a selective prostaglandin e2 receptor antagonist rq 15986 on inflammation related colon tumorigenesis in apc mutant rats
url https://journals.plos.org/plosone/article/file?id=10.1371/journal.pone.0251942&type=printable
work_keys_str_mv AT yoheishirakami inhibitoryeffectsofaselectiveprostaglandine2receptorantagonistrq15986oninflammationrelatedcolontumorigenesisinapcmutantrats
AT takayukinakanishi inhibitoryeffectsofaselectiveprostaglandine2receptorantagonistrq15986oninflammationrelatedcolontumorigenesisinapcmutantrats
AT noritakaozawa inhibitoryeffectsofaselectiveprostaglandine2receptorantagonistrq15986oninflammationrelatedcolontumorigenesisinapcmutantrats
AT takayasuideta inhibitoryeffectsofaselectiveprostaglandine2receptorantagonistrq15986oninflammationrelatedcolontumorigenesisinapcmutantrats
AT takahirokochi inhibitoryeffectsofaselectiveprostaglandine2receptorantagonistrq15986oninflammationrelatedcolontumorigenesisinapcmutantrats
AT masayakubota inhibitoryeffectsofaselectiveprostaglandine2receptorantagonistrq15986oninflammationrelatedcolontumorigenesisinapcmutantrats
AT hiroyasusakai inhibitoryeffectsofaselectiveprostaglandine2receptorantagonistrq15986oninflammationrelatedcolontumorigenesisinapcmutantrats
AT takashiibuka inhibitoryeffectsofaselectiveprostaglandine2receptorantagonistrq15986oninflammationrelatedcolontumorigenesisinapcmutantrats
AT takujitanaka inhibitoryeffectsofaselectiveprostaglandine2receptorantagonistrq15986oninflammationrelatedcolontumorigenesisinapcmutantrats
AT masahitoshimizu inhibitoryeffectsofaselectiveprostaglandine2receptorantagonistrq15986oninflammationrelatedcolontumorigenesisinapcmutantrats