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Novel Selective Estrogen Receptor Modulator Ameliorates Murine Colitis

Institute of Biomedicine, University of Turku, FI-20520 Turku, Finland
Faculty of Science and Engineering, Department Biosciences, Cell Biology; Åbo Akademi University, FI-20520 Turku, Finland
Forendo Pharma Ltd., FI-20520 Turku, Finland
Turku Center for Disease Modeling, FI-20520 Turku, Finland
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2019, 20(12), 3007;
Received: 22 May 2019 / Revised: 14 June 2019 / Accepted: 18 June 2019 / Published: 20 June 2019
(This article belongs to the Special Issue Molecular Pathways of Estrogen Receptor Action 2.0)
Estrogen-receptor-mediated signaling has been suggested to decrease the inflammatory response in monocyte macrophages. Previously, we showed that a novel selective estrogen receptor modulator (SERM2) promotes anti-inflammatory phenotype of monocytes in vitro. In this study, we demonstrate the potential of SERM2 in amelioration of colitis. We utilized a dextran sodium sulfate (DSS)-induced colitis model in FVB/n mice to demonstrate the effects of orally administered SERM2 on the clinical status of the mice and the histopathological changes in the colon, as well as proportion of Mrc-1 positive macrophages. SERM2 nuclear receptor affinities were measured by radioligand binding assays. Orally administered, this compound significantly alleviated DSS-induced colitis in male mice and induced local estrogen receptor activation in the inflamed colon, as well as promoting anti-inflammatory cytokine expression and infiltration of anti-inflammatory monocytes. We show that this novel drug candidate has an affinity to estrogen receptors α and β and progesterone receptors, but not to glucocorticoid receptor, thus expressing unique binding properties compared to other sex steroid receptor ligands. These results indicate that novel drug candidates to alleviate inflammatory conditions of the colon could be found among sex steroid receptor activating compounds. View Full-Text
Keywords: colitis; selective estrogen receptor modulator; estrogen receptor; progesterone receptor; inflammation; macrophages colitis; selective estrogen receptor modulator; estrogen receptor; progesterone receptor; inflammation; macrophages
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MDPI and ACS Style

Polari, L.; Anttila, S.; Helenius, T.; Wiklund, A.; Linnanen, T.; Toivola, D.M.; Määttä, J. Novel Selective Estrogen Receptor Modulator Ameliorates Murine Colitis. Int. J. Mol. Sci. 2019, 20, 3007.

AMA Style

Polari L, Anttila S, Helenius T, Wiklund A, Linnanen T, Toivola DM, Määttä J. Novel Selective Estrogen Receptor Modulator Ameliorates Murine Colitis. International Journal of Molecular Sciences. 2019; 20(12):3007.

Chicago/Turabian Style

Polari, Lauri, Santeri Anttila, Terhi Helenius, Anu Wiklund, Tero Linnanen, Diana M. Toivola, and Jorma Määttä. 2019. "Novel Selective Estrogen Receptor Modulator Ameliorates Murine Colitis" International Journal of Molecular Sciences 20, no. 12: 3007.

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