Dienogest inhibits Toll-like receptor 4 expression induced by costimulation of lipopolysaccharide and high-mobility group box 1 in endometrial epithelial cells

Shizuka Mita, Yutaka Shimizu, Tatsuto Notsu, Kazunori Imada, Satoru Kyo
Fertility and sterility · 2011 · vol. 96(6) , pp. 1485–1489.e4 · doi:10.1016/j.fertnstert.2011.09.040 · PMID:22014880 · W2088497719
Lab / animal OA: closed CC0 ⤵ 19 in-corpus citations
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Dienogest was found to inhibit the expression of Toll-like receptor 4, which was induced by the combined stimulation of lipopolysaccharide and high-mobility group box 1 in endometrial epithelial cells.

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Abstract

OBJECTIVE: To investigate the effect of dienogest on the expression of Toll-like receptor (TLR) 4 in human endometrial epithelial cells. DESIGN: Prospective basic research study. SETTING: Pharmaceutical research center. PATIENT(S): None. INTERVENTION(S): Not applicable. MAIN OUTCOME MEASURE(S): TLR4 in the immortalized progesterone receptor-expressing human endometrial epithelial cell line, EM-PR, was activated with lipopolysaccharide and high-mobility group box 1 (LPS/HMGB1) in the presence or absence of the synthetic progestin dienogest or endogenous progesterone. The production of interleukin (IL)-8, IL-6, and monocyte chemoattractant protein (MCP)-1 and the mRNA expression of TLR4 were measured with the use of ELISA and real-time reverse-transcription polymerase chain reaction respectively and nuclear factor (NF)-κB reporter gene assays were performed. The role of TLR4 was assayed with the use of TLR4-siRNA-transfected cells. RESULT(S): Coadministration of LPS/HMGB1 induced the production of IL-8, IL-6, and MCP-1, TLR4 mRNA expression, and NF-κB activity in EM-PR cells, and dienogest inhibited all of these parameters. TLR4 knockdown using TLR4 siRNA reduced IL-8 production. CONCLUSION(S): Dienogest inhibits TLR4 mRNA expression and subsequent IL-8 production induced by TLR4 agonists via an inhibitory effect on NF-κB activation in human endometrial epithelial cells. This pharmacologic effect of dienogest may contribute to its therapeutic effect on abnormal inflammation of endometrium.

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MeSH descriptors

Endometrium Epithelial Cells HMGB1 Protein Lipopolysaccharides Nandrolone Toll-Like Receptor 4 Cells, Cultured Dose-Response Relationship, Drug Down-Regulation Down-Regulation Drug Evaluation, Preclinical Endometrium Endometrium Endometrium Epithelial Cells Epithelial Cells Epithelial Cells Female Gene Expression Regulation Gene Expression Regulation

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