In Vitro Effects of a Small-Molecule Antagonist of the Tcf/ß-Catenin Complex on Endometrial and Endometriotic Cells of Patients with Endometriosis

Sachiko Matsuzaki, Claude Darcha
PloS one · 2013 · vol. 8(4) , pp. e61690 · doi:10.1371/journal.pone.0061690 · PMID:23626717 · PMC3634014 · W2070821901
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⚙ AI-generated summary by claude@2026-06, 2026-06-08 ⓘ

A Wnt/ß-catenin pathway inhibitor, PKF 115-584, reduced the migration and invasion of endometrial and endometriotic cells from patients with endometriosis.

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⚙ AI-generated deep summary by claude@2026-06, 2026-06-09 ⓘ

Matsuzaki and Darcha studied how inhibiting Wnt/β-catenin signaling via a small-molecule antagonist of the Tcf/β-catenin complex (PKF 115–584) affects proliferation, migration, invasion, and expression of Wnt target and matrix metalloprotein genes in cultured endometrial and endometriotic epithelial and stromal cells derived from patients with endometriosis and matched controls without endometriosis across menstrual phases. They found that PKF 115–584 more strongly reduced migration and invasion in cells from endometriosis patients than in controls, and that MMP-9 activity was elevated in menstrual-phase endometrium from patients with endometriosis, but was inhibited by PKF 115–584 to undetectable levels; invasive endometriotic epithelial and stromal cell numbers were reduced by 73% and 75%, respectively. A key limitation explicitly noted by the work is that all functional findings are based on in vitro assays of isolated cells and menstrual-phase sampling rather than in vivo outcomes. This paper is centrally about endometriosis — it tests PKF 115–584 effects on endometriotic and eutopic endometrial cells from patients with endometriosis, linking Tcf/β-catenin inhibition to reduced invasion via MMP-9.

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Abstract

BACKGROUND: Our previous studies suggested that aberrant activation of Wnt/ß-catenin signaling might be involved in the pathophysiology of endometriosis. We hypothesized that inhibition of Wnt/ß-catenin signaling might result in inhibition of cell proliferation, migration, and/or invasion of endometrial and endometriotic epithelial and stromal cells of patients with endometriosis. OBJECTIVES: The aim of the present study was to evaluate the effects of a small-molecule antagonist of the Tcf/ß-catenin complex (PKF 115-584) on cell proliferation, migration, and invasion of endometrial and endometriotic epithelial and stromal cells. METHODS: One hundred twenty-six patients (78 with and 48 without endometriosis) with normal menstrual cycles were recruited. In vitro effects of PKF 115-584 on cell proliferation, migration, and invasion and on the Tcf/ß-catenin target genes were evaluated in endometrial epithelial and stromal cells of patients with and without endometriosis, and in endometrial and endometriotic epithelial and stromal cells of the same patients. RESULTS: The inhibitory effects of PKF 115-584 on cell migration and invasion in endometrial epithelial and stromal cells of patients with endometriosis prepared from the menstrual phase were significantly higher than those of patients without endometriosis. Levels of total and active forms of MMP-9 were significantly higher in epithelial and stromal cells prepared from menstrual endometrium in patients with endometriosis compared to patients without endometriosis. Treatment with PKF 115-584 inhibited MMP-9 activity to undetectable levels in both menstrual endometrial epithelial and stromal cells of patients with endometriosis. The number of invasive cells was significantly higher in epithelial and stromal cells of endometriotic tissue compared with matched eutopic endometrium of the same patients. Treatment with PKF 115-584 decreased the number of invasive endometriotic epithelial cells by 73% and stromal cells by 75%. CONCLUSIONS: The present findings demonstrated that cellular mechanisms known to be involved in endometriotic lesion development are inhibited by targeting the Wnt/β-catenin pathway.

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Condition tags

endometriosis

MeSH descriptors

beta Catenin Endometriosis Endometrium Epithelial Cells Perylene Stromal Cells TCF Transcription Factors Adult beta Catenin beta Catenin beta Catenin Case-Control Studies Cell Movement Cell Movement Cell Proliferation Cell Proliferation Cells, Cultured Endometriosis Endometriosis Endometriosis

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