ENMD-1068, a protease-activated receptor 2 antagonist, inhibits the development of endometriosis in a mouse model

Wang Y, Yifeng Wang, Lin M, Min Lin, Huinan Weng, Weng H, Wang X, Xuefeng Wang, Li Yang, Yang L, Fenghua Liu
American journal of obstetrics and gynecology · 2014 · vol. 210(6) , pp. 531.e1–531.e8 · doi:10.1016/j.ajog.2014.01.040 · PMID:24495669 · W2169711167
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This study investigated the effects of ENMD-1068, a protease-activated receptor 2 antagonist, and found it inhibited the development of endometriosis in a mouse model.

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Abstract

ObjectiveProtease-activated receptor 2 plays an important role in the pathogenesis of endometriosis. We studied the effect of ENMD-1068, a protease-activated receptor 2 antagonist, on the development of endometriosis in a noninvasive fluorescent mouse model.Study designA red fluorescent protein-expressing xenograft model of human endometriosis was created in nude mice. After endometriosis induction, the mice were injected intraperitoneally with either 25 mg/kg or 50 mg/kg ENMD-1068 or with 200 μL of the vehicle control daily for 5 days. The endometriotic lesions that developed in the mice were then counted, measured, and collected. The lesions were assessed for the production of interleukin 6 and monocyte chemotactic protein-1 by enzyme-linked immunosorbent assays and evaluated for the activation of nuclear factor-κB and the expression of vascular endothelial growth factor by immunohistochemical analyses. Cell proliferation and apoptosis were assessed by immunohistochemistry for Ki-67 and terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling, respectively.ResultsENMD-1068 dose-dependently inhibited the development of endometriotic lesions (P < .05) without apparent toxicity to various organs of the treated mice. Consistently, ENMD-1068 dose-dependently inhibited the expression of interleukin 6 and nuclear factor-κB (P < .05) and cell proliferation (P < .05) in the lesions, as well as increased the percentage of apoptotic cells (P < .05). ENMD-1068 reduced the levels of monocyte chemotactic protein-1 and vascular endothelial growth factor in the lesions (P < .05), but not in a dose-dependent manner.ConclusionOur study suggests that ENMD-1068 is effective in suppressing the growth of endometriosis, which might be attributed to the drug's antiangiogenic and antiinflammatory activities.

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Condition tags

endometriosis

MeSH descriptors

Angiogenesis Inhibitors Endometriosis Endometrium Neovascularization, Pathologic Piperazines Receptor, PAR-2 Angiogenesis Inhibitors Angiogenesis Inhibitors Animals Apoptosis Apoptosis Cell Proliferation Cell Proliferation Chemokine CCL2 Chemokine CCL2 Disease Models, Animal Endometriosis Endometrium Endometrium Endometrium

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