1-(4-(6-bromobenzo(1-3)dioxol-5-yl)-3a-4-5-9b-tetrahydro-3h-cyclopenta(c)quinolin-8-yl)ethanone and Ovarian-Cysts

To demonstrate the effects of the selective G protein-coupled estrogen receptor 1 (GPER) agonist G-1 in human ovarian endometriotic stromal cells (ESCs).. Experimental in vitro study.. University hospital.. A total of 33 patients with ovarian endometrioma.. Endometriotic stromal cells from ovarian chocolate cysts were treated with the GPER agonist G-1.. The primary outcomes were cell proliferation, measured using the WST-8 assay; cell cycle, as analyzed using flow cytometry, fluorescent immunocytochemistry, and cytotoxicity; caspase activity, as measured by fluorescent and luminescent enzyme assays; and protein expression levels, as determined by Western blot analysis.. G-1 suppressed ESC proliferation in a concentration-dependent manner. The inhibitory effect was not blocked when GPER signaling pathways, including the GPER itself, were inhibited. G-1 induced cell cycle arrest and accumulation in the sub-G1 phase in ESCs. Immunofluorescence analysis demonstrated that G-1 interrupted microtubule assembly at the mitotic phase. G-1 also induced caspase-3-dependent apoptosis without significant cytotoxicity.. G-1 suppressed proliferation and induced apoptosis in ESCs, suggesting the potential use of this compound as a therapeutic drug for the treatment of endometriosis.

Topics: Adult; Apoptosis; Caspase 3; Cell Proliferation; Cells, Cultured; Cyclopentanes; Dose-Response Relationship, Drug; Endometriosis; Female; Humans; M Phase Cell Cycle Checkpoints; Microtubules; Middle Aged; Ovarian Cysts; Ovary; Quinolines; Receptors, Estrogen; Receptors, G-Protein-Coupled; RNA Interference; Signal Transduction; Stromal Cells; Transfection

Topics: Apoptosis; Cell Proliferation; Cyclopentanes; Endometriosis; Female; Humans; M Phase Cell Cycle Checkpoints; Ovarian Cysts; Ovary; Quinolines; Receptors, Estrogen; Receptors, G-Protein-Coupled; Stromal Cells