Dienogest reduces HSD17β1 expression and activity in endometriosis

Taisuke Mori, Fumitake Ito, Hiroshi Matsushima, Osamu Takaoka, Akemi Koshiba, Yukiko Tanaka, Izumi Kusuki, Jo Kitawaki
The Journal of endocrinology · 2015 · vol. 225(2) , pp. 69–76 · doi:10.1530/joe-15-0052 · PMID:25767055 · W1966691125
article OA: bronze CC0 ⤵ 23 in-corpus citations
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⚙ AI-generated summary by claude@2026-06, 2026-06-07 ⓘ

Dienogest treatment reduced the expression and activity of the estrogen-producing enzyme HSD17β1 in endometriotic tissues and cells.

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⚙ AI-generated deep summary by claude@2026-06, 2026-06-07 ⓘ

This study examined how dienogest (DNG) affects enzymes involved in local estrogen metabolism in surgically obtained ovarian endometrioma (OE) specimens, their homologous endometrium (EE), and normal endometrium (NE), using spheroid cultures of primary stromal cells and related molecular assays. OE stromal cells showed higher aromatase, HSD17β1, steroid sulfatase (STS), and estrogen sulfotransferase (EST) expression (with lower HSD17β2) compared with NE/EE, and DNG treatment (1 mg twice daily for 3–5 months) reduced HSD17β1 expression and immunohistochemical staining and inhibited HSD17β1 enzyme activity in vitro. The paper’s main caveat is that it relies on ex vivo/in vitro enzyme expression and activity measurements rather than demonstrating direct clinical outcomes from these mechanistic changes. This paper is centrally about endometriosis — it demonstrates DNG inhibition of HSD17β1 (and aromatase) to reduce abnormally elevated estrogen production in endometriotic tissues.

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Abstract

Endometriosis is an estrogen-dependent disease. Abnormally biosynthesized estrogens in endometriotic tissues induce the growth of the lesion and worsen endometriosis-associated pelvic pain. Dienogest (DNG), a selective progesterone receptor agonist, is widely used to treat endometriosis and efficiently relieves the symptoms. However, its pharmacological action remains unknown. In this study, we elucidated the effect of DNG on enzymes involved in local estrogen metabolism in endometriosis. Surgically obtained specimens of 23 ovarian endometriomas (OE) and their homologous endometrium (EE), ten OE treated with DNG (OE w/D), and 19 normal endometria without endometriosis (NE) were analyzed. Spheroid cultures of stromal cells (SCs) were treated with DNG and progesterone. The expression of aromatase, 17β-hydroxysteroid dehydrogenase 1 (HSD17β1), HSD17β2, HSD17β7, HSD17β12, steroid sulfatase (STS), and estrogen sulfotransferase (EST) was evaluated by real-time quantitative PCR. The activity and protein level of HSD17β1 were measured with an enzyme assay using radiolabeled estrogens and immunohistochemistry respectively. OESCs showed increased expression of aromatase, HSD17β1, STS, and EST, along with decreased HSD17β2 expression, when compared with stromal cells from normal endometria without endometriosis (NESCs) (P<0.01) or stromal cells from homologous endometrium (EESCs) (P<0.01). In OESCs, DNG inhibited HSD17β1 expression and enzyme activity at 10(-7) M (P<0.01). Results of immunohistochemical analysis displayed reduced HSD17β1 staining intensity in OE w/D (P<0.05). In conclusion, DNG exerts comprehensive inhibition of abnormal estrogen production through inhibition of aromatase and HSD17β1, contributing to a therapeutic effect of DNG on endometriosis.

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Condition tags

endometriosis

MeSH descriptors

Endometriosis Estradiol Dehydrogenases Estradiol Dehydrogenases Nandrolone Adult Aromatase Aromatase Aromatase Cells, Cultured Endometriosis Endometriosis Endometrium Endometrium Endometrium Estradiol Dehydrogenases Estradiol Dehydrogenases Female Gene Expression Regulation, Enzymologic Gene Expression Regulation, Enzymologic Humans

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