AHR agonistic effects of 6-PN contribute to potential beneficial effects of Hops extract

GASTIAZORO, MARÍA PAULA; VOLLMER, GÜNTER; ZIERAU, OLIVER; ZANARDI, MARÍA VICTORIA; WOBER, JANNETTE; DURANDO, MILENA; KRETZSCHMAR, GEORG; VARAYOUD, JORGELINA

MOLECULAR AND CELLULAR ENDOCRINOLOGY.

ELSEVIER IRELAND LTD

Año: 2022 vol. 543

0303-7207

Hops (Humulus lupulus) is used as an alternative to hormone replacement therapy due to the phytoestrogen, 8-prenylnaringenin (8-PN). To examine the potential risks/benefits of hops extract and its compounds (8-PN and 6-prenylnaringenin, 6-PN), we aimed to evaluate the estrogen receptor α (ERα) and aryl hydrocarbon receptor(AHR) signaling pathways in human endometrial cancer cells. Hops extract, 8-PN and 6-PN showed estrogenicactivity. Hops extract and 6-PN activated both ERα and AHR pathways. 6-PN increased the expression of thetumor suppressor gene (AHRR), and that of genes involved in the estrogen metabolism (CYP1A1, CYP1B1).Although 6-PN might activate the detoxification and genotoxic pathways of estrogen metabolism, hops extract asa whole only modulated the genotoxic pathway by an up-regulation of CYP1B1 mRNA expression. These datademonstrate the relevant role of 6-PN contained in the hops extract as potential modulator of estrogen metabolism due to its ERα and AHR agonist activity.