Inhibitory effects of fulvestrant on the growth of estrogen-induced prolactinoma in Fischer 344 rats and its possible mechanism

Guo, Yanjun; Wang, W.; Knosp, Engelbert; Wu, Yiping; Zhao, Yong

doi:10.1016/j.jns.2013.07.2507

Cited by 1 publication

(4 citation statements)

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“…Clinical studies have confirmed that ER expression is positively correlated with tumour PRL level and is significantly increased in invasive PRLomas . Conversely, ER antagonist fulvestrant showed reduced size and PRL secretion of PRLomas, and tamoxifen was successfully used to treat a dopamine agonist‐resistant PRLoma . These data, together, suggest that ER may be responsible for the anti‐PRLoma activity of MET and for its reported sexual dimorphism of the anti‐PRLoma activity …”

Section: Discussionmentioning

confidence: 90%

“…We found here for the first time that MET suppresses ERα and ERβ expression in PRLoma cells and their xenografts. Studies have suggested critical roles for oestrogen and its receptors in the development of PRLoma . Oestrogens retard the effects of dopamine agonists, with direct action on PRL gene transcription, stimulation of mitotic activity, and modulation of the inhibiting effect of dopamine on PRL gene transcription .…”

Section: Discussionmentioning

confidence: 99%

“…Studies have suggested critical roles for oestrogen and its receptors in the development of PRLoma. 16,[30][31][32][33][34][35][36][37] Oestrogens retard the effects of dopamine agonists, with direct action on PRL gene transcription, stimulation of mitotic activity, and modulation of the inhibiting effect of dopamine on PRL gene transcription. 30 Prolonged oestrogen administration in animals, and also in men, induced the appearance of pituitary tumours, especially PRLomas.…”

Section: Met Reduces Er Expression In Prloma Cells and Xenograftsmentioning

confidence: 99%

“…33 Clinical studies have confirmed that ER expression is positively correlated with tumour PRL level 34 and is significantly increased in invasive PRLomas. 35 Conversely, ER antagonist fulvestrant showed reduced size and PRL secretion of PRLomas, 16,36 and tamoxifen was successfully used to treat a dopamine agonist-resistant PRLoma. 37 These data, together, suggest that ER may be responsible for the anti- F I G U R E 3 Metformin activates AMPK, suppressed proliferation, but has no significant effect on apoptosis of both the bromocriptinesensitive MMQ cells and the bromocriptine-resistant GH3 cells.…”

Section: Met Reduces Er Expression In Prloma Cells and Xenograftsmentioning

confidence: 99%

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Metformin inhibits growth and prolactin secretion of pituitary prolactinoma cells and xenografts

Gao

Liu

Han

et al. 2018

J Cellular Molecular Medi

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Metformin (MET) is a diabetes drug that activates AMP‐activated protein kinase (AMPK), and is suggested to have anticancer efficacy. Here, we investigated the role of AMPK signalling in prolactinoma (PRLoma), with particular respect to MET and bromocriptine (BC) as a PRLoma treatment. We analysed AMPK phosphorylation, dopamine D2 receptor (D2R), and oestrogen receptor (ER) expression in both BC‐sensitive and ‐resistant PRLoma samples; effects of the AMPK agonist MET (alone or with BC) on in vitro proliferation and apoptosis, xenograft growth and prolactin (PRL) secretion of BC‐sensitive and ‐resistant cells, and ER expression in xenografts. Some BC‐resistant PRLomas showed high D2R expression but extremely low AMPK activation. MET significantly inhibited proliferation of cultured PRLoma cells; MET + BC notably restrained their PRL secretion. MET + BC further decreased tumour growth and serum PRL levels in xenografts than BC treatment alone. ER was down‐regulated after AMPK activation in both cultured cells and xenografts. Together, we propose that the AMPK signalling pathway down‐regulates ERα and ERβ, and suppresses PRLoma growth as well as PRL secretion. Combined MET + BC is a potential treatment for PRLomas.

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Section: Discussionmentioning

confidence: 90%

Section: Discussionmentioning

confidence: 99%