Niacinamide Binds And Activates GPc Estrogen Receptor

[bdawg]

Another study on GPER. Hydroxytyrosol and Oleuropin counteract 17ß-Estradiols (E2) proliferation effects in breast cancer cells.
They call them "inverse agonist". That's waht Niacinamide is as well.

HyTyrosol and OLEU are phenols from Olive leaf and Olive oil.

Oleuropein and hydroxytyrosol activate GPER/ GPR30-dependent pathways leading to apoptosis of ER-negative SKBR3 breast cancer cells. - PubMed - NCBI

Oleuropein does rais Test and lower Cortisol in rats:
http://www.jnutbio.com/article/S0955-2863(12)00158-1/abstract

an inverse agonist, that does make sense... fantastic research!

 

[LeeLemonoil]

an inverse agonist, that does make sense... fantastic research!

The nomenclature is a joke. "Inverse Agonist" ... not only that it invokes structural images that are not true - moreover, if one stays in that idiom it's patheric
that a harmful substance is classified as the "normal" agonist and beneficial substances are "inverse" ... As if in normal tissue there are protein structures distinctly structured to bind harmful substances...

 

[LeeLemonoil]

Some intriguing discussion about Oleuropein and Tyrosol in this thread. It seems Tyrosol affects T3 and Dopamine:
Oleuropein and Hydroxytyrosol - Discussion - Brain Health

 

[haidut]

Some intriguing discussion about Oleuropein and Tyrosol in this thread. It seems Tyrosol affects T3 and Dopamine:
Oleuropein and Hydroxytyrosol - Discussion - Brain Health

Peat wrote in one of his articles on PUFA that olive oil contained a substance that prevents cancer. I suspect it is oleuropein/hydroxytyrosol. He did not elaborate, so if somebody asks him and gets an answer please post here.

 

[Dragon]

.... Tamoxifen, a known anti-estrogenic pharmacon, is also an agonist.

good post! gracias :)

fyi, I wouldn't call Tamoxifen an "anti-estrogenic". It is said that, in fact, in some parts of the body it binds to "ER" producing same or even stronger effects as estrogen. For example, my wife with breast cancer just had to go in for surgery to scrape out pre-cancerous endometrial hyperplasia, which hits 25% of women taking Tam. It's also said to promote bone density similar to estrogen. Although we in Peatland would have to take that with a grain of salt since he says estrogen doesn't promote bone growth/density.

Anyway, from the hundreds of papers on Tam that I've read over the past 3 yrs, I'd say it has estrogenic effects in many parts of the body. fyi, officially it's part of the 'SERM' class of drugs...selective estrogen receptor modulator.