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FAQ-Aromatase for NBE

#71

I'm not throughly convinced about forskolin being an aromatase promoter yet, although I wouldn't rule it out, plus....the side effects are risky . xxd announced it way back when, it was great info to say the least, although most of the links provided are down from overtime I guess?. From what I've found forkislin will intensify with E2, or with E2 and progesterone. The study below has it at 4 fold increase with the introduction of Dex (dexamethasone) which has already been shown to up-regulate aromatase.


We examined the effects of FSK on aromatase activity in SV-HFO cells. As shown in Fig. 2⇓, aromatase activity in the presence of 100 nM Dex was 3.75 pmol/mg protein per 6 h, and the addition of FSK increased aromatase activity in a dose-dependent manner. When 10 μM FSK was added, aromatase activity increased about 4-fold (15.2 pmol/mg protein per 6 h) compared with Dex alone. Aromatase activity was not up-regulated in the presence of 10 μM FSK alone. These results suggest that the up-regulation of aromatase activity by FSK depends upon Dex.


Forskolin and dexamethasone synergistically induce aromatase (CYP19) expression in the human osteoblastic cell line SV-HFO
http://www.eje.org/content/152/4/619.full


The link from xxd shows an indirect aromatase activity, meaning forskolin by itself may not work. But, when combined with E2, Progesterone or dex it up-regulates aromatase.

xxd
http://www.breastnexus.com/showthread.php?tid=11512&page=2

Assessment of chemical effects on aromatase activity using the H295R cell line.
http://www.ncbi.nlm.nih.gov/pubmed/20087668
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#72

(07-03-2015, 02:09 AM)Lotus Wrote:  Shh!, Vitamin D is a potent aromatase promoter.


Functional analysis of the I.3, I.6, pII and I.4 promoters of CYP19 (aromatase) gene in human osteoblasts and their role in vitamin D and dexamethasone stimulation.


Abstract
OBJECTIVE:
Current evidence suggests that extragonadal estrogens play an important role in bone metabolism. Estrogen biosynthesis is catalyzed by P450aromatase, encoded by the CYP19 gene. The aims of this paper were to study CYP19 gene expression in human osteoblasts under several hormone and cytokine treatments and to define promoter regions involved in this regulation.

METHODS:
CYP19 transcript levels were measured from primary human osteoblasts and MG-63 cells by real-time PCR in basal conditions, and in response to seven different hormones and cytokines. Four promoters of CYP19 gene were cloned upstream of the luciferase gene and transfected into MG-63 cells. The effect of vitamin D and dexamethasone in these promoter activities was evaluated.

RESULTS:
Vitamin D and dexamethasone were potent stimulators of CYP19 transcription, while testosterone and 17beta-estradiol stimulated moderately. Promoter pII proved the most potent in driving transient luciferase expression. Promoter I.4 displayed moderate activity, while promoters I.3 and I.6 were weak. A region upstream of exon I.3, including exon I.6, was identified as containing repressor elements of promoter pII. Promoter I.3 activity was modulated by repressors located within exon I.3, while an enhancer of promoter I.4 was detected within exon I.4. In the absence of fetal calf serum, dexamethasone stimulation was observed on promoters I.3 and I.4, while vitamin D stimulation acted only on promoter I.3.

CONCLUSIONS:
Four regulatory regions of promoters pII, I.3 and I.4 are relevant to CYP19 expression in human osteoblasts. Vitamin D and dexamethasone modulate transcription through these regions.

(06-03-2015, 04:17 AM)Lotus Wrote:  Here's an update on some novel approaches towards aromatase.

cAMP-dependent signaling pathways (cyclic adenosine monophosphat).
COX2 inhibitors (PGE2), problematic
protein kinase A (PKA)
Free fatty acids



aromatase expression is switched to promoters I.3 and II which are transactivated by protein kinase A (PKA) and cAMP-dependent signaling pathways.

These are promoters genes for aromatase.

[Image: attachment.php?aid=9036]



http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3142499/

You'll notice 1.3 and 1.4 are aromatase promoters for breast and adipose (fat).
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#73

(07-03-2015, 02:09 AM)Lotus Wrote:  Shh!, Vitamin D is a potent aromatase promoter.

That is interesting! Coincidentally, I've recently had my vitamin D levels tested (home kit). It's generally reckoned that most people in the higher Northern latitudes are deficient in Vit D, now that we are all scared about skin cancer. There aren't many nutrients that contain, apart from fortified margarine (yuk). There is a double act with Vits D3 and K2 that play an important role in directing calcium to where it is needed. Apparently recent research is showing that Vit D3 is really important in many area, including cardiovascular, skin, bones, and cancer risk.

This one talks about the autoimmune system.
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3166406/

I've been on 5000 I.U. daily for a while now and the home skin prick test that I mailed off came back with "adequate" levels. However, I also take 100mcg K2 along with it.

I hadn't thought it might have a hand in feminisation!

B.

PS re: forskolin, wouldn't it be ironic if a herb that sounds like foreskin had a feminising effect? ;-)
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#74

That's good idea adding k2, how do you supplement it?, I tried grass fed butter in some coffee that Pom suggested, not bad. Egg yolks, gouda and brie cheese are other sources of k2 from what I've read.

That study is a good find (thanks). A healthy immune system is a big priority in NBE for sure. Mine went haywire when I pushed too hard.

ER-beta is in the bones, which is tied into NBE response elements, cancer too. I recently came across that B2 improves ER-a sensitivity.

Everything I read had Vitamin D increasing "total and free T", which imo can be a good thing since E comes from T. The androstenedione pathway converts T to E1 then to E2 and back again to E1. DHT which I understood had no value in NBE takes a exit pathway that possibly has a ER-beta link. (too funny).

It does seem odd why aromatase therapy wouldn't be included with HRT more often. Some treatment protocols for gynecomastia will include aromatase inhibitors with T therapy as a way to control runaway T. The initial supra therapeutic dosage of testosterone gets dumped into E in some cases of gyno, probably more often than not.

You can hardly find any related nbe info on pro-aromatase, when search terms are "promoter gene/expression" the yield is somewhat better, mostly it's about AI's. But here recently I think aromatase comes in many disguises Rolleyes , e.g. 17 beta HSD's, NAPHD (it's another enzyme), NO2 (nitric oxide), a few others too, heck I'd even call the androstenedione pathway an aromatase. Rolleyes

Btw, I'm glad you came out of moth balls, welcome back.
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#75

(09-03-2015, 12:35 AM)Lotus Wrote:  That's good idea adding k2, how do you supplement it?, I tried grass fed butter in some coffee that Pom suggested, not bad. Egg yolks, gouda and brie cheese are other sources of k2 from what I've read.

That study is a good find (thanks). A healthy immune system is a big priority in NBE for sure. Mine went haywire when I pushed too hard.

ER-beta is in the bones, which is tied into NBE response elements, cancer too. I recently came across that B2 improves ER-a sensitivity.

Everything I read had Vitamin D increasing "total and free T", which imo can be a good thing since E comes from T. The androstenedione pathway converts T to E1 then to E2 and back again to E1. DHT which I understood had no value in NBE takes a exit pathway that possibly has a ER-beta link. (too funny).

It does seem odd why aromatase therapy wouldn't be included with HRT more often. Some treatment protocols for gynecomastia will include aromatase inhibitors with T therapy as a way to control runaway T. The initial supra therapeutic dosage of testosterone gets dumped into E in some cases of gyno, probably more often than not.

You can hardly find any related nbe info on pro-aromatase, when search terms are "promoter gene/expression" the yield is somewhat better, mostly it's about AI's. But here recently I think aromatase comes in many disguises Rolleyes , e.g. 17 beta HSD's, NAPHD (it's another enzyme), NO2 (nitric oxide), a few others too, heck I'd even call the androstenedione pathway an aromatase. Rolleyes

Btw, I'm glad you came out of moth balls, welcome back.

Okay, so, I read through this entire thread. I have just one question: what form of white peony would one use? I did a quick search on Google and it is available as a tea, liquid extracts, and 'immune support' capsules.

Liquid extract would obviously work best as a topical treatment, but which of the other two is better for oral administration?
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#76

(07-03-2015, 02:09 AM)Lotus Wrote:  Shh!, Vitamin D is a potent aromatase promoter.

Now that is interesting. In another thread I mentioned that I still seem to be experiencing NBE even though I have been off PM (and all other NBE herbs) for almost 3 months now. I am taking D3, however (just started about 6 weeks ago). I asked in that thread if maybe it was aromatase causing the NBE.

Could be... Tongue

Misty


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#77

(13-04-2015, 04:49 PM)Patience Wrote:  
(09-03-2015, 12:35 AM)Lotus Wrote:  That's good idea adding k2, how do you supplement it?, I tried grass fed butter in some coffee that Pom suggested, not bad. Egg yolks, gouda and brie cheese are other sources of k2 from what I've read.

That study is a good find (thanks). A healthy immune system is a big priority in NBE for sure. Mine went haywire when I pushed too hard.

ER-beta is in the bones, which is tied into NBE response elements, cancer too. I recently came across that B2 improves ER-a sensitivity.

Everything I read had Vitamin D increasing "total and free T", which imo can be a good thing since E comes from T. The androstenedione pathway converts T to E1 then to E2 and back again to E1. DHT which I understood had no value in NBE takes a exit pathway that possibly has a ER-beta link. (too funny).

It does seem odd why aromatase therapy wouldn't be included with HRT more often. Some treatment protocols for gynecomastia will include aromatase inhibitors with T therapy as a way to control runaway T. The initial supra therapeutic dosage of testosterone gets dumped into E in some cases of gyno, probably more often than not.

You can hardly find any related nbe info on pro-aromatase, when search terms are "promoter gene/expression" the yield is somewhat better, mostly it's about AI's. But here recently I think aromatase comes in many disguises Rolleyes , e.g. 17 beta HSD's, NAPHD (it's another enzyme), NO2 (nitric oxide), a few others too, heck I'd even call the androstenedione pathway an aromatase. Rolleyes

Btw, I'm glad you came out of moth balls, welcome back.

Okay, so, I read through this entire thread. I have just one question: what form of white peony would one use? I did a quick search on Google and it is available as a tea, liquid extracts, and 'immune support' capsules.

Liquid extract would obviously work best as a topical treatment, but which of the other two is better for oral administration?

The tea isn't white peony, it's white tea, (credit Amber). The real WP exists in extract or capsule form, life extension has a capsule brand, extract blends are pretty popular. But, I'd spread the dosage over 3-4 times in a typical day, for instance.....15 minutes after each dose of E2, which is about the time it's metabolized. This way, the influence of aromatase is shifted away to form DHT, which as we all know DHT will ruin a perfectly good day of E2. Big GrinRolleyes

Btw, vitamin C improves the bioavailability of E2, so does egg whites.
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#78

(13-04-2015, 06:55 PM)Lotus Wrote:  
(13-04-2015, 04:49 PM)Patience Wrote:  Okay, so, I read through this entire thread. I have just one question: what form of white peony would one use? I did a quick search on Google and it is available as a tea, liquid extracts, and 'immune support' capsules.

Liquid extract would obviously work best as a topical treatment, but which of the other two is better for oral administration?

The tea isn't white peony, it's white tea, (credit Amber). The real WP exists in extract or capsule form, life extension has a capsule brand, extract blends are pretty popular. But, I'd spread the dosage over 3-4 times in a typical day, for instance.....15 minutes after each dose of E2, which is about the time it's metabolized. This way, the influence of aromatase is shifted away to form DHT, which as we all know DHT will ruin a perfectly good day of E2. Big GrinRolleyes

Btw, vitamin C improves the bioavailability of E2, so does egg whites.

Okay, so, liquid extract for topical, capsule for oral, grapefruit and vitamin d to spike E levels and further boost aromatase, continue working out to boost base T production for fuel...and find an endocrinologist to prescribe external E or win the lotto and buy a ton of Purafem.
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#79

(13-04-2015, 06:34 PM)Misty0732 Wrote:  
(07-03-2015, 02:09 AM)Lotus Wrote:  Shh!, Vitamin D is a potent aromatase promoter.

Now that is interesting. In another thread I mentioned that I still seem to be experiencing NBE even though I have been off PM (and all other NBE herbs) for almost 3 months now. I am taking D3, however (just started about 6 weeks ago). I asked in that thread if maybe it was aromatase causing the NBE.

Could be... Tongue

Misty



I believe it, after we gain a therapeutic edge lol over total T we could be producing more E2 in our testes than the typical post-menopausal women, who produce mainly E1 in their peripheral tissues. And if all you took was a minor AA and an aromatase herb you could still maintain the "therapeutic edge" over GID, of course that's just my opinion, but I think we see/hear more and more evidence to support that hypothesis.

I believe DHEA at 25 to 50 mg increases estrogen level, (only after a threshold of estrogen is being produced). However, a woman taking this dose, will see her testosterone increase.

Epidermal growth factor (EGF) increases aromatase activity in adipose (fat) and up regulates cox 2 expression, also PGE2 (prostaglandin), which is done by GLA, gamma linoleic acid, like in evening primrose oil, above 3000mg which goes into AA (Arachidonic Acid), that's when it's gets dicey. It does look like forskolin does up regulate aromatase, but still risky spiking blood pressure.
_______________________________

Prostaglandins can be synthesized in an adrenocortical carcinoma, and they can work in an autocrine or paracrine fashion. In rabbit chondrocyte and human squamous carcinoma cell lines, EGF induced the secretion of PGE2 via up-regulation of the activities of phospholipase A2 (PLA2) and COX-2 (Sato et al. 1997, Huh et al. 2003). This may suggest that PGE2 acts as a secondary factor to EGF in the up-regulation of aromatase expression. Therefore, we checked whether PGE2 was secreted from NCI-H295R cells in response to EGF. In this study, NCI-H295R cells secreted PGE2 in response to EGF (Fig. 13), and PGE2 increased aromatase activity to a greater extent than other prostaglandins (Fig. 6). The inhibition of EGF-induced aromatase expression with PGE2 receptor antagonists confirmed that PGE2 is the secondary factor of aromatase expression with EGF (Fig. 14). PGE1 also increased aromatase activity to a degree similar to that of PGE2, but EGF could not stimu- late NCI-H295R cells to secrete a sufficient concentration of PGE1 (data not shown) to increase aromatase activity. These results suggest that several prostaglandins are secreted in response to EGF, and that these prostaglandins evoke some intracellular signaling pathways. According to the experiments using several protein kinase inhibitors (Fig. 12), the intracellular signaling pathways that include MAP kinase, and calcium-calmodulin kinase are import- ant for up-regulation of aromatase by EGF. In response to EGF, EGF receptors (receptor-type tyrosine kinase) activate the MAP kinase pathway through phosphorylation of Ras protein. It is also well known that EGF receptors increase the intracellular calcium concentration. Therefore, it would be reasonable to conclude that inhibition of MAP kinase kinase and calcium-calmodulin kinase II down- regulate aromatase expression in NCI-H295R cells. Interestingly, a PKA inhibitor (H-89) down-regulated aromatase activity. This result suggests that the cAMP– PKA pathway is involved in the up-regulation of aromatase.

Effect of epidermal growth factor and prostaglandin on the expression of aromatase (CYP19) in human adrenocortical carcinoma cell line NCI-H295R cells

http://joe.endocrinology-journals.org/co.../1/59.full
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#80

(09-03-2015, 12:35 AM)Lotus Wrote:  That's good idea adding k2, how do you supplement it?, I tried grass fed butter in some coffee that Pom suggested, not bad. Egg yolks, gouda and brie cheese are other sources of k2 from what I've read.

Hi Lotus! I'm sorry I missed your reply before!

I get my K2 from Amazon in the UK of all places.

http://www.amazon.co.uk/gp/product/B00QQRQQH2

I believe the kind (MK-7) is important. This product comes from Natto (fermented soybeans). Importantly, is appears not possible to overdose on K2 (though you can on D3)

K2 is _very_ underrated. Without it, the Calcium that the D3 helps to move can get deposited in the arteries instead of the bones and teeth!

Quote:That study is a good find (thanks). A healthy immune system is a big priority in NBE for sure. Mine went haywire when I pushed too hard.

You're welcome! Smile

Quote:...

Btw, I'm glad you came out of moth balls, welcome back.

Thanks! I'll stay longer this time. ("Oh no!" they wail...)

B.


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