Cyproheptadine, an epigenetic modifier, exhibits anti-tumor activity - 2021

Lokzo

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Cyproheptadine, an epigenetic modifier, exhibits anti-tumor activity by reversing the epigenetic silencing of IRF6 in urothelial carcinoma​


Background: Urothelial carcinoma (UC) is the second most common malignancy of the urinary system with high rate of recurrence, UC patients therefore needed to be treated with surgery followed by chemotherapy. Development of novel therapeutics with minimal side-effect is an urgent issue. Our previous study showed that cyproheptadine (CPH), an anti-histamine, exhibited antitumor activity in UC in vitro and in an xenograft model. However, the molecular mechanism of how CPH inhibits tumor progression is not fully understood.
Methods: Genes that were upregulated after treatment with CPH in UC cells, were examined by RNA-Seq. Real-time quantitative PCR (RT-qPCR) was employed to detect IRF6 expression while COBRA assay and bisulphite pyrosequencing were used to examine promoter methylation of IRF6. Enrichment of total H3K27 acetylation and H3K4 mono-methylation were detected by western blotting. Colony formation and flow cytometry were used to examine proliferation and apoptosis in UC cells overexpressed or depleted with IRF6. Nude mice xenograft model was used to examine the effect of IRF6 in UC.
Results: Our result showed that several genes, including IRF6 were upregulated after treatment with CPH in BFTC905 UC cells. Further experiments found that treatment of CPH could restore the expression of IRF6 in several other UC cell lines, probably due to promoter hypomethylation and enrichment of H3K27 acetylation and H3K4 mono-methylation. These results may be due to the fact that CPH could alter the activity, but not the expression of epigenetic modifiers. Finally, re-expression of IRF6 in UC inhibited tumor growth in vitro and in an xenograft mouse model, by inducing apoptosis.
Conclusion: In conclusion, our results suggested that CPH may be an epigenetic modifier, modulating the expression of the potential tumor suppressor IRF6, in inhibiting tumor growth in UC.

 

Ignoramus

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I love cypro and how I sleep on it. It seems to make me fat and unmotivated though. My ex broke up with me because of how different it made me (happy but indifferent to success + greatly reduced sex drive). Does anyone know a way around this? Currently I just use it if I'm chronically under-slept.
 
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Lokzo

Lokzo

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I love cypro and how I sleep on it. It seems to make me fat and unmotivated though. My ex broke up with me because of how different it made me (happy but indifferent to success + greatly reduced sex drive). Does anyone know a way around this? Currently I just use it if I'm chronically under-slept.

Super interesting man.

It raises prolactin without a doubt with back to back usage.

Everyone is waiting for @haidut to release a cyproheptadine alternative... Was it a Harmala alkaloid?
 

PaRa

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cypro is anti histamine so yeah it will crashes motivation, drive, libido and shoots hunger up so basically you'll just be inactive and hungry, perfect combo to put on fat
 

Beastmode

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Peat has mentioned to me that most people use way too much of cypro at a time.

.5 mg, especially @haidut's one, is more than enough for general use.

For emergency, short term situations, I can see how higher doses are more relevant.
 

osar

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I definitely notice the appetite surge and low motivation. But the rebound effect 4 days later is truly amazing.
I noticed increased strength when using it, also mush faster recovery even between sets. Have you noticed this?
 

opethfeldt

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I had the most motivated period of my life on Cypro. It can make me lethargic but only if it's the weekend or if I have nothing going on.
 

Beastmode

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I had the most motivated period of my life on Cypro. It can make me lethargic but only if it's the weekend or if I have nothing going on.

Interesting. When I've taken it early in the day, at a very low dose (.5 mg,) I definitely noticed a higher capacity to work and my vision even became sharper.
 
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Peat has mentioned to me that most people use way too much of cypro at a time.

.5 mg, especially @haidut's one, is more than enough for general use.

For emergency, short term situations, I can see how higher doses are more relevant.
I’ll second that. It is very potent. The sweet spot for me is actually even less than that - around 0,2-0,3 mg twice daily. I remember reading through this forum in the past it’s the recommended dosage by Ray, but don’t quote me on that.
 

tankasnowgod

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I love cypro and how I sleep on it. It seems to make me fat and unmotivated though. My ex broke up with me because of how different it made me (happy but indifferent to success + greatly reduced sex drive). Does anyone know a way around this?
I'm using both Metergoline and the Tyrosine/BCAA combo, and I am finding that solves most of those types of issues. I certainly got the "happy but indifferent" feeling on cypro. Now, I'm feeling good mood wise, but also more driven. I got a lot more productive in June of this year, partially by "willpower," but I think I might have also reduced or eliminated my cypro dose around the same time. I made the switch to the above combo about a month ago (to focus more on upping dopamine), and I am tackling things I couldn't/wouldn't do for the past year or so. Like a mini Dynamo. I kept up the positive changes from June, so this is on top of those habits.

I also added some "sleep hacks" that I think is keeping stress more at bay when asleep, I'll prolly be starting a thread on those in about a week. They had some instant positive effects, and that has held steady for a couple weeks now.
 

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