5ar inhibitors listed on wikipedia

[Dr. B]

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[Dr. B]

Inhibition of the enzyme can be classified into two categories: steroidal, which are irreversible, and nonsteroidal. There are more steroidal inhibitors, with examples including finasteride (MK-906), dutasteride (GG745), 4-MA, turosteride, MK-386, MK-434, and MK-963. Researchers have pursued synthesis of nonsteroidals to inhibit 5α-reductase due to the undesired side effects of steroidals. The most potent and selective inhibitors of 5α-R1 are found in this class, and include benzoquinolones, nonsteroidal aryl acids, butanoic acid derivatives, and more recognizably, polyunsaturated fatty acids (especially linolenic acid), zinc, and green tea.[8] Riboflavin was also identified as a 5α-reductase inhibitor .[18]

Additionally, it has been claimed that alfatradiol works through this mechanism of activity (5α-reductase), as well as the Ganoderic acids in lingzhi mushroom, and the Saw Palmetto.

Inhibition of 5α-reductase results in decreased conversion of testosterone to DHT, leading to increased testosterone and estradiol. Other enzymes compensate to a degree for the absent conversion, specifically with local expression at the skin of reductive 17β-hydroxysteroid dehydrogenase, oxidative 3α-hydroxysteroid dehydrogenase, and 3β-hydroxysteroid dehydrogenase enzymes.[19]

Gynecomastia, erectile dysfunction, impaired cognitive function, fatigue, hypoglycemia, impaired liver function, constipation, and depression, are only a few of the possible side-effects of 5α-reductase inhibition. Long term side effects, that continued even after discontinuation of the drug have been reported.


Its interesting wikipedia has PUFA listed as 5ar inhibitors, and these side effects listed. so despite being a mainstream site, it still seems accurate often.

its concerning they have things like zinc and riboflavin listed as 5ar inhibitors... maybe its only the supplemental isolated forms that have this effect, not the food sources? or the food sources have another factor inhibiting the 5ar inhibiting effect?

this is the article linked for riboflavin RIBOFLAVIN, A TESTOSTERONE 5α-REDUCTASE INHIBITOR and for zinc The 5 Alpha-Reductase Isozyme Family: A Review of Basic Biology and Their Role in Human Diseases

"Polyunsaturated fatty acids, found in vegetable oils, have been found to inhibit human and rat microsomal 5α-R activity. In this group, y-linolenic acid is the most potent compound tested. Since 5α-R isozymes are intrinsic membrane proteins, their activity may depend on the unique environment of the lipid bilayer. Whether and how fatty acids may function as endogenous regulators of 5α-R remain unknown."

is also concerning, PUFA are still found in ground beef fat, butter, milkfat, and many fats...

"
Some cations, especially zinc, have been reported to reduce sebum production in vivo and have been used to treat acne. In vitro assays have indicated that zinc specifically inhibits 5α-R1. This inhibition may be mediated both by non-competitive inhibition of T binding to 5α-R and by reduced formation of the NADPH co-factor.

(6)
Other nonsteroidal inhibitors include epicatechin-3-gallate and epigallocatechin-3-gallate, which are major constituents of green tea. Also included are 7-hydroxycoumarin derivatives, 2,6-disubstituted 4-hydroxy-4-hydroxymethyl biphenyl derivatives, isoflavonoids, and 3,3-diphenylpentane derivatives [9]."

@Hans @Lokzo

 

[MyUsernameHere]

Something to keep in mind is that this is generally applicable to the free forms of these fatty acids.

For instance, I have used supercritical CO2 extract of rice bran as a topical for hair. This contains high amounts of free PUFA's, such as GLA, which is a very strong 5-AR inhibitor.

If you just dump a bit of this extract into alcohol and apply it that way, the side effects are quite debilitating.

However, when I added some other components to it such as glycerine, PEG-40 hydrogenated castor oil, etc. these will bind up the fats and more closely resemble the forms they are found as in food and nature.

Once I did this most of the side effects (and effects) were gone.

Hence, most of the PUFAs found in food will be bound and not free-form and especially once they pass digestion probably won't have anything resembling strong 5-AR effects.

I have experienced more 5-AR symptoms from eating a tablespoon of coconut oil than most other foods (however I don't eat much high PUFA).

 

[Dr. B]

Something to keep in mind is that this is generally applicable to the free forms of these fatty acids.

For instance, I have used supercritical CO2 extract of rice bran as a topical for hair. This contains high amounts of free PUFA's, such as GLA, which is a very strong 5-AR inhibitor.

If you just dump a bit of this extract into alcohol and apply it that way, the side effects are quite debilitating.

However, when I added some other components to it such as glycerine, PEG-40 hydrogenated castor oil, etc. these will bind up the fats and more closely resemble the forms they are found as in food and nature.

Once I did this most of the side effects (and effects) were gone.

Hence, most of the PUFAs found in food will be bound and not free-form and especially once they pass digestion probably won't have anything resembling strong 5-AR effects.

I have experienced more 5-AR symptoms from eating a tablespoon of coconut oil than most other foods (however I don't eat much high PUFA).

strange
coconut oil is due maybe to its progesterone like effect, having a castrating type effect? doesnt progesterone in high amounts cause temporary castration, basically returns you to more like a childlike state or eunuch state?

did you use that supercritical rice bran extract for hair loss? what was the purpose
just applying it to your hair caused side effects? what kind of side effects?

what was the purpose of mixing it with glycerine etc then applying to hair?

does that mean capsules of fish oil or black seed oil would have a stronger anti 5AR effect, than, like eating omega 3 in a salmon, or chewing black seeds?
although these are still initially food sources, theyre just processed to remove the solid masses, since its an oil.,..

 

[MyUsernameHere]

strange
coconut oil is due maybe to its progesterone like effect, having a castrating type effect? doesnt progesterone in high amounts cause temporary castration, basically returns you to more like a childlike state or eunuch state?

did you use that supercritical rice bran extract for hair loss? what was the purpose
just applying it to your hair caused side effects? what kind of side effects?

what was the purpose of mixing it with glycerine etc then applying to hair?

does that mean capsules of fish oil or black seed oil would have a stronger anti 5AR effect, than, like eating omega 3 in a salmon, or chewing black seeds?
although these are still initially food sources, theyre just processed to remove the solid masses, since its an oil.,..

I was trying to replicate these studies:

Safety and efficacy of rice bran supercritical CO₂ extract for hair growth in androgenic alopecia: A 16-week double-blind randomized controlled trial

koreauniv.pure.elsevier.com

(PDF) In Vivo Hair Growth-Promoting Effect of Rice Bran Extract Prepared by Supercritical Carbon Dioxide Fluid

PDF | The potential hair growth-promoting activity of rice bran supercritical CO2 extract (RB-SCE) and major components of RB-SCE, linoleic acid,... | Find, read and cite all the research you need on ResearchGate

www.researchgate.net

If you note there the formulation that they actually applied consists of rice bran extract mixed with numerous other emulsifiers, surfactants etc. to create the final topical.
Initially I did not have these ingredients and only used the raw rice bran extract dissolved in ethanol, the side effects were brutal - vertigo, brain fog, nipple sensations, complete loss of libido, tinnitus, etc.

When I added the remaining ingredients the potency decreased greatly but it also seemed to lose most of its hair promoting effects as well. At that point I decided it was not worth messing with it anymore.

I believe as long as the fats are bound and not free-form (as they usually will be in most of these supplements) they don't have much of an inhibitory effect.

Regarding coconut oil, I don't think it's progesterone - that feels different. I may just be very sensitive since I had PFS, but I note similarities to the way I feel when I am exposed to other 5-AR inhibitory substances, so I don't consume it regularly. Policosanol (another loved substance here), is also something I won't touch with a 10-foot pole anymore.

 

[Dr. B]

I was trying to replicate these studies:

Safety and efficacy of rice bran supercritical CO₂ extract for hair growth in androgenic alopecia: A 16-week double-blind randomized controlled trial

koreauniv.pure.elsevier.com

(PDF) In Vivo Hair Growth-Promoting Effect of Rice Bran Extract Prepared by Supercritical Carbon Dioxide Fluid

PDF | The potential hair growth-promoting activity of rice bran supercritical CO2 extract (RB-SCE) and major components of RB-SCE, linoleic acid,... | Find, read and cite all the research you need on ResearchGate

www.researchgate.net

If you note there the formulation that they actually applied consists of rice bran extract mixed with numerous other emulsifiers, surfactants etc. to create the final topical.
Initially I did not have these ingredients and only used the raw rice bran extract dissolved in ethanol, the side effects were brutal - vertigo, brain fog, nipple sensations, complete loss of libido, tinnitus, etc.

When I added the remaining ingredients the potency decreased greatly but it also seemed to lose most of its hair promoting effects as well. At that point I decided it was not worth messing with it anymore.

I believe as long as the fats are bound and not free-form (as they usually will be in most of these supplements) they don't have much of an inhibitory effect.

Regarding coconut oil, I don't think it's progesterone - that feels different. I may just be very sensitive since I had PFS, but I note similarities to the way I feel when I am exposed to other 5-AR inhibitory substances, so I don't consume it regularly. Policosanol (another loved substance here), is also something I won't touch with a 10-foot pole anymore.

whats issue with policosanol, its 5 ar inhibiting?
i briefly used saw palmetto years ago, got some odd side effects, pain in the balls for some time

what were you using this mixture for, topical for hair loss?