Indole-3-carbinol inhibition of androgen receptor

[DoctorHouse]

I have some DIM and every time I take it, I get bad bloating and intestinal gas. Anyone experience this?

 

[squeegee]

What brand are you using???

 

[DoctorHouse]

Nature's Way Dim Plus which is suppose to have great absorption. My stomach feel like a balloon ready to burst when I take it.

 

[gjp2222]

Nature's Way Dim Plus which is suppose to have great absorption. My stomach feel like a balloon ready to burst when I take it.

That was the first brand I tried, had the problem periodically too. I thought it was normal but it has not happened since I switched to ActivMune, guess there is a difference in the processing.

 

[DoctorHouse]

Nature's Way Dim Plus which is suppose to have great absorption. My stomach feel like a balloon ready to burst when I take it.

That was the first brand I tried, had the problem periodically too. I thought it was normal but it has not happened since I switched to ActivMune, guess there is a difference in the processing.

Thanks for the tip. Have you noticed any benefit to taking DIM?

 

[gjp2222]

Nature's Way Dim Plus which is suppose to have great absorption. My stomach feel like a balloon ready to burst when I take it.

That was the first brand I tried, had the problem periodically too. I thought it was normal but it has not happened since I switched to ActivaMune, guess there is a difference in the processing.

Thanks for the tip. Have you noticed any benefit to taking DIM?

Definitely, just posted this earlier...

If you are looking for the best DIM supplement on the market, consider using this product. I began using it Feb this year as a method of offsetting some of the finasteride sides. Not only did it accomplish this but it has improved my hair, much thicker with increased growth in crown area. It has also improved my general health including leaning me out a bit and better skin texture. Its not cheap but it is the most technically advanced DIM supplement around. Guess you get what you pay for.

http://www.activamune.com/product.htm

 

[CCS]

inhibiting estrogen production is not good.

 

[el_duterino]

i ordered 25grams of research-grade, 98% pure DIM powder. I have some problems disolving it. i know that it is liposoluble and seems that it will also dissolve in DMSO.
My goal is to use it as a topical to replace RU58841 as it is much cheaper and has no side effects it seems.

people are taking 200mg a day oral and experience no libido issues, so it could have a good potential as a topical provided we can mix it into a good vehicle.

I never used DMSO, does anyone have some comment in using DMSO as topical on the scalp ?

thanks
El Duterino

 

[gjp2222]

i ordered 25grams of research-grade, 98% pure DIM powder. I have some problems disolving it. i know that it is liposoluble and seems that it will also dissolve in DMSO.
My goal is to use it as a topical to replace RU58841 as it is much cheaper and has no side effects it seems.

people are taking 200mg a day oral and experience no libido issues, so it could have a good potential as a topical provided we can mix it into a good vehicle.

I never used DMSO, does anyone have some comment in using DMSO as topical on the scalp ?

thanks
El Duterino

I wouldn't mess too much with DMSO, it is really overkill, this stuff will drive everything it touches into your scalp and become systematic. I have used DMSO in the past for injuries and within a few minutes you can taste it in your mouth. You only need something that is capable of making it to the follicle.

BTW... a doctor once told me that DMSO is similar to WD-40, makes you think.

 

[bornthisway]

i ordered 25grams of research-grade, 98% pure DIM powder. I have some problems disolving it. i know that it is liposoluble and seems that it will also dissolve in DMSO.
My goal is to use it as a topical to replace RU58841 as it is much cheaper and has no side effects it seems.

people are taking 200mg a day oral and experience no libido issues, so it could have a good potential as a topical provided we can mix it into a good vehicle.

I never used DMSO, does anyone have some comment in using DMSO as topical on the scalp ?

thanks
El Duterino

I wouldn't mess too much with DMSO, it is really overkill, this stuff will drive everything it touches into your scalp and become systematic. I have used DMSO in the past for injuries and within a few minutes you can taste it in your mouth. You only need something that is capable of making it to the follicle.

BTW... a doctor once told me that DMSO is similar to WD-40, makes you think.

I'll admit I've been reluctant to use DMSO since I first read people using it, if others can reaffirm it's safety then I suppose it can't hurt to try.

From Wikipedia:
Safety

MSDS recommends wearing safety glasses because DMSO can cause chronic damage to the eyes.[10] Glove selection is important when working with DMSO. Thick rubber gloves are recommended. Nitrile gloves, which are very commonly used in chemical laboratories, have been found to dissolve rapidly with exposure to DMSO.[11] Because DMSO easily penetrates the skin, substances dissolved in DMSO may be quickly absorbed. For instance, a solution of sodium cyanide in DMSO can cause cyanide poisoning through skin contact. DMSO by itself has low toxicity.[12] Dimethyl sulfoxide can produce an explosive reaction when exposed to acid chlorides; at a low temperature, this reaction produces the oxidant for Swern oxidation.

http://en.wikipedia.org/wiki/Dimethyl_sulfoxide

 

[gjp2222]

i ordered 25grams of research-grade, 98% pure DIM powder. I have some problems disolving it. i know that it is liposoluble and seems that it will also dissolve in DMSO.
My goal is to use it as a topical to replace RU58841 as it is much cheaper and has no side effects it seems.

people are taking 200mg a day oral and experience no libido issues, so it could have a good potential as a topical provided we can mix it into a good vehicle.

I never used DMSO, does anyone have some comment in using DMSO as topical on the scalp ?

thanks
El Duterino

I wouldn't mess too much with DMSO, it is really overkill, this stuff will drive everything it touches into your scalp and become systematic. I have used DMSO in the past for injuries and within a few minutes you can taste it in your mouth. You only need something that is capable of making it to the follicle.

BTW... a doctor once told me that DMSO is similar to WD-40, makes you think.

I'll admit I've been reluctant to use DMSO since I first read people using it, if others can reaffirm it's safety then I suppose it can't hurt to try.

From Wikipedia:
Safety

MSDS recommends wearing safety glasses because DMSO can cause chronic damage to the eyes.[10] Glove selection is important when working with DMSO. Thick rubber gloves are recommended. Nitrile gloves, which are very commonly used in chemical laboratories, have been found to dissolve rapidly with exposure to DMSO.[11] Because DMSO easily penetrates the skin, substances dissolved in DMSO may be quickly absorbed. For instance, a solution of sodium cyanide in DMSO can cause cyanide poisoning through skin contact. DMSO by itself has low toxicity.[12] Dimethyl sulfoxide can produce an explosive reaction when exposed to acid chlorides; at a low temperature, this reaction produces the oxidant for Swern oxidation.

http://en.wikipedia.org/wiki/Dimethyl_sulfoxide

Seems real safe to me! Go on, try it! :jackit:

 

[DoctorHouse]

GJP, I am using Activamune and it did not upset my stomach as you suggested. I am just wondering how long did it take to see results from it. I am hoping to see some increase in thickness from it.

 

[gjp2222]

I started using it this past February, started noticing more thickness around July and still progressing, slowly but surely. Never bought it with intentions of hair growth, its just a real healthy supplement.

 

[el_duterino]

I am about to start my experiment with Topical DIM, dissolved in a bit of DMSO, since it is supposed to be a powerful anti-androgen in the same league as Flutamide.

One thing I cannot understand, though : since if it has the same anti-androgenic power as flutamide or Casodex, why are there no anti-androgenic side effects reported. I mean, a lot of people take oral DIM supplements, like 150mg a day.

However, I cannot find a single report that hints some side effects related to using systemc anti-androgens..such as low libido, brain fog, tiredenss and the like.

DIM half life is usppsed to be rather long..something like 48 hours if I remember right.

 

[squeegee]

I've been taking DIM for months and got no side at all. Dim is good!

 

[joseph49853]

Be careful experimenting with DIM... it's powerful stuff if taken correctly.

I had been using supplemental curcumin (along with many other anti inflammatory supplements: green tea, grape seed, holy basil, milk thistle, resveratrol etc.) emulsified in olive oil with bioperine and orotic acid to enhance bioavailability. I decided to try 100MG of Source Naturals DIM in the mixture for a week. I even foolheartedly placed 50MG in my topical. I should have left well enough alone.

As a diffuse thinner, I had been doing so amazingly well with needling, scalp topicals, and biomagnetics.... well enough to have ceased all treatments for days/weeks at a time. These past three years I have more hair with a thicker hairline than I ever did on either propecia or minoxidil.

Within one week of DIM supplementation tufts of hair started falling out like CRAZY. I had only taken 7 tablets. Now Instead of finding the usual 5-10 hairs in the shower, they were numbering around 100, and growing steadily. And they were THICK. I immediately remembered what the panic of hairloss felt like. I was leaving a trail of hair everywhere. For the first time in almost two years, you could see major parts of my scalp, especially on the vertex and frontal crown (near the hairline.) It was as if I had turned on a switch or a faucet. Crazy.

After ceasing DIM, within around three days my hair stopped falling out. Now I'm back to around 5-15 hairs in the shower. I've learned my lesson, and decided not to mess with anti-androgens without a hormone test. In SOME people, altering the body's delicate hormonal balance can be deleterious.

I wanted to lower bad estrogen and lose body fat, but instead it lowered estrogen too much in general. I figure it should take around six months to recover what was lost.

 

[squeegee]

Down-regulation of Androgen Receptor by 3,3'-Diindolylmethane Contributes to Inhibition of Cell Proliferation and Induction of Apoptosis in Both Hormone-Sensitive LNCaP and Insensitive C4-2B Prostate Cancer Cells

http://cancerres.aacrjournals.org/cgi/c ... 6/20/10064

In Men D.I.M. helps to eliminate active estrogen by promoting its conversion into the "good" metabolites. These metabolites then free up testosterone by bumping it off the testosterone-binding proteins. The end result is a healthier balance of testosterone to estrogen and more free (unbound) testosterone circulating in the body. This has been linked to lean body mass, an efficient fat-burning metabolism, low abdominal obesity, increased libido, lower incidence of prostate enlargement (BPH) and a dramatically lower risk of prostate cancer.

 

[squeegee]

Why no one here never tried DIM or Indole-3 carbinol in a Topical?

http://www.primordialperformance.com/st ... ution.html as a vehicle with a good DIM brand will probably do the job... or will start to overdose it orally!


Toxicol Sci. 2001 May;61(1):40-8. Links
2,3,7,8-Tetrachlorodibenzo-p-dioxin and diindolylmethanes differentially induce cytochrome P450 1A1, 1B1, and 19 in H295R human adrenocortical carcinoma cells.Sanderson JT, Slobbe L, Lansbergen GW, Safe S, van den Berg M.
Research Institute for Toxicology, Utrecht University, P.O. Box 80176, 3508 TD Utrecht, The Netherlands. t.sanderson@ritox.vet.uu.nl

Diindolylmethane (DIM) is an acid-catalyzed condensation product of indole-3-carbinol, a constituent of cruciferous vegetables, and is formed in the stomach. DIM alters estrogen metabolism and inhibits carcinogen-induced mammary tumor growth in rodents. DIM is a weak agonist for the aryl hydrocarbon (Ah) receptor and blocks the effects of estrogens via inhibitory Ah receptor-estrogen receptor cross-talk. DIM and various structural analogs were examined in H295R cells for effects on 3 cytochrome P450 (CYP) enzymes involved in estrogen synthesis and/or metabolism: CYP1A1, CYP1B1, and CYP19 (aromatase). Aromatase activity was measured by conversion of 1 beta-(3)H-androstenedione to estrone and (3)H(2)O. H295R cells were exposed to the test chemicals dissolved in dimethyl sulfoxide for 24 h prior to analyses. 2,3,7,8-Tetrachlorodibenzo-p-dioxin (TCDD) (0--30 nM) and DIM (0--10 microM) induced ethoxyresorufin-O-deethylase (EROD) activity, as a measure of CYP1A1 and possibly 1B1 activity, with EC(50) values of about 0.3 nM and 3 microM, respectively. DIM, but not TCDD, induced aromatase activity with an apparently maximal 2-fold increase at 10 microM; higher concentrations of DIM and many of its analogs were cytotoxic. TCDD (30 nM) significantly increased CYP1A1 and 1B1 mRNA levels, but had no effect on mRNA for CYP19. DIM (3 microM) significantly increased mRNA levels for all three CYPS: DIM analogs with substitutions on the 5 and 5' position (3 microM) induced aromatase and EROD activity, together with mRNA levels of CYP1A1, 1B1, and 19; analogs that were substituted on the central carbon of the methane group showed little or no inductive activity toward the CYPS: In conclusion, DIM and several of its analogs appear to induce CYPs via multiple yet distinct pathways in H295R human adrenocortical carcinoma cells.

1: a*** Bioanal Chem. 2008 Feb;390(4):1111-9. Epub 2008 Jan 11. Links
Screening of synthetic and plant-derived compounds for (anti)estrogenic and (anti)androgenic activities.Bovee TF, Schoonen WG, Hamers AR, Bento MJ, Peijnenburg AA.
Department of Safety & Health, RIKILT-Institute of Food Safety, P.O. Box 230, 6700 AE, Wageningen, The Netherlands. toine.bovee@wur.nl

Recently we constructed yeast cells that either express the human estrogen receptor alpha or the human androgen receptor in combination with a consensus ERE or ARE repeat in the promoter region of a green fluorescent protein (yEGFP) read-out system. These bioassays were proven to be highly specific for their cognate agonistic compounds. In this study the value of these yeast bioassays was assessed for analysis of compounds with antagonistic properties. Several pure antagonists, selective estrogen receptor modulators (SERMs) and plant-derived compounds were tested. The pure antiestrogens ICI 182,780 and RU 58668 were also classified as pure ER antagonists in the yeast estrogen bioassay and the pure antiandrogen flutamide was also a pure AR antagonist in the yeast androgen bioassay. The plant-derived compounds flavone and guggulsterone displayed both antiestrogenic and antiandrogenic activities, while 3,3'-diindolylmethane (DIM) and equol combined an estrogenic mode of action with an antiandrogenic activity. Indol-3-carbinol (I3C) only showed an antiandrogenic activity. Coumestrol, genistein, naringenin and 8-prenylnaringenin were estrogenic and acted additively, while the plant sterols failed to show any effect. Although hormonally inactive, in vitro and in vivo metabolism of the aforementioned plant sterols may still lead to the formation of active metabolites in other test systems.


To examine the androgen antagonist effects of DIM, we conducted a series of cell proliferation and gene activation studies in androgen-dependent (LNCaP) and androgen-independent (PC-3) human prostate cancer cell lines. LNCaP cells were derived from lymph node metastasis, and PC-3 cells were derived from bone metastasis (22, 23, 24, 25). We found that DIM is a strong antiandrogen that inhibited androgen-dependent tumor cell growth and competitively inhibited androgen receptor translocation and signal transduction. In addition, DIM down-regulated prostate-specific antigen (PSA) expression at the transcriptional level. Results from androgen receptor (AR) competitive binding assays, nuclear translocation studies, and structural modeling computations suggest that DIM disrupts AR function in a manner similar to a chemically dissimilar synthetic antiandrogen, Casodex. Our results identify DIM as a structurally novel, naturally occurring, pure androgen antagonist of potential cancer preventive and therapeutic usefulness for prostate cancer.


DIM is an powerful antiandrogen and anti-aromatase!wow!!!!!!!!!!!

 

[el_duterino]

I did try it DIM as a topical on my whole scalp for several weeks.

I am sure to be the first and only known human to have done such an experiment so far.

I bought 99% pure, pharma/research grade DIM. DIM is not very expensive.

I used pharma grade pure DMSO as vehicle since DIM is very hard to dissolve. I tryied to dissolve DIM in various liquids: ethanol, PG, water etc.. but as written in the MDS it only dissolves in DMSO.

I just used the minimum of DMSO to dissolve the DIM and the rest was Ethanol, PG and D-Panthenol. I think that 1g dissolves into 3ml of DMSO so I ended up with about 5 or 10% DMSO, 10% D-Panthenol, 50% ETOH and the rest was PG.

DIM is a powerful skin irritant, it does burn the scalp in a lotion withtout a humectant.THe humectant will remove the irritation.

Glycerine works ok as humectant but is bad for absorption and leaves a greasy residue. I used USP D-Panthenol at about 10% in the mix.

I found out that DIM dissolves in ethanol in small quantities up to 0.4% if you want to avoid using DMSO.
But 0.4% is a bit weak by anti-androgen standards if we compare it to RU or flutamide.

DMSO is still very controversial in human use and has recently been found to hinder youg brain developpements in rats.

My trials involved using 0.5 %, 1 %, 1.5% and 2% once and even twice a day on my whole scalp as I am diffuse thinner. I was only using dutasteride as an internal during that time.

The first week on 1.5%, it seemed that my hair were getting thicker and shedding stopped.

After 2 weeks I started to shed a lot, and hair were looking thinner in diameter. I was shedding a lot of healthy thick hair and never had sheds before on any drugs. Not a good sign.
I stopped DIM and the shedding stopped the next day.

Conclusion: DIM might be a good anti-androgen but it does also 2 other things that are bad for hair.

DIM is a powerful anti-angiogenic, meaning that it will prevent new, small blood vessels from forming. This feature is good to fight or prevent cancer but very bad for hair growth.

DIM is also a powerful aromatase inhibitor, meaning that it will prevent testosterone from converting into estrogen in the scalp. this is also very bad for hair- more Test will trigger shedding. I think that this is was what caused my shedding.

While on DIM my libido was very, very high and acne was high, both signs pointing to a sharp increase in testosterone.

Final note: I switched to using RU. this is a powerful anti-androgen that works well and has no other adverse effects on hair. No shedding. No need to use DMSO.

Only drawback: RU is 10 times more expensive than pure DIM..

 

[waynakyo]

As a diffuse thinner, I had been doing so amazingly well with needling, scalp topicals, and biomagnetics.... well enough to have ceased all treatments for days/weeks at a time. These past three years I have more hair with a thicker hairline than I ever did on either propecia or minoxidil.

.

Can you please tell me about this : needling and biomagnetics ??

Thanks.