The test results of several DHT inhibitors/& drawbacks

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michael barry

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Ive found a patent that analyzes many known alpha five reductase inhibtiors in WHOLE CELL assay tests (meaning they can penetrate cells and still inhibit alpha five reductase). I'll highlight a few of these.............




TABLE 3
Inhibition of 5 α-reductase isozymes by various natural
flavonoidsa
5 α-Reductase
Cell-Free assay IC50 (µM) Whole-cell assay IC50
(µM)
Polyphenol Type 1 Type 2 Type 1 Type 2
Myricetin 23 (96) >100 (31) >100 (11) >100 (11)
Quercitin 23 (96) >100 (14) >100 (15) >100 (29)
Baicalein 29 (79) 99 (51) >100 (24) >100 (4)
Fisetin 57 (97) >100 (4) >100 (42) >100 (27)
Biochanin A >100 (50) 17 (74) 64 (64) 5 (93)
Daidzein >100 (3) 29 (69) 10 (13) 7 (89)
Kaempferol >100 (22) 12 (62) 79 (60) 20 (85)
Flavone >100 (20) >100 (-52) NDb ND
Genistein >100 (16) 23 (76) >100 (22) 20 (89)




TABLE 1
Inhibition of 5 α-reductase isozymes by green tea catechinsa
5 α-Reductase
Cell-Free assay IC50 (µM) Whole-cell assay IC50
(µM)
Catechin Type 1 Type 2 Type 1 Type 2
EC >100 (14) >100 (4) >100 (0) >100 (1)
EGC >100 (15) >100 (3) >100 (15) >100 (1)
ECG 11 (100) 69 (83) >100 (0) >100 (0)
EGCG 15 (99) 74 (74) >100 (6) >100 (0)
a IC50 : concentration (µM) of compound producing 50%
inhibition of 5 α-reductase activity. Values in parentheses are
percent inhibition of 5 α-reductase activity in the presence of 100
µM concentration of the indicated compound.




TABLE 4
Inhibition of 5 α-reductase by compounds containing catecholsa
5 α-Reductase
Whole-cell
Cell-free assay IC50 (µM) assay IC50 (µM)
Catechol Type 1 Type 2 Type 1 Type 2
Anthrarobon 4 (99) 50 (97) 6 (91) >100 (31)
Bromopyrogallol 7 (98) 84 (58) NDb ND
red
)Gossypol 7 (99) 21 (99) 7 (100) 6 (99)
Pyrogallol red 15 (97) >100 (27) ND ND
Nordihydro- 19 (99) 50 (80) 19 (99) 22 (99)[
guaiaretic acid
Caffeic acid 26 (97) >100 (36) 8 (99) 7 (98)
phenethyl ester
Octyl gallate 27 (99) 58 (90) 7 (99) 18 (94)
Purpurogallin 30 (81) >100 (31) ND ND
Hydroxydopamine 42 (69) >100 (41) ND ND
Dodecyl gallate 43 (88) >100 (36) 3 (99) 7 (98)
Pyrocatechol violet 48 (85) 100 (47) ND ND
Pyrogallol 70 (60) >100 (28) >100 (7) >100 (15)
Hematoxylin 83 (59) >100 (38) ND ND
HZIV-82 >100 (43) >100 (0) 3 (79) >100 (15)


TABLE 6
Inhibition of 5 α-reductase isozymes by quinonesa
5 α-Reductase
Cell-Free Whole-cell
assay IC50 (µM) assay IC50 (µM)
Quinone Type 1 Type 2 Type 1 Type 2
Purpurin 2 (95) >100 (20) NDb ND
Alizarin 3 (95) >100 (54) 6 (75) >100 (27)
Anthrarobin 4 (99) 50 (97) 6 (91) >100 (31)
Menadione 6 (77) 5 (81) 51 (82) 79 (62)
Coenzyme q 12 (77) 22 (81) ND ND
2,5- 15 (78) 17 (97) ND ND



A few of these jump out at you, but there are some problems with their topical application.

Caffeic acid is a skin irritant. Its in white grapes, white wine, and in a few other things.

Octyl and Doctyl Gallates are preservatives, they mix with alcohol well, but they are both skin irritants..........

Gossypol might be terrific, but its in very small quantities in nature. Its about one-tenth of one measley percent of cottonseed oil.

Curcumin would be terrific, but it would stain your scalp yellow. White curcumin wasn't as effective.

Alizarin would be good, but it would stain your scalp red. Its from the madder plant.

EGCG didn't have an effect on whole cell assays, but is effective at inhiting alpha five if you can get it to the cell with a carrier. Alot of people dont know this, but black tea has a pretty suficient quantity of this stuff. Not as much as green tea, but its there.

Biochanin A, Genistein, Daidzien are all in red clover.............................this might be a real possibility. Red clover tea is drank, so its not an unusual substance. It would be interesting to see these put on a flank organ........


One other substance we have bandied about: Licorice...................it basically suppresses melanocytes. Its used in skin-LIGHTENING creams. Just great................a headfull of white hair. No thanks on that one.

Arnica Montana is an androgen-receptor blocker, but its internally literally poisonous. Don't know if Id risk absorbing small amounts of that stuff over the years.


Peppermint (alpha five inhibitor) and clove (alpha five inhibitor) and rose hips (receptor binding inhibition) are real possibilities.


Cedarwood oil is another real possibility. Im testing that on my beard right now.

Kaempferol is in black and green tea.....................but are not much of those substances.
 
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michael barry said:
One other substance we have bandied about: Licorice...................it basically suppresses melanocytes. Its used in skin-LIGHTENING creams. Just great................a headfull of white hair. No thanks on that one.
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If your hair did come out at a ligher hue, you can always dye it, seems alright to me.

michael barry said:
Gossypol might be terrific, but its in very small quantities in nature. Its about one-tenth of one measley percent of cottonseed oil.
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Gossypol isn't that expensive $45 for 50mg, see for example http://www.echemshop.com/product.php?productid=180

However, it is toxic internally so you may not want to risk it. Eating it will also make you sterile (it has been tested for long periods of time as a male contraceptive).
 
blueshard

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MB, do you think curcumin could be made into a topical with just distilled water? Alcohol/pg/glycerin can make scalp health worse for some people.
 
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michael barry

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regardless, it wont turn your hair white
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how do you know this? Have you been using licorice topically for several years? Melanocytes are what stain the hair follicle and give it color. Licorice has been shown to slow their production in human skin by some 41%



Glabridine is a fraction of licorice extract (hydrophobic compound). It has a double activity : tyrosinase inhibition and anti-inflammatory (10). Human normal melanocytes stimulated by a-MSH and treated with licorice extract at 0.0002% , during 4 days, had an inhibition of melanin synthesis of 41% (Fig 7)*.

Fig 7. Licorice extract effects on stimulated melanocytes. Melanin synthesis was assessed by 14C-DOPA inclusion, and expressed in cpm/mg proteines/ 24h*.
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http://www.srd.ro/?pid=386




Thats why we might keep looking to find the optimal topical anti-androgen that doesn't have this effect. There are other receptor blockers (rose hips, gossypol, possibly cedarwood, maybe arnica, green tea, possibly beta sitosterol) out there, and other alpha five inhibitors out there. We need human testing to find one that doesn't stain the scalp, isn't absorbed internally, doesn't smell awful, and isn't too greasy. Its a tall task, but Im pretty confident one can be found. Getting excited over one study showing strong inhibition with a small amount of a substance is great, but substances that only have decent inhibition can be just as good, one might have to just use a bit more of it (a couple of extra pumps from a sprayer). Truth be told, topical green tea extract is probably "enough". I hope licorice is too..................but I really wouldn't want to be a guy whose hair started turning white three years or so down the line like Richard Gere. Caution, always.
 
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michael barry

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Blueshard........................curcumin would probably stain the scalp pretty yellow. I dont think (right off the top of my head) that curcumin is very soluble in water. You might check and see. Sometimes water can be heated up and something can become more soluble. Perhaps some creams can be made with regular curcumin, as a matter of fact I know that some have. They might make you hair look a bit greasy though. Im sure a curcumin topical can be made, but it will take some chemistry in doing so. AJCS-9 is a product based on it that Androscience is in phase two with right now.
 
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rusty_y2k2

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So if i was looking for something to add that acts as a receptor blocker that i could add to my shampoo, cedarwood oil would be a pretty good bet?

I'm already on finasteride, and am using a minoxidil solution with some topical dht reducing agents (including ket, which i believe is thought to be something of a receptor site blocker in terms of its mode of action? is that correct?) but want something to help prevent testosterone from having it's wicked way with my poor defenseless follicles....

cheers for any help!
 
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Charly

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So green tea and black tea both have egcg and caffeic acid....................Would caffeic acid be the same thing as caffeine?

Also i've been using mint toothbrush and my beard thinned and color hue lightened as well.......From black...to brown........Mint and licorice have both been lumped together in previous stuidies...Can we assume they might have similar reactions? Also......shouldn't it have the opposite reaction on scalp hair?
 
hair today gone tomorrow

hair today gone tomorrow

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Michael, they sell licorice shampoos....I dont know the concentrations of licorice in the shampoo, but do you think using this shampoo for years would cause your hair to go white??
 
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michael barry

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So if i was looking for something to add that acts as a receptor blocker that i could add to my shampoo, cedarwood oil would be a pretty good bet?
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Im testing it on my beard hair now. In a couple of months I'll be able to tell you if I have less hair where Im putting it.



Joined: Wed Mar 07, 2007 1:08 pm
Posts: 170 michael...did they put numbers for clove in that table? and quantities used
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?
The didn't test "clove", although a japanes study says its an alpha five inhihbitor. They DID test genistein, daidzien, and biochanin A.....which are all in RED clove, and found them to be good inhibitors of alpha five reductase




?
Location: Chicago, IL So green tea and black tea both have egcg and caffeic acid....................Would caffeic acid be the same thing as caffeine?
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Caffeic acid is not in green or black tea. Its in coffee a little bit, white grapes and white wine, a smidgen of it is in rosemary, I think a tidbit of it is in broccholi. Its a skin irritant by iteslf though.

Also i've been using mint toothbrush and my beard thinned and color hue lightened as well.......From black...to brown........Mint and licorice have both been lumped together in previous stuidies...Can we assume they might have similar reactions?
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yes, they are both anti-androgens

Also......shouldn't it have the opposite reaction on scalp hair?
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Yep, they should help it grow



Posts: 2592 Michael, they sell licorice shampoos....I dont know the concentrations of licorice in the shampoo, but do you think using this shampoo for years would cause your hair to go white??
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I know its been shown to slow melanocytes down by 41%. Maybe it doesnt kill them, but just chemically suppresses them. It would seem to be something that would lighten hair color. Did you know that peppermint makes melanocytes more active, darkening hair? Prox-n has definitely darkened my own hair. Licorice might not make the hair white, it might just lighten it. If someone tried it for a few years, then we could say for sure. Im sure its a potent anti-androgen.




Im still pretty high on green tea being a "good one", and peppermint too. We will see about the cedarwood oil.
 
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bornthisway

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I remember you posted about the suppressive effects of honey on prostaglandins, though I don't believe it's therapeutic and preventive effects for seborrheic dermatitis/dandruff have been posted.

Honey has antibacterial, antifungal and antioxidants activities and has high nutrient value. In this study we investigated the potential use of topical application of crude honey in the management of seborrheic dermatitis and dandruff. Thirty patients with chronic seborrheic dermatitis of scalp, face and front of chest were entered for study. Twenty patients were males and 10 were females, their ages ranged between 15 and 60 years. The patients had scaling, itching and hair loss. The lesions were scaling macules, papules and dry white plaques with crust and fissures. The patients were asked to apply diluted crude honey (90% honey diluted in warm water) every other day on the lesions with gentle rubbing for 2-3 mins. Honey was left for 3 hr before gentle rinsing with warm water. The patients were followed daily for itching, scaling, hair loss and the lesions were examined. Treatment was continued for 4 weeks. The improved patients were included in a prophylactic phase, lasting six months. Half patients were treated with the topical honey once weekly and the other half served as control. All the patients responded markedly with application of honey. Itching was relieved and scaling disappeared within one week. Skin lesions were healed and disappeared completely within 2 weeks. In addition, patients showed subjective improvement in hair loss. None of the patients ( 15 patients) treated with honey application once weekly for six months showed relapse while the 12/15 patients who had no prophylactic treatment with honey experienced a relapse of the lesions 2-4 months after stopping treatment. It might be concluded that crude honey could markedly improve seborrheic dermatitis and associated hair loss and prevent relapse when applied weekly.

PMID: 11485891

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Regarding piperine if you didn't catch the post I made:

Testosterone 5alpha-reductase inhibitory active constituents of Piper nigrum leaf.

School of Pharmaceutical Sciences, Kinki University, 3-4-1 Kowakae, Higashiosaka, Osaka 577-8502, Japan.

Previously we reported that Piper nigrum leaf extract showed a potent stimulation effect on melanogenesis and that (-)-cubebin (1) and (-)-3,4-dimethoxy-3,4-desmethylenedioxycubebin (2) were isolated as active constituents. As a part of our continuous studies on Piper species for the development of cosmetic hair-care agents, testosterone 5alpha-reductase inhibitory activity of aqueous ethanolic extracts obtained from several different parts of six Piper species, namely Piper nigrum, P. methysticum, P. betle, P. kadsura, P. longum, and P. cubeba, were examined. Among them, the extracts of P. nigrum leaf, P. nigrum fruit and P. cubeba fruit showed potent inhibitory activity. Activity-guided fractionation of P. nigrum leaf extract led to the isolation of 1 and 2. Fruits of P. cubeba contain 1 as a major lignan, thus inhibitory activity of the fruit may be attributable to 1. As a result of further assay on other known constituents of the cited Piper species, it was found that piperine, a major alkaloid amide of P. nigrum fruit, showed potent inhibitory activity, thus a part of the inhibitory activity of P. nigrum fruit may depend on piperine. The 5alpha-reductase inhibitory activities of 1 and piperine were found for the first time. In addition, the P. nigrum leaf extract showed in vivo anti-androgenic activity using the hair regrowth assay in testosterone sensitive male C57Black/6CrSlc strain mice.

BTW, the piper nigrum study I posted was based on topical application, it also stimulated melanogenesis.

PDF: http://www.jstage.jst.go.jp/article/bpb/30/12/2402/_pdf
 
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michael barry

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Bornthisway..

Ive never written about honey, but Doctor has mentioned it a time or two.




Very interesting about piperene in the mouse. Did you know piperene counteracts propecia when both are used? I suppose we can add piperene to black tea as far as "things that reduce DHT in mice". Id love to see one man try it in vivo and get his DHT levels checked, it would be interesting.



I think peppermint stimulates melanocytes also, been a long time since I read about that though...............maybe it was something else.
 
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rusty_y2k2

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michael barry said:
Did you know piperene counteracts propecia when both are used?
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saaaaaaaaay what now?

I was intending to use piperine to increase the oral bioavailability of resveratrol.... by what mechanism does it inhibit propecia?
 
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goata007

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michael...you mentioned clove extract, is that same as clove oil? Also, do you have link to study that test serveral oils/herbs for their anti-androgenic effects and provided the data?
 
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CCS

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Well, I'll keep using lavendar and EGCG in my shampoo, and will add http://www.evitamins.com/product.asp?pid=446. How long do you think it lasts in shampoo? I could use a smaller shampoo bottle, and acidify it a bit with alpha lipoic acid. Most stuff seems to be more stable at acid conditions around pH 4.

As for body wash, I'll use peppermint and EGCG.
 
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