Is Chrysin effective ??
- Thread starter Rickyroid
- Start date
liftsiron
Community Veteran, Longtime Vet
I believe that it is marginally effective at reducing estro bloat, but I would strongly urge you to have some nolva on hand if symptoms of gyno appear. Chrysin just isn't going to do the trick. I've read in a few articles that chrysin only is capable of reducing estro by about 20%.
Last edited:
Nelson Montana
Community Veteran, Bodybuilding Author
Will Chrysin lower estrogen levels? Absolutely.
Will it be enough to stop gyno if you're highly suseptable to it and you do a long, heavy cycle? Probably not.
Calcium D Clucerate also removes e. So adding a supp that has both can be useful for after light cycles, in addition to other lower dosed anti -e's (preferably Proviron or a-dex) and for anytime you want to keep a good T/e balance. You can read more about this in depth here: www.proteinfactory.com
Will it be enough to stop gyno if you're highly suseptable to it and you do a long, heavy cycle? Probably not.
Calcium D Clucerate also removes e. So adding a supp that has both can be useful for after light cycles, in addition to other lower dosed anti -e's (preferably Proviron or a-dex) and for anytime you want to keep a good T/e balance. You can read more about this in depth here: www.proteinfactory.com
hhajdo
Community Veteran
There is no evidence that Chrysin is an aromatase inhibitor in vivo:
J Steroid Biochem Mol Biol. 2001 Sep;78(3):231-9. Related Articles, Links
No evidence for the in vivo activity of aromatase-inhibiting flavonoids.
Saarinen N, Joshi SC, Ahotupa M, Li X, Ammala J, Makela S, Santti R.
Institute of Biomedicine, University of Turku, Kiinamyllynkatu 10, FIN-20520, Turku, Finland.
Measurements of the aromatase-inhibiting and antioxidative capacities of flavonoids in vitro showed that slight changes in flavonoid structure may result in marked changes in biological activity. Several flavonoids such as 7-hydroxyflavone and chrysin (5,7-dihydroxyflavone) were shown to inhibit the formation of 3H-17beta-estradiol from 3H-androstenedione (IC(50)<1.0 microM) in human choriocarcinoma JEG-3 cells and in human embryonic kidney cells HEK 293 transfected with human aromatase gene (Arom+HEK 293). Flavone and quercetin (3,3',4',5,7-pentahydroxyflavone) showed no inhibition (IC(50)>100 microM). None of the requirements for optimal antioxidative capacity (2,3-double bond with 4'-hydroxy group, 3-hydroxyl group, 5,7-dihydroxy structure and the orthodihydroxy structure in the B-ring) is relevant for the maximum inhibition of aromatase by flavonoids. After oral administration to immature rats at a dose of 50 mg/kg body weight, which considerably exceeds amounts found in daily human diets, neither aromatase-inhibiting nonestrogenic flavonoids, such as chrysin, nor estrogenic flavonoids, such as naringenin and apigenin, induced uterine growth or reduced estrogen- or androgen-induced uterine growth. The inability of flavonoids to inhibit aromatase and, consequently, uterine growth in short-term tests may be due to their relatively poor absorption and/or bioavailability
----------------------------
Int J Sport Nutr Exerc Metab. 2000 Sep;10(3):340-59. Related Articles, Links
Effects of anabolic precursors on serum testosterone concentrations and adaptations to resistance training in young men.
Brown GA, Vukovich MD, Reifenrath TA, Uhl NL, Parsons KA, Sharp RL, King DS.
Exercise Biochemistry Laboratory, Department of Health and Human Performance, Iowa State University, Ames, IA 50011, USA.
The effects of androgen precursors, combined with herbal extracts designed to enhance testosterone formation and reduce conversion of androgens to estrogens was studied in young men. Subjects performed 3 days of resistance training per week for 8 weeks. Each day during Weeks 1, 2, 4, 5, 7, and 8, subjects consumed either placebo (PL; n = 10) or a supplement (ANDRO-6; n = 10), which contained daily doses of 300 mg androstenedione, 150 mg DHEA, 750 mg Tribulus terrestris, 625 mg Chrysin, 300 mg Indole-3-carbinol, and 540 mg Saw palmetto. Serum androstenedione concentrations were higher in ANDRO-6 after 2, 5, and 8 weeks (p <.05), while serum concentrations of free and total testosterone were unchanged in both groups. Serum estradiol was elevated at Weeks 2, 5, and 8 in ANDRO-6 (p <.05), and serum estrone was elevated at Weeks 5 and 8 (p <.05). Muscle strength increased (p <.05) similarly from Weeks 0 to 4, and again from Weeks 4 to 8 in both treatment groups. The acute effect of one third of the daily dose of ANDRO-6 and PL was studied in 10 men (23 +/- 4 years). Serum androstenedione concentrations were elevated (p <.05) in ANDRO-6 from 150 to 360 min after ingestion, while serum free or total testosterone concentrations were unchanged. These data provide evidence that the addition of these herbal extracts to androstenedione does not reduce the estrogenic effect of androstenedione, and does not augment the adaptations to resistance training.
--------------------------
Endocrine and Lipid Responses to Chronic Androstenediol-Herbal Supplementation in 30 to 58 Year Old Men
Gregory A. Brown, MS, Matthew D. Vukovich, PhD, Emily R. Martini, BS, Marian L. Kohut, PhD, Warren D. Franke, PhD, David A. Jackson, MS and Douglas S. King, PhD
Objective: The effectiveness of an androgenic nutritional supplement designed to enhance serum testosterone concentrations and prevent the formation of dihydrotestosterone and estrogen was investigated in healthy 30 to 58 year old men.
Design: Subjects were randomly assigned to consume a nutritional supplement (AND-HB) containing 300-mg androstenediol, 480-mg saw palmetto, 450-mg indole-3-carbinol, 300-mg chrysin, 1,500 mg gamma-linolenic acid and 1,350-mg Tribulus terrestris per day (n = 28), or placebo (n = 27) for 28 days. Subjects were stratified into age groups to represent the fourth (30 year olds, n = 20), fifth (40 year olds, n = 20) and sixth (50 year olds, n = 16) decades of life.
Measurements: Serum free testosterone, total testosterone, androstenedione, dihydrotestosterone, estradiol, prostate specific antigen and lipid concentrations were measured before supplementation and weekly for four weeks.
Results: Basal serum total testosterone, estradiol, and prostate specific antigen (PSA) concentrations were not different between age groups. Basal serum free testosterone concentrations were higher (p < 0.05) in the 30- (70.5 ± 3.6 pmol/L) than in the 50 year olds (50.8 ± 4.5 pmol/L). Basal serum androstenedione and dihydrotestosterone (DHT) concentrations were significantly higher in the 30- (for androstenedione and DHT, respectively, 10.4 ± 0.6 nmol/L and 2198.2 ± 166.5 pmol/L) than in the 40- (6.8 ± 0.5 nmol/L and 1736.8 ± 152.0 pmol/L) or 50 year olds (6.0 ± 0.7 nmol/L and 1983.7 ± 147.8 pmol/L). Basal serum hormone concentrations did not differ between the treatment groups. Serum concentrations of total testosterone and PSA were unchanged by supplementation. Ingestion of AND-HB resulted in increased (p < 0.05) serum androstenedione (174%), free testosterone (37%), DHT (57%) and estradiol (86%) throughout the four weeks. There was no relationship between the increases in serum free testosterone, androstenedione, DHT, or estradiol and age (r2 = 0.08, 0.03, 0.05 and 0.02, respectively). Serum HDL-C concentrations were reduced (p < 0.05) by 0.14 mmol/L in AND-HB.
Conclusions: These data indicate that ingestion of androstenediol combined with herbal products does not prevent the formation of estradiol and dihydrotestosterone.
-----------------------
Int J Vitam Nutr Res 2001 Sep;71(5):293-301 Related Articles, Links
Effects of androstenedione-herbal supplementation on serum sex hormone concentrations in 30- to 59-year-old men.
Brown GA, Vukovich MD, Martini ER, Kohut ML, Franke WD, Jackson DA, King DS.
Exercise Biochemistry Laboratory, Department of Health and Human Performance, Iowa State University, Ames, IA, USA.
The effectiveness of a nutritional supplement designed to enhance serum testosterone concentrations and prevent the formation of dihydrotestosterone and estrogens from the ingested androgens was investigated in healthy 30- to 59-year old men. Subjects were randomly assigned to consume DION (300 mg androstenedione, 150 mg dehydroepiandrosterone, 540 mg saw palmetto, 300 mg indole-3-carbinol, 625 mg chrysin, and 750 mg Tribulus terrestris per day; n = 28) or placebo (n = 27) for 28 days. Serum free testosterone, total testosterone, androstenedione, dihydrotestosterone, estradiol, prostate-specific antigen (PSA), and lipid concentrations were measured before and throughout the 4-week supplementation period. Serum concentrations of total testosterone and PSA were unchanged by supplementation. DION increased (p < 0.05) serum androstenedione (342%), free testosterone (38%), dihydrotestosterone (71%), and estradiol (103%) concentrations. Serum HDL-C concentrations were reduced by 5.0 mg/dL in DION (p < 0.05). Increases in serum free testosterone (r2 = 0.01), androstenedione (r2 = 0.01), dihydrotestosterone (r2 = 0.03), or estradiol (r2 = 0.07) concentrations in DION were not related to age. While the ingestion of androstenedione combined with herbal products increased serum free testosterone concentrations in older men, these herbal products did not prevent the conversion of ingested androstenedione to estradiol and dihydrotestosterone.
J Steroid Biochem Mol Biol. 2001 Sep;78(3):231-9. Related Articles, Links
No evidence for the in vivo activity of aromatase-inhibiting flavonoids.
Saarinen N, Joshi SC, Ahotupa M, Li X, Ammala J, Makela S, Santti R.
Institute of Biomedicine, University of Turku, Kiinamyllynkatu 10, FIN-20520, Turku, Finland.
Measurements of the aromatase-inhibiting and antioxidative capacities of flavonoids in vitro showed that slight changes in flavonoid structure may result in marked changes in biological activity. Several flavonoids such as 7-hydroxyflavone and chrysin (5,7-dihydroxyflavone) were shown to inhibit the formation of 3H-17beta-estradiol from 3H-androstenedione (IC(50)<1.0 microM) in human choriocarcinoma JEG-3 cells and in human embryonic kidney cells HEK 293 transfected with human aromatase gene (Arom+HEK 293). Flavone and quercetin (3,3',4',5,7-pentahydroxyflavone) showed no inhibition (IC(50)>100 microM). None of the requirements for optimal antioxidative capacity (2,3-double bond with 4'-hydroxy group, 3-hydroxyl group, 5,7-dihydroxy structure and the orthodihydroxy structure in the B-ring) is relevant for the maximum inhibition of aromatase by flavonoids. After oral administration to immature rats at a dose of 50 mg/kg body weight, which considerably exceeds amounts found in daily human diets, neither aromatase-inhibiting nonestrogenic flavonoids, such as chrysin, nor estrogenic flavonoids, such as naringenin and apigenin, induced uterine growth or reduced estrogen- or androgen-induced uterine growth. The inability of flavonoids to inhibit aromatase and, consequently, uterine growth in short-term tests may be due to their relatively poor absorption and/or bioavailability
----------------------------
Int J Sport Nutr Exerc Metab. 2000 Sep;10(3):340-59. Related Articles, Links
Effects of anabolic precursors on serum testosterone concentrations and adaptations to resistance training in young men.
Brown GA, Vukovich MD, Reifenrath TA, Uhl NL, Parsons KA, Sharp RL, King DS.
Exercise Biochemistry Laboratory, Department of Health and Human Performance, Iowa State University, Ames, IA 50011, USA.
The effects of androgen precursors, combined with herbal extracts designed to enhance testosterone formation and reduce conversion of androgens to estrogens was studied in young men. Subjects performed 3 days of resistance training per week for 8 weeks. Each day during Weeks 1, 2, 4, 5, 7, and 8, subjects consumed either placebo (PL; n = 10) or a supplement (ANDRO-6; n = 10), which contained daily doses of 300 mg androstenedione, 150 mg DHEA, 750 mg Tribulus terrestris, 625 mg Chrysin, 300 mg Indole-3-carbinol, and 540 mg Saw palmetto. Serum androstenedione concentrations were higher in ANDRO-6 after 2, 5, and 8 weeks (p <.05), while serum concentrations of free and total testosterone were unchanged in both groups. Serum estradiol was elevated at Weeks 2, 5, and 8 in ANDRO-6 (p <.05), and serum estrone was elevated at Weeks 5 and 8 (p <.05). Muscle strength increased (p <.05) similarly from Weeks 0 to 4, and again from Weeks 4 to 8 in both treatment groups. The acute effect of one third of the daily dose of ANDRO-6 and PL was studied in 10 men (23 +/- 4 years). Serum androstenedione concentrations were elevated (p <.05) in ANDRO-6 from 150 to 360 min after ingestion, while serum free or total testosterone concentrations were unchanged. These data provide evidence that the addition of these herbal extracts to androstenedione does not reduce the estrogenic effect of androstenedione, and does not augment the adaptations to resistance training.
--------------------------
Endocrine and Lipid Responses to Chronic Androstenediol-Herbal Supplementation in 30 to 58 Year Old Men
Gregory A. Brown, MS, Matthew D. Vukovich, PhD, Emily R. Martini, BS, Marian L. Kohut, PhD, Warren D. Franke, PhD, David A. Jackson, MS and Douglas S. King, PhD
Objective: The effectiveness of an androgenic nutritional supplement designed to enhance serum testosterone concentrations and prevent the formation of dihydrotestosterone and estrogen was investigated in healthy 30 to 58 year old men.
Design: Subjects were randomly assigned to consume a nutritional supplement (AND-HB) containing 300-mg androstenediol, 480-mg saw palmetto, 450-mg indole-3-carbinol, 300-mg chrysin, 1,500 mg gamma-linolenic acid and 1,350-mg Tribulus terrestris per day (n = 28), or placebo (n = 27) for 28 days. Subjects were stratified into age groups to represent the fourth (30 year olds, n = 20), fifth (40 year olds, n = 20) and sixth (50 year olds, n = 16) decades of life.
Measurements: Serum free testosterone, total testosterone, androstenedione, dihydrotestosterone, estradiol, prostate specific antigen and lipid concentrations were measured before supplementation and weekly for four weeks.
Results: Basal serum total testosterone, estradiol, and prostate specific antigen (PSA) concentrations were not different between age groups. Basal serum free testosterone concentrations were higher (p < 0.05) in the 30- (70.5 ± 3.6 pmol/L) than in the 50 year olds (50.8 ± 4.5 pmol/L). Basal serum androstenedione and dihydrotestosterone (DHT) concentrations were significantly higher in the 30- (for androstenedione and DHT, respectively, 10.4 ± 0.6 nmol/L and 2198.2 ± 166.5 pmol/L) than in the 40- (6.8 ± 0.5 nmol/L and 1736.8 ± 152.0 pmol/L) or 50 year olds (6.0 ± 0.7 nmol/L and 1983.7 ± 147.8 pmol/L). Basal serum hormone concentrations did not differ between the treatment groups. Serum concentrations of total testosterone and PSA were unchanged by supplementation. Ingestion of AND-HB resulted in increased (p < 0.05) serum androstenedione (174%), free testosterone (37%), DHT (57%) and estradiol (86%) throughout the four weeks. There was no relationship between the increases in serum free testosterone, androstenedione, DHT, or estradiol and age (r2 = 0.08, 0.03, 0.05 and 0.02, respectively). Serum HDL-C concentrations were reduced (p < 0.05) by 0.14 mmol/L in AND-HB.
Conclusions: These data indicate that ingestion of androstenediol combined with herbal products does not prevent the formation of estradiol and dihydrotestosterone.
-----------------------
Int J Vitam Nutr Res 2001 Sep;71(5):293-301 Related Articles, Links
Effects of androstenedione-herbal supplementation on serum sex hormone concentrations in 30- to 59-year-old men.
Brown GA, Vukovich MD, Martini ER, Kohut ML, Franke WD, Jackson DA, King DS.
Exercise Biochemistry Laboratory, Department of Health and Human Performance, Iowa State University, Ames, IA, USA.
The effectiveness of a nutritional supplement designed to enhance serum testosterone concentrations and prevent the formation of dihydrotestosterone and estrogens from the ingested androgens was investigated in healthy 30- to 59-year old men. Subjects were randomly assigned to consume DION (300 mg androstenedione, 150 mg dehydroepiandrosterone, 540 mg saw palmetto, 300 mg indole-3-carbinol, 625 mg chrysin, and 750 mg Tribulus terrestris per day; n = 28) or placebo (n = 27) for 28 days. Serum free testosterone, total testosterone, androstenedione, dihydrotestosterone, estradiol, prostate-specific antigen (PSA), and lipid concentrations were measured before and throughout the 4-week supplementation period. Serum concentrations of total testosterone and PSA were unchanged by supplementation. DION increased (p < 0.05) serum androstenedione (342%), free testosterone (38%), dihydrotestosterone (71%), and estradiol (103%) concentrations. Serum HDL-C concentrations were reduced by 5.0 mg/dL in DION (p < 0.05). Increases in serum free testosterone (r2 = 0.01), androstenedione (r2 = 0.01), dihydrotestosterone (r2 = 0.03), or estradiol (r2 = 0.07) concentrations in DION were not related to age. While the ingestion of androstenedione combined with herbal products increased serum free testosterone concentrations in older men, these herbal products did not prevent the conversion of ingested androstenedione to estradiol and dihydrotestosterone.
Last edited by a moderator:
Nelson Montana
Community Veteran, Bodybuilding Author
Well, there are always studies that show opposing conclusions and there are studies showing the effectiveness as well. But let's look at the ones presented.
The first study was done in vitro. And with an insufficient amount. And without bioperine to improve absorbtion. So basically, the study is invalid since was not conducted with the proper dosage or under real world circumstances.
The other studies were all done using chrysin IN CONJUNCTION WITH ANDROSTEINE!!! Now, everyone knows that androsteine significantly raises estrogen so how can they possible make an evaluation? That's like taking Arimidex with a bith control pill and saying that e levels weren't lowered much. Of course not! You're raising it at the same time.
In the third study DIM was also used. DIM acts as a mild estrogen.
This is yet another example of how poorly some studies are conducted. The conclusions are useless. Just because someone did a study doesn't mean they came up with the right conclusion. In this case, it's a no-brainer.
The first study was done in vitro. And with an insufficient amount. And without bioperine to improve absorbtion. So basically, the study is invalid since was not conducted with the proper dosage or under real world circumstances.
The other studies were all done using chrysin IN CONJUNCTION WITH ANDROSTEINE!!! Now, everyone knows that androsteine significantly raises estrogen so how can they possible make an evaluation? That's like taking Arimidex with a bith control pill and saying that e levels weren't lowered much. Of course not! You're raising it at the same time.
In the third study DIM was also used. DIM acts as a mild estrogen.
This is yet another example of how poorly some studies are conducted. The conclusions are useless. Just because someone did a study doesn't mean they came up with the right conclusion. In this case, it's a no-brainer.
hhajdo
Community Veteran
The first sudy was done in vivo, Chrysin is effective in vitro but it doesn't work in vivo probably due to low oral BV.
The studies in which Chrysin was used with andro show that it's not able to attenuate the aromatization of andro to E.
( they compared the results to some previous research in which andro was administered alone), so the conclusion is definitely not useless, and is in agreement with previous research which shows that it's not effective in vivo...
Indole-3-carbinol carbinol is supposed to inhibit aromatization and enhance estrogen clearance...
The studies in which Chrysin was used with andro show that it's not able to attenuate the aromatization of andro to E.
( they compared the results to some previous research in which andro was administered alone), so the conclusion is definitely not useless, and is in agreement with previous research which shows that it's not effective in vivo...
Indole-3-carbinol carbinol is supposed to inhibit aromatization and enhance estrogen clearance...
hhajdo
Community Veteran
Here's an article about it by Pat Arnold with a few additional references:
The Sad Truth About Chrysin
by Pat Arnold
Flavonoids are a group of compounds widely distributed in plants which have a characteristic molecular structure. They have been found to have many beneficial activities, such as anti-inflammatory and anti-carcinogenic properties. Lucky for us, an average human diet contains about 1g/day of these healthy substances.
Certain flavones have generated considerable interest in the bodybuilding community. This is because they have been found to have the ability to prevent the conversion of androgens to estrogen by inhibiting an enzyme called aromatase. Obviously, any compound which could potentially decrease the peripheral synthesis of estrogen has the potential to be a powerful bodybuilding tool.
The flavonoid which has created the greatest publicity is chrysin (5,7-dihydroxyflavone). Chrysin has several studies supporting its in vitro aromatase inhibitory activity. The first of these studies was done in 1984 using placental microsomes.(1) They found that chrysin had significant aromatase inhibitory activity, which could lead to a decrease in estrogen. As great as this sounds, its important to note that this is a study which was done in a petri dish, and not in an animal. Therefore, more research would need to be done to figure out if chrysin would work in real life.
To create a system which more closely mimicked a 220-lb bodybuilder, researchers used preadipocytes, which is a fancy term for young fat cells. They introduced the flavonoids into the medium surrounding the cells, and assayed for estrogen. This time, chrysin’s activity was reduced 10-fold, presumably because the chrysin could not effectively enter the cells.(2) Thus, these researchers discovered the first barrier to the possibility of chrysin working in an animal system.
However, not all hope was lost...yet. The obvious next question in chrysin’s effectiveness is: Can chrysin reduce estrogen in an animal model? Can estrogen be stopped with an easily available over-the-counter food supplement?
Our last group of researchers decided to stop fooling around and administer chrysin to mice both orally and via injection to see if chrysin effectively reduced serum estrogen levels. They had 10 mice in 4 groups: one receiving nothing, one taking chrysin orally at 5mg/kg, one receiving an intraperitoneal injection with the vehicle solution only, and one receiving chrysin at 5mg/kg in the vehicle solution via an intraperitoneal injection. The mice received the appropriate intervention for 30 days, and then blood samples were drawn. A radio immunoassay kit was then used to determine serum estrogen levels.
Guess what? They found that estrogen levels were the SAME in ALL of the groups.(3)
What went wrong? How can chrysin work in a petri dish, but not in an animal? We can only hypothesize, but it is easy to imagine that somewhere between chrysin being absorbed intact, reaching the cell without being metabolized, entering the cell (chrysin’s poor solubility could affect this), and inhibiting aromatase, that something could, and does, go wrong.
Another upsetting finding from this study was the chrysin treated rats were noticeably FATTER than the controls. How could this be? One possibility is that the chrysin disrupted thyroid function. T4 to T3 conversion (a key step in thyroid hormone metabolism) is controlled by an enzyme called deiodinase and this enzyme has been shown to be inhibited by chrysin.(4) Another possibility is an inhibition in testosterone production through disruption of 17beta-hydroxysteroid dehydrogenase (another enzyme shown to be disrupted by chrysin).(5) Why these two enzyme systems would be affected, but not aromatase, would be strange
Other flavonoids might show more promise than chrysin. One of these is simple flavone. It is the simplest of flavones, as it has no chemical groups coming off its three ring basic structure. In some of the studies examining aromatase inhibition, flavone has assayed out quite favorably, although in a couple it strangely did not. Why I think flavone might perform OK in-vivo is largely due to the fact that it has much better solubility properties than chrysin does. For instance, in my lab it took about 1000 milliliters of methanol to dissolve only one gram of chrysin, while one gram of flavone dissolved in 50 milliliters or less. This good solubility would allow it to be absorbed well through the gut and also to enter cells with greater ease.
Another possible advantage of flavone deals with its metabolism in the liver. Unlike other flavonoids which can have their free hydroxyl groups conjugated, which deactivates them, flavone has no hydroxyl groups and so cannot suffer the same fate. Actually, flavone can be hydroxylated and then undergo this conjugation, but we are talking two steps and that means it would not be nearly as immediate as it is with the hydroxylated flavonoids. This immunity to immediate deactivation could extend the half-life and increase the amount of flavone that gets to the target sites in the body.
Flavone also has not been shown to be a strong inhibitor of 5’ deiodinase or 17beta-hydroxysteroid dehydrogenase. As a result, thyroid action and testosterone production should not be significantly altered.
I have to emphasize that this all must be put into perspective. Most of you probably do not know the story of chrysin in the sports supplement market. What happened was back in ’95 I unearthed the research on flavonoids and aromatase (including chrysin) and compiled a review on the subject for the supplement industry. I introduced the concept of chrysin as an estrogen modulator and possible testosterone enhancer to a major supplement company. I also told my friend Dan Duchaine about it. However the one thing I was totally adamant about was that NO ONE should think about selling it until in-vivo (live human being) tests had proven that the theory panned out in the real world.
Unfortunately the chrysin thing soon left my hands and the hype from the "scientifically unconcerned" supplement industry took control. MM2K wrote an article by Duchaine which unjustifiably made the compound sound more proven to work than it really was, and every company under the sun looked for a chrysin source. One company even started selling a fake chrysin (you know who you are)! Consumers for the most part knew no better and bought up the chrysin (fake and real) with fervor. If you were one of those people, after reading this article you are probably thinking you would have been better off if it was the fake brand you bought!
Now that you guys have learned your lesson with chrysin (I hope), please don’t make the same mistake with flavone. Although it seems much more promising than chrysin, we still don’t know if it works in humans at all, or even if it has undesirable effects. I have no intentions of selling flavone (or testing it), but I am sure there will be someone who will market it based only on this article. I think there are much better candidates for supplemental anti-estrogens that are not flavonoids. Of course, if you don’t mind being a guinea pig and trying flavone then that is your decision. But if you end up getting fat like those poor sacrificial rats don’t come crying to me!
References:
1. Kellis, JT and Vickery, LE: Inhibition of Human Estrogen Synthetase (Aromatase) by Flavones. Science 225 (1984) 1032-34.
2. Campbell, DR and Kurzer, MS: Flavonoid Inhibition of Aromatase Enzyme Activity in Human Preadipocytes. Journal of Steroid Biochemistry and Molecular Biology 46 (1993) 381-388.
3. Shibayama, J, et al. The Oral Bioavailability and In Vivo Activity of Chrysin in Exercising and Non-Exercising Mice Submitted for publication.
4. Koehrle, J, et.al. Iodothyronine deiodinase is inhibited by plant flavonoids, Prog Clin Biol Res 213 (1986) 359-371
5. Le Bail, J.C., et.al. Aromatase and 17beta-hydroxysteroid dehydrogenase inhibition by flavonoids, Cancer Letters, 133 (1998) 101-106
The Sad Truth About Chrysin
by Pat Arnold
Flavonoids are a group of compounds widely distributed in plants which have a characteristic molecular structure. They have been found to have many beneficial activities, such as anti-inflammatory and anti-carcinogenic properties. Lucky for us, an average human diet contains about 1g/day of these healthy substances.
Certain flavones have generated considerable interest in the bodybuilding community. This is because they have been found to have the ability to prevent the conversion of androgens to estrogen by inhibiting an enzyme called aromatase. Obviously, any compound which could potentially decrease the peripheral synthesis of estrogen has the potential to be a powerful bodybuilding tool.
The flavonoid which has created the greatest publicity is chrysin (5,7-dihydroxyflavone). Chrysin has several studies supporting its in vitro aromatase inhibitory activity. The first of these studies was done in 1984 using placental microsomes.(1) They found that chrysin had significant aromatase inhibitory activity, which could lead to a decrease in estrogen. As great as this sounds, its important to note that this is a study which was done in a petri dish, and not in an animal. Therefore, more research would need to be done to figure out if chrysin would work in real life.
To create a system which more closely mimicked a 220-lb bodybuilder, researchers used preadipocytes, which is a fancy term for young fat cells. They introduced the flavonoids into the medium surrounding the cells, and assayed for estrogen. This time, chrysin’s activity was reduced 10-fold, presumably because the chrysin could not effectively enter the cells.(2) Thus, these researchers discovered the first barrier to the possibility of chrysin working in an animal system.
However, not all hope was lost...yet. The obvious next question in chrysin’s effectiveness is: Can chrysin reduce estrogen in an animal model? Can estrogen be stopped with an easily available over-the-counter food supplement?
Our last group of researchers decided to stop fooling around and administer chrysin to mice both orally and via injection to see if chrysin effectively reduced serum estrogen levels. They had 10 mice in 4 groups: one receiving nothing, one taking chrysin orally at 5mg/kg, one receiving an intraperitoneal injection with the vehicle solution only, and one receiving chrysin at 5mg/kg in the vehicle solution via an intraperitoneal injection. The mice received the appropriate intervention for 30 days, and then blood samples were drawn. A radio immunoassay kit was then used to determine serum estrogen levels.
Guess what? They found that estrogen levels were the SAME in ALL of the groups.(3)
What went wrong? How can chrysin work in a petri dish, but not in an animal? We can only hypothesize, but it is easy to imagine that somewhere between chrysin being absorbed intact, reaching the cell without being metabolized, entering the cell (chrysin’s poor solubility could affect this), and inhibiting aromatase, that something could, and does, go wrong.
Another upsetting finding from this study was the chrysin treated rats were noticeably FATTER than the controls. How could this be? One possibility is that the chrysin disrupted thyroid function. T4 to T3 conversion (a key step in thyroid hormone metabolism) is controlled by an enzyme called deiodinase and this enzyme has been shown to be inhibited by chrysin.(4) Another possibility is an inhibition in testosterone production through disruption of 17beta-hydroxysteroid dehydrogenase (another enzyme shown to be disrupted by chrysin).(5) Why these two enzyme systems would be affected, but not aromatase, would be strange
Other flavonoids might show more promise than chrysin. One of these is simple flavone. It is the simplest of flavones, as it has no chemical groups coming off its three ring basic structure. In some of the studies examining aromatase inhibition, flavone has assayed out quite favorably, although in a couple it strangely did not. Why I think flavone might perform OK in-vivo is largely due to the fact that it has much better solubility properties than chrysin does. For instance, in my lab it took about 1000 milliliters of methanol to dissolve only one gram of chrysin, while one gram of flavone dissolved in 50 milliliters or less. This good solubility would allow it to be absorbed well through the gut and also to enter cells with greater ease.
Another possible advantage of flavone deals with its metabolism in the liver. Unlike other flavonoids which can have their free hydroxyl groups conjugated, which deactivates them, flavone has no hydroxyl groups and so cannot suffer the same fate. Actually, flavone can be hydroxylated and then undergo this conjugation, but we are talking two steps and that means it would not be nearly as immediate as it is with the hydroxylated flavonoids. This immunity to immediate deactivation could extend the half-life and increase the amount of flavone that gets to the target sites in the body.
Flavone also has not been shown to be a strong inhibitor of 5’ deiodinase or 17beta-hydroxysteroid dehydrogenase. As a result, thyroid action and testosterone production should not be significantly altered.
I have to emphasize that this all must be put into perspective. Most of you probably do not know the story of chrysin in the sports supplement market. What happened was back in ’95 I unearthed the research on flavonoids and aromatase (including chrysin) and compiled a review on the subject for the supplement industry. I introduced the concept of chrysin as an estrogen modulator and possible testosterone enhancer to a major supplement company. I also told my friend Dan Duchaine about it. However the one thing I was totally adamant about was that NO ONE should think about selling it until in-vivo (live human being) tests had proven that the theory panned out in the real world.
Unfortunately the chrysin thing soon left my hands and the hype from the "scientifically unconcerned" supplement industry took control. MM2K wrote an article by Duchaine which unjustifiably made the compound sound more proven to work than it really was, and every company under the sun looked for a chrysin source. One company even started selling a fake chrysin (you know who you are)! Consumers for the most part knew no better and bought up the chrysin (fake and real) with fervor. If you were one of those people, after reading this article you are probably thinking you would have been better off if it was the fake brand you bought!
Now that you guys have learned your lesson with chrysin (I hope), please don’t make the same mistake with flavone. Although it seems much more promising than chrysin, we still don’t know if it works in humans at all, or even if it has undesirable effects. I have no intentions of selling flavone (or testing it), but I am sure there will be someone who will market it based only on this article. I think there are much better candidates for supplemental anti-estrogens that are not flavonoids. Of course, if you don’t mind being a guinea pig and trying flavone then that is your decision. But if you end up getting fat like those poor sacrificial rats don’t come crying to me!
References:
1. Kellis, JT and Vickery, LE: Inhibition of Human Estrogen Synthetase (Aromatase) by Flavones. Science 225 (1984) 1032-34.
2. Campbell, DR and Kurzer, MS: Flavonoid Inhibition of Aromatase Enzyme Activity in Human Preadipocytes. Journal of Steroid Biochemistry and Molecular Biology 46 (1993) 381-388.
3. Shibayama, J, et al. The Oral Bioavailability and In Vivo Activity of Chrysin in Exercising and Non-Exercising Mice Submitted for publication.
4. Koehrle, J, et.al. Iodothyronine deiodinase is inhibited by plant flavonoids, Prog Clin Biol Res 213 (1986) 359-371
5. Le Bail, J.C., et.al. Aromatase and 17beta-hydroxysteroid dehydrogenase inhibition by flavonoids, Cancer Letters, 133 (1998) 101-106
Nelson Montana
Community Veteran, Bodybuilding Author
Pat Arnold sells 6OXO which has been shown to be comparable to Chrysin but 5X's the price. Take it for what it's worth. Also, he claims that 6OXO increases testosterone over 200% yet there isn't one shread of proof that it increases testosterone even 1 %. Take that for what it's worth too.
The bioavailability of Chrysin has been a factor and the addition of Bioperine has shown to improve it.
The bioavailability of Chrysin has been a factor and the addition of Bioperine has shown to improve it.
Y
YellowJacket
Guest
Nice work hhajdo.....
Nelson Montana
Community Veteran, Bodybuilding Author
hhajdo: I know you're the king of posting studies. I'm surprised you couldn't find one thatshowed Bioperine increased the effectiveness of Chrysin. Several exist. Can you post something that concurs with your statement that it lowers testosterone? Never heard that one before.
Yellow jacket will agree with anything that disagrees with me. That's the way it is with teenage experts. They're still ignorant enough to think they know everything.
Yellow jacket will agree with anything that disagrees with me. That's the way it is with teenage experts. They're still ignorant enough to think they know everything.
Y
YellowJacket
Guest
..
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Nelson Montana
Community Veteran, Bodybuilding Author
YellowJacket said:
AND he thinks only he is entitled to an opinion while others who have actually accomplished something are dubasses. After all, his credentials ARE impressive. He has a gym membership and a computer.
Y
YellowJacket
Guest
Nelson Montana said:
I guess I could write a book full of useless opinions and then self-proclaim myself as a 'bodybuilding guru'.
Nelson Montana
Community Veteran, Bodybuilding Author
YellowJacket said:
You can certainly try. Until that time....ssssh.
You know, it's nice to have people like Dave Draper, and Dr. Eric Serrano and Rick Collins endorsing my books, but I think there's no better evaluation than the fact that the staunchest criticisms always come from someone who never actuallly read them. That says it all.
hhajdo
Community Veteran
It doesn't lower gonadotropins, it can act directly on testis :
J Ethnopharmacol. 1999 Mar;64(3):219-25. Related Articles, Links
Effects of piperine on testis of albino rats.
Malini T, Manimaran RR, Arunakaran J, Aruldhas MM, Govindarajulu P.
Department of Endocrinology, Dr ALM Post Graduate Institute of Basic Medical Sciences, Taramani, Madras, India.
Piperine was administered to mature male albino rats at doses of 5 and 10 mg/kg body weight, p.o., respectively, for 30 days. Only a 10 mg dose of piperine treatment caused a significant reduction in the weights of testis and accessory sex organs. Histological studies revealed that piperine at a 5 mg dose caused partial degeneration of germ cell types, whereas at a 10 mg dose, it caused severe damage to the seminiferous tubule, decrease in seminiferous tubular and Leydig cell nuclear diameter and desquamation of spermatocytes and spermatids. Correlated to the structural changes, a fall in caput and cauda epididymal sperm concentrations was also evident....
--------------------
Thyroid:
: Horm Metab Res. 2003 Sep;35(9):523-6. Related Articles, Links
Piperine lowers the serum concentrations of thyroid hormones, glucose and hepatic 5'D activity in adult male mice.
Panda S, Kar A.
School of Life Sciences, Devi Ahilya University, Indore, India.
Piperine, the main alkaloid of Piper nigrum fruits, was evaluated for its thyroid hormone and glucose regulatory efficacy in adult male Swiss albino mice. Its daily oral administration (2.50 mg/kg) for 15 days lowered the serum levels of both the thyroid hormones, thyroxin (T (4)) and triiodothyronine (T (3)) as well as glucose concentrations with a concomitant decrease in hepatic 5'D enzyme and glucose-6-phospatase (G-6-Pase) activity. However, no significant alterations were observed in animals treated with 0.25 mg/kg of piperine in any of the activities studied except an inhibition in serum T (3) concentration. The decrease in T (4), T (3) concentrations and in G-6-Pase were comparable to that of a standard antithyroid drug, Proylthiouracil (PTU). The hepatic lipid-peroxidation (LPO) and the activity of endogenous antioxidants, superoxide dismutase (SOD), and catalase (CAT) were not significantly altered in either of the doses. It appears that the action of P. nigrum on thyroid functions is mediated through its active alkaloid, piperine. We also suggest that a higher dose of piperine may inhibit thyroid function and serum glucose concentration in euthyroid individuals.
J Ethnopharmacol. 1999 Mar;64(3):219-25. Related Articles, Links
Effects of piperine on testis of albino rats.
Malini T, Manimaran RR, Arunakaran J, Aruldhas MM, Govindarajulu P.
Department of Endocrinology, Dr ALM Post Graduate Institute of Basic Medical Sciences, Taramani, Madras, India.
Piperine was administered to mature male albino rats at doses of 5 and 10 mg/kg body weight, p.o., respectively, for 30 days. Only a 10 mg dose of piperine treatment caused a significant reduction in the weights of testis and accessory sex organs. Histological studies revealed that piperine at a 5 mg dose caused partial degeneration of germ cell types, whereas at a 10 mg dose, it caused severe damage to the seminiferous tubule, decrease in seminiferous tubular and Leydig cell nuclear diameter and desquamation of spermatocytes and spermatids. Correlated to the structural changes, a fall in caput and cauda epididymal sperm concentrations was also evident....
--------------------
Thyroid:
: Horm Metab Res. 2003 Sep;35(9):523-6. Related Articles, Links
Piperine lowers the serum concentrations of thyroid hormones, glucose and hepatic 5'D activity in adult male mice.
Panda S, Kar A.
School of Life Sciences, Devi Ahilya University, Indore, India.
Piperine, the main alkaloid of Piper nigrum fruits, was evaluated for its thyroid hormone and glucose regulatory efficacy in adult male Swiss albino mice. Its daily oral administration (2.50 mg/kg) for 15 days lowered the serum levels of both the thyroid hormones, thyroxin (T (4)) and triiodothyronine (T (3)) as well as glucose concentrations with a concomitant decrease in hepatic 5'D enzyme and glucose-6-phospatase (G-6-Pase) activity. However, no significant alterations were observed in animals treated with 0.25 mg/kg of piperine in any of the activities studied except an inhibition in serum T (3) concentration. The decrease in T (4), T (3) concentrations and in G-6-Pase were comparable to that of a standard antithyroid drug, Proylthiouracil (PTU). The hepatic lipid-peroxidation (LPO) and the activity of endogenous antioxidants, superoxide dismutase (SOD), and catalase (CAT) were not significantly altered in either of the doses. It appears that the action of P. nigrum on thyroid functions is mediated through its active alkaloid, piperine. We also suggest that a higher dose of piperine may inhibit thyroid function and serum glucose concentration in euthyroid individuals.
Nelson Montana
Community Veteran, Bodybuilding Author
hhajdo said:
10 mgs on a MOUSE?! Fuck, I think 10 mgs of anything will have a negitive effect on just about anything on a mouse.
School of "Life Sciences" in India, eh? Hmmm: rolleyes:
