Something I didn't know about Chrysin

[Big Johnson]

Passiflora Coerulea, also known as Chrysin. This naturally occurring compound is a potent inhibitor of aromatase, the enzyme that converts testosterone to the particular estrogen- estradiol (believed to be "bad" estrogen). Passiflora Coerulea also has a direct effect on the neuro-receptors of the brain creating a calming effect. The beneficial effects of this phytonutrient are not seen when it is taken orally, as its potency is destroyed by the digestive process.

Time to break out the DMSO.

Hmmm...I wonder if you could add chrysin to your fina kit?

Hmmm...

 

[swoldier]

chrysin is crap and that is all I got say about that

 

[Big Johnson]

You are right, swol:

by Pat Arnold
[email protected]

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!

 

[JP@Ironology]

chrysin is crap and that is all I got say about that

Yep.