Suppression of rat and human androgen biosynthetic enzymes by apigenin

[mrseb]

Hello,

apigenin is often said to increase testosterone by increasing STAR protein activity and blocking COX2 in the testes. But this study that apigenin blocks androgen-producing enzymes.

What do you think about that ? have you had feedback after supplementation... there are now liposomal forms...

Suppression of rat and human androgen biosynthetic enzymes by apigenin: Possible use for the treatment of prostate cancer - PubMed

Suppression of rat and human androgen biosynthetic enzymes by apigenin: Possible use for the treatment of prostate cancer​

Abstract​

Apigenin is a natural flavone. It has recently been used as a chemopreventive agent. It may also have some beneficial effects to treat prostate cancer by inhibiting androgen production. The objective of the present study was to investigate the effects of apigenin on the steroidogenesis of rat immature Leydig cells and some human testosterone biosynthetic enzyme activities. Rat immature Leydig cells were incubated for 3h with 100μM apigenin without (basal) or with 1ng/ml luteinizing hormone (LH), 10mM 8-bromoadenosine 3',5'-cyclic monophosphate (8BR), and 20μM of the following steroid substrates: 22R-hydroxychloesterol (22R), pregnenolone (P5), progesterone (P4), and androstenedione (D4). The medium levels of 5α-androstane-3α, 17β-diol (DIOL), the primary androgen produced by rat immature Leydig cells, were measured. Apigenin significantly inhibited basal, 8BR, 22R, PREG, P4, and D4 stimulated DIOL production in rat immature Leydig cells. Further study showed that apigenin inhibited rat 3β-hydroxysteroid dehydrogenase, 17α-hydroxylase/17, 20-lyase, and 17β-hydroxysteroid dehydrogenase 3 with IC50 values of 11.41±0.7, 8.98±0.10, and 9.37±0.07μM, respectively. Apigenin inhibited human 3β-hydroxysteroid dehydrogenase and 17β-hydroxysteroid dehydrogenase 3 with IC50 values of 2.17±0.04 and 1.31±0.09μM, respectively. Apigenin is a potent inhibitor of rat and human steroidogenic enzymes, being possible use for the treatment of prostate cancer.

 

[Hans]

Hello,

apigenin is often said to increase testosterone by increasing STAR protein activity and blocking COX2 in the testes. But this study that apigenin blocks androgen-producing enzymes.

What do you think about that ? have you had feedback after supplementation... there are now liposomal forms...

Suppression of rat and human androgen biosynthetic enzymes by apigenin: Possible use for the treatment of prostate cancer - PubMed

It's most likely due to a dose-dependent effect.
This study found that 10μM apigenin boosted progesterone and testosterone production.
The study you listed used 100μM apigenin.
Another example of an inverse effect is flavonoids' anti-estrogenic effect. In smaller doses they are anti-estrogenic, but in larger doses, they are estrogenic.
But it's almost highly unlikely that such high concentrations (100μM) will ever be reached in the testes unless someone takes massive amounts of apigenin or applies it directly to the testes.

 

[LeeLemonoil]

cells incubated with a high concentration - enzyme inhibition mostly always the result. I don’t think it bears any real world significance

 

[mrseb]

It's most likely due to a dose-dependent effect.
This study found that 10μM apigenin boosted progesterone and testosterone production.
The study you listed used 100μM apigenin.
Another example of an inverse effect is flavonoids' anti-estrogenic effect. In smaller doses they are anti-estrogenic, but in larger doses, they are estrogenic.
But it's almost highly unlikely that such high concentrations (100μM) will ever be reached in the testes unless someone takes massive amounts of apigenin or applies it directly to the testes.

Thank you Hans, I am currently taking a liposomal apigenin supplement dosed at 200mg per capsule so very absorbable, do you think this dose could cause a concentration of 100uM?

 

[SaltiestSardine]

Apigenin has pretty awful absorption as a supplement. I think i remember reading it was about 7%, liposomal is not likely to increase it by that by much or probably not much at all if its just apigenin suspended in a lipid like lecithin(doesn't make it a true liposome but wont stop people marketing them as such)

You'd never be able to get this amount of apigenin unless you drank 20-30 cups of chamomile tea throughout the day(was about 12% absorption i think) and you certainly wont get it through powdered supplements (they showed virtually no absorption of apigenin at all)

 

[mrseb]

Apigenin has pretty awful absorption as a supplement. I think i remember reading it was about 7%, liposomal is not likely to increase it by that by much or probably not much at all if its just apigenin suspended in a lipid like lecithin(doesn't make it a true liposome but wont stop people marketing them as such)

You'd never be able to get this amount of apigenin unless you drank 20-30 cups of chamomile tea throughout the day(was about 12% absorption i think) and you certainly wont get it through powdered supplements (they showed virtually no absorption of apigenin at all)

Here is the supplement I use:

Apigenin Pro Liposomal, 200mg

IMPROVED ABSORPTION with New Liposomal Formula: to maximize absorption*, we formulated a unique liposomal blend that includes phospholipids from organic sunflower lecithin & chitosan, to promote the formation of neutrally charged liposomes (LongLifeLipoTech™)

A major approach known to maximize bio-availability of natural compounds is the phospholipid-based formulation. Such formulations are known as liposomal formulations and commercially, they come as liquid emulsions or solid formulations promoting the formation of liposomal structures (bubble-like structures surrounded by a fat-based layer) that can encapsulate the active ingredients such as Apigenin. This phospholipid layer is similar to the cell walls in our body. As a result, liposomes are well received by the body and absorbed in higher quantities by the body, to reach the blood stream.


While liposomal formulations are a great way to deliver increased amount of supplements and drugs to the blood stream, when turning these into products, it leads to various disadvantages for the users. Liposomal products are liquid, heavy and difficult to carry. They have difficult taste. Making their taste better may come with various undesired additives. And typically they have short shelf life, even shorter after the bottle is open. Furthermore, liquid liposomal products need to stay stored at low temperature.


In contrast to the liquid liposomal supplements, liposomal promoting formulations as dry powder in capsules have no taste, they are easy to carry, and they can be stored at room temperature with a long shelf life. The quality is therefore even better since the product is more stable.


Furthermore, phospholipids can be negatively or positively charged leading to a lower absorption and time to circulate in the blood stream, compared to neutrally charged liposomes. In order to address this and further maximize the absorption, our Pro Liposomal formula includes LongLifeLipoTech™

 

[golder]

Does anyone know what a serving of Georgi’s Melanon equates to? Wanted to know if that goes above the 100uM threshold?

 

[SaltiestSardine]

Here is the supplement I use:

Apigenin Pro Liposomal, 200mg

This doesn't tell you anything. You need to contact them and ask them what the size of their liposomes are, and if they don't know, or wont tell you, then you have your answer

Anything above 200 nm isn't a true liposome

 

[Hans]

Thank you Hans, I am currently taking a liposomal apigenin supplement dosed at 200mg per capsule so very absorbable, do you think this dose could cause a concentration of 100uM?

Blood and urine samples from 11 German adults (ages 23-41) were taken following a meal consisting of 2g parsley/kg body weight-which was equivalent to ∼17mg of apigenin (Meyer et al., 2006). Plasma concentrations of apigenin ranged from 28-337nmol/L at 6-10h after consumption and fell below detection at 28h. (R)
1 uM = 1000 nmol/l, so 337nmol/ would be 0.34uM. If we extrapolate linearly, 170mg will reach a concentration of between 280-3370 nmol/L (0.28-3.37uM). This number is still well below 10 uM which has been shown to stimulate steroidogenesis.

How do you feel on 200mg apigenin? Do you exercise? Have you noticed a performance-enhancing effect? Maybe more energy?

 

[mrseb]

Blood and urine samples from 11 German adults (ages 23-41) were taken following a meal consisting of 2g parsley/kg body weight-which was equivalent to ∼17mg of apigenin (Meyer et al., 2006). Plasma concentrations of apigenin ranged from 28-337nmol/L at 6-10h after consumption and fell below detection at 28h. (R)
1 uM = 1000 nmol/l, so 337nmol/ would be 0.34uM. If we extrapolate linearly, 170mg will reach a concentration of between 280-3370 nmol/L (0.28-3.37uM). This number is still well below 10 uM which has been shown to stimulate steroidogenesis.

How do you feel on 200mg apigenin? Do you exercise? Have you noticed a performance-enhancing effect? Maybe more energy?

thanks, yes I do a lot of sports: bouldering, bodybuilding, jump rope. I've only been taking it for 4 days now. I don't feel any effect on performance. I take 200mg before sleeping and it seems to slightly improve my deep sleep by a few minutes but I still have too little perspective. To be seen over several weeks...

 

[mrseb]

Blood and urine samples from 11 German adults (ages 23-41) were taken following a meal consisting of 2g parsley/kg body weight-which was equivalent to ∼17mg of apigenin (Meyer et al., 2006). Plasma concentrations of apigenin ranged from 28-337nmol/L at 6-10h after consumption and fell below detection at 28h. (R)
1 uM = 1000 nmol/l, so 337nmol/ would be 0.34uM. If we extrapolate linearly, 170mg will reach a concentration of between 280-3370 nmol/L (0.28-3.37uM). This number is still well below 10 uM which has been shown to stimulate steroidogenesis.

How do you feel on 200mg apigenin? Do you exercise? Have you noticed a performance-enhancing effect? Maybe more energy?

Here is a little feedback: I have my total testosterone measured and I have never seen it so high: 44 nmol/l, the last two times I measured my testo a few years ago the values were 30 and 37 nmol/l.

My libido is very good but no more than before apigenin. My usual sport is bouldering and bodybuilding. I still added loads since August and I took 2kg of muscle without gaining fat (I'm very dry MG = between 5 and 6%).

I don't know if it's the apigenin that I've been taking for several weeks... but it's possible that it is because it's the only supplement I've changed in my routine. In terms of feeling I find that I have better energy than usual and more deep sleep.

 

[Hans]

Here is a little feedback: I have my total testosterone measured and I have never seen it so high: 44 nmol/l, the last two times I measured my testo a few years ago the values were 30 and 37 nmol/l.

My libido is very good but no more than before apigenin. My usual sport is bouldering and bodybuilding. I still added loads since August and I took 2kg of muscle without gaining fat (I'm very dry MG = between 5 and 6%).

I don't know if it's the apigenin that I've been taking for several weeks... but it's possible that it is because it's the only supplement I've changed in my routine. In terms of feeling I find that I have better energy than usual and more deep sleep.

That's really awesome, thanks for sharing.

 

[LadyRae]

Each 8 drop serving of MelaNon contains 3 mg each Apigenin and Naringenin