Amentoflavone

mr.cooper69

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Amentoflavone

Mood/CNS effects

There are a whole host of studies examining the effects of Amentoflavone on various neurological endpoints. Without going into each one individually, research highlights will be presented.
Amentoflavone interacts with the GABA-A receptor by acting as a negative modulator. This would produce a central stimulant effect by inducing wakefulness/alertness. Amentoflavone uptake into the CNS is limited by P-glycoprotein, an efflux pump that pumps specific compounds back outside of the CNS. There are numerous ways to overcome the P-glycoprotein transporter; a very well-documented one is by consuming grapefruit or its constituents.
In addition, amentoflavone has demonstrated antidepressant and anxiolytic (anti-anxiety) effects in vivo by interacting with not only the GABA-A receptor, but also the serotonin and alpha-adrenergic receptors. In fact, of all the tested constituents of St. John’s Wort (a known antidepressant/anti-anxiety plant), amentoflavone displayed the strongest anxiolytic activity.

Summary: CNS stimulant, anxiolytic, anti-depressant

Sources:
Determinants of amentoflavone interaction at... [Eur J Pharmacol. 2005] - PubMed - NCBI
Inhibition of benzodiazepine binding in vitr... [Pharm Acta Helv. 1997] - PubMed - NCBI
Biflavones from Rhus species with affinity ... [J Ethnopharmacol. 2006] - PubMed - NCBI
Semisynthetic preparation of amentoflav... [Bioorg Med Chem Lett. 2003] - PubMed - NCBI
Transport of amentoflavone across the blood-brain... [Planta Med. 2002] - PubMed - NCBI
Antidepressant and anxiolytic effect... [Pharmacol Biochem Behav. 2012] - PubMed - NCBI
Review on plants with CNS-effects used in t... [J Ethnopharmacol. 2008] - PubMed - NCBI
Effects of St. John's wort extract and single con... [Planta Med. 2006] - PubMed - NCBI
Isolation of amentoflavone from Selaginella rupes... [Planta Med. 1981] - PubMed - NCBI


Fatty Acid Synthase Inhibition

Fatty acid synthase, as the name implies, is responsible for the endogenous synthesis of fatty acids in humans. It is currently a drug target for metabolic syndrome. In at least three separate trials, amentoflavone has demonstrated the ability to inhibit fatty acid synthase, and thus fat production.

Summary: Reduced fatty acid synthesis

Fatty acid synthase inhibition by amentoflav... [Biol Pharm Bull. 2009] - PubMed - NCBI
Fatty acid synthase inhibition by amentoflavon... [Phytother Res. 2013] - PubMed - NCBI
Inhibition of fatty acid synthase by amentoflavon... [Arch Virol. 2012] - PubMed - NCBI



Phosphodiesterase (PDE) Inhibition

PDE is the enzyme responsible for breaking down cAMP/cGMP. cAMP/cGMP promote smooth muscle relaxation (vasodilation; this is how PDE5 inhibitors help with erectile dysfunction) and lipolysis. Indeed, Forskolin has documented lipolytic activity by increasing cAMP levels via increased cAMP production. PDE inhibition, as with amentoflavone, hits the opposite side of the coin: reduced cAMP breakdown. By increasing cAMP levels, amentoflavone can synergize with adrenergic agonists (i.e. b-agonists) because second messenger pathways follow the rule of amplification.
Amentoflavone inhibits a broad array of PDE isoforms, and it is the most potent inhibitor out of all tested flavonoids in Ginkgo biloba. Further, of all tested constituents of Allanblackia monticola, Amentoflavone was the strongest vasodilator, inhibiting norepinephrine-induced vasoconstriction by a whopping 35%.
Summary: Increased lipolysis (fat loss) and increased vasodilation

Inhibition of cAMP-phosphodiesterase by biflavone... [J Nat Prod. 1998] - PubMed - NCBI
Biflavones of Decussocarpus rospigliosii as phosp... [Planta Med. 2007] - PubMed - NCBI
Inhibition of cGMP-phosphodiesterase-5 by biflavo... [Planta Med. 2006] - PubMed - NCBI
Antimalarial and vasorelaxant constit... [Ann Trop Med Parasitol. 2007] - PubMed - NCBI
Vasorelaxation by amentoflavone isolated from Sel... [Planta Med. 2004] - PubMed - NCBI
Inhibition of human platelet cyclic AMP ph... [Biochem Pharmacol. 1986] - PubMed - NCBI


Muscular Strength and Endurance

One well-documented mechanism of increasing exercise performance is vasodilation, which helps supply (oxygen; waste removal) meet the demand of exercising muscle tissue (hypoxia; metabolic waste accumulation). Amentoflavone has a well-documented effect on vasodilation as described above.
In addition to this, Amentoflavone provides a relatively unique mechanism for increasing power output: increased Ca2+ release from the sarcoplasmic reticulum. By increasing intracellular Ca2+ downstream of the signal for muscle contraction, binding to troponin-C is increased and the force of muscular contraction, on a cell-by-cell basis, also increases.
Caffeine acts via a similar mechanism to increase strength output, and researchers found that not only does Amentoflavone likely bind to the caffeine-binding site, but it does so with 20 times greater potency than caffeine.

Summary: Improved strength (Ca2+ release) and improved endurance (vasodilation)
Properties of amentoflavone, a potent caffei... [Eur J Pharmacol. 1999] - PubMed - NCBI

Insulin Sensitivity/GDA - PTP1B inhibition

PTP1B is an enzyme involved in insulin signaling, and inhibition of PTP1B is being investigated as a possible treatment for obesity and diabetes. PTP1B inhibition will chiefly improve insulin sensitivity by augmenting insulin’s actions within the cell at a lower circulating level of insulin. This is a fairly novel approach to improving insulin sensitivity and will continue to be investigated.

Summary: Improved insulin sensitivity

Protein tyrosine phosphatase 1B inhibitory a... [Biol Pharm Bull. 2007] - PubMed - NCBI


Dyslipidemia

Amentoflavone has been shown in vivo to reduce circulating lipids (LDL/TG), making it of further benefit to obesity/diabetes/metabolic syndrome.

Summary: Reduced lipids

Antidyslipidemic and antioxidant activity of t... [Phytomedicine. 2012] - PubMed - NCBI

Credit and thanks to neuron: http://hightowerpharmacology.blogspot.com/2012/09/future-pharmacy-amentoflavone.html
 

cbsharpe

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Thanks for breaking this down Coop! Get my Norcodrene tomorrow...can't wait.
 
Driven2lift

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Excited to try this out pre-workout now.


Assuming that taking in EAA's (AminoIV) would somewhat inhibit the fat-loss benefits of this?
But the energy, focus, and strength boost should still be there?
 

mr.cooper69

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Excited to try this out pre-workout now.


Assuming that taking in EAA's (AminoIV) would somewhat inhibit the fat-loss benefits of this?
But the energy, focus, and strength boost should still be there?
The effects will still be present for amentoflavone
 

urosinho10

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Increased Ca2+ release from the sarcoplasmic reticulum

Hey man, I tried to pm you but your inbox is full so I'll just post it here instead:I have a pretty uniqe goal but I think you would know how to do it. I want to increase Ca2+ release from the sarcoplasmic reticulum as much as possible because this would increase contracts frequency and this would help me incredible a lot especially since I am a sprinter. Bottom line, do you know supplements (other than caffeine since its banned by WADA) that will do this and that I can get a hold of, I can't find a pure source for amentoflavone anywhere. I really need your help, especially since i'm only 18.Thanks a lot in advance man!
 

kissdadookie

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Any chance AS will make this ingredient a product in the future? I like the ingredient but don't always want to use Uncut and in the future I'm obviously not going to be constantly running Norcodrene.

In the mean time, I've been using AppNut's other product (non-stim) just so that I can have some amentoflavone in on non-UnCut days but that's not really cost effective.
 
RecompMan

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Amentoflavone

Mood/CNS effects

There are a whole host of studies examining the effects of Amentoflavone on various neurological endpoints. Without going into each one individually, research highlights will be presented.
Amentoflavone interacts with the GABA-A receptor by acting as a negative modulator. This would produce a central stimulant effect by inducing wakefulness/alertness. Amentoflavone uptake into the CNS is limited by P-glycoprotein, an efflux pump that pumps specific compounds back outside of the CNS. There are numerous ways to overcome the P-glycoprotein transporter; a very well-documented one is by consuming grapefruit or its constituents.
In addition, amentoflavone has demonstrated antidepressant and anxiolytic (anti-anxiety) effects in vivo by interacting with not only the GABA-A receptor, but also the serotonin and alpha-adrenergic receptors. In fact, of all the tested constituents of St. John's Wort (a known antidepressant/anti-anxiety plant), amentoflavone displayed the strongest anxiolytic activity.

Summary: CNS stimulant, anxiolytic, anti-depressant

Sources:
Determinants of amentoflavone interaction at... [Eur J Pharmacol. 2005] - PubMed - NCBI
Inhibition of benzodiazepine binding in vitr... [Pharm Acta Helv. 1997] - PubMed - NCBI
Biflavones from Rhus species with affinity ... [J Ethnopharmacol. 2006] - PubMed - NCBI
Semisynthetic preparation of amentoflav... [Bioorg Med Chem Lett. 2003] - PubMed - NCBI
Transport of amentoflavone across the blood-brain... [Planta Med. 2002] - PubMed - NCBI
Antidepressant and anxiolytic effect... [Pharmacol Biochem Behav. 2012] - PubMed - NCBI
Review on plants with CNS-effects used in t... [J Ethnopharmacol. 2008] - PubMed - NCBI
Effects of St. John's wort extract and single con... [Planta Med. 2006] - PubMed - NCBI
Isolation of amentoflavone from Selaginella rupes... [Planta Med. 1981] - PubMed - NCBI

Fatty Acid Synthase Inhibition

Fatty acid synthase, as the name implies, is responsible for the endogenous synthesis of fatty acids in humans. It is currently a drug target for metabolic syndrome. In at least three separate trials, amentoflavone has demonstrated the ability to inhibit fatty acid synthase, and thus fat production.

Summary: Reduced fatty acid synthesis

Fatty acid synthase inhibition by amentoflav... [Biol Pharm Bull. 2009] - PubMed - NCBI
Fatty acid synthase inhibition by amentoflavon... [Phytother Res. 2013] - PubMed - NCBI
Inhibition of fatty acid synthase by amentoflavon... [Arch Virol. 2012] - PubMed - NCBI

Phosphodiesterase (PDE) Inhibition

PDE is the enzyme responsible for breaking down cAMP/cGMP. cAMP/cGMP promote smooth muscle relaxation (vasodilation; this is how PDE5 inhibitors help with erectile dysfunction) and lipolysis. Indeed, Forskolin has documented lipolytic activity by increasing cAMP levels via increased cAMP production. PDE inhibition, as with amentoflavone, hits the opposite side of the coin: reduced cAMP breakdown. By increasing cAMP levels, amentoflavone can synergize with adrenergic agonists (i.e. b-agonists) because second messenger pathways follow the rule of amplification.
Amentoflavone inhibits a broad array of PDE isoforms, and it is the most potent inhibitor out of all tested flavonoids in Ginkgo biloba. Further, of all tested constituents of Allanblackia monticola, Amentoflavone was the strongest vasodilator, inhibiting norepinephrine-induced vasoconstriction by a whopping 35%.
Summary: Increased lipolysis (fat loss) and increased vasodilation

Inhibition of cAMP-phosphodiesterase by biflavone... [J Nat Prod. 1998] - PubMed - NCBI
Biflavones of Decussocarpus rospigliosii as phosp... [Planta Med. 2007] - PubMed - NCBI
Inhibition of cGMP-phosphodiesterase-5 by biflavo... [Planta Med. 2006] - PubMed - NCBI
Antimalarial and vasorelaxant constit... [Ann Trop Med Parasitol. 2007] - PubMed - NCBI
Vasorelaxation by amentoflavone isolated from Sel... [Planta Med. 2004] - PubMed - NCBI
Inhibition of human platelet cyclic AMP ph... [Biochem Pharmacol. 1986] - PubMed - NCBI

Muscular Strength and Endurance

One well-documented mechanism of increasing exercise performance is vasodilation, which helps supply (oxygen; waste removal) meet the demand of exercising muscle tissue (hypoxia; metabolic waste accumulation). Amentoflavone has a well-documented effect on vasodilation as described above.
In addition to this, Amentoflavone provides a relatively unique mechanism for increasing power output: increased Ca2+ release from the sarcoplasmic reticulum. By increasing intracellular Ca2+ downstream of the signal for muscle contraction, binding to troponin-C is increased and the force of muscular contraction, on a cell-by-cell basis, also increases.
Caffeine acts via a similar mechanism to increase strength output, and researchers found that not only does Amentoflavone likely bind to the caffeine-binding site, but it does so with 20 times greater potency than caffeine.

Summary: Improved strength (Ca2+ release) and improved endurance (vasodilation)
Properties of amentoflavone, a potent caffei... [Eur J Pharmacol. 1999] - PubMed - NCBI

Insulin Sensitivity/GDA - PTP1B inhibition

PTP1B is an enzyme involved in insulin signaling, and inhibition of PTP1B is being investigated as a possible treatment for obesity and diabetes. PTP1B inhibition will chiefly improve insulin sensitivity by augmenting insulin's actions within the cell at a lower circulating level of insulin. This is a fairly novel approach to improving insulin sensitivity and will continue to be investigated.

Summary: Improved insulin sensitivity

Protein tyrosine phosphatase 1B inhibitory a... [Biol Pharm Bull. 2007] - PubMed - NCBI

Dyslipidemia

Amentoflavone has been shown in vivo to reduce circulating lipids (LDL/TG), making it of further benefit to obesity/diabetes/metabolic syndrome.

Summary: Reduced lipids

Antidyslipidemic and antioxidant activity of t... [Phytomedicine. 2012] - PubMed - NCBI

Credit and thanks to neuron: http://hightowerpharmacology.blogspot.com/2012/09/future-pharmacy-amentoflavone.html
Definitely an ingredient to have in the arsenal, I believe it also increases the capsases 3 and 9 causing apoptosis is certain cell lines through down regulation on bcl-2.
 
PharmAnalyst

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How would standalone amentoflavone stack with the new combustion?
 
CJ_Xfit89

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Please sticky this thread
 

raekwonse

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Would the increase in strength result in a increase in muscle building or is it just a temporary thing?
 

chedapalooza

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Any stims we should BOLO to not stack with amentoflavone?

I picked up two bottles with the AS sale and I plan on starting them next week for an 8 week run with EC leading Into summer. I was impressed by 4 weeks of norco so I'm very hopeful for an additional 4
 

mr.cooper69

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Would the increase in strength result in a increase in muscle building or is it just a temporary thing?
Increased strength will result in improved body composition (not to mention the fat loss benefits)
 

mr.cooper69

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Any stims we should BOLO to not stack with amentoflavone?

I picked up two bottles with the AS sale and I plan on starting them next week for an 8 week run with EC leading Into summer. I was impressed by 4 weeks of norco so I'm very hopeful for an additional 4
I don't know what BOLO means but it will work fine with EC
 
3clipseGT

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BOLO I think stands for be on the look out.
 
PharmAnalyst

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Could you post the profile

Amount Per Serving % Daily Value
Higenamine 22 mg **
Alstonia Scholaris 40% 125 mg **
Caffeine 125 mg **
Piperine 5 mg **
b-PEA 125 mg **
Morus Alba 20:1 200 mg **
Forskolin 40 mg **

(Used Jimbuick's Link)
 

chedapalooza

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Starting 8 week run today til July 1st. Can't believe July 1st is only 8 weeks away. Looking forward to some happy moods and fat loss!
 
Androflaven

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Bought some of the AS amentoflavone, any idea how I should time my dosing to maximize the strength/endurance benefits?
 

Pec.Major

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Is there any drug interaction in conjunction with amentoflavone administration?

Sounds like a thing worth to try. Was thinking on Katana pwo, looks solid.
 
Quadzilla99

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Coop, is it okay to take a dose 45minutes to an hour pre work out?
Probably doesn't matter; I think the effects last for several hours iirc. neuron used to have a great writeup on it but its gone from his blog now
 
PharmAnalyst

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Due to the antagonistic effects on angiogenesis from amentoflavone and (transdermal) ursolic acid respectively, would it be ideal to run them separately for maximum benefit?
 
PharmAnalyst

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Given that both affect the GABAergic system, would it be advisable to avoid combining picamilon and amentoflavone?
 
Synapsin

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Can u guys elaborate on this? What else should once avoid near amento dosing?
They both act on GABA receptors and their interaction wouldn't be favorable. Other supplements to avoid near amento would be GABA but people don't really take that preworkout.
 
PharmAnalyst

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Yes, take the picamilon away from when you dose your amentoflavone.
Many thanks, I suspected they might interactive negatively but thought it best to consult someone with a better grasp of the two.
 

mr.cooper69

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None of these interactions would be bad per se. Just expect your picamilon or gaba not to work too well if you take them exactly with amentoflavone
 
dinot1985

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Do you know anything about Methoxy Amentoflavone form Coop?
 

chedapalooza

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Due to the antagonistic effects on angiogenesis from amentoflavone and (transdermal) ursolic acid respectively, would it be ideal to run them separately for maximum benefit?
Does this not apply to oral ursolic acid?
 

chedapalooza

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Does this not apply to oral ursolic acid?
Found this

in the present study we evaluated the efficacy of UA against tumor growth and angiogenesis in vivo and in vitro and investigated the underlying molecular mechanisms. We found that administration of UA significantly inhibited tumor volume but had no effect on body weight changes in CRC mice, suggesting that UA can suppress colon cancer growth in vivo without noticeable signs of toxicity. In addition, UA treatment reduced intratumoral microvessel density (MVD) in CRC mice, decreased the total number of blood vessels in the CAM model, and dose and time-dependently inhibited the proliferation, migration and tube formation of HUVECs, demonstrating UA's antitumor angiogenesis in vivo and in vitro. Moreover, UA treatment inhibited the expression of critical angiogenic factors, such as VEGF-A and bFGF. Furthermore, UA suppressed the activation of sonic hedgehog (SHH), STAT3, Akt and p70S6K pathways. Collectively, our findings suggest that inhibition of tumor angiogenesis via suppression of multiple signaling pathways might be one of the mechanisms whereby UA can be effective in cancer treatment

http://www.ncbi.nlm.nih.gov/m/pubmed/24042330/

Important for me since colon cancer runs on my mothers side of the family.
 

chedapalooza

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These findings indicate that amentoflavone inhibits angiogenesis by disrupting the integrity of endothelial cells and by altering the endogenous factors that are required for the process of neovascularization.

http://www.ncbi.nlm.nih.gov/m/pubmed/18298378/

From what I am gathering, these two products should help inhibit angiogenesis. May I ask what led you to ask if they should be used with caution RE stimulating angiogenesis?
 

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Here's another Amento question: I see some literature suggesting putative anti-inflammatory properties of amentoflavone, and even an inhibition of nitric oxide synthase. Would this make it a poor coupling in situations where you're promoting inflammation, e.g. an ArA cycle? I'm sure the effects are too subtle to matter otherwise, but if you're going all-out to optimize ArA by including lodhra, GMS, and carnitine, it'd seem like it would make sense to avoid amentoflavone if it had deleterious effects.
 

mr.cooper69

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Here's another Amento question: I see some literature suggesting putative anti-inflammatory properties of amentoflavone, and even an inhibition of nitric oxide synthase. Would this make it a poor coupling in situations where you're promoting inflammation, e.g. an ArA cycle? I'm sure the effects are too subtle to matter otherwise, but if you're going all-out to optimize ArA by including lodhra, GMS, and carnitine, it'd seem like it would make sense to avoid amentoflavone if it had deleterious effects.
It would not interfere. We aren't avoiding anti-inflammatories with ArA, we're avoiding fish oil and COX-2 inhibitors
 
PharmAnalyst

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These findings indicate that amentoflavone inhibits angiogenesis by disrupting the integrity of endothelial cells and by altering the endogenous factors that are required for the process of neovascularization.

http://www.ncbi.nlm.nih.gov/m/pubmed/18298378/

From what I am gathering, these two products should help inhibit angiogenesis. May I ask what led you to ask if they should be used with caution RE stimulating angiogenesis?
No idea how I missed that question, sorry. At the time I was stacking pump spray and amentomax. While my emphasis at the time was recomposition and fat loss, I had also been considering (but not actively researching) possible beneficial effects of angiogenesis on conditions marked by increased vascular resistance.
 
tyrub42

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Tried 1 cap Amentomax PWO last night for the first time. I can't be positive it was all because of the Amento, but I had more fun in the gym than I have had since last year. Even coming back after I f**ked my wrist up with a modified workout. I seemed to be chomping at the bit to get more sets done, seemed to recover faster between sets, and most of all, I was in such a bright mood the whole time.

Granted, I am coming back from an injury, so I am enjoying being back in general, but something just seemed different about the whole experience. I can't wait to try this again.
 
bolt10

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Tried 1 cap Amentomax PWO last night for the first time. I can't be positive it was all because of the Amento, but I had more fun in the gym than I have had since last year. Even coming back after I f**ked my wrist up with a modified workout. I seemed to be chomping at the bit to get more sets done, seemed to recover faster between sets, and most of all, I was in such a bright mood the whole time. Granted, I am coming back from an injury, so I am enjoying being back in general, but something just seemed different about the whole experience. I can't wait to try this again.
That sounds like the usual benefits of amentoflavone. ;)

Mood elevation and increased workout performance are always plentiful for me.
 
Synapsin

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That sounds like the usual benefits of amentoflavone. ;)

Mood elevation and increased workout performance are always plentiful for me.
Yep, sounds like a classic amentomax moment to me!
 
kbayne

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Tried 1 cap Amentomax PWO last night for the first time. I can't be positive it was all because of the Amento, but I had more fun in the gym than I have had since last year. Even coming back after I f**ked my wrist up with a modified workout. I seemed to be chomping at the bit to get more sets done, seemed to recover faster between sets, and most of all, I was in such a bright mood the whole time. Granted, I am coming back from an injury, so I am enjoying being back in general, but something just seemed different about the whole experience. I can't wait to try this again.
Definitely sounds like what others are experiencing as well :)
 
Synapsin

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Amentoflavone also antagonizes kappa opioid receptors; this would also lead to expressional reductions in phosphodieasterase activity..in which that means, amentoflavone is a direct and indirect PDE inhibitor
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2265593/
http://en.wikipedia.org/wiki/Κ-opioid_receptor
http://www.longecity.org/forum/topic/65951-help-building-a-kor-antagonisticanti-dynorphic-stack-depersonalization-stack/
Indeed, AmentoMax would help with erection quality because of this mechanism.
 

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