mr.cooper69
Legend
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:
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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
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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
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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)
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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
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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
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Credit and thanks to neuron: Invalid Link Removed