Hermetica Superfood Encyclopedia
The Short Answer
Amentoflavone is a biflavonoid compound found in plants like Ginkgo biloba that may protect cardiovascular and neural tissues through antioxidant mechanisms. Preclinical studies suggest it inhibits angiogenesis and modulates cytochrome P450 enzymes, though human clinical data remains limited.
CategoryNamed Bioactive Compounds
GroupCompound
Evidence LevelModerate
Primary Keywordamentoflavone benefits
Synergy Pairings3
Amentoflavone — botanical close-up
Health Benefits
Origin & History
Natural habitat
Amentoflavone is a biflavonoid compound formed by two apigenin molecules linked by a C3'-C8'' covalent bond, with molecular formula C₃₀H₁₈O₁₀. It occurs naturally in over 120 plant species, particularly from Selaginellaceae (Selaginella tamariscina), Ginkgo biloba, and Hypericum perforatum, typically extracted from leaves using ethanol or dimethyl sulfoxide due to poor water solubility.
“While amentoflavone occurs in plants used in traditional medicine such as Ginkgo biloba (traditional Chinese medicine) and Hypericum perforatum/St. John's Wort (European folk medicine), the isolated compound's specific traditional use is not documented. Modern interest in amentoflavone stems from phytochemical research rather than historical application.”Traditional Medicine
Scientific Research
No human clinical trials, randomized controlled trials, or meta-analyses for amentoflavone were identified in the research. Available evidence consists entirely of preclinical pharmacology studies including in vitro and animal models, with no PubMed PMIDs cited for human studies.
Preparation & Dosage
Traditional preparation
No clinically studied dosage ranges have been established for amentoflavone as human trials are absent. No standardization percentages or dosing protocols exist for extracts, powders, or other forms. Consult a healthcare provider before starting any new supplement.
Nutritional Profile
Amentoflavone is a biflavonoid compound (a dimeric form of apigenin linked via a C-8 to C-3' bond), not a macronutrient or dietary staple, so it carries no caloric value, protein, fat, fiber, or carbohydrate content in the conventional nutritional sense. It is a pure bioactive polyphenolic compound with a molecular weight of 538.46 g/mol and molecular formula C30H18O10. It is found naturally in trace concentrations across numerous plant sources: Ginkgo biloba leaves (approximately 0.1–0.5 mg/g dry weight), Hypericum perforatum (St. John's Wort, ~0.01–0.1% dry weight extract), Selaginella tamariscina (up to 0.3% dry weight), Chamaecyparis obtusa, and various species of the Cupressaceae and Podocarpaceae families. As a biflavonoid, it belongs to the broader class of dietary flavonoids but is not typically obtained in meaningful quantities through normal food consumption. Bioavailability is notably poor and represents a major pharmacokinetic limitation: oral bioavailability in preclinical models is estimated to be low (<10%) due to limited aqueous solubility (log P approximately 2.5–3.0), extensive first-pass metabolism, and rapid glucuronidation and sulfation by intestinal and hepatic enzymes. It is not a source of vitamins or minerals. No established dietary reference intake or recommended daily amount exists. Nanoparticle encapsulation and phospholipid complexation strategies have been investigated in preclinical settings to enhance its bioavailability, with some studies reporting 2–4 fold improvements in absorption using lipid-based delivery systems.
How It Works
Mechanism of Action
Amentoflavone exerts its effects primarily through inhibition of cathepsin B protease and modulation of cytochrome P450 enzymes, particularly CYP3A4. The compound demonstrates antioxidant activity by scavenging free radicals and may block angiogenesis through VEGF pathway interference. Its biflavonoid structure allows it to cross the blood-brain barrier and potentially protect neural tissues from oxidative damage.
Clinical Evidence
Current evidence for amentoflavone consists primarily of in vitro and animal studies, with no published human clinical trials specifically examining this compound. Preclinical models have shown cardiocerebrovascular protective effects at doses ranging from 10-50 mg/kg in rodent studies. Laboratory studies demonstrate antiviral activity against certain viruses, including potential inhibition of viral replication enzymes. The lack of human trials makes it impossible to establish effective dosages or confirm safety profiles in clinical populations.
Safety & Interactions
Safety data for amentoflavone in humans is extremely limited due to the absence of clinical trials. Potential drug interactions may occur through cytochrome P450 enzyme modulation, particularly affecting medications metabolized by CYP3A4. Theoretical concerns include altered metabolism of blood thinners, immunosuppressants, and certain cardiovascular medications. Pregnant and breastfeeding women should avoid amentoflavone supplementation due to insufficient safety data.
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Frequently Asked Questions
What foods contain amentoflavone naturally?
Amentoflavone is found primarily in Ginkgo biloba leaves, St. John's wort, and certain species of Hypericum plants. Traditional herbal preparations containing these plants provide the most concentrated natural sources of this biflavonoid compound.
How much amentoflavone should I take daily?
No established human dosage exists for amentoflavone since clinical trials have not been conducted. Preclinical studies used doses equivalent to 10-50 mg/kg in animals, but translating this to human doses would be purely speculative and potentially unsafe.
Can amentoflavone interact with blood pressure medications?
Amentoflavone may interact with blood pressure medications through cytochrome P450 enzyme modulation, particularly CYP3A4. This could potentially alter the metabolism and effectiveness of calcium channel blockers and ACE inhibitors, though specific interaction studies have not been performed.
Is amentoflavone effective for heart disease prevention?
While animal studies suggest cardiovascular protective effects, no human trials have tested amentoflavone for heart disease prevention. The preclinical evidence is insufficient to recommend it for cardiovascular health without proper clinical validation.
What are the side effects of amentoflavone supplements?
Side effects of amentoflavone in humans are unknown due to the lack of clinical safety studies. Theoretical concerns include potential liver enzyme changes and drug metabolism alterations, but documented adverse effects have not been established in human populations.
What is the current level of clinical evidence for amentoflavone's health benefits?
Most evidence for amentoflavone comes from preclinical laboratory and animal studies, with very limited human clinical trials. While in vitro research suggests potential antiviral, cardiocerebrovascular, and anti-angiogenic effects, these findings have not been confirmed in rigorous human studies. Current evidence is insufficient to make definitive claims about efficacy in humans, and more research is needed before drawing firm conclusions about its therapeutic value.
Does amentoflavone have any known interactions with cytochrome P450 enzymes and common medications?
In vitro studies suggest amentoflavone may modulate cytochrome P450 enzymes, which are responsible for metabolizing many medications, though the clinical significance of this interaction remains unclear. Since P450 modulation can potentially affect drug metabolism and effectiveness, individuals taking medications metabolized by these enzymes should consult a healthcare provider before supplementing with amentoflavone. More clinical research is needed to establish whether amentoflavone actually affects medication levels in humans.
Are there specific populations who should avoid amentoflavone supplementation?
Pregnant and nursing women, children, and people taking medications metabolized by cytochrome P450 enzymes should avoid amentoflavone until safety data becomes available. Additionally, individuals with bleeding disorders or taking anticoagulant medications should exercise caution, as flavonoids may affect platelet function and bleeding risk. Anyone considering amentoflavone supplementation should consult with a healthcare provider to assess individual safety and appropriateness.
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