Amentoflavone

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.

Origin & History

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.

Historical & Cultural Context

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.

Health Benefits

• Potential cardiocerebrovascular protection (based on preclinical models only)
• Possible antiviral activity (in vitro studies, no human trials)
• May inhibit angiogenesis (preclinical evidence only)
• Could modulate P450 enzymes (in vitro data, clinical relevance unknown)
• Potential cathepsin B inhibition (laboratory studies only)

How It Works

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.

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.

Clinical Summary

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.

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.

Preparation & Dosage

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.

Synergy & Pairings

Apigenin, Quercetin, Ginkgo biloba extract, St. John's Wort extract, Other biflavonoids

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.