Amentoflavone
Also known as: Biflavonoid, amentoflavone, C30H18O10, Amentoflavone
Overview
Amentoflavone is a naturally occurring biflavonoid compound found in various plant families, including Selaginellaceae, Cupressaceae, Euphorbiaceae, Podocarpaceae, and Calophyllaceae. It is classified as a polyphenolic compound and has garnered significant scientific interest due to its diverse biological activities. Research has primarily focused on its potential anti-inflammatory, anti-oxidative, anti-diabetic, anti-senescence, and anti-tumor properties. While in vitro and animal studies have shown promising results, particularly in cancer research, human clinical trials are currently limited. The compound exhibits multiple bioactivities, suggesting therapeutic potential in various diseases, including cancer and neurodegenerative disorders. Its mechanism of action involves modulating cellular signaling pathways related to apoptosis and cell cycle regulation. Despite its promising profile, the research on amentoflavone is still in its early stages, with a need for more extensive human studies to confirm its efficacy and safety.
Benefits
Amentoflavone has demonstrated several evidence-based benefits, primarily in preclinical settings. Its most significant effects are observed in its anti-tumor properties. In bladder cancer cells (TSGH8301), amentoflavone at concentrations of 150 and 200 μM significantly induced apoptosis and inhibited tumor progression, increasing late apoptotic cells by 30-50% and reducing anti-apoptotic proteins by 50-80%. Similarly, in non-small cell lung cancer (NSCLC) cells, concentrations of 75 and 150 μM led to G1 cell-cycle arrest, apoptosis, and suppressed invasion. These effects are typically observed within 48 hours of treatment in vitro. Beyond its anti-tumor actions, amentoflavone also exhibits anti-inflammatory and anti-oxidative activities, although these are less extensively studied than its anti-cancer effects. While current studies are focused on cancer cell lines, the broader anti-inflammatory and anti-oxidative properties suggest potential benefits for other populations, though human data is lacking. The strength of evidence for these benefits is currently strong for in vitro and animal models, but clinical significance in humans remains to be established.
How it works
Amentoflavone exerts its biological effects primarily by modulating key cellular signaling pathways. Its anti-tumor action involves inducing apoptosis through both extrinsic (FAS/FASL-dependent) and intrinsic (mitochondria-dependent) pathways. It also inhibits cell proliferation and invasion by inducing G1 cell-cycle arrest and reducing the expression of proteins crucial for tumor progression, such as VEGF, MMP-2, MMP-9, uPA, and cyclin D1. Amentoflavone interacts with various cellular systems, influencing processes like cell cycle regulation and angiogenesis. Its known molecular targets include pro-apoptotic proteins (FAS, FASL, BAX) and anti-apoptotic proteins (MCL-1, C-FLIP). The compound undergoes extensive metabolism, including oxidation, hydrolysis, methylation, and glucuronidation, which can influence its bioavailability and overall efficacy within the body.
Side effects
The safety profile of amentoflavone, especially in humans, is not yet fully established. Current data is primarily derived from in vitro and animal studies, which suggest it is generally well-tolerated at the concentrations tested. However, there is no available data on common, uncommon, or rare side effects in human subjects. Due to the lack of human clinical trials, specific adverse effects, their severity, or frequency cannot be determined. Limited information exists regarding potential drug interactions; however, given its extensive metabolic pathways, amentoflavone could potentially interact with other drugs metabolized by similar enzyme systems. No specific contraindications have been identified in the available literature. Furthermore, there is no data regarding the use of amentoflavone in special populations, such as pregnant women, children, or individuals with pre-existing health conditions. Comprehensive safety warnings and contraindications for human use are pending further research.
Dosage
The optimal and safe dosage of amentoflavone for human use has not been established due to the limited number of human clinical trials. In vitro studies have shown efficacy at concentrations ranging from 75 μM to 200 μM for inducing cell-cycle arrest and apoptosis in cancer cells. For instance, concentrations as low as 75 μM were effective in non-small cell lung cancer cells. However, these in vitro concentrations do not directly translate to human oral dosages. There is no established minimum effective dose, optimal dosage range, or maximum safe dose for human consumption. Information regarding timing of administration, form-specific recommendations, or required cofactors for efficacy is also unavailable. The absorption and bioavailability of amentoflavone are influenced by its extensive metabolic pathways, which could impact its effective concentration in vivo. Therefore, any human use of amentoflavone should be approached with caution, as its safety and efficacy profile in humans are largely unknown.
FAQs
Is Amentoflavone safe for human consumption?
The safety of Amentoflavone for human consumption is not fully established. While in vitro and animal studies suggest it is generally well-tolerated, there is a lack of human clinical data on its side effects and overall safety profile.
What are the primary benefits of Amentoflavone?
Preclinical studies indicate Amentoflavone has promising anti-tumor effects, inducing apoptosis and inhibiting cancer cell proliferation. It also shows anti-inflammatory and anti-oxidative properties, though these are less studied.
How should Amentoflavone be taken?
There are no established dosing guidelines, timing considerations, or specific recommendations for the form of Amentoflavone for human use. All current data is from laboratory and animal studies.
Can Amentoflavone interact with medications?
Limited information is available on drug interactions. However, its extensive metabolic pathways suggest a potential for interaction with other drugs metabolized by similar enzymes. Consult a healthcare professional.
Is Amentoflavone a clinically proven supplement?
No, Amentoflavone is not a clinically proven supplement for human use. Despite promising in vitro and animal study results, it requires further large-scale human clinical trials to validate its efficacy and safety.
Research Sources
- https://ar.iiarjournals.org/content/39/7/3641 – This in vitro study investigated the effects of Amentoflavone on human bladder cancer cells (TSGH8301). It found that Amentoflavone induced significant cytotoxicity and apoptosis, and reduced the expression of anti-apoptotic proteins, indicating its potential as an anti-tumor agent. The study provides strong evidence for Amentoflavone's anti-cancer properties in a laboratory setting.
- https://pubmed.ncbi.nlm.nih.gov/28212342/ – This review article provides a comprehensive overview of the phytochemistry, pharmacology, and pharmacokinetics of Amentoflavone. It summarizes various bioactivities, including anti-inflammatory, anti-oxidative, and anti-tumor effects, and discusses its potential therapeutic applications. The review highlights the broad spectrum of Amentoflavone's biological activities based on existing research.
- https://pubmed.ncbi.nlm.nih.gov/33322906/ – This study employed a systematic strategy to identify and characterize the metabolites of Amentoflavone in vivo (rats) and in vitro (rat microsomes). It identified numerous metabolites, revealing that Amentoflavone undergoes extensive metabolic transformations. This research is crucial for understanding the bioavailability and potential drug interactions of Amentoflavone.
- https://ar.iiarjournals.org/content/41/3/1357 – This in vitro study explored the effects of Amentoflavone on non-small cell lung cancer (NSCLC) cells. It demonstrated that Amentoflavone induced G1 cell-cycle arrest, apoptosis, and suppressed invasion in these cancer cells. The findings support Amentoflavone's potential as an anti-cancer agent by targeting cell cycle progression and metastatic processes.