# Acacetin

**Canonical URL:** https://ingredients.hermeticasuperfoods.com/ingredients/acacetin
**Data Source:** Hermetica Superfoods Ingredient Encyclopedia
**Updated:** 2026-03-30
**Evidence Score:** 2 / 10
**Category:** Compound
**Also Known As:** 5,7-dihydroxy-4'-methoxyflavone, 4'-methoxyapigenin, linarin aglycone, acacetin flavone, CAS 480-44-4

## Overview

Acacetin is a flavonoid compound that modulates [NF-κB](/ingredients/condition/inflammation) signaling pathways to provide cardioprotective and anti-cancer effects. This bioactive flavone demonstrates particular efficacy in reducing cardiac arrhythmias and inhibiting hepatocellular carcinoma cell proliferation.

## Health Benefits

• Prevents atrial fibrillation in anesthetized dogs, showing effectiveness in cardiac health [5]. • Reduces cardiomyocyte apoptosis in mice with myocardial infarction by regulating NF-κB signaling [1]. • Inhibits liver cancer cell proliferation by inducing apoptosis in HepG2 cells [4]. • Improves motor function and reduces neuro[inflammation](/ingredients/condition/inflammation) in mice with spinal cord injury [6]. • Demonstrates low toxicity across multiple preclinical models, supporting its safety in further research [3].

## Mechanism of Action

Acacetin exerts its therapeutic effects primarily through inhibition of NF-κB signaling pathways, reducing [inflammatory](/ingredients/condition/inflammation) cytokine production and cellular apoptosis. The compound also modulates potassium and calcium ion channels in cardiac tissue, contributing to its antiarrhythmic properties. Additionally, acacetin induces apoptosis in cancer cells through [mitochondrial](/ingredients/condition/energy) pathway activation and caspase-3 upregulation.

## Clinical Summary

Animal studies demonstrate acacetin's effectiveness in preventing atrial fibrillation in anesthetized dogs and reducing cardiomyocyte death in mice with induced myocardial infarction. In vitro research shows significant inhibition of HepG2 liver cancer cell proliferation with IC50 values in the micromolar range. However, human clinical trials are currently limited, and most evidence stems from preclinical animal and cell culture studies. The therapeutic potential appears promising but requires further clinical validation in human populations.

## Nutritional Profile

Acacetin (4'-methoxy-5,7-dihydroxyflavone) is a pure bioactive flavonoid compound (molecular formula C16H12O5, molecular weight 284.26 g/mol), not a whole food ingredient, and therefore does not carry conventional macronutrient or micronutrient profiles. As an isolated compound, it contains no meaningful protein, fat, carbohydrate, fiber, vitamins, or dietary minerals in its purified form. Its profile is defined entirely by its bioactive nature: it is a O-methylated flavone belonging to the flavonoid subclass, structurally characterized by a methoxy group at the 4' position and hydroxyl groups at positions 5 and 7 of the flavone backbone. Acacetin is naturally found in trace concentrations in plants such as Robinia pseudoacacia (black locust flowers), damiana (Turnera diffusa), and certain Clerodendrum species, where it occurs typically in the low microgram-to-milligram per gram dry weight range (estimated 0.1–5 mg/g depending on plant source and extraction method). Bioavailability is limited due to poor aqueous solubility (lipophilic character, logP approximately 2.5–3.0); absorption is enhanced in lipid-based delivery systems or nanoformulations. It undergoes hepatic Phase I and Phase II [metabolism](/ingredients/condition/weight-management), including glucuronidation and sulfation, with primary metabolites detected in urine and bile. No dietary reference intake or recommended daily allowance exists for acacetin as it is studied exclusively in experimental and pharmacological contexts.

## Dosage & Preparation

Animal studies have used oral doses of 25–50 mg/kg in mice and intravenous doses of 5 mg/kg in rats. No standardized human dosages have been established. Consult a healthcare provider before starting any new supplement.

## Safety & Drug Interactions

Limited safety data exists for acacetin supplementation in humans, as most research has been conducted in animal models. Potential interactions may occur with anticoagulant medications due to acacetin's effects on cardiac ion channels and blood flow. Pregnant and breastfeeding women should avoid acacetin supplements due to insufficient safety data. Individuals with existing cardiac conditions should consult healthcare providers before use, as the compound's effects on [heart rhythm](/ingredients/condition/heart-health) could interact with cardiac medications.

## Scientific Research

Current evidence for acacetin is predominantly preclinical, with no published human randomized controlled trials identified. The research consists primarily of in vitro and animal model studies, highlighting the need for human clinical trials to confirm these findings.

## Historical & Cultural Context

No traditional or historical uses of acacetin are documented in the provided literature. The historical context remains uncharacterized in available sources.

## Synergistic Combinations

Quercetin, Resveratrol, Curcumin, Green Tea Extract, Vitamin C

## Frequently Asked Questions

### What foods contain acacetin naturally?

Acacetin is found naturally in chrysanthemum flowers, Robinia pseudoacacia (black locust), and various Asteraceae family plants. Traditional Chinese herbal preparations often contain significant amounts of this flavonoid compound.

### How does acacetin help with heart problems?

Acacetin prevents atrial fibrillation by modulating cardiac ion channels and reduces heart muscle cell death through NF-κB pathway inhibition. Studies in dogs showed effective prevention of irregular heartbeats when administered intravenously.

### What is the effective dosage of acacetin for cancer?

In vitro studies used acacetin concentrations of 10-100 μM to effectively inhibit liver cancer cell growth. However, no established human dosage exists, as clinical trials have not yet determined safe and effective oral supplementation levels.

### Can acacetin be taken with blood thinners?

Acacetin may interact with anticoagulant medications due to its effects on cardiovascular function and potential impact on bleeding risk. Consultation with a healthcare provider is essential before combining acacetin with warfarin or other blood-thinning medications.

### How long does it take for acacetin to show effects?

Animal studies showed cardiac protective effects within hours of intravenous administration, while anti-cancer effects in cell cultures appeared after 24-72 hours of exposure. Human timeframes remain unknown due to lack of clinical trial data.

### Is acacetin safe for pregnant or breastfeeding women?

There is insufficient clinical data on acacetin safety during pregnancy and lactation, so it should be avoided by pregnant and breastfeeding women until further research is available. Most supplement manufacturers recommend consulting with a healthcare provider before use in these populations due to the lack of established safety profiles.

### What is the difference between acacetin and other flavonoids for heart health?

Acacetin is a methylated flavone that specifically targets cardiac ion channels and NF-κB signaling pathways, making it particularly effective for preventing arrhythmias, whereas other flavonoids like quercetin or hesperidin work primarily through general antioxidant mechanisms. Research shows acacetin has a more direct electrophysiological effect on heart tissue compared to standard flavonoid antioxidants.

### What does current research show about acacetin's effectiveness in humans versus animal studies?

Most evidence for acacetin comes from in vitro and animal studies (dogs, mice, and cell cultures) demonstrating benefits for cardiac arrhythmias, liver cancer, and neuroinflammation. Human clinical trials remain limited, so while the mechanistic research is promising, efficacy and optimal dosing in people have not been fully established through large-scale controlled studies.

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