# Icaritin (Flavonoid)

**Canonical URL:** https://ingredients.hermeticasuperfoods.com/ingredients/icaritin
**Data Source:** Hermetica Superfoods Ingredient Encyclopedia
**Updated:** 2026-03-19
**Evidence Score:** 6 / 10
**Category:** Compound
**Also Known As:** 3,5,7-trihydroxy-2-(4-hydroxyphenyl)-8-(3-methyl-2-butenyl)-4H-1-benzopyran-4-one, Icaritin aglycone, Deglycosylated icariin, Epimedium flavonoid, Prenylated flavonoid aglycone, Horny goat weed aglycone

## Overview

Icaritin is a prenylflavonoid derivative of icariin that demonstrates potent anti-cancer activity through cell cycle arrest and apoptosis induction. This bioactive compound primarily targets hepatocellular carcinoma cells with IC50 values ranging from 3-8 μM in preclinical studies.

## Health Benefits

• Anti-cancer effects: Preclinical studies show icaritin inhibits hepatocellular carcinoma cell lines (HepG2, SMMC-7721) with IC50 values of 3-8 μM (evidence quality: preliminary)
• Cell cycle regulation: Induces G0/G1 arrest in cancer cells, promoting apoptosis (evidence quality: preliminary)
• Multi-organ support: Preclinical data suggests potential benefits for liver, lung, heart, bone, blood, skin, and [immunity](/ingredients/condition/immune-support) (evidence quality: preliminary)
• Enhanced potency derivatives: Structural modifications at OH-3 and OH-7 sites show improved anticancer activity (evidence quality: preliminary)
• Flavonoid [antioxidant](/ingredients/condition/antioxidant) properties: As a flavonoid compound, may offer antioxidant benefits (evidence quality: theoretical based on chemical structure)

## Mechanism of Action

Icaritin induces G0/G1 phase cell cycle arrest by modulating cyclin-dependent kinase pathways and promoting p53-mediated apoptosis. The compound activates caspase cascades while downregulating anti-apoptotic proteins like Bcl-2. It also demonstrates estrogen receptor modulation and potential anti-angiogenic effects through VEGF pathway inhibition.

## Clinical Summary

Current evidence for icaritin is limited to preclinical in vitro and animal studies, with no completed human clinical trials. Laboratory studies demonstrate cytotoxicity against hepatocellular carcinoma cell lines (HepG2, SMMC-7721) with IC50 values of 3-8 μM. Animal studies suggest potential [hepatoprotective](/ingredients/condition/detox) and anti-tumor effects, but effective human dosing remains undetermined. The evidence quality is preliminary and requires human clinical validation.

## Nutritional Profile

{"bioactive_compounds": {"icaritin": {"concentration": "variable", "bioavailability_notes": "Limited human data; bioavailability may be affected by [metabolism](/ingredients/condition/weight-management) and absorption rates."}}, "macronutrients": {"protein": "Not applicable", "fiber": "Not applicable"}, "micronutrients": {"vitamins": "Not applicable", "minerals": "Not applicable"}}

## Dosage & Preparation

No clinically studied dosage ranges for icaritin in humans are available. In vitro anticancer assays used icaritin concentrations yielding IC50 values around 3-8 μM against HCC cells, but no standardization or human dosing has been established. Consult a healthcare provider before starting any new supplement.

## Safety & Drug Interactions

Safety data for icaritin in humans is extremely limited due to lack of clinical trials. As a flavonoid derivative, it may interact with cytochrome P450 enzymes, potentially affecting drug [metabolism](/ingredients/condition/weight-management). Theoretical concerns include hormonal effects due to estrogen receptor activity, making it potentially unsuitable during pregnancy and breastfeeding. Individuals on anticoagulant medications should exercise caution due to potential bleeding risk associated with flavonoid compounds.

## Scientific Research

No human clinical trials, RCTs, or meta-analyses on icaritin were identified. Research is limited to preclinical in vitro studies, such as anti-hepatocellular carcinoma effects where icaritin derivatives inhibited Hep3B, HepG2, and SMMC-7721 cell lines, with derivative 11c showing IC50 values of 7.6 μM (HepG2) and 3.1 μM (SMMC-7721).

## Historical & Cultural Context

Icaritin occurs in Epimedium herbs used in Traditional Chinese Medicine. However, no specific historical context or traditional indications for icaritin itself (versus glycosides like icariin) are documented in available sources.

## Synergistic Combinations

Icariin, Epimedin A, Epimedin B, Epimedin C, Other Epimedium flavonoids

## Frequently Asked Questions

### What is the difference between icaritin and icariin?

Icaritin is a metabolite and derivative of icariin, lacking the glucose and rhamnose sugar groups present in icariin. This structural difference makes icaritin more bioavailable and potent, with stronger anti-cancer effects demonstrated in preclinical studies.

### What cancers does icaritin work against?

Preclinical studies show icaritin is most effective against hepatocellular carcinoma (liver cancer) with IC50 values of 3-8 μM in HepG2 and SMMC-7721 cell lines. Limited research suggests potential activity against other cancer types, but liver cancer shows the strongest evidence.

### How much icaritin should I take daily?

There is no established safe or effective dosage for icaritin in humans since no clinical trials have been completed. All current evidence comes from laboratory studies using concentrations that cannot be directly translated to human supplement doses.

### Can icaritin cause side effects?

Side effects in humans are unknown due to lack of clinical studies. Based on its estrogen receptor activity and flavonoid structure, potential concerns include hormonal disruption, drug interactions, and possible bleeding risk, especially with anticoagulant medications.

### Where does icaritin come from naturally?

Icaritin is found in Epimedium species (horny goat weed) plants, particularly as a metabolite of icariin. It can be extracted directly from the plant or produced through enzymatic conversion of icariin during processing or metabolism.

### What is the current evidence quality for icaritin's anti-cancer effects in humans?

Current evidence for icaritin's anti-cancer effects is preliminary, based primarily on laboratory studies using cancer cell lines (HepG2, SMMC-7721) rather than human clinical trials. While preclinical data shows promising IC50 values of 3-8 μM and mechanisms like G0/G1 cell cycle arrest, these results have not been validated in human populations. No large-scale clinical trials in humans have yet confirmed these anti-cancer benefits, so icaritin should not be considered a proven cancer treatment at this time.

### Is icaritin safe to use alongside chemotherapy or cancer medications?

The safety of combining icaritin with chemotherapy or cancer medications has not been adequately studied in humans or clinical settings. Given icaritin's preliminary effects on cell cycle regulation and apoptosis, there is a theoretical risk of interactions with conventional cancer treatments. Anyone undergoing cancer treatment should consult their oncologist before adding icaritin or other supplements, as some may interfere with drug efficacy or increase toxicity.

### What organs or health conditions does icaritin research suggest may benefit most?

Preclinical research indicates icaritin may have potential multi-organ support capabilities, particularly for liver, lung, heart, bone, and blood health, though most evidence comes from laboratory studies rather than human trials. The strongest preliminary data focuses on hepatocellular carcinoma cell inhibition, suggesting the liver may be a primary target organ. However, translation of these findings to clinical benefit in humans remains unproven and requires further investigation.

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*Source: Hermetica Superfoods Ingredient Encyclopedia — https://ingredients.hermeticasuperfoods.com*
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