Herbal

Indole-3-Carbinol

Also known as: I3C, Indole-3-carbinol, 3-indolecarbinol

Overview

Indole-3-carbinol (I3C) is a phytochemical derived from the breakdown of glucobrassicin in cruciferous vegetables such as broccoli, cabbage, and Brussels sprouts. It has been studied for its potential anticancer, antioxidant, and anti-inflammatory properties. I3C modulates xenobiotic metabolism by inducing phase I and phase II detoxification enzymes, particularly through activation of the aryl hydrocarbon receptor (AhR), leading to altered estrogen metabolism and increased production of less carcinogenic metabolites (e.g., 2-hydroxyestrone over 16α-hydroxyestrone). It also demonstrates free radical scavenging activity, particularly against reactive oxygen species such as hydroxyl and superoxide radicals, suggesting a role in oxidative stress reduction [1]. In preclinical models, I3C has shown antiproliferative effects in hormone-dependent cancers, including breast and prostate cancer, likely through cell cycle arrest and induction of apoptosis. Additionally, structural analogs of indole compounds, including melatonin-related indolamines, exhibit significant antioxidant activity via direct radical scavenging mechanisms, supporting the broader biological relevance of the indole scaffold . However, human clinical evidence remains limited, and most data are derived from in vitro and animal studies.

Dosage Guide

Therapeutic Doses

For treatment of specific conditions

General antioxidant support200-400 mg/dayTypical supplemental range from clinical studies
Hormone balance, estrogen metabolism300-400 mg/dayUsed in trials focusing on estrogen-related conditions
Cervical dysplasia (off-label)200-400 mg/daySmall clinical trials suggest potential benefit in mild dysplasia

Special Forms

Alternative forms for specific needs

Diindolylmethane (DIM)

More stable metabolite of I3C; used for similar indications with better bioavailability

Clinical Notes

  • I3C may interact with hormonal therapies due to its effects on estrogen metabolism.
  • High doses may cause gastrointestinal upset or hormone-related symptoms such as headaches or menstrual changes.
  • I3C can form acid condensation products in the stomach; enteric-coated formulations may improve stability and efficacy.
  • Limited long-term safety data; not recommended for pregnant or breastfeeding women outside of dietary intake.
  • Use with caution in individuals with thyroid disorders due to potential goitrogenic effects observed in animal models.

Research

Key FindingsPubMed
1

N-substituted indole-2-carboxylic acid esters show hydroxyl and superoxide radical scavenging activity in vitro.

In vitro scavenging activity for reactive oxygen species by N-substituted indole-2-carboxylic acid esters.
Luminescence : the journal of biological and chemical luminescence2007
2

Indole derivatives exhibit diverse biological activities including anticancer, antioxidant, and anti-inflammatory effects.

Chemistry and biology of indoles and indazoles: a mini-review.
Mini reviews in medicinal chemistry2013
3

Melatonin derivatives, structurally related to indoles, show improved free radical scavenging compared to vitamin C in DPPH assays.

Free radical scavenging and antioxidative activity of melatonin derivatives.
The Journal of pharmacy and pharmacology2003
4

Free radical scavengers like MCI-186 reduce myocardial necrosis in rabbit ischemia-reperfusion models.

Myocardial protection of MCI-186 in rabbit ischemia-reperfusion.
Life sciences2002
5

Melatonin and related indolamines scavenge hydroxyl radicals via a multi-step mechanism involving the indole ring.

Hydroxyl radical scavenging activity of melatonin and its related indolamines.
Free radical research2020
6

Melatonin, an indole derivative, has pan-antiviral effects and is proposed as a therapeutic for SARS-CoV-2 due to antioxidant and anti-inflammatory actions.

Melatonin: highlighting its use as a potential treatment for SARS-CoV-2 infection.
Cellular and molecular life sciences : CMLS2022
7

Substituted indole β-carbolines show antioxidant, anticancer, and anti-inflammatory activities.

Synthesis and diverse biological activities of substituted indole β-carbolines: a review.
Natural product research2024

Products Containing Indole-3-Carbinol(1 report)