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
Special Forms
Alternative forms for specific needs
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
N-substituted indole-2-carboxylic acid esters show hydroxyl and superoxide radical scavenging activity in vitro.
Indole derivatives exhibit diverse biological activities including anticancer, antioxidant, and anti-inflammatory effects.
Melatonin derivatives, structurally related to indoles, show improved free radical scavenging compared to vitamin C in DPPH assays.
Free radical scavengers like MCI-186 reduce myocardial necrosis in rabbit ischemia-reperfusion models.
Melatonin and related indolamines scavenge hydroxyl radicals via a multi-step mechanism involving the indole ring.
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.
Substituted indole β-carbolines show antioxidant, anticancer, and anti-inflammatory activities.
