Apigenin Side Effects
Apigenin is generally well-tolerated with minimal side effects reported in clinical contexts, though high-dose exposure may pose genotoxic risks, and its safety profile in humans requires further clinical investigation.
Primary Safety Concerns
Genotoxic Potential at High Doses
- High doses of apigenin (10-100 μM) demonstrated dose-dependent micronuclei induction in human lymphocytes, indicating potential clastogenic effects 1
- Flavonoids including apigenin may act as mutagens or pro-oxidants depending on consumption levels and physiological parameters 1
- This genotoxic hazard was demonstrated in vitro using cytochalasin-B blocked micronucleus assay in peripheral human lymphocytes 1
General Tolerability Profile
- Apigenin exhibits low toxicity on normal neuronal cells while maintaining cytotoxic effects on cancer cells 2
- The compound has been characterized as having minimal side effects compared to conventional immunosuppressive drugs used in autoimmune diseases 3
- Natural plant-derived compounds like apigenin are investigated specifically for their potential to provide therapeutic benefits with fewer adverse effects than synthetic pharmaceuticals 4, 5
Clinical Context and Bioavailability Issues
Absorption and Distribution Limitations
- Low bioavailability represents the primary limitation of apigenin rather than toxicity concerns 2
- The compound has unique ability to cross the blood-brain barrier, which is relevant for both therapeutic potential and safety considerations 2
- Nano-delivery systems using liposomes and poly lactic-co-glycolide nanoparticles have been developed to improve functionality and bioavailability 2
Important Caveats
Lack of Robust Human Safety Data
- Most safety and efficacy data derive from preclinical studies rather than clinical trials 4, 3
- Further clinical trials are needed to establish definitive safety profiles in human populations 4
- The dose-response relationship in humans remains poorly characterized 1