Pterostilbene
Pterostilbene
Pterostilbene is a naturally occurring stilbenoid found in blueberries and grapes, structurally similar to resveratrol but with superior bioavailability due to two methoxy groups replacing hydroxyl groups. It is primarily used for its antioxidant, anti-inflammatory, and metabolic benefits, with research supporting applications in cardiovascular health, blood glucose regulation, cognitive function, and longevity-related pathways.
Mechanism of Action
Pterostilbene activates SIRT1 and AMPK pathways, mimicking caloric restriction and promoting mitochondrial biogenesis and cellular energy regulation. It inhibits NF-κB signaling to reduce pro-inflammatory cytokine production, and acts as a potent activator of Nrf2, upregulating endogenous antioxidant enzymes such as superoxide dismutase and catalase. Its enhanced lipophilicity compared to resveratrol results in approximately 80% oral bioavailability versus roughly 20% for resveratrol, with longer tissue retention.
Evidence by Health Goal(18 goals)
Dosing Protocols
With meals containing dietary fat to enhance absorption
Most human clinical trials have used 50-150mg/day for metabolic and cardiovascular benefits. Higher doses up to 250mg/day have been used for cognitive effects. Split dosing (e.g., 50-125mg twice daily) may provide more consistent plasma levels. Start at the lower end to assess tolerance.
Safety & Side Effects
Pterostilbene has a generally favorable safety profile with human trials up to 250mg/day demonstrating tolerability over several months; however, one clinical study noted LDL cholesterol increases at 250mg/day, warranting caution in individuals with dyslipidemia. It is not a controlled substance and is widely available as a dietary supplement, but safety data beyond 6-12 months and in pregnant or breastfeeding populations is limited.
Possible Side Effects
- !Mild gastrointestinal discomfort including nausea or loose stools at higher doses
- !Headache reported by some users, particularly at doses above 150mg/day
- !Elevations in LDL cholesterol observed in some clinical trials at higher doses (250mg/day)
- !Mild hypoglycemia risk in individuals with blood sugar regulation issues
- !Insomnia or sleep disturbance if taken late in the day
- !Rare allergic reactions including skin flushing in sensitive individuals
Interactions
- -May potentiate anticoagulant and antiplatelet drugs (warfarin, aspirin, clopidogrel) due to platelet aggregation inhibition - monitor bleeding risk
- -Additive blood glucose-lowering effect with metformin, insulin, or other antidiabetic medications - monitor glycemic levels
- -May inhibit CYP2C9 and CYP3A4 enzymes, potentially increasing plasma levels of drugs metabolized by these pathways
- -Synergistic antioxidant effects with resveratrol, quercetin, and other polyphenols - combinations are generally safe but may amplify effects
- -Can lower blood pressure - use caution when combined with antihypertensive medications due to additive hypotensive effects
Cost & Where to Buy
Cost varies by dose and brand; bulk powder is significantly cheaper than capsules. Quality third-party tested brands (e.g., NSF, Informed Sport certified) tend to be at the higher end of the range.
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