The Bioavailability of Xanthohumol in Humans and the Influence of Formulation and Dose: Randomized Controlled Trial...

Area of Science:

• Nutritional biochemistry
• Pharmacokinetics
• Human physiology

Background:

• Xanthohumol, a prenylated chalcone from hops, exhibits potential cardioprotective effects.
• Limited human studies exist on xanthohumol bioavailability and efficacy.
• Understanding xanthohumol absorption is crucial for its therapeutic application.

Purpose of the Study:

• To compare the bioavailability of micellar and native xanthohumol formulations in humans.
• To investigate the dose-dependent plasma kinetics of xanthohumol.
• To assess the acute bioactivity of micellar xanthohumol.

Main Methods:

• Randomized crossover bioavailability trial with micellar and native xanthohumol (86 mg and 172 mg).
• Plasma concentration analysis of xanthohumol and its metabolites (glucuronide, sulfate) up to 24 hours.
• Randomized placebo-controlled crossover bioactivity trial assessing resting energy expenditure, blood pressure, and heart rate.

Main Results:

• Micellation significantly increased the area under the plasma concentration-time curve (AUC) and maximum plasma concentration (p < 0.001).
• Bioavailability of micellar xanthohumol was approximately ninefold higher than the native form, irrespective of dose.
• No acute effects of 172 mg micellar xanthohumol on resting energy expenditure, blood pressure, or heart rate were observed.

Conclusions:

• Micellar formulation dramatically improves xanthohumol bioavailability in humans.
• Xanthohumol bioavailability is primarily influenced by micellation, not dose.
• Micellar xanthohumol lacks acute effects on key physiological parameters, warranting further investigation into chronic efficacy.