Laura A Calvo-Castro1,2, Markus Burkard3, Nadine Sus1, Gabriel Scheubeck4, Christian Leischner3, Ulrich M Lauer4, Anja Bosy-Westphal5, Verena Hund6, Christian Busch7, Sascha Venturelli3, Jan Frank1. 1. Institute of Biological Chemistry and Nutrition, University of Hohenheim, Stuttgart, Germany. 2. Centro de Investigación en Biotecnología, Instituto Tecnológico de Costa Rica, Cartago, Costa Rica. 3. Institute of Physiology, Department of Vegetative and Clinical Physiology, University Hospital Tuebingen, Tuebingen, Germany. 4. Department of Internal Medicine VIII, University Hospital Tuebingen, Tuebingen, Germany. 5. Institute of Nutritional Medicine, University of Hohenheim, Stuttgart, Germany. 6. Hospital Pharmacy, University Hospital Tuebingen, Tuebingen, Germany. 7. Department of Dermatology and Allergology, University of Tuebingen, Tuebingen, Germany.
Abstract
SCOPE: Prenylated chalcones and flavonoids from hop (Humulus lupulus L.), such as 6-prenylnaringenin (6-PN) and 8-prenylnaringenin (8-PN), are investigated for their health beneficial and anticancer activities. We, thus, compare the oral bioavailability and safety of 6-PN and 8-PN in healthy young women and men, and investigated their effects on peripheral blood mononuclear cells (PBMC). METHODS AND RESULTS: A double-blind, placebo-controlled, crossover trial is conducted with 16 healthy volunteers (eight women, eight men) given asingle oral dose of 500 mg 6-PN, 8-PN, or placebo in random order. Maximum total concentrations of 6-PN and 8-PN in plasma (Cmax ; 543 and 2834 nmol L-1 ) and their respective area under the plasma concentration-time curve (AUC; 3635 and 15801 nmol L-1 × h) are significantly (5.2- and 4.3-fold) higher for 8-PN than for 6-PN (p ˂ 0.05). PBMC for ex vivo experiments are isolated from blood sampled before and 6 h after intake of 6-PN, 8-PN, or placebo. Despite the single-treatment regime and low blood concentrations, both 6-PN and 8-PN increase the survival of PBMC relative to control. CONCLUSION:8-PN is significantly more bioavailable in healthy humans than its isomer 6-PN. Interestingly, 6-PN, despite being less bioavailable, is similarly effective as 8-PN in enhancing PBMC viability.
RCT Entities:
SCOPE: Prenylated chalcones and flavonoids from hop (Humulus lupulus L.), such as 6-prenylnaringenin (6-PN) and 8-prenylnaringenin (8-PN), are investigated for their health beneficial and anticancer activities. We, thus, compare the oral bioavailability and safety of 6-PN and 8-PN in healthy young women and men, and investigated their effects on peripheral blood mononuclear cells (PBMC). METHODS AND RESULTS: A double-blind, placebo-controlled, crossover trial is conducted with 16 healthy volunteers (eight women, eight men) given a single oral dose of 500 mg 6-PN, 8-PN, or placebo in random order. Maximum total concentrations of 6-PN and 8-PN in plasma (Cmax ; 543 and 2834 nmol L-1 ) and their respective area under the plasma concentration-time curve (AUC; 3635 and 15801 nmol L-1 × h) are significantly (5.2- and 4.3-fold) higher for 8-PN than for 6-PN (p ˂ 0.05). PBMC for ex vivo experiments are isolated from blood sampled before and 6 h after intake of 6-PN, 8-PN, or placebo. Despite the single-treatment regime and low blood concentrations, both 6-PN and 8-PN increase the survival of PBMC relative to control. CONCLUSION:8-PN is significantly more bioavailable in healthy humans than its isomer 6-PN. Interestingly, 6-PN, despite being less bioavailable, is similarly effective as 8-PN in enhancing PBMC viability.
Authors: Ryan T Hitzman; Tareisha L Dunlap; Caitlin E Howell; Shao-Nong Chen; Günter Vollmer; Guido F Pauli; Judy L Bolton; Birgit M Dietz Journal: Chem Res Toxicol Date: 2020-10-12 Impact factor: 3.739