Oral Bioavailability and Bioactivity of Prenylflavonoids From Hops

Early Phase 1CompletedNCT03140397

University of Hohenheim16 enrolled

Overview

The prenylflavonoids 6-prenylnaringenin (6-PN) and 8-prenylnaringenin (8-PN) are secondary plant substances, almost exclusively found in hops (Humulus lupulus). Both compounds have known potential biological properties, but poor bioavailability due to their low oral absorption and retention. Our study followed a single dose (500 mg 6- or 8-PN), placebo controlled, randomized, double-blind, three armed crossover study design with ≥2-week washout periods. Plasma, PBMC and urine samples were collected at intervals up to 24 h after intake. Investigators investigated the safety, pharmacokinetics and impact of oral prenylflavonoids on the function of cells of the immune system.

Study Type

INTERVENTIONAL

Allocation

RANDOMIZED

Purpose

BASIC_SCIENCE

Masking

DOUBLE

Enrollment

Conditions

Safety After Oral Intake Pharmacokinetics After Oral Intake Immune Cells Activity

Interventions

PlaceboDIETARY_SUPPLEMENT

6-prenylnaringeninDIETARY_SUPPLEMENT

8-prenylnaringeninDIETARY_SUPPLEMENT

Eligibility

Sex: ALLMin age: 18 YearsMax age: 45 YearsHealthy volunteers:

Medical Language ↔ Plain English

Inclusion Criteria: * Healthy Volunteers with blood chemistry values within normal ranges * Age: 18-45 years * BMI: 19-25 kg/m2 Exclusion Criteria: * Pregnancy or lactation * Alcohol and/or drug abuse * Use of dietary supplements or any medications, except contraceptives * Any known malignant, metabolic and endocrine diseases * Previous cardiac infarction * Dementia * Participation in a clinical trial within the past 6 weeks prior to recruitment * Physical activity of more than 5 h/wk

Locations (2)

University of Hohenheim

Stuttgart, Baden-Wurttemberg, Germany

Eberhard Karls University Tuebingen

Tübingen, Baden-Wurttemberg, Germany

Outcomes

Primary Outcomes

Mean area under the curve (AUC) of plasma concentration vs. time of total 6-prenylnaringenin [nmol/L*h]

Total 6-PN after deconjugation with beta-glucuronidase/sulphatase

Time frame: 0, 0.5, 1, 2, 4, 6, 8 and 24 h post dose

Mean area under the curve (AUC) of plasma concentration vs. time of total 8-prenylnaringenin [nmol/L*h]

Total trans-epsilon-viniferin after deconjugation with beta-glucuronidase/sulphatase

Time frame: 0, 0.5, 1, 2, 4, 6, 8 and 24 h post dose

Mean maximum plasma concentration (Cmax) of total 6-prenylnaringenin [nmol/L]

Total trans-resveratrol after deconjugation with beta-glucuronidase/sulphatase

Time frame: 0, 0.5, 1, 2, 4, 6, 8 and 24 h post dose

Mean maximum plasma concentration (Cmax) of total 8-prenylnaringenin [nmol/L]

Total trans-epsilon-viniferin after deconjugation with beta-glucuronidase/sulphatase

Time frame: 0, 0.5, 1, 2, 4, 6, 8 and 24 h post dose

Time to reach maximum plasma concentration (Tmax) of total 6-prenylnaringenin [h]

Total trans-resveratrol after deconjugation with beta-glucuronidase/sulphatase

Time frame: 0, 0.5, 1, 2, 4, 6, 8 and 24 h post dose

Time to reach maximum plasma concentration (Tmax) of total 8-prenylnaringenin [h]

Total trans-epsilon-viniferin after deconjugation with beta-glucuronidase/sulphatase

Time frame: 0, 0.5, 1, 2, 4, 6, 8 and 24 h post dose

Cumulative urinary excretion of total 6-prenylnaringenin [nmol/g creatinine]

Total trans-resveratrol after deconjugation with beta-glucuronidase/sulphatase

Time frame: 0, 0.5, 1, 2, 4, 6, 8 and 24 h post dose

Cumulative urinary excretion of total 8-prenylnaringenin [nmol/g creatinine]

Total trans-epsilon-viniferin after deconjugation with beta-glucuronidase/sulphatase

Time frame: 0, 0.5, 1, 2, 4, 6, 8 and 24 h post dose

Cell count (dead cells/ml and living cells/ml) of PBMCs after 6-PN administration

Time frame: 0, 6, and 24 h post dose

Cell count (dead cells/ml and living cells/ml) of PBMCs after 8-PN administration

Time frame: 0, 6, and 24 h post dose

Cell viability of PBMCs after 6-PN administration

Time frame: 0, 6, and 24 h post dose

Cell viability of PBMCs after 8-PN administration

Time frame: 0, 6, and 24 h post dose