Oral Bioavailability and Bioactivity of Prenylflavonoids From Hops

Pharmacokinetics After Oral Intake Clinical Trial

Official title:

Examination of the Bioavailability and Bioactivity of the Two Natural Food Ingredients 6-Prenylnaringenin and 8-Prenylnaringenin.

Clinical Trial Details — Status: Completed

Administrative data

• NCT number: NCT03140397
• Other study ID #: HS-PF1-2016
• Status: Completed
• Phase: Early Phase 1
• First received: May 2, 2017
• Last updated: March 29, 2018
• Start date: January 2016
• Est. completion date: December 31, 2017

Study information

• Verified date: March 2018
• Source: University of Hohenheim
• Contact: n/a
• Is FDA regulated: No
• Study type: Interventional

Clinical Trial Summary

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.

Recruitment information / eligibility

• Status: Completed
• Enrollment: 16
• Est. completion date: December 31, 2017
• Est. primary completion date: April 2017
• Accepts healthy volunteers: Accepts Healthy Volunteers
• Gender: All
• Age group: 18 Years to 45 Years

Eligibility

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

Related Conditions & MeSH terms

• Immune Cells Activity
• Pharmacokinetics After Oral Intake
• Safety After Oral Intake

Intervention

Dietary Supplement:
• Placebo

• 6-prenylnaringenin

• 8-prenylnaringenin

Locations

Country	Name	City	State
Germany	University of Hohenheim	Stuttgart	Baden-Württemberg
Germany	Eberhard Karls University Tuebingen	Tübingen	Baden-Württemberg

Sponsors (2)

Lead Sponsor	Collaborator
University of Hohenheim	Universität Tübingen

Country where clinical trial is conducted

Germany, 

Outcome

Type	Measure	Description	Time frame	Safety issue
Primary	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	0, 0.5, 1, 2, 4, 6, 8 and 24 h post dose
Primary	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	0, 0.5, 1, 2, 4, 6, 8 and 24 h post dose
Primary	Mean maximum plasma concentration (Cmax) of total 6-prenylnaringenin [nmol/L]	Total trans-resveratrol after deconjugation with beta-glucuronidase/sulphatase	0, 0.5, 1, 2, 4, 6, 8 and 24 h post dose
Primary	Mean maximum plasma concentration (Cmax) of total 8-prenylnaringenin [nmol/L]	Total trans-epsilon-viniferin after deconjugation with beta-glucuronidase/sulphatase	0, 0.5, 1, 2, 4, 6, 8 and 24 h post dose
Primary	Time to reach maximum plasma concentration (Tmax) of total 6-prenylnaringenin [h]	Total trans-resveratrol after deconjugation with beta-glucuronidase/sulphatase	0, 0.5, 1, 2, 4, 6, 8 and 24 h post dose
Primary	Time to reach maximum plasma concentration (Tmax) of total 8-prenylnaringenin [h]	Total trans-epsilon-viniferin after deconjugation with beta-glucuronidase/sulphatase	0, 0.5, 1, 2, 4, 6, 8 and 24 h post dose
Primary	Cumulative urinary excretion of total 6-prenylnaringenin [nmol/g creatinine]	Total trans-resveratrol after deconjugation with beta-glucuronidase/sulphatase	0, 0.5, 1, 2, 4, 6, 8 and 24 h post dose
Primary	Cumulative urinary excretion of total 8-prenylnaringenin [nmol/g creatinine]	Total trans-epsilon-viniferin after deconjugation with beta-glucuronidase/sulphatase	0, 0.5, 1, 2, 4, 6, 8 and 24 h post dose
Primary	Cell count (dead cells/ml and living cells/ml) of PBMCs after 6-PN administration		0, 6, and 24 h post dose
Primary	Cell count (dead cells/ml and living cells/ml) of PBMCs after 8-PN administration		0, 6, and 24 h post dose
Primary	Cell viability of PBMCs after 6-PN administration		0, 6, and 24 h post dose
Primary	Cell viability of PBMCs after 8-PN administration		0, 6, and 24 h post dose
Secondary	Serum aspartate transaminase activity [U/L]		0, 4, 24h post-dose
Secondary	Serum alanine transaminase activity [U/L]		0, 4, 24h post-dose
Secondary	Serum gamma-glutamyl transferase activity [U/L]		0, 4, 24h post-dose
Secondary	Serum alkaline phosphatase activity [U/L]		0, 4, 24h post-dose
Secondary	Serum bilirubin		0, 4, 24h post-dose
Secondary	Serum uric acid [mg/dL]		0, 4, 24h post-dose
Secondary	Serum creatinine [mg/dL]		0, 4, 24h post-dose
Secondary	Serum total cholesterol [mg/dL]		0, 4, 24h post-dose
Secondary	Serum HDL cholesterol [mg/dL]		0, 4, 24h post-dose
Secondary	Serum LDL cholesterol [mg/dL]		0, 4, 24h post-dose
Secondary	Serum triacylglycerols [mg/dL]		0, 4, 24h post-dose
Secondary	LDL/HDL cholesterol ratio		0, 4, 24h post-dose
Secondary	Serum cystatin C [mg/mL]		0, 4, 24h post-dose
Secondary	Glomerular filtration rate [mL/min]		0, 4, 24h post-dose
Secondary	Serum glucose [mg/dL]		0, 24h post-dose
Secondary	Hemoglobin [g/dL]		0, 24h post-dose
Secondary	Mean corpuscular hemoglobin concentration [g/dL]		0, 24h post-dose
Secondary	Mean corpuscular hemoglobin [pg]		0, 24h post-dose
Secondary	Mean corpuscular volume [fL]		0, 24h post-dose
Secondary	Hematocrit [%]		0, 24h post-dose
Secondary	Erythrocytes [/pL]		0, 24h post-dose
Secondary	Thrombocytes [/nL]		0, 24h post-dose
Secondary	Leucocytes [/nL]		0, 24h post-dose
Secondary	Segmented granulocytes [%]		0, 24h post-dose
Secondary	Lymphocytes [%]		0, 24h post-dose
Secondary	Monocytes [%]		0, 24h post-dose
Secondary	Basophil granulocytes [%]		0, 24h post-dose
Secondary	Eosinophil granulocytes [%]		0, 24h post-dose

External Links

•   Website of the research group