Examination of the Bioavailability and Bioactivity of the Two Natural Food Ingredients 6-Prenylnaringenin and 8-Prenylnaringenin.
| Registry | NCT03140397 |
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| Status | Completed |
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| Phase | Early Phase 1 |
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| Study type | Interventional; randomized, crossover, masking: double, basic science |
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| Enrollment | 16 (Actual) |
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| Sponsor | University of Hohenheim (Other); collaborators: Universität Tübingen |
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| Conditions | Safety After Oral Intake, Pharmacokinetics After Oral Intake, Immune Cells Activity |
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| Interventions | Placebo, 6-prenylnaringenin, 8-prenylnaringenin (Dietary supplement) |
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| Dates | start 2016-01-01, primary completion 2017-04-01, completion 2017-12-31, first posted 2017-05-04, last updated 2018-03-30 |
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| Locations | 2 sites in Germany |
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-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.
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+Arms and interventions
| Arm | Type | Interventions | Description |
|---|
| Placebo | Placebo comparator | Dietary Supplement: Placebo | Capsules filled with mannitol and silicon dioxide |
| 6-prenylnaringenin | Experimental | Dietary Supplement: 6-prenylnaringenin | 500 mg 6-PN plus mannitol and silicon dioxide |
| 8-prenylnaringenin | Experimental | Dietary Supplement: 8-prenylnaringenin | 500 mg 8-PN plus mannitol and silicon dioxide |
- Placebo (Dietary supplement)
- 6-prenylnaringenin (Dietary supplement), also known as 6-PN
- 8-prenylnaringenin (Dietary supplement), also known as 8-PN
+Outcome measures
Primary outcomes
- Mean area under the curve (AUC) of plasma concentration vs. time of total 6-prenylnaringenin [nmol/L*h] [0, 0.5, 1, 2, 4, 6, 8 and 24 h post dose]: Total 6-PN after deconjugation with beta-glucuronidase/sulphatase
- Mean area under the curve (AUC) of plasma concentration vs. time of total 8-prenylnaringenin [nmol/L*h] [0, 0.5, 1, 2, 4, 6, 8 and 24 h post dose]: Total trans-epsilon-viniferin after deconjugation with beta-glucuronidase/sulphatase
- Mean maximum plasma concentration (Cmax) of total 6-prenylnaringenin [nmol/L] [0, 0.5, 1, 2, 4, 6, 8 and 24 h post dose]: Total trans-resveratrol after deconjugation with beta-glucuronidase/sulphatase
- Mean maximum plasma concentration (Cmax) of total 8-prenylnaringenin [nmol/L] [0, 0.5, 1, 2, 4, 6, 8 and 24 h post dose]: Total trans-epsilon-viniferin after deconjugation with beta-glucuronidase/sulphatase
- Time to reach maximum plasma concentration (Tmax) of total 6-prenylnaringenin [h] [0, 0.5, 1, 2, 4, 6, 8 and 24 h post dose]: Total trans-resveratrol after deconjugation with beta-glucuronidase/sulphatase
- Time to reach maximum plasma concentration (Tmax) of total 8-prenylnaringenin [h] [0, 0.5, 1, 2, 4, 6, 8 and 24 h post dose]: Total trans-epsilon-viniferin after deconjugation with beta-glucuronidase/sulphatase
- Cumulative urinary excretion of total 6-prenylnaringenin [nmol/g creatinine] [0, 0.5, 1, 2, 4, 6, 8 and 24 h post dose]: Total trans-resveratrol after deconjugation with beta-glucuronidase/sulphatase
- Cumulative urinary excretion of total 8-prenylnaringenin [nmol/g creatinine] [0, 0.5, 1, 2, 4, 6, 8 and 24 h post dose]: Total trans-epsilon-viniferin after deconjugation with beta-glucuronidase/sulphatase
- Cell count (dead cells/ml and living cells/ml) of PBMCs after 6-PN administration [0, 6, and 24 h post dose]
- Cell count (dead cells/ml and living cells/ml) of PBMCs after 8-PN administration [0, 6, and 24 h post dose]
- Cell viability of PBMCs after 6-PN administration [0, 6, and 24 h post dose]
- Cell viability of PBMCs after 8-PN administration [0, 6, and 24 h post dose]
Secondary outcomes
- Serum aspartate transaminase activity [U/L] [0, 4, 24h post-dose]
- Serum alanine transaminase activity [U/L] [0, 4, 24h post-dose]
- Serum gamma-glutamyl transferase activity [U/L] [0, 4, 24h post-dose]
- Serum alkaline phosphatase activity [U/L] [0, 4, 24h post-dose]
- Serum bilirubin [0, 4, 24h post-dose]
- Serum uric acid [mg/dL] [0, 4, 24h post-dose]
- Serum creatinine [mg/dL] [0, 4, 24h post-dose]
- Serum total cholesterol [mg/dL] [0, 4, 24h post-dose]
- Serum HDL cholesterol [mg/dL] [0, 4, 24h post-dose]
- Serum LDL cholesterol [mg/dL] [0, 4, 24h post-dose]
- Serum triacylglycerols [mg/dL] [0, 4, 24h post-dose]
- LDL/HDL cholesterol ratio [0, 4, 24h post-dose]
- Serum cystatin C [mg/mL] [0, 4, 24h post-dose]
- Glomerular filtration rate [mL/min] [0, 4, 24h post-dose]
- Serum glucose [mg/dL] [0, 24h post-dose]
- Hemoglobin [g/dL] [0, 24h post-dose]
- Mean corpuscular hemoglobin concentration [g/dL] [0, 24h post-dose]
- Mean corpuscular hemoglobin [pg] [0, 24h post-dose]
- Mean corpuscular volume [fL] [0, 24h post-dose]
- Hematocrit [%] [0, 24h post-dose]
- Erythrocytes [/pL] [0, 24h post-dose]
- Thrombocytes [/nL] [0, 24h post-dose]
- Leucocytes [/nL] [0, 24h post-dose]
- Segmented granulocytes [%] [0, 24h post-dose]
- Lymphocytes [%] [0, 24h post-dose]
- Monocytes [%] [0, 24h post-dose]
- Basophil granulocytes [%] [0, 24h post-dose]
- Eosinophil granulocytes [%] [0, 24h post-dose]
+Eligibility
Sex: All, ages: 18 Years to 45 Years, accepts healthy volunteers
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)
| Facility | City | Country | Status |
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| University of Hohenheim | Stuttgart, Baden-Wurttemberg | Germany | |
| Eberhard Karls University Tuebingen | Tübingen, Baden-Wurttemberg | Germany | |
+Publications
- Results publication: Calvo-Castro LA, Burkard M, Sus N, Scheubeck G, Leischner C, Lauer UM, Bosy-Westphal A, Hund V, Busch C, Venturelli S, Frank J. The Oral Bioavailability of 8-Prenylnaringenin from Hops (Humulus Lupulus L.) in Healthy Women and Men is Significantly Higher than that of its Positional Isomer 6-Prenylnaringenin in a Randomized Crossover Trial. Mol Nutr Food Res. 2018 Apr;62(7):e1700838. doi: 10.1002/mnfr.201700838. Epub 2018 Mar 1. PMID 29363261
+Investigators