No disease. Investigation of the bioavailability and metabolism of iridoid glycosides (monotropein and its hydroxycinnamic acid esters) from Vaccinium myrtillus and Gaultheria poeppigii berries in healthy volunteers.
Conditions
Interventions
Group 1: 60 mg of monotropeine (pure substance) in 250 mL of drinking water
Group 2: Vaccinium myrtillus (freeze-dried, commercially sourced), equimolar to 60 mg of monotropein as vaccinoside, in 250
Sponsors
University of Hohenheim
Eligibility
Sex/Gender
All
Age
18 Years to 35 Years
Inclusion criteria
Inclusion criteria: Healthy, competent male and female volunteers aged 18–35 years. Prerequisites for inclusion: Body Mass Index (BMI) between 18.5 and 25 kg/m² Normal values within reference ranges of the contracted laboratory for: complete blood count; liver and kidney function parameters; lipid and glucose metabolism; inflammatory markers Normotensive blood pressure values Women using hormonal contraceptives may participate
Exclusion criteria
Exclusion criteria: Use of any medication (except hormonal contraceptives) Pregnancy or breastfeeding Known allergy or intolerance to berries or components of the study preparations Cardiovascular disease, diabetes mellitus, malignant disease, dementia or other serious chronic conditions Hypertension (>160/105 mmHg) Smoking or regular nicotine or drug use Excessive alcohol consumption Use of dietary supplements or multivitamin preparations Extreme physical activity (>5 hours of intense exercise per week) Restrictive dietary habits Participation in another clinical study within the last 6 weeks or concurrent participation in another study
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Plasma pharmacokinetic parameters of monotropein and its phase II metabolites (glucuronide and sulfate conjugates) following oral administration, including maximum plasma concentration (C_max), time to maximum concentration (T_max), area under the plasma concentration-time curve (AUC0?24), and elimination half-life (t1/2). Blood samples collected at 0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, and 24 h after oral administration. Quantification of monotropein and metabolites in plasma by LC-MS/MS (QTRAP 6500+) using a validated HILIC-Amide chromatographic method with stable isotope-labeled internal standard. | — |
Secondary
| Measure | Time frame |
|---|---|
| Endpoint 1: Urinary excretion of monotropein and its metabolites — cumulative urinary recovery (% of administered dose) over 24 h When: Urine collected as complete voids at 0–8, and 8–24 h intervals How: Quantification by LC-MS/MS as above; urine volume measured gravimetrically Endpoint 2: Relative bioavailability of monotropein from the test compounds vs. ester (monotropein vs vaccinoside, monotropein-10-trans-coumarate) — comparison of AUC values across the three intervention arms When: Derived from plasma pharmacokinetic profiles at all collection time points How: Non-compartmental pharmacokinetic analysis using Phoenix WinNonlin or R. Endpoint 3: Inter-individual variability in monotropein metabolism — identification of high vs. low metabolizer phenotypes based on metabolite ratios in plasma and urine When: Assessed from 24 h plasma and urine samples How: LC-MS/MS quantification of phase II metabolites relative to parent compound | — |
Countries
Germany
Contacts
Public ContactFelipe Jimenez Aspee
University of Hohenheim
Outcome results
None listed