Acute balenine supplementation in humans as a natural carnosinase-resistant alternative to carnosine
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Dokumenter
- de Jager et al_Scientific Reports_2023_ Vol 13_e6484
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Balenine possesses some of carnosine’s and anserine’s functions, yet it appears more resistant to the hydrolysing CN1 enzyme. The aim of this study was to elucidate the stability of balenine in the systemic circulation and its bioavailability in humans following acute supplementation. Two experiments were conducted in which (in vitro) carnosine, anserine and balenine were added to plasma to compare degradation profiles and (in vivo) three increasing doses (1–4–10 mg/kg) of balenine were acutely administered to 6 human volunteers. Half-life of balenine (34.9 ± 14.6 min) was respectively 29.1 and 16.3 times longer than that of carnosine (1.20 ± 0.36 min, p = 0.0044) and anserine (2.14 ± 0.58 min, p = 0.0044). In vivo, 10 mg/kg of balenine elicited a peak plasma concentration (Cmax) of 28 µM, which was 4 and 18 times higher than with 4 (p = 0.0034) and 1 mg/kg (p = 0.0017), respectively. CN1 activity showed strong negative correlations with half-life (ρ = − 0.829; p = 0.0583), Cmax (r = − 0.938; p = 0.0372) and incremental area under the curve (r = − 0.825; p = 0.0433). Overall, balenine seems more resistant to CN1 hydrolysis resulting in better in vivo bioavailability, yet its degradation remains dependent on enzyme activity. Although a similar functionality as carnosine and anserine remains to be demonstrated, opportunities arise for balenine as nutraceutical or ergogenic aid.
Originalsprog | Engelsk |
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Artikelnummer | 6484 |
Tidsskrift | Scientific Reports |
Vol/bind | 13 |
Antal sider | 10 |
ISSN | 2045-2322 |
DOI | |
Status | Udgivet - 2023 |
Bibliografisk note
CURIS 2023 NEXS 115
Funding Information:
Sarah de Jager is a recipient of a PhD fellowship by Research Foundation Flanders (FWO).
Funding Information:
The plasma concentrations of HCDs were determined using an UHPLC-MS/MS instrument part of the Ghent University MSsmall Expertise Centre for advanced mass spectrometry analysis of small organic molecules. The practical contribution of Anneke Volkaert is greatly acknowledged. We thank Dr. Giulio Vistoli, Dr. Silvia Gervasoni, Dr. Luca Regazzoni and Dr. Giancarlo Aldini (University of Milano) for the discussion of results and in silico exploration of substrate specificity of the hPepT2 transporter that was valuable in interpretation of the data.
Publisher Copyright:
© 2023, The Author(s).
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