Preclinical Bioavailability, Tissue Distribution, and Protein Binding Studies of Erinacine A, a Bioactive Compound from Hericium erinaceus Mycelia Using Validated LC-MS/MS Method

Erinacine A, derived from the mycelia of Hericium erinaceus, has attracted much attention due to its neuroprotective properties. However, very few studies have been conducted on the bioavailability, tissue distribution, and protein binding of erinacine A. This study aimed to investigate the bioavail...

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Published inMolecules (Basel, Switzerland) Vol. 26; no. 15; p. 4510
Main Authors Tsai, Pei-Ching, Wu, Yi-Kai, Hu, Jun-Hao, Li, I-Chen, Lin, Ting-Wei, Chen, Chin-Chu, Kuo, Chia-Feng
Format Journal Article
LanguageEnglish
Published Basel MDPI AG 27.07.2021
MDPI
Subjects
Alzheimer's disease
Animals
Bias
Binding
Bioactive compounds
Bioavailability
Blood-brain barrier
Diffusion barriers
Dosage
erinacine A
excretion
Hericium erinaceus
Hericium erinaceus mycelia
Intravenous administration
Ischemia
Mycelia
Neuroprotection
Oral administration
Pharmacokinetics
Proteins
R&D
Research & development
tissue distribution
Tissues
Canada
United States > US
Taiwan
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Summary:Erinacine A, derived from the mycelia of Hericium erinaceus, has attracted much attention due to its neuroprotective properties. However, very few studies have been conducted on the bioavailability, tissue distribution, and protein binding of erinacine A. This study aimed to investigate the bioavailability, tissue distribution, and protein binding of erinacine A in Sprague-Dawley rats. After oral administration (po) and intravenous administration (iv) of 2.381 g/kg BW of the H. erinaceus mycelia extract (equivalent to 50 mg/kg BW of erinacine A) and 5 mg/kg BW of erinacine A, respectively, the absolute bioavailability of erinacine A was estimated as 24.39%. Erinacine A was detected in brain at 1 h after oral dosing and reached the peak at 8 h. Protein binding assay showed unbound erinacine A fractions in brain to blood ratio is close to unity, supporting passive diffusion as the dominating transport. Feces was the major route for the elimination of erinacine A. This study is the first to show that erinacine A can penetrate the blood-brain barrier of rats by the means of passive diffusion and thus support the development of H. erinaceus mycelia for the improvement of neurohealth.
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These authors contributed equally to this work.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules26154510