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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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Autores principales: Tsai, Pei-Ching, Wu, Yi-Kai, Hu, Jun-Hao, Li, I-Chen, Lin, Ting-Wei, Chen, Chin-Chu, Kuo, Chia-Feng
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8347307/
https://www.ncbi.nlm.nih.gov/pubmed/34361662
http://dx.doi.org/10.3390/molecules26154510
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author Tsai, Pei-Ching
Wu, Yi-Kai
Hu, Jun-Hao
Li, I-Chen
Lin, Ting-Wei
Chen, Chin-Chu
Kuo, Chia-Feng
author_facet Tsai, Pei-Ching
Wu, Yi-Kai
Hu, Jun-Hao
Li, I-Chen
Lin, Ting-Wei
Chen, Chin-Chu
Kuo, Chia-Feng
author_sort Tsai, Pei-Ching
collection PubMed
description 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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spelling pubmed-83473072021-08-08 Preclinical Bioavailability, Tissue Distribution, and Protein Binding Studies of Erinacine A, a Bioactive Compound from Hericium erinaceus Mycelia Using Validated LC-MS/MS Method Tsai, Pei-Ching Wu, Yi-Kai Hu, Jun-Hao Li, I-Chen Lin, Ting-Wei Chen, Chin-Chu Kuo, Chia-Feng Molecules Article 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. MDPI 2021-07-27 /pmc/articles/PMC8347307/ /pubmed/34361662 http://dx.doi.org/10.3390/molecules26154510 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Tsai, Pei-Ching
Wu, Yi-Kai
Hu, Jun-Hao
Li, I-Chen
Lin, Ting-Wei
Chen, Chin-Chu
Kuo, Chia-Feng
Preclinical Bioavailability, Tissue Distribution, and Protein Binding Studies of Erinacine A, a Bioactive Compound from Hericium erinaceus Mycelia Using Validated LC-MS/MS Method
title Preclinical Bioavailability, Tissue Distribution, and Protein Binding Studies of Erinacine A, a Bioactive Compound from Hericium erinaceus Mycelia Using Validated LC-MS/MS Method
title_full Preclinical Bioavailability, Tissue Distribution, and Protein Binding Studies of Erinacine A, a Bioactive Compound from Hericium erinaceus Mycelia Using Validated LC-MS/MS Method
title_fullStr Preclinical Bioavailability, Tissue Distribution, and Protein Binding Studies of Erinacine A, a Bioactive Compound from Hericium erinaceus Mycelia Using Validated LC-MS/MS Method
title_full_unstemmed Preclinical Bioavailability, Tissue Distribution, and Protein Binding Studies of Erinacine A, a Bioactive Compound from Hericium erinaceus Mycelia Using Validated LC-MS/MS Method
title_short Preclinical Bioavailability, Tissue Distribution, and Protein Binding Studies of Erinacine A, a Bioactive Compound from Hericium erinaceus Mycelia Using Validated LC-MS/MS Method
title_sort preclinical bioavailability, tissue distribution, and protein binding studies of erinacine a, a bioactive compound from hericium erinaceus mycelia using validated lc-ms/ms method
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8347307/
https://www.ncbi.nlm.nih.gov/pubmed/34361662
http://dx.doi.org/10.3390/molecules26154510
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