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- 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.
- Authors
Tsai, Pei-Ching; Wu, Yi-Kai; Hu, Jun-Hao; Li, I-Chen; Lin, Ting-Wei; Chen, Chin-Chu; Kuo, Chia-Feng
- Abstract
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.
- Subjects
HERICIUM erinaceus; BIOAVAILABILITY; PROTEIN binding; BINDING site assay; SPRAGUE Dawley rats; BIOACTIVE compounds
- Publication
Molecules, 2021, Vol 26, Issue 15, p4510
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules26154510