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Article

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

1
Department of Food Science, Nutrition, and Nutraceutical Biotechnology, Shih Chien University, Taipei 10462, Taiwan
2
Biotech Research Institute, Grape King Bio Ltd., Taoyuan 32542, Taiwan
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Molecules 2021, 26(15), 4510; https://doi.org/10.3390/molecules26154510
Submission received: 15 June 2021 / Revised: 22 July 2021 / Accepted: 23 July 2021 / Published: 27 July 2021
(This article belongs to the Special Issue Bioactive Compounds from Nature: New Research and Prospects)

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.
Keywords: Hericium erinaceus mycelia; erinacine A; bioavailability; tissue distribution; excretion Hericium erinaceus mycelia; erinacine A; bioavailability; tissue distribution; excretion

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MDPI and ACS Style

Tsai, P.-C.; Wu, Y.-K.; Hu, J.-H.; Li, I.-C.; Lin, T.-W.; Chen, C.-C.; Kuo, C.-F. Preclinical Bioavailability, Tissue Distribution, and Protein Binding Studies of Erinacine A, a Bioactive Compound from Hericium erinaceus Mycelia Using Validated LC-MS/MS Method. Molecules 2021, 26, 4510. https://doi.org/10.3390/molecules26154510

AMA Style

Tsai P-C, Wu Y-K, Hu J-H, Li I-C, Lin T-W, Chen C-C, Kuo C-F. Preclinical Bioavailability, Tissue Distribution, and Protein Binding Studies of Erinacine A, a Bioactive Compound from Hericium erinaceus Mycelia Using Validated LC-MS/MS Method. Molecules. 2021; 26(15):4510. https://doi.org/10.3390/molecules26154510

Chicago/Turabian Style

Tsai, Pei-Ching, Yi-Kai Wu, Jun-Hao Hu, I-Chen Li, Ting-Wei Lin, Chin-Chu Chen, and Chia-Feng Kuo. 2021. "Preclinical Bioavailability, Tissue Distribution, and Protein Binding Studies of Erinacine A, a Bioactive Compound from Hericium erinaceus Mycelia Using Validated LC-MS/MS Method" Molecules 26, no. 15: 4510. https://doi.org/10.3390/molecules26154510

APA Style

Tsai, P.-C., Wu, Y.-K., Hu, J.-H., Li, I.-C., Lin, T.-W., Chen, C.-C., & Kuo, C.-F. (2021). Preclinical Bioavailability, Tissue Distribution, and Protein Binding Studies of Erinacine A, a Bioactive Compound from Hericium erinaceus Mycelia Using Validated LC-MS/MS Method. Molecules, 26(15), 4510. https://doi.org/10.3390/molecules26154510

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