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Mar. Drugs 2018, 16(3), 94; https://doi.org/10.3390/md16030094

Anti-BACE1 and Antimicrobial Activities of Steroidal Compounds Isolated from Marine Urechis unicinctus

1
College of Chemistry and Pharmaceutical Science, Qingdao Agricultural University, Changcheng Rd, Chengyang district, Qingdao 266109, China
2
School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou 325035, China
3
Division of Crop Protection, National Institute of Agricultural Science, Rural Development Administration, Jeollabuk-do 55365, Korea
4
Department of Agricultural Biotechnology, Seoul National University, 599 Gwanak-ro, Silim-dong, Gwanak-Gu, Seoul 151742, Korea
5
Department of Plant Science, University of Connecticut, 1376 Storrs Road, U-4163, Storrs, CT 06269, USA
*
Author to whom correspondence should be addressed.
Received: 27 December 2017 / Revised: 1 February 2018 / Accepted: 12 March 2018 / Published: 14 March 2018
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Abstract

The human β-site amyloid cleaving enzyme (BACE1) has been considered as an effective drug target for treatment of Alzheimer’s disease (AD). In this study, Urechis unicinctus (U. unicinctus), which is a Far East specialty food known as innkeeper worm, ethanol extract was studied by bioassay-directed fractionation and isolation to examine its potential β-site amyloid cleaving enzyme inhibitory and antimicrobial activity. The following compounds were characterized: hecogenin, cholest-4-en-3-one, cholesta-4,6-dien-3-ol, and hurgadacin. These compounds were identified by their mass spectrometry, 1H, and 13C NMR spectral data, comparing those data with NIST/EPA/NIH Mass spectral database (NIST11) and published values. Hecogenin and cholest-4-en-3-one showed significant inhibitory activity against BACE1 with EC50 values of 116.3 and 390.6 µM, respectively. Cholesta-4,6-dien-3-ol and hurgadacin showed broad spectrum antimicrobial activity, particularly strongly against Escherichia coli (E. coli), Salmonella enterica (S. enterica), Pasteurella multocida (P. multocida), and Physalospora piricola (P. piricola), with minimal inhibitory concentration (MIC) ranging from 0.46 to 0.94 mg/mL. This is the first report regarding those four known compounds that were isolated from U. unicinctus and their anti-BACE1 and antimicrobial activity, highlighting the fact that known natural compounds may be a critical source of new medicine leads. These findings provide scientific evidence for potential application of those bioactive compounds for the development of AD drugs and antimicrobial agents. View Full-Text
Keywords: Alzheimer’s disease; antimicrobial activity; BACE1; bioassay-directed isolation; marine bioactive; Urechis unicinctus Alzheimer’s disease; antimicrobial activity; BACE1; bioassay-directed isolation; marine bioactive; Urechis unicinctus
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Zhu, Y.-Z.; Liu, J.-W.; Wang, X.; Jeong, I.-H.; Ahn, Y.-J.; Zhang, C.-J. Anti-BACE1 and Antimicrobial Activities of Steroidal Compounds Isolated from Marine Urechis unicinctus. Mar. Drugs 2018, 16, 94.

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