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  3. Comparative analysis of stilbene and benzofuran neolignan derivatives as acetylcholinesterase inhibitors with neuroprotective and anti-inflammatory activities

Comparative analysis of stilbene and benzofuran neolignan derivatives as acetylcholinesterase inhibitors with neuroprotective and anti-inflammatory activities

  • Bioorg Med Chem Lett. 2019 Sep 1;29(17):2475-2479. doi: 10.1016/j.bmcl.2019.07.026.
Mina Nagumo 1,  Masayuki Ninomiya 1,  Natsuko Oshima 1,  Tomohiro Itoh 2,  Kaori Tanaka 3,  Atsuyoshi Nishina 4,  Mamoru Koketsu 5
Affiliations

Affiliations

  • 1 Department of Chemistry and Biomolecular Science, Faculty of Engineering, Gifu University, 1-1 Yanagido, Gifu 501-1193, Japan.
  • 2 Laboratory for Molecular Chemistry of Aquatic Materials, Department of Life Sciences, Graduate School of Bioresources, Mie University, 1577 Kurimamachiya, Tsu, Mie 514-8507, Japan.
  • 3 Division of Anaerobe Research, Life Science Research Center, Gifu University, 1-1 Yanagido, Gifu 501-1194, Japan; United Graduate School of Drug Discovery and Medicinal Information Sciences, Gifu University, 1-1 Yanagido, Gifu 501-1194, Japan.
  • 4 College of Science and Technology, Nihon University, Chiyoda, Tokyo 101-0062, Japan.
  • 5 Department of Chemistry and Biomolecular Science, Faculty of Engineering, Gifu University, 1-1 Yanagido, Gifu 501-1193, Japan. Electronic address: koketsu@gifu-u.ac.jp.
PMID: 31350127 DOI: 10.1016/j.bmcl.2019.07.026
Abstract

Stilbenes and benzofuran neolignans are important groups of plant phenolics therefore they play a significant role in Plants and human health. The objective of this study was to investigate the structure-activity relationships of naturally occurring stilbene and benzofuran neolignan derivatives as acetylcholinesterase inhibitors. A series of these compounds were prepared and assessed for their inhibition on acetylcholinesterase activity. δ-Viniferin, pterostilbene trans-dehydrodimer, pallidol, grossamide, and boehmenan exerted acetylcholinesterase inhibitory potential. The several oligomeric compounds protected against cell damage resulting from t-BHP exposure and inhibited lipopolysaccharide/interferon-gamma (LPS/IFNγ)-induced NO production in vitro. Our findings highlight the great potential of pterostilbene trans-dehydrodimer, pallidol, and boehmenan as multifunctional nutraceuticals for management of neurodegenerative diseases.

Keywords

Acetylcholinesterase inhibitor; Anti-inflammatory activity; Benzofuran neolignan; Neuroprotective activity; Stilbene dimer.

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