Hopeahainol A: An Acetylcholinesterase Inhibitor from Hopea hainanensis

Authors

  • Hui Ming Ge Dr.,

    1. Institute of Functional Biomolecules, State Key Laboratory of Pharmaceutical Biotechnology, School of Medicine, Nanjing University, Nanjing, 210093, PR China, Fax: (+86) 25-8330-2728
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  • Chun Hua Zhu,

    1. Institute of Functional Biomolecules, State Key Laboratory of Pharmaceutical Biotechnology, School of Medicine, Nanjing University, Nanjing, 210093, PR China, Fax: (+86) 25-8330-2728
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  • Da Hua Shi,

    1. Institute of Functional Biomolecules, State Key Laboratory of Pharmaceutical Biotechnology, School of Medicine, Nanjing University, Nanjing, 210093, PR China, Fax: (+86) 25-8330-2728
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  • Li Dong Zhang Dr.,

    1. Department of Chemistry and Institute of Theoretical and Computational Chemistry, Key Laboratory of Mesoscopic Chemistry, Nanjing University, Nanjing 210093, PR China
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  • Dai Qian Xie Prof.,

    1. Department of Chemistry and Institute of Theoretical and Computational Chemistry, Key Laboratory of Mesoscopic Chemistry, Nanjing University, Nanjing 210093, PR China
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  • Jie Yang Prof.,

    1. Institute of Functional Biomolecules, State Key Laboratory of Pharmaceutical Biotechnology, School of Medicine, Nanjing University, Nanjing, 210093, PR China, Fax: (+86) 25-8330-2728
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  • Seik Weng Ng Prof.,

    1. University of Malaya, Kuala Lumpur 50603, Malaysia
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  • Ren Xiang Tan Prof.

    1. Institute of Functional Biomolecules, State Key Laboratory of Pharmaceutical Biotechnology, School of Medicine, Nanjing University, Nanjing, 210093, PR China, Fax: (+86) 25-8330-2728
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Abstract

A phytochemical study of Hopea hainanensis has led to the isolation of three new polyphenols and one known compound. The most important of these compounds are hopeahainols A (2) and B (3), which contain an unprecedented carbon skeleton. The structures were elucidated by analysis of the spectroscopic data including single-crystal X-ray spectroscopy and computational methods. Hopeahainol A was an acetylcholinesterase inhibitor with an IC50 value of 4.33 μM, which is comparable to that of huperzine A, a presently prescribed drug for the treatment of Alzheimer, while other similar structures were inactive. This observation was complemented by a 3D interaction model of the inhibitor with active sites.

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