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Resources » Paper

Liew KF et al. (2018) Biomed Pharmacother "Multi-targeting aurones with monoamine oxidase and amyloid-beta inhibitory activities: Structure-activity relationship and translating multi-potency to neuroprotection."

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  • Comments on Liew KF et al. (2018) Biomed Pharmacother "Multi-targeting aurones with monoamine oxidase and amyloid-beta inhibitory activities: Structure-activity relationship and translating multi-potency to neuroprotection." (0)

  • Overview

    PMID:
    30466001
    DOI:
    10.1016/j.biopha.2018.11.054
    Status:
    Publication type:
    Journal_article
    WormBase ID:
    WBPaper00055779

    Liew KF, Lee EH, Chan KL, & Lee CY (2018). Multi-targeting aurones with monoamine oxidase and amyloid-beta inhibitory activities: Structure-activity relationship and translating multi-potency to neuroprotection. Biomed Pharmacother, 110, 118-128. doi:10.1016/j.biopha.2018.11.054

    Previously, a series of aurones bearing amine and carbamate functionalities was synthesized and evaluated for their cholinesterase inhibitory activity and drug-like attributes. In the present study, these aurones were evaluated for their multi-targeting properties in two Alzheimer's disease (AD)-related activities namely, monoamine oxidase (MAO) and amyloid-beta (A) inhibition. Evaluation of the aurones for MAO inhibitory activity disclosed several potent selective inhibitors of MAO-B, particularly those with 6-methoxyl group attached at ring A. Of the different amine moieties attached as side chains, pyrrolidine-bearing aurones were prominent as represented by 2-2, the most potent inhibitor. Evaluation on the A aggregation inhibition identified 4-3 as the best inhibitor with a percentage inhibition comparable to that of a known A inhibitor curcumin. Examination on the neuroprotective ability of the more drug-like aurone 4-3 in two Caenorhabditis elegans neurodegeneration models showed 4-3 to protect the nematodes against both A- and 6-hydroxydopamine-induced toxicities. These new activities further support 4-3 as a promising lead to develop the aurones as potential multipotent agents for neurodegenerative diseases.


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