Natural products as butyrylcholinesterase inhibitors - Screening of a small compound collection

D Karlsson, Adyary Fallarero, I Busygin, Reko Leino, P Vuorela

    Research output: Contribution to journalArticleScientificpeer-review

    Abstract

    Investigation of the involvement of butyrylcholinesterase (BChE) in diseases such as Alzheimer's disease (AD), type 2 diabetes mellitus (T2DM) and multiple sclerosis (MS) makes it a valuable target for drug discovery. Cholinesterase inhibitors of natural origin have shown success in AD therapy and have encouraged further exploration of nature as a source of cholinesterase inhibitors. Using the Ellman's reaction a collection of 111 compounds containing commercially available compounds e.g. flavonoids and coumarins, as well as a subset of cinchona alkaloid derivatives synthesized by our group, were screened for anti-cholinesterase activity. Two cinchona alkaloids were found to inhibit the hydrolase activity of BChE in the micromolar range (IC50 ≤10µM) and were further characterized. Considering their wide medical use (mostly as antimalarials) the cinchona alkaloid scaffold may serve as an advantage in drug development for various diseases.

    Original languageUndefined/Unknown
    Pages (from-to)1102–1102
    Number of pages1
    JournalPlanta Medica
    Volume78
    Issue number11
    DOIs
    Publication statusPublished - 2012
    MoE publication typeA1 Journal article-refereed

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