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

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

    Tutkimustuotos: LehtiartikkeliArtikkeliTieteellinenvertaisarvioitu


    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.

    AlkuperäiskieliEi tiedossa
    JulkaisuPlanta Medica
    DOI - pysyväislinkit
    TilaJulkaistu - 2012
    OKM-julkaisutyyppiA1 Julkaistu artikkeli, soviteltu