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  1. Article ; Online: Lerisetron Analogues with Antimalarial Properties

    Rudolf Mueller / Virsinha Reddy / Aloysius T. Nchinda / Fanuel Mebrahtu / Dale Taylor / Nina Lawrence / Lloyd Tanner / Marine Barnabe / Charles J. Eyermann / Bin Zou / Ravinder R. Kondreddi / Suresh B. Lakshminarayana / Matthias Rottmann / Leslie J. Street / Kelly Chibale

    ACS Omega, Vol 5, Iss 12, Pp 6967-

    Synthesis, Structure–Activity Relationship Studies, and Biological Assessment

    2020  Volume 6982

    Keywords Chemistry ; QD1-999
    Language English
    Publishing date 2020-03-01T00:00:00Z
    Publisher American Chemical Society
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  2. Article ; Online: Intestinal Transport Characteristics and Metabolism of C-Glucosyl Dihydrochalcone, Aspalathin

    Sandra Bowles / Elizabeth Joubert / Dalene de Beer / Johan Louw / Christel Brunschwig / Mathew Njoroge / Nina Lawrence / Lubbe Wiesner / Kelly Chibale / Christo Muller

    Molecules, Vol 22, Iss 4, p

    2017  Volume 554

    Abstract: Insight into the mechanisms of intestinal transport and metabolism of aspalathin will provide important information for dose optimisation, in particular for studies using mouse models. Aspalathin transportation across the intestinal barrier (Caco-2 ... ...

    Abstract Insight into the mechanisms of intestinal transport and metabolism of aspalathin will provide important information for dose optimisation, in particular for studies using mouse models. Aspalathin transportation across the intestinal barrier (Caco-2 monolayer) tested at 1–150 µM had an apparent rate of permeability (Papp) typical of poorly absorbed compounds (1.73 × 10−6 cm/s). Major glucose transporters, sodium glucose linked transporter 1 (SGLT1) and glucose transporter 2 (GLUT2), and efflux protein (P-glycoprotein, PgP) (1.84 × 10−6 cm/s; efflux ratio: 1.1) were excluded as primary transporters, since the Papp of aspalathin was not affected by the presence of specific inhibitors. The Papp of aspalathin was also not affected by constituents of aspalathin-enriched rooibos extracts, but was affected by high glucose concentration (20.5 mM), which decreased the Papp value to 2.9 × 10−7 cm/s. Aspalathin metabolites (sulphated, glucuronidated and methylated) were found in mouse urine, but not in blood, following an oral dose of 50 mg/kg body weight of the pure compound. Sulphates were the predominant metabolites. These findings suggest that aspalathin is absorbed and metabolised in mice to mostly sulphate conjugates detected in urine. Mechanistically, we showed that aspalathin is not actively transported by the glucose transporters, but presumably passes the monolayer paracellularly.
    Keywords aspalathin ; bioavailability ; Caco-2 ; transport ; metabolism ; Organic chemistry ; QD241-441
    Subject code 500
    Language English
    Publishing date 2017-03-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

    Full text online

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    Inter-library loan at ZB MED

    Your chosen title can be delivered directly to ZB MED Cologne location if you are registered as a user at ZB MED Cologne.

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