@article{HofmannFayezScheineretal.2020,
  author    = {Hofmann, Julian and Fayez, Shaimaa and Scheiner, Matthias and Hoffmann, Matthias and Oerter, Sabrina and Appelt-Menzel, Antje and Maher, Pamela and Maurice, Tangui and Bringmann, Gerhard and Decker, Michael},
  title     = {Sterubin: Enantioresolution and Configurational Stability, Enantiomeric Purity in Nature, and Neuroprotective Activity in Vitro and in Vivo},
  series = {Chemistry - A European Journal},
  volume    = {26},
  journal   = {Chemistry - A European Journal},
  number    = {32},
  doi       = {10.1002/chem.202001264},
  url       = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-215993},
  pages     = {7299 -- 7308},
  year      = {2020},
  abstract  = {Alzheimer′s disease (AD) is a neurological disorder with still no preventive or curative treatment. Flavonoids are phytochemicals with potential therapeutic value. Previous studies described the flavanone sterubin isolated from the Californian plant Eriodictyon californicum as a potent neuroprotectant in several in vitro assays. Herein, the resolution of synthetic racemic sterubin (1) into its two enantiomers, (R)-1 and (S)-1, is described, which has been performed on a chiral chromatographic phase, and their stereochemical assignment online by HPLC-ECD coupling. (R)-1 and (S)-1 showed comparable neuroprotection in vitro with no significant differences. While the pure stereoisomers were configurationally stable in methanol, fast racemization was observed in the presence of culture medium. We also established the occurrence of extracted sterubin as its pure (S)-enantiomer. Moreover, the activity of sterubin (1) was investigated for the first time in vivo, in an AD mouse model. Sterubin (1) showed a significant positive impact on short- and long-term memory at low dosages.},
  language  = {en}
}
@article{Appelt‐MenzelOerterMathewetal.2020,
  author    = {Appelt-Menzel, Antje and Oerter, Sabrina and Mathew, Sanjana and Haferkamp, Undine and Hartmann, Carla and Jung, Matthias and Neuhaus, Winfried and Pless, Ole},
  title     = {Human iPSC-Derived Blood-Brain Barrier Models: Valuable Tools for Preclinical Drug Discovery and Development?},
  series = {Current Protocols in Stem Cell Biology},
  volume    = {55},
  journal   = {Current Protocols in Stem Cell Biology},
  number    = {1},
  doi       = {10.1002/cpsc.122},
  url       = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-218509},
  year      = {2020},
  abstract  = {Translating basic biological knowledge into applications remains a key issue for effectively tackling neurodegenerative, neuroinflammatory, or neuroendocrine disorders. Efficient delivery of therapeutics across the neuroprotective blood-brain barrier (BBB) still poses a demanding challenge for drug development targeting central nervous system diseases. Validated in vitro models of the BBB could facilitate effective testing of drug candidates targeting the brain early in the drug discovery process during lead generation. We here review the potential of mono- or (isogenic) co-culture BBB models based on brain capillary endothelial cells (BCECs) derived from human-induced pluripotent stem cells (hiPSCs), and compare them to several available BBB in vitro models from primary human or non-human cells and to rodent in vivo models, as well as to classical and widely used barrier models [Caco-2, parallel artificial membrane permeability assay (PAMPA)]. In particular, we are discussing the features and predictivity of these models and how hiPSC-derived BBB models could impact future discovery and development of novel CNS-targeting therapeutics.},
  language  = {en}
}