Sterubin: [...] Neuroprotective Activity in Vitro and in Vivo.

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lumia
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Sterubin: [...] Neuroprotective Activity in Vitro and in Vivo.

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PMID 32358806
Full text: PMC7317536
Chemistry. 2020 Jun 5;26(32):7299-7308.

doi: 10.1002/chem.202001264. Epub 2020 May 15.

Sterubin: Enantioresolution and Configurational Stability, Enantiomeric Purity in Nature, and Neuroprotective Activity in Vitro and in Vivo
Julian Hofmann 1 , Shaimaa Fayez 2 3 , Matthias Scheiner 1 , Matthias Hoffmann 1 4 , Sabrina Oerter 5 , Antje Appelt-Menzel 5 6 , Pamela Maher 7 , Tangui Maurice 4 , Gerhard Bringmann 2 , Michael Decker 1
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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.
The main things related to AD is in Figures 5, and 7 and 8. There are some potential with this compound, but it seems that the dosage needs to be adjusted--both in vitro and in vivo data shows "over"-dosing on sterubin decrease its effectiveness.
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