<abstract xmlns="http://www.w3.org/1999/xhtml">

<p>In preclinical studies, simple coumarins (scoparone, limettin) and furanocoumarins (imperatorin, xanthotoxin, bergapten) have already found to demonstrate procognitive abilities. This suggests that they hold antioxidative, anti-inflammatory and inhibitory action towards acetylcholinesterase activities. However, little is known about their influence on the amyloidal structure formation, the leading cause of Alzheimer’s disease (AD). <italic>In vitro</italic> and <italic>in cellulo</italic> assays were applied to evaluate the effect of selected coumarins on the different stages of Aβ40/42 and <italic>tau</italic> protein aggregation. Kinetic analyses were performed to evaluate their inhibiting abilities in time. Limettin revealed the most potent inhibiting profile towards Aβ40 aggregation, however, all tested compounds presented low influence on Aβ42 and <italic>tau</italic> protein aggregation inhibition. Despite the preliminary stage of the project, the promising effects of coumarins on Aβ40 aggregation were shown. This suggests the coumarin scaffold can serve as a potential multitarget agent in AD treatment, but further studies are required to confirm this.</p>
</abstract>

In preclinical studies, simple coumarins (scoparone, limettin) and furanocoumarins (imperatorin, xanthotoxin, bergapten) have already found to demonstrate procognitive abilities. This suggests that they hold antioxidative, anti-inflammatory and inhibitory action towards acetylcholinesterase activities. However, little is known about their influence on the amyloidal structure formation, the leading cause of Alzheimer’s disease (AD). In vitro and in cellulo assays were applied to evaluate the effect of selected coumarins on the different stages of Aβ40/42 and tau protein aggregation. Kinetic analyses were performed to evaluate their inhibiting abilities in time. Limettin revealed the most potent inhibiting profile towards Aβ40 aggregation, however, all tested compounds presented low influence on Aβ42 and tau protein aggregation inhibition. Despite the preliminary stage of the project, the promising effects of coumarins on Aβ40 aggregation were shown. This suggests the coumarin scaffold can serve as a potential multitarget agent in AD treatment, but further studies are required to confirm this.

Coumarin derivatives against amyloid-beta 40 – 42 peptide and <italic>tau</italic> protein

Independent Laboratory of Behavioral Studies

Department of Pharmacology and Toxicology

Department of Pharmacy and Pharmaceutical Technology and Physical-Chemistry

Current Issues in Pharmacy and Medical Sciences

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Coumarin derivatives against amyloid-beta 40 – 42 peptide and  protein

In preclinical studies, simple coumarins (scoparone, limettin) and furanocoumarins (imperatorin, xanthotoxin, bergapten) have already found to demonstrate...

Coumarin derivatives against amyloid-beta 40 – 42 peptide and tau protein

Published Online: Sep 02, 2022

Page range: 67 - 74

Received: Mar 13, 2022

Accepted: Jun 17, 2022

DOI: https://doi.org/10.2478/cipms-2022-0013

Keywords
neurodegeneration, A40/42, coumarins

© 2022 Joanna Kowalczyk et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Coumarin derivatives against amyloid-beta 40 – 42 peptide and tau protein

Published Online: Sep 02, 2022

Page range: 67 - 74

Received: Mar 13, 2022

Accepted: Jun 17, 2022

DOI: https://doi.org/10.2478/cipms-2022-0013

Keywordsneurodegeneration, A40/42, coumarins

© 2022 Joanna Kowalczyk et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Keywords
neurodegeneration, A40/42, coumarins