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Article

Homotaurine and Curcumin Analogues as Potential Anti-Amyloidogenic Agents

1
School of Pharmacy, Massachusetts College of Pharmacy and Health Sciences, Boston, MA 02115, USA
2
School of Pharmacy, American University of Health Sciences, Signal Hill, CA 90755, USA
*
Author to whom correspondence should be addressed.
Chemistry 2023, 5(1), 223-241; https://doi.org/10.3390/chemistry5010018
Submission received: 24 July 2022 / Revised: 13 January 2023 / Accepted: 6 February 2023 / Published: 7 February 2023

Abstract

Currently, there is neither a cure for Alzheimer’s disease (AD) nor a way to stop the progressive death of neuronal cells associated with this devastating aliment. To date, there are only medications that temporarily slow its progression, and do not interfere with its pathogenesis. One of the hallmarks of AD is the presence of amyloid-beta plaques derived from the metabolism of the amyloid precursor protein, via the cleavage by beta followed by gamma secretase. Homotaurine, a naturally occurring small molecule found in some seaweeds, and curcumin, a phenolic antioxidant found in Curcuma longa, have been extensively studied as potential compounds to prevent/reverse plaque formation. In this study, libraries of chalcones and extended chalcones based on curcumin, as well as aminopropylsulfonamides inspired by homotaurine, were synthesized. Using fluorescence spectroscopic analysis with Thioflavin T, the anti-aggregation effect on Aβ42 was determined. A select number of newly synthesized chalcones and extended chalcone analogs were revealed to be potential anti-amyloidogenic agents. These were further evaluated with regard to their neurotoxicity/neuroprotection. The extended chalcone analogs that displayed the most anti-aggregation effect on Aβ42 were further analyzed in an MTT assay. Although none of the compounds alone displayed any neurotoxicity, none were able to provide neuroprotection against Aβ42.
Keywords: Alzheimer’s disease; anti-amyloidogenic; aminopropylsulfonamides; extended chalcones Alzheimer’s disease; anti-amyloidogenic; aminopropylsulfonamides; extended chalcones

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MDPI and ACS Style

Quiroz, J.P.; Zeng, A.; Young, M.; Gordon, P.; Jaipuria, A.; Reed, K.J.; Landry, G.M.; Yang, S.; Asher, S.; Zhang, S.R.C.; et al. Homotaurine and Curcumin Analogues as Potential Anti-Amyloidogenic Agents. Chemistry 2023, 5, 223-241. https://doi.org/10.3390/chemistry5010018

AMA Style

Quiroz JP, Zeng A, Young M, Gordon P, Jaipuria A, Reed KJ, Landry GM, Yang S, Asher S, Zhang SRC, et al. Homotaurine and Curcumin Analogues as Potential Anti-Amyloidogenic Agents. Chemistry. 2023; 5(1):223-241. https://doi.org/10.3390/chemistry5010018

Chicago/Turabian Style

Quiroz, Jose Paredes, Andi Zeng, Michelle Young, Patrick Gordon, Aadya Jaipuria, Kristi J. Reed, Greg M. Landry, Suhui Yang, Shreya Asher, Sabrina Ruoyao Chen Zhang, and et al. 2023. "Homotaurine and Curcumin Analogues as Potential Anti-Amyloidogenic Agents" Chemistry 5, no. 1: 223-241. https://doi.org/10.3390/chemistry5010018

APA Style

Quiroz, J. P., Zeng, A., Young, M., Gordon, P., Jaipuria, A., Reed, K. J., Landry, G. M., Yang, S., Asher, S., Zhang, S. R. C., & Priefer, R. (2023). Homotaurine and Curcumin Analogues as Potential Anti-Amyloidogenic Agents. Chemistry, 5(1), 223-241. https://doi.org/10.3390/chemistry5010018

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