Multitarget trehalose-carnosine conjugates inhibit Aβ aggregation, tune copper(II) activity and decrease acrolein toxicity

July 28, 2017

Title

Multitarget trehalose-carnosine conjugates inhibit Aβ aggregation, tune copper(II) activity and decrease acrolein toxicity

Author

Giuseppa Ida Grasso, Francesco Bellia, Giuseppe Arena, Cristina Satriano, Graziella Vecchio, Enrico Rizzarelli

Year

2017

Journal

European Journal of Medicinal Chemistry

Abstract

Increasing evidence is accumulating, showing that neurodegenerative disorders are somehow associated with the toxicity of amyloid aggregates, metal ion dyshomeostasis as well as with products generated by oxidative stress. Within the biological oxidation products, acrolein does have a prominent role. A promising strategy to deal with the above neurogenerative disorders is to use multi-functions bio-molecules. Herein, we show how a class of bio-conjugates takes advantage of the antiaggregating, antioxidant and antiglycating properties of trehalose and carnosine. Their ability to sequester acrolein and to inhibit both self- and metal-induced aggregation is here reported. The copper(II) coordination properties of a new trehalose-carnosine conjugate and the relative antioxidant effects have also been investigated.

Instrument

J-810

Keywords

Circular dichroism, Secondary structure, Tertiary structure, Ligand binding, Coordination chemistry, Biochemistry