Mitochondria-directed antioxidants 2-5 were designed by conjugating curcumin congeners with different polyamine motifs as vehicle tools. The conjugates emerged as efficient antioxidants in mitochondria and fibroblasts and also exerted a protecting role through heme oxygenase-1 activation. Notably, the insertion of a polyamine function into the curcumin-like moiety allowed an efficient intracellular uptake and mitochondria targeting. It also resulted in a significant decrease in the cytotoxicity effects. 2-5 are therefore promising molecules for neuroprotectant lead discovery.

Polyamine conjugation of curcumin analogues toward the discovery of mitochondria-directed neuroprotective agents.

SIMONI, ELENA;BERGAMINI, CHRISTIAN;FATO, ROMANA;TAROZZI, ANDREA;CAVALLI, ANDREA;BOLOGNESI, MARIA LAURA;MINARINI, ANNA;HRELIA, PATRIZIA;LENAZ, GIORGIO;ROSINI, MICHELA;MELCHIORRE, CARLO
2010

Abstract

Mitochondria-directed antioxidants 2-5 were designed by conjugating curcumin congeners with different polyamine motifs as vehicle tools. The conjugates emerged as efficient antioxidants in mitochondria and fibroblasts and also exerted a protecting role through heme oxygenase-1 activation. Notably, the insertion of a polyamine function into the curcumin-like moiety allowed an efficient intracellular uptake and mitochondria targeting. It also resulted in a significant decrease in the cytotoxicity effects. 2-5 are therefore promising molecules for neuroprotectant lead discovery.
Simoni E.; Bergamini C.; Fato R.; Tarozzi A.; Bains S.; Motterlini R.; Cavalli A.; Bolognesi M.L.; Minarini A.; Hrelia P.; Lenaz G.; Rosini M.; Melchiorre C.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11585/92049
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