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., et al. (2010). Polyamine conjugation of curcumin analogues toward the discovery of mitochondria-directed neuroprotective agents. JOURNAL OF MEDICINAL CHEMISTRY, 53, 7264-7268 [10.1021/jm100637k].
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.