Polyamine Conjugation of Curcumin Analogues toward the Discovery of Mitochondria-Directed Neuroprotective Agents

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• 作者：Elena Simoni ; Christian Bergamini ; Romana Fato ; Andrea Tarozzi ; Sandip Bains ; Roberto Motterlini ; Andrea Cavalli ; Maria Laura Bolognesi ; Anna Minarini ; Patrizia Hrelia ; Giorgio Lenaz ; Michela Rosini ; C
• 刊名：Journal of Medicinal Chemistry
• 出版年：2010
• 出版时间：October 14, 2010
• 年：2010
• 卷：53
• 期：19
• 页码：7264-7268
• 全文大小：803K
• 年卷期：v.53,no.19(October 14, 2010)
• ISSN：1520-4804

文摘

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.