1. Academic Validation
  2. Flavaglines as potent anticancer and cytoprotective agents

Flavaglines as potent anticancer and cytoprotective agents

  • J Med Chem. 2012 Nov 26;55(22):10064-73. doi: 10.1021/jm301201z.
Nigel Ribeiro 1 Frédéric Thuaud Yohann Bernard Christian Gaiddon Thierry Cresteil Audrey Hild Etienne C Hirsch Patrick Pierre Michel Canan G Nebigil Laurent Désaubry
Affiliations

Affiliation

  • 1 Therapeutic Innovation Laboratory, UMR7200, CNRS/Université de Strasbourg, Illkirch, France.
Abstract

Flavaglines represent a family of plant Natural Products that display potent Anticancer, cardioprotective, and neuroprotective activities. Novel flavagline derivatives were synthesized and examined for their cytotoxicity on a panel of human Cancer cell lines, their cardioprotection against doxorubicin-induced Apoptosis in cardiomyocytes, and their neuroprotection in culture models of Parkinson's disease and cisplatin-induced neurotoxicity. The structural requirements of flavaglines for cardio- and neuroprotection were for the first time unraveled and appeared to be slightly different from those for cytotoxicity on Cancer cells. We provide also the first evidence that flavaglines may alleviate cisplatin-induced neurotoxicity, suggesting a prophylactic potential of these compounds to prevent this frequently encountered adverse effect of Cancer chemotherapies.

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