In last few years, several research programs have been focused on the pharmaco-chemical investigation of marine invertebrates. The reasons of this growing interest can be found in the high level of chemical diversity, structural peculiarity, and pharmacological activity of compounds isolated from these organisms. The marine environment appears an attractive source of biodiversity also for identifying new AntiMalarials. In this context, we have recently examined extracts of the sponge Plakortis simplex and isolated a series of structurally simple endoperoxide derivatives endowed with antiplasmodial activity in the ng/mL range, with higher potency against chloroquine-resistant strains of P.falciparum and no general cytotoxicity (Fattorusso E et al AAC 2002). In addition, we have prepared a series of semisynthetic derivatives of the natural endoperoxides with improved in vitro activity. Programme: The future research will be focused on: 1- further characterisation and lead optimisation of the endoperoxides with AntiMalarial activity; 2- screening of extracts of different sponges that, on the basis of the data in the literature and chemotaxonomic considerationpotential producers of endoperoxides.

Natural endoperoxides from marine organisms / Fattorusso, Ernesto. - (2006). (Intervento presentato al convegno Development of New Drugs for the Treatment of Malaria nel 01/05/2006).

Natural endoperoxides from marine organisms

FATTORUSSO, ERNESTO
2006

Abstract

In last few years, several research programs have been focused on the pharmaco-chemical investigation of marine invertebrates. The reasons of this growing interest can be found in the high level of chemical diversity, structural peculiarity, and pharmacological activity of compounds isolated from these organisms. The marine environment appears an attractive source of biodiversity also for identifying new AntiMalarials. In this context, we have recently examined extracts of the sponge Plakortis simplex and isolated a series of structurally simple endoperoxide derivatives endowed with antiplasmodial activity in the ng/mL range, with higher potency against chloroquine-resistant strains of P.falciparum and no general cytotoxicity (Fattorusso E et al AAC 2002). In addition, we have prepared a series of semisynthetic derivatives of the natural endoperoxides with improved in vitro activity. Programme: The future research will be focused on: 1- further characterisation and lead optimisation of the endoperoxides with AntiMalarial activity; 2- screening of extracts of different sponges that, on the basis of the data in the literature and chemotaxonomic considerationpotential producers of endoperoxides.
2006
Natural endoperoxides from marine organisms / Fattorusso, Ernesto. - (2006). (Intervento presentato al convegno Development of New Drugs for the Treatment of Malaria nel 01/05/2006).
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11588/337170
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