Modified jatrophane diterpenes as modulators of multidrug resistance from Euphorbia dendroides L.

Gabriella Corea, Ernesto Fattorusso, Virginia Lanzotti, Orazio Taglialatela-Scafati, Giovanni Appendino, Mauro Ballero, Pierre Noël Simon, Charles Dumontet, Attilio Di Pietro

Dipartimento di Chimica delle Sostanze Naturali, Università di Napoli 'Federico II', Via D. Montesano 49, I-80131, Napoli, Italy.

Bioorganic & medicinal chemistry 2003 Nov 17

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The new diterpenoids terracinolides J-L (1-3), 13alpha-OH terracinolide F (8), abeodendroidin F (11) and epiabeodendroidin F (12) have been identified from Euphorbia dendroides L. The new compounds and six co-occurring known terracinolides were tested as inhibitors of the drug-efflux activity of P-glycoprotein from cancer cells. The results were used to extend the structure-activity relationships established for this class of compounds highlighting the relevance of substitution at positions 2, 3, 6, and 15 and disclosing a remarkable tolerance toward connectivity changes in the terpenoid core.

Citation

Gabriella Corea, Ernesto Fattorusso, Virginia Lanzotti, Orazio Taglialatela-Scafati, Giovanni Appendino, Mauro Ballero, Pierre Noël Simon, Charles Dumontet, Attilio Di Pietro. Modified jatrophane diterpenes as modulators of multidrug resistance from Euphorbia dendroides L. Bioorganic & medicinal chemistry. 2003 Nov 17;11(23):5221-7