: A new series of diterpenes, the jatrophanes euphoscopin M (1), euphoscopin N (2) and euphornin L (3), and the lathyrane euphohelioscopin C (7) were isolated from plants of Euphorbia helioscopia L., together with four other known analogues, euphoscopin C (4), euphornin (5), epieuphoscopin B (6) and euphohelioscopin A (8). The new compound stereostructures were elucidated by NMR analysis and computational data. The resulting isolated diterpenes were found to be potent inhibitors of P-glycoprotein (ABCB1), while showing an absence of significant activity against BCRP (ABCG2), despite the high substrate overlapping of these transporters, thus including them in the third-generation class of specific multidrug transporter modulators.
Discovery of a new series of jatrophane and lathyrane diterpenes as potent and specific P-glycoprotein modulators / Barile, E.; Borriello, M.; Di Pietro, A.; Doreau, A.; Fattorusso, C.; Fattorusso, E.; Lanzotti, V.. - In: ORGANIC & BIOMOLECULAR CHEMISTRY. - ISSN 1477-0520. - 6:10(2008), pp. 1756-1762. [10.1039/b800485d]
Discovery of a new series of jatrophane and lathyrane diterpenes as potent and specific P-glycoprotein modulators
Barile, E.;Di Pietro, A.;Fattorusso, C.;Fattorusso, E.;Lanzotti, V.
2008
Abstract
: A new series of diterpenes, the jatrophanes euphoscopin M (1), euphoscopin N (2) and euphornin L (3), and the lathyrane euphohelioscopin C (7) were isolated from plants of Euphorbia helioscopia L., together with four other known analogues, euphoscopin C (4), euphornin (5), epieuphoscopin B (6) and euphohelioscopin A (8). The new compound stereostructures were elucidated by NMR analysis and computational data. The resulting isolated diterpenes were found to be potent inhibitors of P-glycoprotein (ABCB1), while showing an absence of significant activity against BCRP (ABCG2), despite the high substrate overlapping of these transporters, thus including them in the third-generation class of specific multidrug transporter modulators.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.