Issue 10, 2008

Discovery of a new series of jatrophane and lathyrane diterpenes as potent and specific P-glycoprotein modulators

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.

Graphical abstract: Discovery of a new series of jatrophane and lathyrane diterpenes as potent and specific P-glycoprotein modulators

Supplementary files

Article information

Article type
Paper
Submitted
10 Jan 2008
Accepted
20 Feb 2008
First published
28 Mar 2008

Org. Biomol. Chem., 2008,6, 1756-1762

Discovery of a new series of jatrophane and lathyrane diterpenes as potent and specific P-glycoprotein modulators

E. Barile, M. Borriello, A. Di Pietro, A. Doreau, C. Fattorusso, E. Fattorusso and V. Lanzotti, Org. Biomol. Chem., 2008, 6, 1756 DOI: 10.1039/B800485D

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