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Org Biomol Chem. 2008 May 21;6(10):1756-62. doi: 10.1039/b800485d. Epub 2008 Mar 28.

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

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1
DISTAAM, Università degli Studi del Molise, Via F. De Sanctis, I-86100 Campobasso, Italy.

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.

PMID:
18452010
DOI:
10.1039/b800485d
[Indexed for MEDLINE]
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