Euphosalicin, a new diterpene polyester with multidrug resistance reversing activity from Euphorbia salicifolia

Improving the MDR reversal activity of 6,17-epoxylathyrane diterpenes

“…10 Our previous studies with jolkinol D derivatives on the ability of macrocyclic diterpenes to revert Pgp-mediated MDR corroborate this structural feature. 9 Therefore, in this work, using several aromatic acyl chlorides, six new analogues of epoxyboetirane A (1) were prepared (7)(8)(9)(10)(11)(12). Compounds 13 and 14 were also prepared aiming to evaluate the influence of the number of carbon atoms of the alkanoyl residues on the activity.…”

“…7,8 Aiming to optimize macrocyclic diterpenes as MDR reversal agents, 9,10 herein we report the isolation of five lathyrane diterpenes http://dx.doi.org/10.1016/j.bmc.2014.09.041 0968-0896/Ó 2014 Elsevier Ltd. All rights reserved. (1)(2)(3)(4)(5), including two new compounds (1 and 2), from Euphorbia boetica.…”

“…(1)(2)(3)(4)(5), including two new compounds (1 and 2), from Euphorbia boetica. Furthermore, compound 1, isolated in large amounts, was hydrolyzed and the resulting parental polyalcohol (6) was subsequently acylated affording eight new derivatives (7)(8)(9)(10)(11)(12)(13)(14). Compounds 1-14 were evaluated for their ability as Pgp modulators, through the rhodamine-123 exclusion assay.…”

Progress in the Preparation of Jatrophane Diterpenes

“…The unspecific nature of the binding region allows the active transport of a great variety of molecules through the cell membrane, but also complicates the elucidation and design of potent inhibitors. [32] Over the last few years, newly isolated diterpenes of the lathyrane [33] and jatrophane [34] skeleton were evaluated with respect to their mdr-reversal properties and several secondary metabolites with highly promising activities have been identified. Furthermore, the evaluation of a great number of structurally similar substrates has provided preliminary information on the structural requirements for significant levels of activity.…”

Isolation and Structure Elucidation of Diterpenes from Euphorbia pannonica, E. esula and E. falcata

“…In the course of these studies, many diterpene esters of different skeletal types have been isolated. [22][23][24][25][26][27][28][29][30][31][32][33] One part of this programme involved the investigation of Euphorbia pannonica Host., E. esula L. and E. falcata L. The present thesis summarizes the results of these phytochemical works.…”