Euphorbia and Momordica metabolites for overcoming multidrug resistance

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.…”

Effective MDR reversers through phytochemical study of Euphorbia boetica

“…In the last decades, Euphorbia species have been the subject of intensive phytochemical studies that have resulted in the isolation of a high diversity of compounds, some of them exhibiting very important biological activities . In particular, these species have afforded a large number of structurally unique macrocyclic diterpenes with the lathyrane and jatrophane skeletons . Apart from their importance as biogenetic and chemotaxonomic markers, since they are exclusively isolated from Euphorbiaceae plants, several studies have revealed that they are promising modulators of multidrug resistance (MDR) in tumour cells …”

“…3,4 In particular, these species have afforded a large number of structurally unique macrocyclic diterpenes with the lathyrane and jatrophane skeletons. 4,5 Apart from their importance as biogenetic and chemotaxonomic markers, since they are exclusively isolated from Euphorbiaceae plants, 6 several studies have revealed that they are promising modulators of multidrug resistance (MDR) in tumour cells. 4,5,[7][8][9][10][11][12][13][14] Currently, resistance towards many clinically used drugs is a major limitation to effective cancer therapies.…”