Jatrophane diterpenes from Euphorbia mellifera and their activity as P-glycoprotein modulators on multidrug-resistant mouse lymphoma and human colon a...
Basic Information
ID: ALA2176993
Journal: J Nat Prod
Title: Jatrophane diterpenes from Euphorbia mellifera and their activity as P-glycoprotein modulators on multidrug-resistant mouse lymphoma and human colon adenocarcinoma cells.
Authors: Valente I, Reis M, Duarte N, Serly J, Molnár J, Ferreira MJ.
Abstract: Three new macrocyclic jatrophane diterpenes, named euphomelliferine (1) and euphomelliferenes A (2) and B (3), and one new tetracyclic triterpene, 19(10→9)-abeo-8α,9β,10α-tirucalla-5,25-diene-3β,24-diol (6, C-24 epimers), were isolated from the methanolic extract of Euphorbia mellifera. A known ingenane (7) and two jatrophane diterpenes (4 and 5) were also isolated. Their structures were elucidated by extensive spectroscopic methods, including 1D and 2D homo- and heteronuclear NMR experiments. Jatrophane diterpenes 1-3 and 5 were evaluated for their effects on the reversion of multidrug resistance (MDR) mediated by P-glycoprotein, by using the rhodamine-123 exclusion test, on human MDR1 gene-transfected mouse lymphoma cells (L5178Y MDR) and on human colon adenocarcinoma cells (COLO 320). The apoptosis-inducing activity of these compounds was also tested on COLO 320 cells, using the annexin-V/propidium iodide assay. Diterpenes 1 and 2 displayed significant MDR reversing activity, in a dose-dependent manner, on both cancer cell models. The tested compounds did not induce apoptosis in the COLO 320 cells.
CiteXplore: 23098168
DOI: 10.1021/np3004003
Patent ID: ┄