Figure 3
From: Activation of PKC supports the anticancer activity of tigilanol tiglate and related epoxytiglianes
Changes in B-ring hydroxylation profile and C20 modification of epoxytiglianes purified from Fontainea picrosperma show varying potency. (A) EcoBiotics Compounds (EBC) isolated from Fontainea picrosperma; color highlights indicate structural similarities. (B) Bioactivity of EBC analogues. K562 leukemia cell growth/survival assay (a surrogate for PKC activation) and NF-κB reporter system reveal differences in potency between EBC analogues. % Growth/Survival vs. Log10 [compound] curves were generated using K562 cells for select tiglianes. These were subsequently used to calculate mean IC50 values (± 95% CI) (lower left panel), which was subsequently arranged into heatmap format (upper panel) for visualization. The fold change in luminescent signal from an NF-κB reporter assay was also determined for each tigliane at three concentrations (500, 50 and 5 nM; lower right panel; mean ± SD). These data were converted into log2 values and displayed in heatmap format (upper panel). The lipophilic efficiency (LiPE) of each tigliane was calculated using pIC50 values [− log10(IC50)] and experimentally determined logP values (see Supplementary data file 1). n = 2 or 3 for all EBC analogues.
