An inhibitor of 5-LO
2,5-Dihydroxycinnamic acid phenethyl ester is an inhibitor of 5-lipoxygenase (5-LO) with an IC50 value of 0.33 μM for inhibition of 5-LO product synthesis in polymorphonuclear leukocytes (PMNLs) stimulated with the sarcoendoplasmic reticulum calcium ATPase (SERCA) inhibitor thapsigargin .1 It scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals (IC50 = 16.41 μM) in a cell-free assay. 2,5-Dihydroxycinnamic acid phenethyl ester selectively decreases viability of RCC4 and 786-O cells lacking the Von Hippel-Lindau (VHL) tumor suppressor gene (IC50s = 8 and 34.8 μM, respectively) over cells homozygously expressing VHL (IC50s = 99.6 and >100 μM, respectively). However, it also decreases viability of RCC10 VHL-/- and RCC10 VHL+/+ cells (IC50s = 5.04 and 0.96 μM, respectively). It increases the levels of pro-caspase-3a, LC3B-I, and LC3B-II in RCC4 VHL-/- cells in a concentration-dependent manner.
|1. Selka, A., Doiron, J.A., Lyons, P.A., et al. Discovery of a novel 2,5-dihydroxycinnamic acid-based 5-lipoxygenase inhibitor that induces apoptosis and may impair autophagic flux in RCC4 renal cancer cells. Eur. J. Med. Chem. 179, 347-357 (2019).
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