Differential modulation of Bax/Bcl-2 ratio and onset of caspase-3/7 activation induced by derivatives of Justicidin B in human melanoma cells A375.

ABSTRACT: Diphyllin and its derivatives are well known cytotoxic natural products structurally related to the anti-cancer drug podophyllotoxin. We here study their structure-activity relationship upon human melanoma cells for first time. To this end, human melanoma A375 cells were incubated with Justicidin B and its 4-methoxylated or 4-glycosylated derivatives to evaluate their selective cytotoxicity and study their effects on cell cycle distribution, caspase activation, apoptosis induction using Annexin V-FITC/PI staining, cell morphology and western blot analysis. Diphyllin methyl ether (GI₅₀ = 3.66 μM) and Justicidin B (GI₅₀ = 1.70 μM) caused an elevation of both early and late apoptosis populations whereas Diphyllin apioside (GI₅₀ = 0.84 μM) and its acetate (GI

SUBMITTER: Al-Qathama A 

PROVIDER: S-EPMC5707076 | biostudies-literature | 2017 Nov

REPOSITORIES: biostudies-literature