Abstract
BackgroundBioactivity-guided fractionation of extracts of Aglaia loheri Blanco (Meliaceae) yielded a cytotoxic isolate, termed Maldi 531.2[M + H]+. This phenolic ester was further investigated for its in vitro cytotoxicity toward human CCRF-CEM leukemia cells and their multi-drug resistant (MDR) subline, CEM/ADR5000. The intrinsic mitochondrial membrane potential (ΔΨm) and induction of apoptosis by this isolate were evaluated.MethodsChromatography techniques, mass spectrometry and proton NMR were employed to isolate Maldi 531.2[M + H]+. XTT cell proliferation and viability assay was used for cytotoxic test, and JC-1[5’,5’,6,6’,-tetrachloro-1,1’,3,3’-tetraethylbenzimidazoyl carbocyanine iodide was used to assess ΔΨm and initiation of apoptosis; Annexin V/FITC-PI staining was employed to analyse apoptosis.ResultsMaldi 531.2[M + H]+ was cytotoxic towards both CCRF-CEM and CEM/ADR5000 cells with IC50 values of 0.02 and 0.03 μM, respectively. The mitochondrial membrane potential (ΔΨm) of MDR cells was significantly reduced in a dose-dependent manner leading to apoptosis as detected by flow cytometric Annexin V-FITC/ PI staining.ConclusionMaldi 531.2[M + H]+ may be a potential anti-cancer drug candidate whose mode of action include reduction of the mitochondrial membrane potential and induction of apoptosis.
Highlights
Bioactivity-guided fractionation of extracts of Aglaia loheri Blanco (Meliaceae) yielded a cytotoxic isolate, termed Maldi 531.2[M + H]+
JC-1 and annexin V-FITC detection kit was obtained from eBioscience (Frankfurt, Germany); propidium iodide and carbonyl cyanide 3chlorophenylhydrazone (CCCP) from Sigma-Aldrich (Taufkirchen, Germany)
Bioactivity-guided isolation of an active fraction from A. loheri Approximately 15.23 g (1.96%) of ethyl acetate crude extract were obtained from 777 g of dried ground leaf samples of A. loheri after solvent partitioning
Summary
Bioactivity-guided fractionation of extracts of Aglaia loheri Blanco (Meliaceae) yielded a cytotoxic isolate, termed Maldi 531.2[M + H]+. This phenolic ester was further investigated for its in vitro cytotoxicity toward human CCRF-CEM leukemia cells and their multi-drug resistant (MDR) subline, CEM/ADR5000. ALL involves rapid transformation of a single normal progenitor cell [2] triggered by several factors associated with exposure to radiation and chemicals. These factors cause genetic damage, resulting in complete destruction of cellular regulatory controls on proliferation, differentiation and apoptosis [3,4,5,6].
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