Abstract
In this study, the potential antileukemic activity of grandisin, a lignan extracted from Piper solmsianum, was evaluated against the leukemic line K562. The cytotoxicity of grandisin (0.018 to 2.365 µM) was evaluated in K562 and normal peripheral blood lymphocytes by Trypan Blue Exclusion and MTT methods after 48h exposure to the drug. In both methods, cellular viability was concentration-dependent and the IC50 values were lower than 0.85µM. Analysis of K562 cells after treatment with grandisin showed that the cell cycle was arrested in the G1 phase with a 12.31% increase, while both S and G2 phases decreased. Morphological studies conducted after the exposure of K562 to grandisin revealed changes consistent with the apoptosis process, which was confirmed by anexin V stain and caspase activation. Thus, lignan grandisin showed antileukemic activities against the K562 cell line and the cell death process occurred via apoptosis.
Highlights
Chronic myeloid leukemia (CML) is a clonal myeloproliferative syndrome characterized by the presence of the Philadelphia chromosome - Ph (Faderl et al, 1999)
Our data demonstrated that grandisin was more cytotoxic for lymphocytes than for K562 cells in the Trypan blue assay
Grandisin proved to be cytotoxic to K562 cells, it was toxic for lymphocytes in the same range of concentrations tested
Summary
Chronic myeloid leukemia (CML) is a clonal myeloproliferative syndrome characterized by the presence of the Philadelphia chromosome - Ph (Faderl et al, 1999). The effects of this potential drug on the cell cycle and death mechanism were investigated by flow cytometry with caspase activation. Cells were seeded (1 x 106 cells/mL) in 96-well microtiter plates and incubated with different concentrations of grandisin for 48 hours (Queiroz et al, 2009).
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