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We describe the screening of a set of cryptopleurine derivatives, namely thienoquinolizidine derivatives and (epi-)benzo analogs with bioactive phenanthroquinolizidine alkaloids that induce cytotoxic effects in the mouse lymphocytic leukemia cell line L1210. We used three variants of L1210 cells: i) parental cells (S) negative for P-glycoprotein (P-gp) expression; ii) P-glycoprotein positive cells (R), obtained by selection with vincristine; iii) P-glycoprotein positive cells (T), obtained by stable transfection with a human gene encoding P-glycoprotein. We identified the most effective derivative  11  with a median lethal concentration of ≈13 μM in all three L1210 cell variants. The analysis of the apoptosis/necrosis induced by derivative  11  revealed that cell death was the result of apoptosis with late apoptosis characteristics. Derivative  11  did not induce a strong alteration in the proportion of cells in the G 1 , S or G 2 /M phase of the cell cycle, but a strong increase in the number of S, R and T cells in the subG 1  phase was detected. These findings indicated that we identified the most effective inducer of cell death, derivative  11 , and this derivative effectively induced cell death in S, R and T cells at similar inhibitory concentrations independent of P-gp expression.

molecules/molecules online/molecules annual

Screening of Phenanthroquinolizidine Alkaloid Derivatives for Inducing Cell Death of L1210 Leukemia Cells with Negative and Positive P-glycoprotein Expression