Cell death‐inducing properties of selected dendrimers against different breast cancer and leukemia cell lines

Abstract

Dendrimers represent an opportunity for targeted drug delivery into tumor cells. This is facilitated, for example, by loading of dendrimers with anticancer compounds. However, to assess the effects caused by such conjugates, knowledge of the cytotoxicity of the dendrimers themselves is necessary. The poly(amido amine)-derived dendrimers G 1 (Phe) 6 , G 1 (Dan) 3 , and G 2 were selected due to their different numbers of free amino groups and the poly(propylene imine) (PPI) dendrimer PPI-G 3 served as a reference. The compounds were evaluated for cell-death induction using breast cancer (MCF-7, MDA-MB-231) and leukemia (LAMA-84, K562, SD-1, SUP-B15) cell lines. The compounds exhibited concentration-dependent effects in the low micromolar range against the mammary carcinoma cells. A dependency on the generation, and particularly on the type of dendrimer, was deduced while the quantity of the free amino groups was subsidiary. G 2 revealed to be most cytotoxic, also against all tested leukemia cell lines. The cell line SD-1, however, was susceptible to all dendrimers. The mode of cell death was mainly determined by necrosis, especially at higher concentrations, while apoptosis played a subordinate role. The other dendrimers exerted no antimetabolic effects against LAMA-84, K562, and SUP-B15 cells. Therefore, these dendrimers are generally suitable as nontoxic drug carriers for leukemia cells.

Anticancer Potential of Dendritic Poly(aryl ether)-Substituted Polypyridyl Ligand-Based Ruthenium(II) Coordination Entities

“…The fluorescence intensity profile shows a higher cell death in MDA MB 231 cells compared to that of A549 and HepG2 cells in all three coordination entities. Coordination entity RuG0 has exhibited a higher cell death in all three cell lines; this may infer that RuG0 disrupts the cell membrane and induces cell death by a necrosis mechanism compared to other coordination complexes …”

“…The ability of PI to stain the cells depends upon the integrity of its cell membrane; therefore, PI cannot stain a live or early apoptotic cells. 65 This is clearly evident from the coordination entity-untreated control experiments, wherein very little or no red stains are observed; this indicates that the cell membranes are intact and do not allow the passage of PI. In cases of RuG0-, RuG1-, and RuG2-treated cell lines, stronger red images are observed indicating the presence of death cells; it is clearly concluded that on treatment with the coordination entities the integrity of the cell membrane is lost, and PI very well gets access to the DNA molecules and emits strong red fluorescence.…”

Synthesis and biological evaluation of salophen nickel(II) and cobalt(III) complexes as potential anticancer compounds

“…[ 17 ] This paves the way for future conjugation of the complexes to dendrimers or polymers by ester binding to enable targeted drug delivery. [ 18 ]…”

“…[17] This paves the way for future conjugation of the complexes to dendrimers or polymers by ester binding to enable targeted drug delivery. [18] Also [Fe(II)SAP] complexes demonstrated outstanding apoptotic activity against U-937 non-Hodgkin's lymphoma, HL-60, and K-562 leukemia cells. [19] As [Co(III)SAP] mimics isoelectric conditions of [Fe (II)SAP] and cobalt is, like iron, also a member of the iron triad, this metal was selected for further analysis in this study.…”