Cytotoxic activity of G3 PAMAM-NH2 dendrimer-chlorambucil conjugate in human breast cancer cells

Evaluation of the cytotoxicity of a novel G3 PAMAM-NH2 dendrimer–chlorambucil conjugate employing a MTT assay and inhibition of [3H]thymidine incorporation into DNA in both MDA-MB-231 and MCF-7 breast cancer cells demonstrated that the conjugate was more potent antiproliferative agent than chlorambucil. It was found that dendrimer–chlorambucil conjugate was more active inhibitor of collagen biosynthesis than chlorambucil. Our experiments carried out with flow cytometry assessment of annexin V binding and fluorescent microscopy assay revealed that PAMAM–CH conjugate inhibited the proliferation of MCF-7 and MDA-231 malignant cells by increasing the number of apoptotic and necrotic cells. The apoptotic effect of PAMAM–CH conjugate was found to be stronger than that caused by chlorambucil.

► Novel G3 PAMAM-NH2 dendrimer–chlorambucil conjugate in breast cancer cells proved to be more potent antiproliferative agent than chlorambucil.
► G3 PAMAM-NH2 dendrimer–chlorambucil conjugate was more active inhibitor of collagen biosynthesis than chlorambucil.
► G3 PAMAM-NH2 dendrimer–chlorambucil conjugate inhibited the proliferation of breast cancer cells by increasing the number of apoptotic and necrotic cells.