title: Cytotoxic activity of G3 PAMAM-NH₂ dendrimer-chlorambucil conjugate in human breast cancer cells.
abstract: Evaluation of the cytotoxicity of a novel G3 PAMAM-NH(2) dendrimer-chlorambucil conjugate employing a MTT assay and inhibition of [(3)H]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.
authors: Department of Medicinal Chemistry, Medical University of Białystok, Kilińskiego 1, 15-089 Białystok, Poland. kbiel@umwb.edu.pl
authors: Krzysztof
authors: K
authors: Bielawski
authors: Anna
authors: A
authors: Bielawska
authors: Anna
authors: A
authors: Muszyńska
authors: Bożena
authors: B
authors: Popławska
authors: Robert
authors: R
authors: Czarnomysy
mesh_terms: D017304:Annexin A5 / Q000378:metabolism; D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000473:pathology; D045744:Cell Line, Tumor; D049109:Cell Proliferation; D002699:Chlorambucil / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D003094:Collagen / Q000096:biosynthesis; D050091:Dendrimers / Q000737:chemistry / Q000494:pharmacology*; D005260:Female; D006801:Humans
chemical_list: D017304:Annexin A5; D000970:Antineoplastic Agents; D050091:Dendrimers; C104700:PAMAM Starburst; D002699:Chlorambucil; D003094:Collagen