Cytotoxic and cytostatic activity of copper(II) complexes. Importance of the speciation for the correct interpretation of the in vitro biological results.
The cytotoxicity of some copper(II) compounds against the mouse cancer cell line B16, murine L929, human KB cells, and fibroblasts was investigated. All the copper(II) systems tested were shown to have pronounced toxicity against transformed cells and a cytostatic effect against untransformed cells, i.e., human fibroblasts. A careful speciation of the actual in vitro conditions reveals that copper(II) is essentially present as mixed complexes formed with the amino acids of the culture medium, [Cu(glutamine)(histidine)] being the main species. It was found that the cytotoxic activity is related to the amount of copper(II) contained in the tested compounds.
Arena
G
G
Dipartimento di Scienze Chimiche, Università di Catania, Italy.
Bindoni
M
M
Cardile
V
V
Maccarrone
G
G
Riello
M C
MC
Rizzarelli
E
E
Sciuto
S
S
D000085:Acetates / Q000737:chemistry / Q000494:pharmacology; D000596:Amino Acids; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D016923:Cell Death / Q000187:drug effects; D002455:Cell Division / Q000187:drug effects; D003300:Copper / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D005347:Fibroblasts / Q000166:cytology / Q000187:drug effects; D006801:Humans; D007093:Imidazoles / Q000737:chemistry / Q000494:pharmacology; D008546:Melanoma, Experimental / Q000188:drug therapy / Q000473:pathology; D009062:Mouth Neoplasms / Q000188:drug therapy / Q000473:pathology; D014407:Tumor Cells, Cultured
D000085:Acetates; D000596:Amino Acids; D000970:Antineoplastic Agents; D007093:Imidazoles; D003300:Copper