title: Cytotoxicity of electrophilic iron(II)-clathrochelates in human promyelocytic leukemia cell line.
abstract: We observed that electrophilic iron(II)-clathrochelates exhibit significant cytotoxicity in human promyelocytic leukemia cells (IC50=6.5±4.6μM), which correlates with the enhancement of intracellular oxidative stress (17-fold increase with respect to the cells treated with the solvent only). Based on in vitro studies we suggested that this effect is caused by alkylation of glutathione leading to inhibition of the cellular antioxidative system and by catalytic generation of reactive oxygen species by products of the alkylation reaction.
authors.affiliation: Friedrich-Alexander-University of Erlangen-Nürnberg, Department of Chemistry and Pharmacy, Organic Chemistry Chair II, Henkestr. 42, 91054 Erlangen, Germany.
authors.forename: Jenny
authors.initials: J
authors.lastname: Blechinger
authors.affiliation: Institute of General and Inorganic Chemistry NASU, 32/34 Palladin Av., 03680 Kyiv, Ukraine.
authors.forename: Oleg A
authors.initials: OA
authors.lastname: Varzackii
authors.affiliation: Institute of Molecular Biology and Genetics NASU, 150, Zabolotnogo Str., 03143 Kyiv, Ukraine.
authors.forename: Vladyslava
authors.initials: V
authors.lastname: Kovalska
authors.affiliation: Nesmeyanov Institute of the Organoelement Compounds RAS, Moscow, Russia.
authors.forename: Genrikh E
authors.initials: GE
authors.lastname: Zelinskii
authors.affiliation: Nesmeyanov Institute of the Organoelement Compounds RAS, Moscow, Russia.
authors.forename: Yan Z
authors.initials: YZ
authors.lastname: Voloshin
authors.affiliation: Friedrich-Alexander-University of Erlangen-Nürnberg, Department of Chemistry and Pharmacy, Organic Chemistry Chair II, Henkestr. 42, 91054 Erlangen, Germany.
authors.forename: Elisa
authors.initials: E
authors.lastname: Kinski
authors.affiliation: Friedrich-Alexander-University of Erlangen-Nürnberg, Department of Chemistry and Pharmacy, Organic Chemistry Chair II, Henkestr. 42, 91054 Erlangen, Germany.
authors.forename: Andriy
authors.initials: A
authors.lastname: Mokhir
mesh_terms: D000478:Alkylation / Q000187:drug effects; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D005296:Ferrous Compounds / Q000737:chemistry* / Q000494:pharmacology*; D005978:Glutathione / Q000378:metabolism; D042381:Granulocyte Precursor Cells / Q000187:drug effects* / Q000378:metabolism / Q000473:pathology; D006801:Humans; D015473:Leukemia, Promyelocytic, Acute / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D018384:Oxidative Stress / Q000187:drug effects*; D017382:Reactive Oxygen Species / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D005296:Ferrous Compounds; D017382:Reactive Oxygen Species; D005978:Glutathione
keywords: Alkylation; Cancer; Clathrochelate; Glutathione; Iron