title: In vitro evaluation of a stable monomeric gold(II) complex with hematoporphyrin IX: cytotoxicity against tumor and kidney cells, cellular accumulation, and induction of apoptosis.
abstract: The antineoplastic potential of a stable monomeric Au(II) complex with hematoporphyrin IX (Hp), namely [Au(II)Hp(-2H).(H(2)O)(2)], was investigated in a panel of tumor cell lines. The complex exhibits strong cytotoxicity, whereby the leukaemia- and lymphoma-derived cell lines are more sensitive, with IC(50) values comparable to those of the reference anticancer drug cisplatin. In contrast, the solid tumor models are more sensitive to the platinum drug. A comparative assessment of both agents against the human kidney cell line 293T has shown that [Au(II)Hp(-2H).(H(2)O)(2)] is less cytotoxic. The gold complex induces oligonucleosomal DNA fragmentation in tumour cells following 24-hour treatment and hence its cytotoxic effect is at least partly mediated by induction of apoptotic cell death. A prominent intracellular gold accumulation was detected after treating tumor cells with [Au(II)Hp(-2H).(H(2)O)(2)] which shows that its putative pharmacological targets are readily accessible after a short incubation period.
authors.affiliation: Laboratory of Molecular Pharmacology and Experimental Chemotherapy, Department of Pharmacology, Pharmacotherapy, and Toxicology, Faculty of Pharmacy, Medical University of Sofia, 2 Dunav Street, 1000 Sofia, Bulgaria.
authors.forename: Georgi
authors.initials: G
authors.lastname: Momekov
authors.forename: Dilyan
authors.initials: D
authors.lastname: Ferdinandov
authors.forename: Spiro
authors.initials: S
authors.lastname: Konstantinov
authors.forename: Sonja
authors.initials: S
authors.lastname: Arpadjan
authors.forename: Daniela
authors.initials: D
authors.lastname: Tsekova
authors.forename: Galina
authors.initials: G
authors.lastname: Gencheva
authors.forename: Panayot R
authors.initials: PR
authors.lastname: Bontchev
authors.forename: Margarita
authors.initials: M
authors.lastname: Karaivanova