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Journal of Enzyme Inhibition and Medicinal Chemistry Volume 26, 2011 - Issue 4
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Inhibition of lipoxygenase (LOX) and anticancer activity caused by gold(I) mixed ligands complexes of triphenylphosphine and thioamides

E. Georgiou
,
A. MetsiosDepartment of Experimental Physiology, Medical School, University of Ioannina, 45110, Ioannina, Greece
,
N. KourkoumelisMedical Physics Laboratory, Medical School, University of Ioannina, Ioannina, Greece
,
S. KarkabounasDepartment of Experimental Physiology, Medical School, University of Ioannina, 45110, Ioannina, GreeceCorrespondence[email protected] [email protected]
,
K. CharalabopoulosDepartment of Experimental Physiology, Medical School, University of Ioannina, 45110, Ioannina, Greece
,
A. BadekaDepartment of Chemistry, Laboratory of Food Chemistry and Technology, University of Ioannina, Greece
&
S.K. HadjikakouDepartment of Chemistry, Inorganic and Analytical Chemistry, University of Ioannina, Ioannina, Greece
 show all
Pages 592-597 | Received 08 Jun 2010, Accepted 04 Oct 2010, Published online: 19 Nov 2010
 
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Abstract

Four mixed ligand gold(I) complexes with the thioamides 2-mercapto-thiazolidine (mtzdH), 2-mercapto-benzothiazole (mbztH) and 5-chloro-2-mercapto-benzothiazole (ClmbztH) and triphenylphosphine (tpp) of formulae [Au(tpp)Cl] (1) [Au(tpp)(mtzd)] (2), [Au(tpp)(mbzt)] (3) and [Au(tpp)(Clmbzt)] (4), already known, were used to study their mechanism of inhibition activity towards the catalytic oxidation of linoleic acid to hydroperoxylinoleic acid by the enzyme lipoxygenase (LOX), kinetically and theoretically. The results are compared to those of cisplatin. In addition, the anticancer cell screening results against leimyosarcoma (LMS) cells have shown that 2-4 complexes were more active than cisplatin. The uptake of complexes in LMS cells were also studied with electrospray ionisation mass spectrometry spectroscopy.

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