Abstract:
:The bifunctional Pt(IV) conjugate cis,cis,trans-diamminedichloridobis(valproato)platinum(IV), based on the cisplatin square-plane with two axial valproato (2-propylpentanoate, VPA) ligands, has been re-synthesized with a modified procedure and its biological activity was compared with that of its isomer cis,cis,trans-diamminedichloridobis(n-octanoato)platinum(IV). Both complexes showed a striking cytotoxic effect (in the micro or sub-micromolar range) on various human carcinoma cell lines (namely ovarian, colon, breast and lung cancer), and, in particular, on cells derived from malignant pleural mesothelioma. This remarkable activity is due to the action of the cisplatin metabolite only, generated by the intracellular Pt(IV)→Pt(II) reduction, which concentration is greatly increased by the enhanced cellular accumulation of the original, highly lipophilic Pt(IV)-bis(carboxylato) complexes. The two axial VPA ligands are released in a too low concentration to act as histone deacetylase inhibitor (HDACI), as VPA works in the millimolar range, so that no synergism can be claimed. Moreover, n-octanoic acid is substantially deprived of any HDACI propensity.
journal_name
J Inorg Biochemjournal_title
Journal of inorganic biochemistryauthors
Alessio M,Zanellato I,Bonarrigo I,Gabano E,Ravera M,Osella Ddoi
10.1016/j.jinorgbio.2013.09.003subject
Has Abstractpub_date
2013-12-01 00:00:00pages
52-7eissn
0162-0134issn
1873-3344pii
S0162-0134(13)00236-5journal_volume
129pub_type
杂志文章abstract::The inhibitory effect of Cu2+, Mn2+, Co2+, and I- on naproxen-induced photohemolysis was investigated. In order to better understand this effect, these ions were also tested for lipid peroxidation and protein crosslinking, which are among the main processes involved in erythrocyte membrane damage. The overall results ...
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journal_title:Journal of inorganic biochemistry
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journal_title:Journal of inorganic biochemistry
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journal_title:Journal of inorganic biochemistry
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journal_title:Journal of inorganic biochemistry
pub_type: 杂志文章
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更新日期:2010-04-01 00:00:00
abstract::Nickel-containing carbon monoxide dehydrogenases, acetyl-CoA synthases, nickel-iron hydrogenases, and diron hydrogenases are distinct metalloenzymes yet they share a number of important characteristics. All are O(2)-sensitive, with active-sites composed of iron and/or nickel ions coordinated primarily by sulfur ligand...
journal_title:Journal of inorganic biochemistry
pub_type: 杂志文章,评审
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更新日期:2012-01-01 00:00:00
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journal_title:Journal of inorganic biochemistry
pub_type: 杂志文章
doi:10.1016/j.jinorgbio.2005.09.003
更新日期:2005-12-01 00:00:00