The in vitro antitumour activity of novel, mitochondrial-interactive, gold-based lipophilic cations.

Metal-based Drugs
Sherika MahepalConstance Elizabeth Jansen van Rensburg

Abstract

In this study we compared the effects of two previously described antimitochondrial gold complexes, that is, [A] [Au(dppe)(2)]Cl and [B] [Au(d4pype)(2)]Cl with two novel lipophilic cations, that is, [C] [Au(dpmaaH(2))(dpmaaSnMe(2))]Cl and [D] [Au(dpmaaSnMe(2))(2)]Cl as antimitochondrial agents. The results of this study indicate that [C] and [D] have intermediate partition coefficients and exhibited a selective uptake by cells. They exhibited a higher selectivity for the various cell lines than [A] but were more cytotoxic than [B]. There is a significant correlation between the cytotoxic potential of [A], [B], [C], and [D] and their octanol/water partition coefficients in both MCF-7 (breast cancer) and MCF-12A (nonmalignant breast) cells, whereas their cytotoxic potential and ability to induce the release of cytochrome c correlated only in the case of the MCF-12A cells. Complexes [C] and [D] are promising new chemotherapeutic drugs. These compounds target the mitochondrial membranes of certain cancer cells exploiting the differences between the mitochondrial membrane potential of these cells and normal cells. Although the concentrations of these compounds necessary to eradicate cancer cells are very high, the results provide a ...Continue Reading

References

Nov 1, 1986·Geburtshilfe und Frauenheilkunde·P W Klug
Sep 22, 1999·European Journal of Biochemistry·P BernardiF Di Lisa
Dec 29, 2000·Cancer Chemotherapy and Pharmacology·M J McKeageB C Baguley
May 30, 2001·Advanced Drug Delivery Reviews·J S Modica-Napolitano, J R Aprille

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Citations

Apr 14, 2012·Journal of Inorganic Biochemistry·Ulrike E I HorvathHelgard G Raubenheimer
Mar 13, 2009·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·M J NellC E J van Rensburg
Aug 26, 2011·Journal of Inorganic Biochemistry·Laura VelaIsabel Marzo

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