Zusammenfassung
Aqua[meso-1,2-bis(2,6-difluoro-3-hydroxyphenyl)ethylenediamine]sulfato-platinum(II) (meso-3-PtSO4) and its racemate (rac-3-PtSO4) are highly active on the hormone-sensitive MXT-M-3,2 breast cancer of the mouse. In vitro, on the MXT+ cell culture derived from this tumor, however, they are inactive (meso-3PtSO(4)) or moderately active (rac-3-PtSO4) in concentrations corresponding to levels of these ...
Zusammenfassung
Aqua[meso-1,2-bis(2,6-difluoro-3-hydroxyphenyl)ethylenediamine]sulfato-platinum(II) (meso-3-PtSO4) and its racemate (rac-3-PtSO4) are highly active on the hormone-sensitive MXT-M-3,2 breast cancer of the mouse. In vitro, on the MXT+ cell culture derived from this tumor, however, they are inactive (meso-3PtSO(4)) or moderately active (rac-3-PtSO4) in concentrations corresponding to levels of these drugs in animal experiments. The in vivo effect is mainly caused by a reduction of the endogenous estrogen level in the host animals due to an interference with the ovarian steroid biosynthesis as demonstrated for meso-3PtSO(4). Therefore, a reversal of the breast cancer inhibiting effect of meso-3PtSO(4) can be achieved by simultaneous estrone administration. Histological results on ovaries, uterus, and tumor of meso-3-PtSO4-treated mice also favor such a mode of action. However, especially for rac-3-PtSO4 cytotoxic effects contributing to the anti-breast cancer activity cannot be excluded. Considerations on the mode of action of Pt-bomplexes which inhibit breast cancer by interference with estrogen receptor mediated processes of growth control and with DNA replication are presented.
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