More insight into the mode of action of lipophilic antitumor drugs containing a platinum (II) fragment
Journal Title: Journal of Medical Biomedical and Applied Sciences - Year 2017, Vol 5, Issue 3
Abstract
Cis-Diammine (1,1-cyclobutanedicarboxylato) platinum (II)) (Carboplatin 2) is a second generation platinum anticancer drug following Cis-diammine dichloro platinum (II) (Cisplatin 1). In the present study Cisplatin and Carboplatin analogs are attached to the acid group of the bile acid via an ester link called as ChAPt (n) Cis and ChAPt (n) Carbo. The in vitro antitumor activity of Cisplatin 1 long with the corresponding ChAPt derivatives evaluated against a panel of five tumor cell lines of different histogenic origin. A series of biological methods starting from Sulforhodamine B (SRB) assay to determine IC50, Cell cycle analysis, Annexin Vassay and Caspase assays were performed with the aim to scrutinize the anticancer mode of action on HepG2 (hepatocellular carcinoma) cell line. The compounds exerted a dose dependent antiproliferative action at micromolar concentrations and the effect of these structural variations on anticancer activity was elaborated and discussed more in detail. To summarize, several compounds revealed significant antitumor activity and surprisingly the ChAPt (11) Cis and ChAPt(11)Carbo induce programmed cell death with molecular features different from each other, suggesting that both drugs induce apoptosis through different initial pathways.
Authors and Affiliations
Kranthi Vanchanagiri Sebastian Paschke, Thomas Mueller, Hans-Joachim Schmoll
Keywords
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- EP ID EP312959
- DOI 10.15520/.v5i3.54
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More insight into the mode of action of lipophilic antitumor drugs containing a platinum (II) fragment
Cis-Diammine (1,1-cyclobutanedicarboxylato) platinum (II)) (Carboplatin 2) is a second generation platinum anticancer drug following Cis-diammine dichloro platinum (II) (Cisplatin 1). In the present study Cisplatin and C...