Abstract

Betulinic acid (1) and Cisplatin (CP) are apoptosis causing antitumor agents. In our previous report we demonst a-ted the synthesis, characterization and in vitro anticancer activity of novel conjugates containing Betulinic acid (1) at one end and Cisplatin (CP) similar ligand at other end [Emmerich et al., 2014]. The property of presence of two cytotoxic groups is called “Double loading”. Preliminary results showed that all novel conjugates exerted a dose dependent antiproliferative action at micromolar concentrations towards target tumor cell lines. In order to complement the previous results, in this report we looked for the anticancer mechanism of action of novel conjugates with their precursor molecules on A549 lung cancer cell line, which contributes to the understanding of the cytotoxic potential and their structure-activity relationship. A series of investigations had been carried out successfully which includes Microscopic studies, DNA Fragmentation assay, Cell cycle analysis, Annexin V/Propidium Iodide (PI) assay and Caspase assays. Interestingly, the results revealed that novel conjugates retain cytotoxicty and they induce apoptotic cell death which is identical to that of Betulinic acid (1).