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ANANBIOANAL - 2010
Pharmaceutical R & D Summit
doi:10.4172/2155-9872.1000042
Antiproliferative and Anticancer Activity of Copper Complexes
that Works without Chemical or hn as Stimulant
C.P. Rao
Department of Chemistry, Indian Institute of Technology Bombay, Powai, Mumbai, India
M
etallo-organic compounds are ever interesting to study their antitumor activity.
This talk deals with the syntheses, characterization and structure determination
of a Cu (II)-complex of anthtracenyl terpyridine and its plasmid cleavage, and
cytotoxicity towards different cancer cell lines. The plasmid cleavage studies were
carried out in presence of 1 in dark, under UV light and under visible light. While
all the three forms of the plasmid DNA are seen when carried out under visible
light, only closed and nicked circular forms were seen under UV light. In dark the
plasmid cleavage was spontaneous. 1 showed remarkable antiproliferative activity
for cancer cell lines, viz., cervical (HeLa, SiHa, CaSki), breast (MCF–7), liver
(HepG2), and lung (H1299). The IC50
values are in the range of 0.8 to 6.3 µM, which
is far superior as compared to the platin-drugs. Incubation of cells with 1 results in
granular structures only with the HPV infected ones and not with others as studied
by phase contrast and fluorescence microscopy (Figure). The role of HPV has
been further confirmed by transfecting the MCF-7 cells with E6. To our knowledge
this is the first copper complex that causes the cell death by interacting with HPV
viral protein. We have also shown antiproliferative activity of Cu(II)-complexes of
glycoconjugates. Therefore, our current focus is to modify the anthracenyl terpyridine
ligand with some glycosylation and/or by attaching some cellular receptors, so that
cell targeting can be achieved. Results of all these will be discussed.
ANALBIOANAL-2010
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