Summary: | Signal transduction disregulation, i.e. MAP kinase pathway leads to
degenerative disease development, including cancer. Today, people are seeking
for co-chemotherapeutic agent to increase chemotherapeutic agent�s effectiveness
and decrease its side effect. Curcumin is a potential chemopreventive agent
targeting kinase proteins on their ATP binding site. Thus, Faculty of Pharmacy
UGM developed curcumin analogue, PGV-0. Due to its insolubility, Na PGV-0
was then synthesized. This research was done to study Na PGV-0 potential as cochemotherapeutic
agent targeting proteins involved in MAP kinase pathway,
especially EGFR and IKK, and its effector protein, Pgp and COX-2.
Co-chemotherapeutic activity was determined by cytotoxicity single and in
combination with doxorubicin on MCF-7 ori, MCF-7/DOX, HeLa, and WiDr
cells using MTT assay. While the molecular mechanisms were explored in silico
using PLANTS software. Na PGV-0 as ligand was prepared using Marvin Sketch,
while protein targets were prepared using YASARA.
Na PGV-0 exhibited cytotoxic property on MCF-7 ori, MCF-7/DOX,
HeLa, and WiDr cells with IC50 values of 52.33 + 6.36
|