ABAZA, M. S, KHAN, Akram and AFZAL, M (2012). Chemistry, biochemistry and selective cytotoxicity of curcumin analogues against human cancer cell lines. In: SASAKI, Jun and KICHIDA, Masaki, (eds.) Curcumin: Biosynthesis, medicinal uses and health benefits. Nova science publishers, 105-132. [Book Section]
Abstract
Several curcuminoids including curcumin have been identified from the rhizome of a
common spice Curcuma longa (Zingaberaceae). These natural curcuminoids display
several pharmacological activities including anticancer activity. We have synthesized a
range of curcumin analogues with phenolic, thiophene, furanyl, ascorbyl, indole,
naphthyl, haloaryl and alkoxyphenyl groups and have shown that from amongst these
compounds alkoxyphenyl curcumins have higher potential as anticancer agents. The
synthetic curcumin analogues (Cd1-Cd6) showed a dose-dependent anti-mitogenic
activity against human colorectal (CCL218), breast (HTB26) and lung (HTB182) cancer
cell lines with minimal effect on normal human fibroblast (CRL1554) (≤ 20%). Our
results demonstrate that synthetic curcumin analogues exerted a potency order Cd5 (IC50
= 12.3 μg/ml) > Cd4 (IC50 = 23.46 μg/ml) > Cd2 (IC50 = 26.15 μg/ml) > Cd6 (IC50 = 28.3
μg/ml) > Cd1 (IC50 = 38.46 μg/ml) > curcumin (IC50 =53.3 μg/ml) against CCL218 and
Cd4 (IC50 = 11.15μg/ml) > Cd5 (IC50 = 12.3 μg/ml) > curcumin(IC50 =13.3μg/ml) against
HTB26 as well as Cd5 (IC50 = 13.85 μg/ml) > curcumin(IC50 = 18.3 μg/ml) against
HTB182. These results indicate that Cd4 and Cd5 curcumin analogues exhibit the highest
anti-proliferative activities toward all the tested cancer cell lines with minimal
cytotoxicity on normal human fibroblast. Further in vitro and in vivo studies are
warranted to evaluate the chemopreventive/chemotherapeutic potential of these
derivatives and to understand the potential molecular mechanisms of their action.
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