Curcumin, which is derived from the plant Curcuma longa, has received considerable attention as a possible anti-cancer agent.
In cell culture, curcumin is capable of inducing apoptosis in cancer cells at concentrations that do not affect normal cells. One draw-back
holding curcumin back from being an effective anti-cancer agent in humans is that it is almost completely insoluble in water and
therefore has poor absorption and subsequently poor bioavailability. Here we have generated a number of curcumin derivatives
(tetrahydro-curcumin, curcumin mono-carboxylic acid, curcumin mono-galactose, curcumin mono-alkyne and dendrimer-curcumin
conjugate) to test whether any of them display both cytotoxicity and water solubility. Of those tested only dendrimer-curcumin conjugate
exhibited both water solubility and cytotoxicity against SKBr3 and BT549 breast cancer cells. When compared to curcumin dissolved in
DMSO, dendrimer-curcumin conjugate dissolved in water was significantly more effective in inducing cytotoxicity, as measured by the
MTT assay and effectively induced cellular apoptosis measured by caspase-3 activation. Since dendrimer-curcumin conjugate is water
soluble and capable of inducing potent cytotoxic effects on breast cancer cell lines, it may prove to be an effective anti-cancer therapy to
be used in humans.
Keywords: Apoptosis, breast cancer, curcumin, dendrimer, solubility.
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