Dendrimer-Curcumin Conjugate: A Water Soluble and Effective Cytotoxic Agent Against Breast Cancer Cell Lines

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)


Volume 16, 12 Issues, 2016


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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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  • 27th of 59 in Chemistry, Medicinal

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Editor-in-Chief:
Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France


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Dendrimer-Curcumin Conjugate: A Water Soluble and Effective Cytotoxic Agent Against Breast Cancer Cell Lines



Anti-Cancer Agents in Medicinal Chemistry, 13(10): 1531-1539.

Author(s): Shawon Debnath, Darin Saloum, Sukanta Dolai, Chong Sun, Saadyah Averick, Krishnaswami Raja and Jimmie E Fata.

Affiliation: Department of Biology, College of Staten Island, 2800 Victory Blvd., Staten Island, NY, 10314, Biology or Biochemistry Doctoral Program, City University of New York Graduate Center, 365 Fifth Ave., NY, 10016, USA.

Abstract

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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Article Details

Volume: 13
Issue Number: 10
First Page: 1531
Last Page: 1539
Page Count: 9
DOI: 10.2174/18715206113139990139
Price: $58
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