title: Dendrimer-curcumin conjugate: a water soluble and effective cytotoxic agent against breast cancer cell lines.
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.
authors: Shawon
authors: S
authors: Debnath
authors: Darin
authors: D
authors: Saloum
authors: Sukanta
authors: S
authors: Dolai
authors: Chong
authors: C
authors: Sun
authors: Saadyah
authors: S
authors: Averick
authors: Krishnaswami
authors: K
authors: Raja
authors: 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. jimmie.fata@csi.cuny.edu.
authors: Jimmie E
authors: JE
authors: Fata
mesh_terms: D000480:Alkynes / Q000737:chemistry; D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002264:Carboxylic Acids / Q000737:chemistry; D053148:Caspase 3 / Q000378:metabolism; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003474:Curcumin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D003603:Cytotoxins / Q000138:chemical synthesis / Q000494:pharmacology*; D050091:Dendrimers / Q000737:chemistry*; D004305:Dose-Response Relationship, Drug; D004789:Enzyme Activation / Q000187:drug effects; D005260:Female; D005690:Galactose / Q000737:chemistry; D006801:Humans; D006865:Hydrogenation; D057927:Hydrophobic and Hydrophilic Interactions; D015394:Molecular Structure; D012995:Solubility; D013329:Structure-Activity Relationship; D014867:Water
chemical_list: D000480:Alkynes; D000972:Antineoplastic Agents, Phytogenic; D002264:Carboxylic Acids; D003603:Cytotoxins; D050091:Dendrimers; D014867:Water; D053148:Caspase 3; D003474:Curcumin; D005690:Galactose