Cyanidin-3-glucoside, a natural product derived from blackberry, exhibits chemopreventive and chemotherapeutic activity

J Biol Chem. 2006 Jun 23;281(25):17359-68. doi: 10.1074/jbc.M600861200. Epub 2006 Apr 17.


Epidemiological data suggest that consumption of fruits and vegetables has been associated with a lower incidence of cancer. Cyanidin-3-glucoside (C3G), a compound found in blackberry and other food products, was shown to possess chemopreventive and chemotherapeutic activity in the present study. In cultured JB6 cells, C3G was able to scavenge ultraviolet B-induced *OH and O2-* radicals. In vivo studies indicated that C3G treatment decreased the number of non-malignant and malignant skin tumors per mouse induced by 12-O-tetradecanolyphorbol-13-acetate (TPA) in 7,12-dimethylbenz[a]anthracene-initiated mouse skin. Pretreatment of JB6 cells with C3G inhibited UVB- and TPA-induced transactivation of NF-kappaB and AP-1 and expression of cyclooxygenase-2 and tumor necrosis factor-alpha. These inhibitory effects appear to be mediated through the inhibition of MAPK activity. C3G also blocked TPA-induced neoplastic transformation in JB6 cells. In addition, C3G inhibited proliferation of a human lung carcinoma cell line, A549. Animal studies showed that C3G reduced the size of A549 tumor xenograft growth and significantly inhibited metastasis in nude mice. Mechanistic studies indicated that C3G inhibited migration and invasion of A549 tumor cells. These finding demonstrate for the first time that a purified compound of anthocyanin inhibits tumor promoter-induced carcinogenesis and tumor metastasis in vivo.

MeSH terms

  • Animals
  • Anthocyanins / metabolism
  • Anthocyanins / physiology*
  • Anticarcinogenic Agents / pharmacology
  • Antineoplastic Agents / pharmacology*
  • Benz(a)Anthracenes
  • Carcinogens
  • Cell Line, Tumor
  • Fruit
  • Glucosides / metabolism
  • Humans
  • Mice
  • Mice, Inbred C57BL
  • Mice, Inbred DBA
  • Neoplasm Metastasis
  • Plant Extracts / pharmacology*
  • Skin Neoplasms / chemically induced
  • Tetradecanoylphorbol Acetate
  • Transcriptional Activation
  • Ultraviolet Rays
  • Wound Healing


  • Anthocyanins
  • Anticarcinogenic Agents
  • Antineoplastic Agents
  • Benz(a)Anthracenes
  • Carcinogens
  • Glucosides
  • Plant Extracts
  • 7,12-dihydroxymethylbenz(a)anthracene
  • cyanidin 3-O-glucoside
  • Tetradecanoylphorbol Acetate