Submitted to: Journal of Agricultural and Food Chemistry
Publication Type: Peer reviewed journal
Publication Acceptance Date: 8/1/2002
Publication Date: 9/6/2002
Citation: MANTHEY, J.A., GUTHRIE, N. ANTIPROLIFERATIVE ACTIVITIES OF CITRUS FLAVONOIDS AGAINST 6 HUMAN CANCER CELL LINES. JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY. 2002. v. 50(2). p. 5837-5843. Interpretive Summary: Citrus fruit contains many health promoting compounds including numerous vitamins and antioxidants. One important class of antioxidants is the flavonoids. The flavonoids in citrus have been known to exhibit beneficial properties, including their potential anticancer activities. These anticancer actions were investigated in this report. A number of these citrus flavonoids were shown to strongly inhibit the growth of different types of human cancer cells. These inhibitory actions appeared to rely on the specific structures of these compounds. These actions further illustrate the health-promoting effects of the active citrus flavonoids.
Technical Abstract: Citrus fruit contain high concentrations of hydroxycinnamates, flavonoid glycosides, and polymethoxylated flavones. The latter group has been shown to inhibit the proliferation of a number of different cancer cell lines. This antiproliferative property was further demonstrated against a number of additional human cancer cell lines. Additionally, the antiproliferative actions of a series of novel synthetic methoxylated flavones were also studied. Similar to the naturally-occurring compounds, the synthetic compounds exhibited strong antiproliferative activities. In most cases the IC50 values occurred below 10 ppm. Other hydroxylated flavone and flavanone aglycones also exhibited antiproliferative activities against the 6 cancer cell lines, with the flavones showing greater activities than the flavanones. Glycosylation of these compounds removed their activity. The strong antiproliferative activities of the polymethoxylated flavones suggest that they may have use as anticancer agents in humans.