ANTIPROLIFERATIVE ACTIVITIES OF SYNTHETIC DERIVATIVES OF METHOXYLATED FLAVONES FROM CITRUS

Authors: Manthey, John; GUTHRIE, NAJLA - KGK SYNERGIZE

Submitted to: American Chemical Society National Meeting
Publication Type: Abstract Only
Publication Acceptance Date: 8/1/2001
Publication Date: 9/1/2001
Citation: Manthey, J.A., Guthrie, N. Antiproliferative activities of synthetic derivatives of methoxylated flavones from citrus. 222nd National Meeting of American Chemical Society. 2001. Paper No. AGFD 68.

Interpretive Summary:

Technical Abstract: Citrus fruit contain high concentrations of several important classes of phenols, especially in the peel. These compounds included numerous hydroxycinnamates, flavonoid glycosides, and the polymethoxylated flavones. The latter species occur without glycosidic linkages, unlike the main flavonoid glycosides in citrus. Recently, the citrus polymethoxylated flavones have been characterized as anticancer agents, mainly in 'in vitro' studies. A series of highly methoxylated flavone derivatives with structures similar to the naturally-occuring polymethoxylated flavones have been synthesized. The antiproliferative activities of these compounds were tested against 5 human cancer cell lines. Similar to the naturally-occurring compounds the synthetic compounds exhibited strong antiproliferative actions. In most cases the IC50 values occurred below 10 ppm. These strong antiproliferative activities provide structure/activity relationship information on the biological actions of the naturally occurring flavonoids in citrus.