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Cytotoxic activity of low molecular weight polyphenols against human oral tumor cell lines.
Authors: Fukai T; Sakagami H; Toguchi M; Takayama F Iwakura I; Atsumi T; Ueha T; Nakashima H; Nomura T
Source: Anticancer Res 2000 Jul-Aug;20(4):2525-36
A total of 150 chemically-defined natural and synthetic polyphenols
(flavonoids, dibenzoylmethanes, dihydrostilbenes,
dihydrophenanthrenes and 3-phenylchromen-4-ones), with molecular
weights ranging from 224 to 824, were investigated for cytotoxic
activity against normal, tumor and human immunodeficiency virus
(HIV)-infected cells. They showed higher cytotoxic activity against
human oral squamous cell carcinoma HSC-2 and salivary gland tumor HSG
cell lines than against normal human gingival fibroblasts HGF. Many
of the active compounds had a hydrophilic group (hydroxyl group) in
the vicinity of a hydrophobic group (prenyl, phenyl,
methylcyclohexene or methylbenzene moiety), similar to
isoprenoid-substituted flavones. Substitution of hydrophobic group
(prenyl or geranyl group) did not significantly change the cytotoxic
activity of flavanones, isoflavans, chalcones or
5-hydroxy-3-phenoxychromen-4-ones. However, the prenylation(s) of an
isoflavone and a 2-arylbenzofuran significantly enhanced the
cytotoxic activity. Agarose gel electrophoresis showed that active
components induced internucleosomal DNA fragmentation in human
promyelocytic leukemic HL-60 cells, but not in HSC-2 cells. Most of
the polyphenols failed to reduce the cytophathic effect of HIV
infection in MT-4 cells.