|
KMID : 1140120060110030211
|
|
Cancer Prevention Research
2006 Volume.11 No. 3 p.211 ~ p.217
|
|
|
Synthesis of Methoxylated Flavone Derivatives and Examination of Their Effects on HT-29 Human Colon Cancer Cell Growth
|
|
Lim Soon-Sung
Lee Yeon-Sil
Cho Han-Jin
Shin Hyun-Kyung
Yoon Jung-Han
|
|
|
Abstract
|
|
|
|
In a search for new potential anticancer agents, we have synthesized methoxylated flavone derivatives and examined their effects on colon cancer cell growth. To examine whether these compounds inhibit HT-29 cell growth, cells were cultured with various concentrations of the test compounds for 2 days and the viable cell numbers were estimated by a colorimetric MTT assay. Among the synthesized compounds, 6,7-dimethyl-3’,4’-dimethoxyflavone (the compound 9) was most potent and efficacious, with an IC50 value as low as 21.68 0.13μM. However, the same concentrations of this compound did not inhibit the growth of IEC-6 cells, normal rat intestinal crypt cells. Staining cells with annexin V revealed that the compound 9 induced apoptosis of HT-29 cells in a dose-dependent manner. Western blot analysis of cell lysates revealed that the compound 9 inhibited phosphorylation of Akt and extracellular signal- regulated kinase (ERK)-1/2 and induced cleavage of caspase-3, -7, -9 and poly (ADP-ribose) polymerase. These results indicate that the induction of apoptosis is one of the mechanisms by which the synthetic flavone (the compound 9) inhibits HT-29 cell growth. The compound 9 may have potential as a chemopreventive agent and/or adjuvant for chemotherapeutic drugs.
|
|
|
KEYWORD
|
|
|
6,7-dimethyl-3’,4’-dimethoxyflavone, HT-29 human colon cancer cells, Apoptosis
|
|
|
FullTexts / Linksout information
|
|
|
|
|
Listed journal information
|
|
 
|
|