| Budget Amount *help |
¥3,640,000 (Direct Cost: ¥2,800,000、Indirect Cost: ¥840,000)
Fiscal Year 2015: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
Fiscal Year 2014: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
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| Outline of Final Research Achievements |
To directly demonstrate the role of hydroxyl groups, we have synthesized 3,7,3',4'-O-tetraacetylquercetin (4Ac-Q) and 3,7,3',4'-O-tetrabenzylquercetin (4Bn-Q), which are substituted the hydroxyl groups of quercetin with acetyl or benzyl groups. Treatment of HCT116 human colon carcinoma cells with quercetin and its derivatives revealed that 4Ac-Q and quercetin, but not 4Bn-Q, significantly inhibit cell viability. Apoptosis as characterized by DNA fragmentation, activation of caspase-3, and PARP cleavage, was detected in the cells treated with quercetin or 4Ac-Q, but not with 4Bn-Q. Mitochondrial ROS data showed that quercetin and 4Ac-Q contributed to superoxide generation, consequently causing apoptosis. Furthermore, quercetin as well as 4Ac-Q treatment also induced autophagy. Taken together, the present study demonstrates that quercetin and 4Ac-Q induces a mitochondrial ROS-mediated apoptosis and the autophagy in HCT116 human colon carcinoma cells.
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