| Project/Area Number |
16K18704
|
|---|
| Research Category |
Grant-in-Aid for Young Scientists (B)
|
| Allocation Type | Multi-year Fund |
|---|
| Research Field |
Food science
|
|---|
| Research Institution | Kagoshima University |
|---|
Principal Investigator |
Kozue Sakao 鹿児島大学, 農水産獣医学域農学系, 助教 (40713285)
|
|---|
| Project Period (FY) |
2016-04-01 – 2019-03-31
|
| Project Status |
Completed (Fiscal Year 2018)
|
| Budget Amount *help |
¥4,030,000 (Direct Cost: ¥3,100,000、Indirect Cost: ¥930,000)
Fiscal Year 2018: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2017: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2016: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
|
|---|
| Keywords | ケルセチン / アセチル化 / 生理活性評価 / 3Ac-Q分離精製 / X線結晶構造解析 / アセチル化ケルセチン |
|---|
| Outline of Final Research Achievements |
In order to elucidate the reason why the biological activity of acetylated quercetin is enhanced over the biological activity of quercetin, we focus on the number of acetyl groups and their substituted position of quercetin. We successfully synthesized quercetin derivatives which were substituted the 1-5 hydroxyl groups of quercetin with acetyl groups. Treatment of HCT-116 human colon cancer cells with quercetin and its derivatives was found to significantly inhibit cell proliferation in the order of 4Ac-Q, 3Ac-Q, 5Ac-Q, and quercetin. This means that the increase in biological activity of acetylated quercetin is due not only to the number of acetyl groups but also to the substitution position. It was also revealed that the acetylated form improves the membrane permeability and the metabolic rate of the acetylated form is slower than that of quercetin, and may be effective by staying in vivo for a long time.
|
| Academic Significance and Societal Importance of the Research Achievements |
天然化合物の一部を修飾し、その生理活性を細胞を用いて評価する研究報告例はあまりなく、中でも生理活性増強が何に起因するかについて深く言及している研究報告はほとんど無い。そのため、本研究においてケルセチンのアセチル誘導体がケルセチンより強い活性を示す理由について、明確な科学的見解を提示し一連の生物学的操作の流れを構築したことは学術的に重要な意義を持つと考えている。また本研究で得ることが出来た最大の成果として、アセチル化による生理活性増強がアセチル基の数ではなく、ヒドロキシル基の修飾部位に起因することが解明されたことがあり、他のフラボノール類の生理活性増強のヒントになりうる点でも意義深いと思われる。
|
