2021 Fiscal Year Final Research Report
Analysis of the interaction between flavones and phospholipid membranes in the early stage of biological activity expression
| Project/Area Number |
19K07138
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Review Section |
Basic Section 47050:Environmental and natural pharmaceutical resources-related
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| Research Institution | Keio University |
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Principal Investigator |
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| Co-Investigator(Kenkyū-buntansha) |
木内 文之 慶應義塾大学, 薬学部(芝共立), 教授 (60161402)
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| Project Period (FY) |
2019-04-01 – 2022-03-31
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| Keywords | フラボノイド類 / フラボン類 / フラボノール類 / リン脂質膜親和性 / NMR / 分子間相互作用 / リン脂質膜 / 構造活性相関 |
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| Outline of Final Research Achievements |
A wide variety of flavonoids that contribute to the structure-activity relationships were isolated from crude drugs or chemically synthesized to elucidate the relationship between the affinity of the flavonoids for phospholipid membranes and the intensity of their biological activities. The affinity of these flavonoids was calculated using immobilized artificial membrane columns showed a strong correlation with the amount of accumulation in the cell membrane, indicating that this method can be evaluated the accumulation of compounds in the membrane more easily and quickly than with conventional methods. Furthermore, by using model phospholipid membranes and NMR spectroscopy, we were able to elucidate the structural basis of the flavonoid dimers, theaflavins, in phospholipid membranes and chemically explain the differences in the intensity of the biological activity exhibited by theaflavins.
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| Free Research Field |
天然物化学，分析化学，食品化学
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| Academic Significance and Societal Importance of the Research Achievements |
化合物の生物活性発現初期機構を個々の分子の物理化学的性質（リン脂質膜親和性）と関連付けて実証している研究は稀であり，本研究課題は先駆的な位置付けであるといえる．また，化合物の細胞膜内蓄積量を簡便に評価することを可能にしたリン脂質カラム分析法の構築や，活性強度の差をリン脂質膜中における化合物の状態分析によって解明した本研究成果は学術的に意義があるといえる．さらに本研究課題によって創出されたフラボノイド類は今後のスクリーニングによって生物活性が見出されることにより，創薬研究のシーズ化合物として利用できると期待される．
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