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Elucidation of the mechanism on the effect of methylquercetin inhibiting cancer metastasis.

Research Project

Project/Area Number 21K14888
Research Category

Grant-in-Aid for Early-Career Scientists

Allocation TypeMulti-year Fund
Review Section Basic Section 40020:Wood science-related
Research InstitutionGifu University

Principal Investigator

Yamauchi Kosei  岐阜大学, 応用生物科学部, 准教授 (10805427)

Project Period (FY) 2021-04-01 – 2024-03-31
Project Status Completed (Fiscal Year 2023)
Budget Amount *help
¥4,550,000 (Direct Cost: ¥3,500,000、Indirect Cost: ¥1,050,000)
Fiscal Year 2023: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2022: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2021: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Keywordsフラボノイド / 癌転移 / quercetin / MMP-1 / 抽出成分 / 遊走阻害
Outline of Research at the Start

クェルセチンは樹木や薬用植物,食品に広く含まれている代表的なフラボノイドの一種であり,多くの生物活性が報告されている。これまでにクェルセチンのメチル化体(MQ)が,クェルセチンよりも癌細胞の転移に関与する遊走を強力に阻害することが明らかとなっている。その作用機序の解明のため,MQの標的タンパク質の単離に用いるMQプローブの合成に成功している。本研究では本合成プローブを用いてMQの標的タンパク質を単離同定し,MQの作用メカニズムを分子レベルで明らかにする。

Outline of Final Research Achievements

Pull-down assays using the synthesized flavonoid probes suggested that MMP-1 was one of the target proteins of the quercetin derivative. Surface Plasmon Resonance (SPR) analysis confirmed that the interaction between the quercetin derivative and the recombinant MMP-1 catalytic domain was concentration-dependent.1H-15N HSQC NMR analysis showed that the quercetin derivative interacts with the metal ion vicinity of MMP-1. These results suggested that quercetin derivatives inhibited the activity of MMP-1 and suppressed the migration of cancer cells by binding near metal ions.

Academic Significance and Societal Importance of the Research Achievements

フラボノイドの生理機能は多岐に渡り、その有用性を示す報告は近年加速度的に増加している。そのため作用機序の解明や合成法、代謝過程などフラボノイドの動物細胞における影響について研究が行われ、年間1万報を超える関連論文が投稿されている。しかし、機能性成分として報告され続けているフラボノイド類の、直接的な作用機構は殆ど明らかにされておらず、その標的タンパク質の探索は世界的な競争になっている。本研究で、代表的なフラボノイドのひとつであるquercetin及びその誘導体の標的タンパク質及び、作用様式をNMR法を用いて初めて明らかにし、フラボノイドの活性メカニズムの一端を明らかにする事に成功した。

Report

(4 results)
  • 2023 Annual Research Report   Final Research Report ( PDF )
  • 2022 Research-status Report
  • 2021 Research-status Report
  • Research Products

    (41 results)

All 2024 2023 2022 2021

All Journal Article (12 results) (of which Int'l Joint Research: 8 results,  Peer Reviewed: 12 results,  Open Access: 6 results) Presentation (29 results) (of which Int'l Joint Research: 6 results,  Invited: 3 results)

  • [Journal Article] Antioxidant components of the three different varieties of Indonesian ginger essential oil: In vitro and computational studies2024

    • Author(s)
      Badrunanto、Wahyuni Wulan Tri、Farid Muhammad、Batubara Irmanida、Yamauchi Kosei
    • Journal Title

      Food Chemistry Advances

      Volume: 4 Pages: 100558-100558

    • DOI

      10.1016/j.focha.2023.100558

    • Related Report
      2023 Annual Research Report
    • Peer Reviewed / Open Access / Int'l Joint Research
  • [Journal Article] Ginsenoside Rg5 as an anticancer drug: a comprehensive review on mechanisms, structure?activity relationship, and prospects for clinical advancement2024

    • Author(s)
      Elsaman Tilal、Muddathir Ali Mahmoud、Mohieldin Ebtihal A. M.、Batubara Irmanida、Rahminiwati Min、Yamauchi Kosei、Mohamed Magdi Awadalla、Asoka Shadila Fira、B?sselberg Dietrich、Habtemariam Solomon、Sharifi-Rad Javad
    • Journal Title

      Pharmacological Reports

      Volume: 76 Issue: 2 Pages: 287-306

    • DOI

      10.1007/s43440-024-00586-5

    • Related Report
      2023 Annual Research Report
    • Peer Reviewed / Int'l Joint Research
  • [Journal Article] New flavan trimer from Daemonorops draco as osteoclastogenesis inhibitor2024

    • Author(s)
      Tsuchiya Ayaka、Suzuki Maki、Ito Ryotaro、Batubara Irmanida、Yamauchi Kosei、Mitsunaga Tohru
    • Journal Title

      Fitoterapia

      Volume: 172 Pages: 105757-105757

    • DOI

      10.1016/j.fitote.2023.105757

    • Related Report
      2023 Annual Research Report
    • Peer Reviewed / Int'l Joint Research
  • [Journal Article] Garcidepsidone B from Garcinia parvifolia: antimicrobial activities of the medicinal plants from East and North Kalimantan against dental caries and periodontal disease pathogen2023

    • Author(s)
      Egra Saat、Kuspradini Harlinda、Kusuma Irawan Wijaya、Batubara Irmanida、Yamauchi Kosei、Mitsunaga Tohru
    • Journal Title

      Medicinal Chemistry Research

      Volume: 32 Issue: 8 Pages: 1658-1665

    • DOI

      10.1007/s00044-023-03071-5

    • Related Report
      2023 Annual Research Report
    • Peer Reviewed / Int'l Joint Research
  • [Journal Article] Chemical Constituent of Acacia auriculiformis Wood Extractives and Their Antioxidant Activity2023

    • Author(s)
      Prayogo Yanico Hadi、Batubara Irmanida、Sari Rita Kartika、Egra Saat、Yamauchi Kosei、Mitsunaga Tohru、Syafii Wasrin
    • Journal Title

      Jurnal Sylva Lestari

      Volume: 11 Issue: 3 Pages: 370-381

    • DOI

      10.23960/jsl.v11i3.753

    • Related Report
      2023 Annual Research Report
    • Peer Reviewed / Open Access / Int'l Joint Research
  • [Journal Article] The potential of five wild growing aromatic plants from Hemaq Beniung Customary Forest on antidiabetic activity2023

    • Author(s)
      Kuspradini Harlinda、Putri Agmi Sinta、Kiswanto Kiswanto、Sa’adah Hayatus、Fajriansyah、Rizqullah, Muhammad Akmal、Larasati, Anisa Gifta、Zulfa, Najmia Afifah、Egra, Saat、Yamauchi, Kosei、Mitsunaga, Tohru
    • Journal Title

      Biodiversitas Journal of Biological Diversity

      Volume: 24 Issue: 4 Pages: 2156-2162

    • DOI

      10.13057/biodiv/d240427

    • Related Report
      2023 Annual Research Report
    • Peer Reviewed / Open Access / Int'l Joint Research
  • [Journal Article] Protein aggregation model to explain the bioactivity of condensed tannins2023

    • Author(s)
      Yamauchi Kosei、Soyano Mayu、Kobayashi Miho、Kamatari Yuji O.、Mitsunaga Tohru
    • Journal Title

      Food Chemistry

      Volume: 416 Pages: 135870-135870

    • DOI

      10.1016/j.foodchem.2023.135870

    • Related Report
      2022 Research-status Report
    • Peer Reviewed
  • [Journal Article] Potential of prospective medicinal plants of Rhizophoraceae from North Kalimantan, Indonesia2023

    • Author(s)
      Egra Saat、Kuspradini Harlinda、Kusuma Irawan Wijaya、Batubara Irmanida、Imra、Nurjannah Nurjannah、Wahyuni Etty、Yamauchi Kosei、Mitsunaga Tohru
    • Journal Title

      Biodiversitas Journal of Biological Diversity

      Volume: 24 Issue: 3 Pages: 1346-1355

    • DOI

      10.13057/biodiv/d240303

    • Related Report
      2022 Research-status Report
    • Peer Reviewed / Open Access / Int'l Joint Research
  • [Journal Article] Development of flavonoid probes and the binding mode of the target protein and quercetin derivatives2022

    • Author(s)
      Tsuchiya Ayaka、Kobayashi Miho、Kamatari Yuji O.、Mitsunaga Tohru、Yamauchi Kosei
    • Journal Title

      Bioorganic & Medicinal Chemistry

      Volume: 68 Pages: 116854-116854

    • DOI

      10.1016/j.bmc.2022.116854

    • Related Report
      2022 Research-status Report
    • Peer Reviewed / Open Access
  • [Journal Article] Arnica montana L. extract containing 6‐O‐methacryloylhelenalin and 6‐O‐isobutyrylhelenalin accelerates growth and differentiation of human subcutaneous preadipocytes and leads volumizing of skin2022

    • Author(s)
      Sakamoto Kotaro、Watanabe Chiharu、Masutani Teruaki、Hirasawa Asuka、Wakamatsu Kanae、Iddamalgoda Arunasiri、Kakumu Yuya、Yamauchi Kosei、Mitsunaga Tohru
    • Journal Title

      International Journal of Cosmetic Science

      Volume: 45 Issue: 1 Pages: 1-13

    • DOI

      10.1111/ics.12815

    • Related Report
      2022 Research-status Report
    • Peer Reviewed / Open Access
  • [Journal Article] Ellagitannins from Rosa roxburghii suppress poly(I:C)-induced IL-8 production in human keratinocytes2021

    • Author(s)
      Takayama Satoru、Kawanishi Miho、Yamauchi Kosei、Tokumitsu Daiki、Kojima Hiroyuki、Masutani Teruaki、Iddamalgoda Arunasiri、Mitsunaga Tohru、Tanaka Hiroyuki
    • Journal Title

      Journal of Natural Medicines

      Volume: in press Issue: 3 Pages: 623-632

    • DOI

      10.1007/s11418-021-01509-x

    • NAID

      40022589326

    • Related Report
      2021 Research-status Report
    • Peer Reviewed
  • [Journal Article] New benzoic acid and caffeoyl derivatives with anti-inflammatory activities isolated from leaves of <i>Ilex kaushue</i>2021

    • Author(s)
      Kakumu Yuya、Nguyen Thi Minh Tu、Yamauchi Kosei、Mitsunaga Tohru
    • Journal Title

      Natural Product Research

      Volume: 12 Issue: 12 Pages: 1-9

    • DOI

      10.1080/14786419.2021.1939334

    • Related Report
      2021 Research-status Report
    • Peer Reviewed / Int'l Joint Research
  • [Presentation] Molecular networking assisted in the rapid discovery of bioactive compounds from Excoecaria cochinchinensis leaves2024

    • Author(s)
      Yen Thi Hoang Kieu, Kosei Yamauchi, Tohru Mitsunaga
    • Organizer
      第74回日本木材学会
    • Related Report
      2023 Annual Research Report
  • [Presentation] Garcidepsidon B from Garcinia parvifolia: Antimicrobial Activities of The Medicinal Plants from North Kalimantan against Dental Caries and Periodontal Disease Pathogens2024

    • Author(s)
      Saat Egra, Kosei Yamauchi, Tohru Mitsunaga, Harlinda Kuspradini, Irawan Wijaya Kusuma, Irmanida Batubara
    • Organizer
      第74回日本木材学会
    • Related Report
      2023 Annual Research Report
  • [Presentation] Daemonorops draco果実由来竜血成分の骨粗鬆症抑制効果と作用機序の一考察2024

    • Author(s)
      土屋 綾香、中嶋 和紀、山内 恒生、光永 徹
    • Organizer
      第74回日本木材学会
    • Related Report
      2023 Annual Research Report
  • [Presentation] マウスのストレス性脳障害改善に及ぼすスギ材精油香気成分Ⅲ2024

    • Author(s)
      竹山 大暁、山内 恒生、光永 徹
    • Organizer
      第74回日本木材学会
    • Related Report
      2023 Annual Research Report
  • [Presentation] Utilization of bioactive compound from plants.2024

    • Author(s)
      Kosei Yamauchi
    • Organizer
      International Conference on Climate Change, Agriculture, Biodiversity, and Environment Study
    • Related Report
      2023 Annual Research Report
  • [Presentation] 竜血抽出物の成分探索と破骨細胞分化に及ぼす効果2023

    • Author(s)
      土屋綾香、山内恒生、光永徹
    • Organizer
      第6回樹木抽出成分研究交流会
    • Related Report
      2023 Annual Research Report
  • [Presentation] Daemonorops draco 果実抽出物の成分探索と破骨細胞ならびに骨粗鬆症モデルマウ スに及ぼす影響2023

    • Author(s)
      土屋綾香、山内恒生、光永 徹
    • Organizer
      東海地区創薬デザイン研究会
    • Related Report
      2023 Annual Research Report
  • [Presentation] 縮合型タンニンの生理作用機序を示すタンパク質凝集モデル2023

    • Author(s)
      山内恒生、征矢野真由、小林美穂、鎌足雄司、光永 徹
    • Organizer
      東海地区創薬デザイン研究会
    • Related Report
      2023 Annual Research Report
  • [Presentation] キリンケツヤシ(Daemonorops draco)果実由来竜血の成分探索と破骨細胞分化ならびに骨粗鬆症モデルマウス骨量に及ぼす効果2023

    • Author(s)
      土屋綾香、山内恒生、光永 徹
    • Organizer
      第73回日本木材学会大会
    • Related Report
      2022 Research-status Report
  • [Presentation] マウスのストレス性脳障害改善に及ぼす杉材精油香気成分2023

    • Author(s)
      竹山大暁、山内恒生、光永 徹
    • Organizer
      第73回日本木材学会大会
    • Related Report
      2022 Research-status Report
  • [Presentation] 苦丁茶は成分の破骨細胞分化に及ぼす効果2022

    • Author(s)
      鈴木真希、各務裕也、山内恒生、光永 徹、Mihn Tu Thi Nguyen
    • Organizer
      日本生薬学会 第68回年会
    • Related Report
      2022 Research-status Report
  • [Presentation] 有色木材心材の色調変化メカニズムの解明2022

    • Author(s)
      多賀勇亮、光永徹、山内恒生
    • Organizer
      日本ポリフェノール学会第15回学術集会
    • Related Report
      2022 Research-status Report
  • [Presentation] 縮合型タンニンのタンパク質凝集モデル2022

    • Author(s)
      山内恒生、征矢野真由、小林美穂、鎌足雄司、光永 徹
    • Organizer
      日本ポリフェノール学会第15回学術集会
    • Related Report
      2022 Research-status Report
  • [Presentation] 破骨細胞分化抑制活性を有するDaemonorops draco抽出物の成分探索2022

    • Author(s)
      土屋綾香、山内恒生、光永 徹
    • Organizer
      日本ポリフェノール学会第15回学術集会
    • Related Report
      2022 Research-status Report
  • [Presentation] NMRを用いたタンニンのタンパク質凝集メカニズムの解明2022

    • Author(s)
      山内恒生、菅原由喜、征矢野真由、小林美穂、鎌足雄司、光永 徹
    • Organizer
      日本木材学会中部支部大会
    • Related Report
      2022 Research-status Report
  • [Presentation] 破骨細胞分化抑制活性を有するDaemonorops draco抽出物の成分探索とそのメカニズム2022

    • Author(s)
      土屋綾香、イルマニダバツバラ、山内恒生、光永 徹
    • Organizer
      日本木材学会中部支部大会
    • Related Report
      2022 Research-status Report
  • [Presentation] Neurite outgrowth effect on PC12 cells from Piper longum fruit extracts2021

    • Author(s)
      Runa Fujimoto, Masahiro Kassai, Kosei Yamauchi, Tohru Mitsunaga
    • Organizer
      The 11th JCK Joint Symposium on Pharmacognosy
    • Related Report
      2021 Research-status Report
    • Int'l Joint Research
  • [Presentation] Structural analysis of saponins from the leaves of Ilex kaushue (Kudingcha)2021

    • Author(s)
      Maki Suzuki, Minh Tu Thi Nguyen, Kosei Yamauchi, Tohru Mitsunaga
    • Organizer
      The 11th JCK Joint Symposium on Pharmacognosy
    • Related Report
      2021 Research-status Report
    • Int'l Joint Research
  • [Presentation] Bioactivity and mechanism of components in medicinal plant2021

    • Author(s)
      Kosei Yamauchi
    • Organizer
      International Guest Lectures on Role Secondary Metabolite in Medicinal Plants
    • Related Report
      2021 Research-status Report
    • Int'l Joint Research / Invited
  • [Presentation] Identification of NK cell activator from Citrus hystrix leaf extracts2021

    • Author(s)
      Takafumi Hara, Masahiro Kassai, Kosei Yamauchi, Tohru Mitsunaga
    • Organizer
      The 11th JCK Joint Symposium on Pharmacognosy
    • Related Report
      2021 Research-status Report
    • Int'l Joint Research
  • [Presentation] Strategy on elucidation of bioactivity mechanism of flavonoids2021

    • Author(s)
      Kosei Yamauchi
    • Organizer
      Kalimantan Plant Biodiversity For The Development Of Medicines Seminar Series
    • Related Report
      2021 Research-status Report
    • Int'l Joint Research / Invited
  • [Presentation] Investigation of Bioactivity Mechanism of Flavonoids in Cancer Cells2021

    • Author(s)
      Kosei Yamauchi, Ayaka Tsuchiya, Tohru Mitsunaga
    • Organizer
      Annual Meeting of the Korean Society of Wood Science and Technology
    • Related Report
      2021 Research-status Report
    • Int'l Joint Research / Invited
  • [Presentation] サイプレス材精油香気雰囲気下飼育によるマウスの肥満抑制 メカニズムの解明2021

    • Author(s)
      林 貴之, 山内 恒生, 光永 徹
    • Organizer
      第71回日本木材学会大会
    • Related Report
      2021 Research-status Report
  • [Presentation] Garcinia kola 種子抽出成分の探索と口腔疾患原因菌に対する抗菌活性2021

    • Author(s)
      日置 裕介, Siaw ONWONA-AGYEMAN, 山内 恒生, 光永 徹
    • Organizer
      第71回日本木材学会大会
    • Related Report
      2021 Research-status Report
  • [Presentation] 紫夏藤 (Millettia reticulata) 由来縮合型タンニンの構造解析とGTase阻害活性2021

    • Author(s)
      征矢野 真由、山内恒生、光永 徹
    • Organizer
      日本木材学会中部支部大会
    • Related Report
      2021 Research-status Report
  • [Presentation] サイプレス材精油雰囲気下におけるマウスの肥満抑制作用とその作用機作2021

    • Author(s)
      林 貴之、山内恒生、光永徹
    • Organizer
      第65回 香料・テルペン及び精油化学に関する討論会
    • Related Report
      2021 Research-status Report
  • [Presentation] がん遊走を阻害するquercetin誘導体の標的タンパク質の探索と作用機序の解明2021

    • Author(s)
      山内恒生,土屋綾香,小林美穂, 鎌足雄司, 光永 徹
    • Organizer
      日本ポリフェノール学会第14回学術集会
    • Related Report
      2021 Research-status Report
  • [Presentation] 破骨細胞分化抑制活性を有する Daemonorops draco抽出物の成分探索2021

    • Author(s)
      土屋綾香,山内恒生,光永 徹
    • Organizer
      日本ポリフェノール学会第14回学術集会
    • Related Report
      2021 Research-status Report
  • [Presentation] パープルハート(Peltogyne spp.) 芯材色素成分の構造と色調発現に関する研究2021

    • Author(s)
      多賀 勇亮,山内 恒生 ,光永 徹
    • Organizer
      日本ポリフェノール学会第14回学術集会
    • Related Report
      2021 Research-status Report

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Published: 2021-04-28   Modified: 2025-01-30  

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