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伝承薬物を素材とする糖吸収抑制作用物質の開拓

Research Project

Project/Area Number 09771932
Research Category

Grant-in-Aid for Encouragement of Young Scientists (A)

Allocation TypeSingle-year Grants
Research Field Chemical pharmacy
Research InstitutionKyoto Pharmaceutical University

Principal Investigator

村上 敏之  京都薬科大学, 薬学部, 助手 (40278445)

Project Period (FY) 1997 – 1998
Project Status Completed (Fiscal Year 1998)
Budget Amount *help
¥1,900,000 (Direct Cost: ¥1,900,000)
Fiscal Year 1998: ¥600,000 (Direct Cost: ¥600,000)
Fiscal Year 1997: ¥1,300,000 (Direct Cost: ¥1,300,000)
KeywordsSalacia reticulata / Salacia oblonga / Kotalanol / α-グリコシダーゼ阻害活性 / 地膚子 / Kochianoside / 血糖値上昇抑制活性 / momordin lc / salacinol / α-グルコシダーゼ阻害活性 / Myrcia sphaerocarpa / myrciacitrin / myrciaphenone / アルドース還元酵素阻害活性
Research Abstract

スリランカにおいて糖尿病の特効薬として用いられるSalacia reticulata根からsalacinolの他に、新たに天然では非常に珍しいチオ糖分子内スルホニウム硫酸塩構造を有するkotalanolを単離し、その平面構造を明らかにした。そしてkotalanolについてin vitroでのα-グルコシダーゼ阻害活性を検討し、salacinolと同様に市販医薬品よりも強い阻害活性のあることを明らかにした。さらに、インド産のアーユルヴェーダ生薬Salacia oblonga根のMeOHエキスにもショ糖負荷でのラットの血糖値上昇に対して非常に強い抑制活性及びin vitroにおいて強いα-グルコシダーゼ阻害活性を見出した。そこで、S.oblongaについても α-グルコシダーゼ阻害活性を指標に有効成分を探索した結果、salacinol及びkotalanolを単離した。
地膚子から新たに、kochianoside A、B、Cを単離し、それらの構造を決定するとともに、地膚子から単離したサポニン類についてラットにおけるグルコース負荷による血糖値上昇抑制作用を検討し、活性発現に関する興味深い知見を得た。また、主成分momordin Ic、IICについて血糖値上昇抑制活性を発現するメカニズムについて検討し、これらサポニン類はインスリン分泌促進作用やインスリン様作用など末梢での糖代謝促進には関与せず、胃から空調への糖質の移行を遅らせ、小腸粘膜上皮細胞に存在するグルコース輸送系を阻害することにより、血中への糖の移行を抑制することを明らかにした。
また、西洋トチノキ種子及びセネガ根から単離したescin Ia、Ib、 E,Z-seneginIIについても血糖値上昇抑制活性及びそのメカニズムを検討し、サポニン構造と活性の相関関係について興味深い知見を得るなど当初の計画をほぼ達成した。

Report

(2 results)
  • 1998 Annual Research Report
  • 1997 Annual Research Report
  • Research Products

    (14 results)

All Other

All Publications (14 results)

  • [Publications] Toshiyuki Murakami: "Kotalanol,a Potent α-Glucosidase Inhibitor with Thiosuger Sulfonium Sulfate Structure,from Antidiabetic Ayurvedic Medicine Salacia reticulata" Chemical & Pharmaceutical Bulletin. 46・8. 1339-1340 (1998)

    • Related Report
      1998 Annual Research Report
  • [Publications] Toshiyuki Murakami: "Mode of Action of Escins Ia and IIa and E,Z-Snegin II on Glucose Absorption in Gastrointestinal Tract" Bioorganic & Medicinal Chemistry. 6. 1019-1023 (1998)

    • Related Report
      1998 Annual Research Report
  • [Publications] Toshiyuki Murakami: "Antidiabetic Pronciples of Natural Medicines.III.Structure-Related Inibitory Activity and Action Mode of Oleanolic Acid Oligoglycosides on Hypoglycemic Activity" Chemical & Pharmaceutical Bulletin. 46・9. 1399-1403 (1998)

    • Related Report
      1998 Annual Research Report
  • [Publications] Toshiyuki Murakami: "Medicinal Foodstuffs.XV.Sugar Beet. (2) : Structures of Betavulgarosides V,VI,VII,VIII,IX,and X from the Roots and Leaves of Sugar Beet (Beta vulgaris L.,Chenopodiaceae)" Chemical & Pharmaceutical Bulletin. 46・11. 1758-1763 (1998)

    • Related Report
      1998 Annual Research Report
  • [Publications] Toshiyuki Murakami: "Strudies on Kochiae Fructus. V.Antipururitic Effects of Oleanolic Acid Glycosides and the Structures-Requirement" Biological & Pharmaceutical Bulletin. 21・11. 1231-1233 (1998)

    • Related Report
      1998 Annual Research Report
  • [Publications] Toshiyuki Murakami: "Structures of New Acylated Oleanene-Type Triterpene Oligolysides,Theasaponins E_1 and E_2,from the Seeds of Tea Plant,Camellia sinensis (L.) O.K UNTZE" Chemical & Pharmaceutical Bulletin. 46・12. 1901-1906 (1998)

    • Related Report
      1998 Annual Research Report
  • [Publications] Toshiyuki Murakami: "Advances in Plant Glycosides,Chemiatry and Biology" Elsevier, 556 (1999)

    • Related Report
      1998 Annual Research Report
  • [Publications] Toshiyuki Murakami: "Towards Natural Medicine Research in the 21st Century" Elsevier, 585 (1998)

    • Related Report
      1998 Annual Research Report
  • [Publications] Toshiyuki Murakami: "Potent Antidiabetic Principle with Unique Thiosugar Sulfonium Sulfate Structure from the Ayurvedic Traditional Medicine Salacia reticulata in Sri-Lanka and India." Tetrahedron Letter. 38・48. 8367-8370 (1997)

    • Related Report
      1997 Annual Research Report
  • [Publications] Toshiyuki Murakami: "Medicinal Foodstuffs.X.Structures of New Triterpene Glycosides,Gymnemosides-c,-d,-e,and-f,from the Leaves of Gymnema sylvestre R.BR.:Influence of Gymnema Glycosides on Glucose Uptake in Rat Small Intestivnal fragments" Chemical & Pharmaceutical Bulletin. 45・12. 2034-2038 (1997)

    • Related Report
      1997 Annual Research Report
  • [Publications] Toshiyuki Murakami: "Antiinflammatory Effects of Escins Ia,Ib,IIa,and IIb from Horse Chestnut,the Seeds of Aesculus hippocastanum L." Bioorganic & Medicinal Chemical Letter. 7・13. 1611-1616 (1997)

    • Related Report
      1997 Annual Research Report
  • [Publications] Toshiyuki Murakami: "Medicinal Foodstuffs.VII.On the Saponin Constituents with Glucose and Alcohol Absorption-Inhibitory Activity from a Food Garnish "Tonburi",the Fruit of Japanese Kochia scoparia(L.)SCHARD.:Structures of Scoparianosides A,B,and C." Chemical & Pharmaceutical Bulletin. 45・8. 1300-1305 (1997)

    • Related Report
      1997 Annual Research Report
  • [Publications] Toshiyuki Murakami: "Inhibitory Mechanisms of Oleanolic Acid 3-O-Monodesmosides on Glucose Absorption in Rats." Biological & Pharmaceutical Bulletin. 20・6. 717-719 (1997)

    • Related Report
      1997 Annual Research Report
  • [Publications] Toshiyuki Murakami: "Absolute Stereostructures of Betavulgarosides III and IV,Inhibitors of Glucose Absorption,from the Roots of Beta vulgaris L.(Sugar Beet)." Chemical & Pharmaceutical Bulletin. 45・3. 561-563 (1997)

    • Related Report
      1997 Annual Research Report

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Published: 1997-04-01   Modified: 2016-04-21  

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