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异型南五昧子(Kadsura heteroclita)中的具有血小板活化因子(PAF)拮抗活性的联苯环辛烯类木脂素

韩桂秋, 代平, 薛荣, Byron R.Arison, David C.Lankin, San Bao Hwang   

  1. 1. 北京医科大学药学院, 北京 100083;
    2. 兰州军医学校化学系, 兰州 730020
    3. Merck Sharp & Dohme Res.Lab.Rahway NJ07065; USA
    4. G.D.Searle & Co; Skokie; IL60077; USA
    5. Cytomed; Inc.; Cambridge; MA01701; USA
  • 收稿日期:1992-01-03 修回日期:1992-03-10 出版日期:1992-06-15 发布日期:1992-06-15

Dibenzocyclooctadiene Lignans with Platelet-Activating Factor (PAF) Antagonist Activity from Kadsura heteroclita

Gui-Qiu Han, Ping Dai Rong Xue, Byron H.Arison, David C.Lankin, San Bao Hwang   

  1. 1. School of Pharmaceutical Sciences; Beijing Medical University; Beijing 100083;
    2. Dept.of Chemistry; Lanzhou Military Medical School; Lanzhou 730020;
    3. Merck Sharp & Dohme Res.Lab; Rahway; NJ 07065; USA;
    4. G.D.Searle & Co; Skokie; IL 60077; USA;
    5.Cytomed Inc.; Cambridge; MA 01701; USA.
  • Received:1992-01-03 Revised:1992-03-10 Online:1992-06-15 Published:1992-06-15

摘要: 自异型南五味子(Kadsure heteroclita)首次分得7个已知的联苯环辛烯类木脂素, tigloylgomisin P(1), angeloylgomisin P(2), gomisin A(3), 五味子素(4), angeloylgomisin H(5), gomisin B(6), R(+)-gomisin M(7)tigloylgomisin P(1)的构型以二维核磁共振光谱技术确定。应用[3H]血小板活化因子(PAF)结合人血小板膜的分析方法测定, 证明化合物(1), (2)(7) PAF 受体拮抗活性。

关键词: 异型南五味子, 血小板活化因子受体拮抗剂 Tigloylgomisin P, angeloylgomisin P, R(+)-gomisin H, 联苯环辛烯类木脂素

Abstract: Seven known dibenzocyclooctadiene lignans, tigloylgomisin P(1), angeloylgomisin P(2), gomisin A(3), Schizandrin(4), angeloylgomisin H(5), gomisin B(6) and R(+)-gomisin M1(7) were isolated from Kadsura heteroclita.The conformation of tiglolylgomisin P(1)was established by 2D NMR techniques. Using [3H] platelet activating factor (PAF) binding to human platelet membrane assay, (1), (2) and (7) showed PAF receptor antagonistic activities.

Key words: Kadsura heteroclita, PAF receptor antagonist, Tigloylgomisin P, Angeloylgomisin P, R(+)-gomisin H, Dibenzocyclooctadiene lignans

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