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    Cytotoxic alkaloid derivatives including Asmarine A and B isolated from a sponge
    3.
    发明授权
    Cytotoxic alkaloid derivatives including Asmarine A and B isolated from a sponge 失效
    细胞毒性生物碱衍生物，包括从海绵中分离的Asmarine A和B

    公开(公告)号：US06420357B1

    公开(公告)日：2002-07-16

    申请号：US09582181

    申请日：2001-06-22

    申请人： Yoel Kashman ,  Amira Rudi ,  Tesfamariam Yosief ,  Dolores G. Gravalos

    发明人： Yoel Kashman ,  Amira Rudi ,  Tesfamariam Yosief ,  Dolores G. Gravalos

    IPC分类号： C07D48706

    CPC分类号： C07D487/16

    摘要： Disclosed are the compounds Asamarine A and B, novel cytotoxic diterpene-alkaloids, that have been isolated from the sponge Raspailia sp. The structure of these compounds have been established on the basis of NMR data and confirmed by X-ray analysis. Also disclosed are compounds (I) and (II), wherein wherein R1 represents hydrogen or lower alkyl or lower alkanoyl; R2 represents hydrogen or lower alkyl; R3 is either an alkyl or a cycloalkyl group containing one or more isoprene units, or a monoterpene or a sesquiterpene or a sesquiterpene or a diterpene group; R4 or R5 represent hydrogen or lower alkyl; R6 represents lower alkyl; and X represents F or Cl or Br or I.

    摘要翻译： 披露了从海绵Raspailia sp。中分离的化合物Asamarine A和B，新的细胞毒二萜生物碱。 这些化合物的结构已经建立在NMR数据的基础上，并通过X射线分析证实。 还公开了化合物（I）和（II），其中R 1表示氢或低级烷基或低级烷酰基; R2代表氢或低级烷基; R3是含有一个或多个异戊二烯单元的烷基或环烷基，或单萜或倍半萜烯或倍半萜烯或双萜基; R4或R5代表氢或低级烷基; R6代表低级烷基; X表示F或Cl或Br或I.

    Biological applications of alkaloids derived from the tunicate Eudistoma sp.
    4.
    发明授权
    Biological applications of alkaloids derived from the tunicate Eudistoma sp. 失效
    生物应用生物碱衍生自细枝柄菌（Eudistoma sp。）

    公开(公告)号：US5432172A

    公开(公告)日：1995-07-11

    申请号：US28322

    申请日：1993-03-09

    申请人： Ilan Spector ,  Nava R. Shochet ,  Yoel Kashman ,  Amira Rudi ,  Gary Gellerman

    发明人： Ilan Spector ,  Nava R. Shochet ,  Yoel Kashman ,  Amira Rudi ,  Gary Gellerman

    IPC分类号： A61K31/44 ,  C07D215/38 ,  C07D215/48 ,  C07D219/08 ,  C07D471/04 ,  C07D471/06 ,  C07D471/16 ,  C07D471/22 ,  A61K31/54

    CPC分类号： C07D471/04 ,  A61K31/44 ,  C07D215/38 ,  C07D215/48 ,  C07D219/08 ,  C07D471/06

    摘要： Biological applications of synthetic and natural alkaloids derived from the tunicate Eudistoma sp. are disclosed. A method regulating cell growth includes contacting one or more cells with an effective concentration of a compound for regulating cell growth. These compounds include: Segoline A, Segoline B, Isosegoline A, Norosegoline, Debromoshermilamine, Eilatin, 4-methylpyrido[2,3,4-kl]acridine, pyrido[2,3,4-kl]acridine, 1-acetyl-2,6-dimethylpyrido[2,3,4-kl]acridine, and derivatives and combinations of these compounds. An effective concentration range for using these compounds can range from approximately 0.1 .mu.M to 100 .mu.M. The effective concentration range for Eilatin, the most potent of these compounds is from 0.01 .mu.M to 0.99 .mu.M, and the effective concentration range for the other compounds of the present invention is from about 1.0 .mu.M to 100 .mu.M. The method has been shown to suppress growth of tumor cells, to induce differentiation of the tumor cells, and induce reverse transformation of the tumor cells. In transformed cells, the method induces reverse transformation. The method also inhibits the proliferation of cells. The examples show that the method of the present invention affects cyclic AMP mediated biological processes. At the effective concentrations this method affects the cyclic AMP mediated biological processes of cells to achieve the results described above.

    摘要翻译： 合成和天然生物碱的生物应用来源于调味汁。 被披露。 调节细胞生长的方法包括使一种或多种细胞与有效浓度的化合物接触以调节细胞生长。 这些化合物包括：Segoline A，Segoline B，Isosegoline A，Norosegoline，脱氯西米明，Eilatin，4-甲基吡啶并[2,3,4-kl]吖啶，吡啶并[2,3,4-kl]吖啶，1-乙酰基-2 ，6-二甲基吡啶并[2,3,4-k]]吖啶，以及这些化合物的衍生物和组合。 使用这些化合物的有效浓度范围可以为约0.1μM至100μM。这些化合物中最有效的Eilatin的有效浓度范围为0.01μM至0.99μM，并且对于 本发明的其它化合物为约1.0μM至100μM。已经显示该方法抑制肿瘤细胞的生长，诱导肿瘤细胞的分化，并诱导肿瘤细胞的逆转化。 在转化细胞中，该方法诱导逆转化。 该方法还抑制细胞增殖。 实施例表明本发明的方法影响环AMP介导的生物过程。 在有效浓度下，该方法影响环AMP介导的细胞生物过程，以达到上述结果。

    Biological applications of alkaloids derived from the tunicate Eudistoma sp.
    7.
    发明授权
    Biological applications of alkaloids derived from the tunicate Eudistoma sp. 失效
    生物应用生物碱衍生自细枝柄菌（Eudistoma sp。）

    公开(公告)号：US5278168A

    公开(公告)日：1994-01-11

    申请号：US924194

    申请日：1992-08-03

    申请人： Ilan Spector ,  Nava R. Shochet ,  Yoel Kashman ,  Amira Rudi

    发明人： Ilan Spector ,  Nava R. Shochet ,  Yoel Kashman ,  Amira Rudi

    IPC分类号： A61K31/44 ,  C07D215/38 ,  C07D215/48 ,  C07D219/08 ,  C07D471/04 ,  C07D471/06 ,  C07D471/16 ,  C07D471/22 ,  A61K31/04 ,  C07D221/18

    CPC分类号： A61K31/44 ,  C07D215/38 ,  C07D215/48 ,  C07D219/08 ,  C07D471/04 ,  C07D471/06

    摘要： Biological applications of synthetic and natural alkaloids derived from the tunicate Eudistoma sp. are disclosed. A method regulating cell growth includes contacting one or more cells with an effective concentration of a compound for regulating cell growth. These compounds include: Segoline A, Segoline B, Isosegoline A, Norosegoline, Debromoshermilamine, Eilatin, 4-methylpyrido[2,3,4-kl] acridine, pyrido[2,3,4-kl]acridine, 1-acetyl-2,6-dimethylpyrido[2,3,4-kl]acridine, and derivatives and combinations of these compounds. An effective concentration range for using these compounds can range from approximately 0.1 .mu.M to 100 .mu.M. The effective concentration range for Eilatin, the most potent of these compounds is from 0.01 .mu.M to 0.99 .mu.M, and the effective concentration range for the other compounds of the present invention is from about 1.0 .mu.M to 100 .mu.M. The method has been shown to suppress growth of tumor cells, to induce differentiation of the tumor cells, and induce reverse transformation of the tumor cells. In transformed cells, the method induces reverse transformation. The method also inhibits the proliferation of cells. The examples show that the method of the present invention affects cyclic AMP mediated biological processes. At the effective concentrations this method affects the cyclic AMP mediated biological processes of cells to achieve the results described above.

    摘要翻译： 合成和天然生物碱的生物应用来源于调味汁。 被披露。 调节细胞生长的方法包括使一种或多种细胞与有效浓度的化合物接触以调节细胞生长。 这些化合物包括：Segoline A，Segoline B，Isosegoline A，Norosegoline，脱氯西米明，Eilatin，4-甲基吡啶（2,3,4-kl）吖啶，吡啶并（2,3,4-kl）吖啶，1-乙酰基-2 ，6-二甲基吡啶（2,3,4-kl）吖啶，以及这些化合物的衍生物和组合。 使用这些化合物的有效浓度范围可以从大约0.1（我）M到100（my）M。 这些化合物中最有效的Eilatin的有效浓度范围为0.01（my）M至0.99（my）M，本发明其它化合物的有效浓度范围为约1.0（my）M至100 （我的）M。 已经显示该方法抑制肿瘤细胞的生长，诱导肿瘤细胞的分化，并诱导肿瘤细胞的逆转化。 在转化细胞中，该方法诱导逆转化。 该方法还抑制细胞增殖。 实施例表明本发明的方法影响环AMP介导的生物过程。 在有效浓度下，该方法影响环AMP介导的细胞生物过程，以达到上述结果。