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    Extensively oxidized derivatives of carotenoids, retinoids and related conjugated polyenes useful as non-toxic cell-differentiation inducers, anti-proliferative agents, and anti-tumor agents
    1.
    发明授权
    Extensively oxidized derivatives of carotenoids, retinoids and related conjugated polyenes useful as non-toxic cell-differentiation inducers, anti-proliferative agents, and anti-tumor agents 失效
    用作无毒细胞分化诱导剂的类胡萝卜素，类视黄醇和相关共轭多烯的广泛氧化衍生物，抗增殖剂和抗肿瘤剂

    公开(公告)号：US5475006A

    公开(公告)日：1995-12-12

    申请号：US288315

    申请日：1994-08-10

    申请人： Graham Burton ,  Janusz Daroszewski ,  Jenny Phipps

    发明人： Graham Burton ,  Janusz Daroszewski ,  Jenny Phipps

    IPC分类号： A61K31/745 ,  A61K31/035 ,  A61K31/07 ,  A61K31/12 ,  A61K31/20 ,  A61P3/02 ,  A61P35/00 ,  A61P43/00 ,  C07C403/00 ,  C07C403/14 ,  C07C403/16 ,  C07C403/24 ,  C07G13/00 ,  C07K5/078 ,  A01N43/00 ,  A61K31/47

    CPC分类号： C07K5/06139

    摘要： .beta.-Carotene and canthaxanthin, as representative carotenoids, and to a lesser extent, retinoic acid, a representative retinoid, undergo extensive oxidation to yield substances, insofar as oxidized .beta.-carotene is a model, which have properties useful as non-toxic agents active against cell proliferation, tumors, and tumorigenic viruses, and useful as promoters of cell differentiation. It is evident from chemical analysis of the highly oxidized .beta.-carotene product mixture that none of the various forms of vitamin A are present or are present only in minor amounts. Furthermore, the biological activities of oxidized canthaxanthin and retinoic acid, which cannot form, vitamin A, indicate the presence of active substances that are different from vitamin A. Although the anti-proliferative and differentiation promotion activities of oxidized .beta.-carotene resemble those of vitamin A itself, generally the effects are more powerful for oxidized .beta.-carotene in a wide variety of circumstances. Unlike vitamin A, the oxidized .beta.-carotene of the invention is non-toxic.

    摘要翻译： β-胡萝卜素和角黄素作为代表性的类胡萝卜素，而在较小程度上，视黄酸（一种有代表性的类视色素）经历广泛的氧化以产生物质，只要氧化的β-胡萝卜素是一种模型，其具有可用作无毒物质活性的性质 针对细胞增殖，肿瘤和致瘤性病毒，并且可用作细胞分化的启动子。 从高度氧化的β-胡萝卜素产物混合物的化学分析可以看出，不存在各种形式的维生素A或仅存在少量的维生素A. 此外，不能形成维生素A的氧化的角黄素和视黄酸的生物活性表明存在与维生素A不同的活性物质。虽然氧化的β-胡萝卜素的抗增殖和分化促进活性类似维生素A的维生素 本身一般来说，在多种情况下，氧化的β-胡萝卜素的作用通常更为强大。 与维生素A不同，本发明的氧化的β-胡萝卜素是无毒的。