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    • 1. 发明授权
    • Low molecular weight components of shark cartilage, processes for their preparation and therapeutic uses thereof
    • 鲨鱼软骨的低分子量组分,其制备方法及其治疗用途
    • US06506414B2
    • 2003-01-14
    • US09751111
    • 2000-12-29
    • Eric DupontYves LachanceDenis LessardSerge Auger
    • Eric DupontYves LachanceDenis LessardSerge Auger
    • A61K3512
    • A61K35/60
    • This invention relates to a process by which organic solvent-containing solutions are used in lieu of pure water for the preparation of cartilage extracts and fractions thereof. Different organic solvents have been tested for the preparation of extracts containing biologically active components possessing at least an activity against a matrix metalloprotease (anti-MMP). This invention also relates to a process by which a total liquid extract of shark cartilage composed of molecules having molecular weights less than about 500kDa (0-500 fraction) is purified into two well separated fractions composed of molecules having molecular weights less than about 1 kDa (0-1 fraction) and between about 1 to 500 kDa (1-500 fraction). In order to prevent the formation of aggregates, to improve the dissolution and the stability of active components, sucrose or other stabilizing agents can be added. The 0-500 fraction, the 0-1 fraction and the 1-500 fraction as well as their equivalents containing 1% w/v sucrose possess have anti-MMP and anti-tumor activities. The invention also provides a component which has at least anti-MMP and anti-tumor activities, and which has a mass of 244 amu (atomic mass unit). The use of the above extracts, derived fractions or components for inhibiting MMP enzyme, neovascularization and/or metastase formation is also described.
    • 本发明涉及使用含有机溶剂的溶液代替纯水来制备软骨提取物及其级分的方法。 已经测试了不同的有机溶剂来制备含有至少对基质金属蛋白酶(抗-MMP)具有活性的生物活性组分的提取物。 本发明还涉及由具有小于约500kDa(0-500级分)的分子组成的鲨鱼软骨的总液体提取物被纯化成由分子量小于约1kDa的分子组成的两个良好分离的级分 (0-1分数)和约1至500kDa(1-500分数)之间。 为了防止聚集体的形成,为了改善活性组分的溶解和稳定性,可以加入蔗糖或其它稳定剂。 0-500级分,0-1级分和1-500级分以及其含有1%w / v蔗糖的当量具有抗MMP和抗肿瘤活性。 本发明还提供了具有至少抗MMP和抗肿瘤活性,并且质量为244amu(原子质量单位)的组分。 还描述了上述提取物,衍生级分或组分用于抑制MMP酶,新血管形成和/或转移形成的用途。
    • 2. 发明授权
    • Low molecular weight components of shark cartilage, processes for their preparation and therapeutic uses thereof
    • 鲨鱼软骨的低分子量组分,其制备方法及其治疗用途
    • US06168807A
    • 2001-01-02
    • US09122481
    • 1998-07-23
    • {acute over (E)}ric DupontYves LachanceDenis LessardSerge Auger
    • {acute over (E)}ric DupontYves LachanceDenis LessardSerge Auger
    • C01B3104
    • A61K35/60
    • This invention relates to a process by which organic solvent-containing solutions are used in lieu of pure water for the preparation of cartilage extracts and fractions thereof. Different organic solvents have been tested for the preparation of extracts containing biologically active components possessing at least an activity against a matrix metalloprotease (anti-MMP). This invention also relates to a process by which a total liquid extract of shark cartilage composed of molecules having molecular weights less than about 500 kDa (0-500 fraction) is purified into two well separated fractions composed of molecules having molecular weights less than about 1 kDa (0-1 fraction) and between about 1 to 500 kDa (1-500 fraction). In order to prevent the formation of aggregates, to improve the dissolution and the stability of active components, sucrose or other stabilizing agents can be added. The 0-500 fraction, the 0-1 fraction and the 1-500 fraction as well as their equivalents containing 1% w/v sucrose possess have anti-MMP and anti-tumor activities. The invention also provides a component which has at least anti-MMP and anti-tumor activities, and which has a mass of 244 amu (atomic mass unit). The use of the above extracts, derived fractions or components for inhibiting MMP enzyme, neovascularization and/or metastase formation is also described.
    • 本发明涉及使用含有机溶剂的溶液代替纯水来制备软骨提取物及其级分的方法。 已经测试了不同的有机溶剂来制备含有至少对基质金属蛋白酶(抗-MMP)具有活性的生物活性组分的提取物。 本发明还涉及一种由分子量小于约500kDa(0-500级分)组成的鲨鱼软骨的总液体提取物被纯化成由分子量小于约1的分子组成的两个井分离的级分 kDa(0-1分数)和约1至500kDa(1-500分数)之间。 为了防止聚集体的形成,为了改善活性组分的溶解和稳定性,可以加入蔗糖或其它稳定剂。 0-500级分,0-1级分和1-500级分以及其含有1%w / v蔗糖的当量具有抗MMP和抗肿瘤活性。 本发明还提供了具有至少抗MMP和抗肿瘤活性,并且质量为244amu(原子质量单位)的组分。 还描述了上述提取物,衍生级分或组分用于抑制MMP酶,新血管形成和/或转移形成的用途。