26-aminocholesterol and derivatives and analogs thereof in the
regulation of cholesterol accumulation in body tissue
    1.
    发明授权
    26-aminocholesterol and derivatives and analogs thereof in the regulation of cholesterol accumulation in body tissue 失效
    26-氨基胆固醇及其衍生物和类似物在体内组织中胆固醇积累的调节

    公开(公告)号:US4939134A

    公开(公告)日:1990-07-03

    申请号:US246444

    申请日:1988-09-19

    IPC分类号: A61K31/575 C07J9/00

    CPC分类号: A61K31/575

    摘要: This invention relates to cholesterol synthesis and to the accumulation and regulation of cholesterol levels in body tissue. More specifically, the invention provides that the compound 26-aminocholesterol, ##STR1## and analogs and derivatives thereof, exhibit biological activity as a potent inhibitor of cholesterol synthesis and/or cholesterol accumulation in body tissue. The compounds strongly inhibit of the enzyme HMGCoA reductase and low density lipoprotein accumulation by non-hepatic cells. Surprisingly, it has been discovered that 26-aminocholesterol is selective for fibroblast (plasma) cells, and has little or no effect on hepato (liver) cells. Therapeutic compounds according to the invention include substituted or unsubstituted sterols of the formula: ##STR2## wherein the carbon atoms at positions 5 and 6 of the sterol are one of saturated and unsaturated, R.sub.1 is one of a 3-hydroxyl group and a 3-keto group, R.sub.2 is one of a hydroxyl group and a keto group, and wherein at least one of R.sub.3, R.sub.4 and R.sub.5 is an amino group and the others are each selected from the group consisting of hydrogen and an amino group.

    摘要翻译: 本发明涉及胆固醇合成和身体组织中胆固醇水平的积累和调节。 更具体地说,本发明提供化合物26-氨基胆固醇及其类似物及其衍生物作为胆固醇合成和/或体内组织中胆固醇积聚的有效抑制剂具有生物活性。 该化合物强烈地抑制HMGCoA还原酶和非肝细胞的低密度脂蛋白积累。 令人吃惊的是,已经发现26-氨基胆固醇对成纤维细胞(血浆)细胞是选择性的,并且对肝细胞(肝)细胞几乎没有或没有影响。 根据本发明的治疗化合物包括具有下式的取代或未取代的甾醇:其中固醇的5和6位的碳原子是饱和和不饱和的之一,R 1是3-羟基和3- 酮基,R2是羟基和酮基之一,其中R3,R4和R5中的至少一个是氨基,其它各自选自氢和氨基。

    Methods for genetic plant transformation using water-soluble fullerene derivatives
    2.
    发明授权
    Methods for genetic plant transformation using water-soluble fullerene derivatives 有权
    使用水溶性富勒烯衍生物进行遗传植物转化的方法

    公开(公告)号:US08614366B2

    公开(公告)日:2013-12-24

    申请号:US12876671

    申请日:2010-09-07

    申请人: Stephen R. Wilson

    发明人: Stephen R. Wilson

    IPC分类号: C07K14/415 B82Y30/00

    CPC分类号: C12N15/8201

    摘要: In various embodiments, methods described herein comprise the use of water-soluble cationic fullerene derivatives for improving plant genetic transformation. Cationic Fullerene derivatives of the invention possess DNA binding and compaction activity and provide a new method to deliver DNA into plant cells for plant transformation. Water-soluble fullerene derivatives of the invention with anionic or non-polar substituents possess antioxidant (free radical scavenging) activity, provide improved yields and efficiency of plant transformation methods such as biolistic, Agrobacterium tumefaciens, or electroporation methods by limiting cellular damage and resulting cell death leading to higher yields of viable transformed cells in the process.

    摘要翻译: 在各种实施方案中,本文所述的方法包括使用水溶性阳离子富勒烯衍生物来改善植物遗传转化。 本发明的阳离子富勒烯衍生物具有DNA结合和压实活性,并提供了将DNA输送到植物转化植物细胞中的新方法。 具有阴离子或非极性取代基的本发明的水溶性富勒烯衍生物具有抗氧化(自由基清除)活性,通过限制细胞损伤和产生的细胞提供植物转化方法如生物射弹,根癌土壤杆菌或电穿孔方法的提高的产量和效率 死亡导致该过程中可行的转化细胞的产量更高。

    Use of Carbon Nanotube for Drug Delivery
    5.
    发明申请
    Use of Carbon Nanotube for Drug Delivery 审中-公开
    碳纳米管用于药物输送

    公开(公告)号:US20080193490A1

    公开(公告)日:2008-08-14

    申请号:US11841087

    申请日:2007-08-20

    IPC分类号: A61K47/04 A61K9/00

    摘要: Compositions and methods for administering a therapeutic agent to a mammal are disclosed. The compositions comprise either (i) vesicles comprising an amphiphilic substituted fullerene, wherein the therapeutic agent is present in the vesicle interior or between layers of the vesicle wall, (ii) a substituted fullerene, comprising a fullerene core and a functional moiety, wherein the therapeutic agent is associated with the substituted fullerene, or (iii) carbon nanotubes, wherein the therapeutic agent is associated with the carbon nanotubes.

    摘要翻译: 公开了向哺乳动物施用治疗剂的组合物和方法。 所述组合物包含(i)包含两亲性取代的富勒烯的囊泡,其中所述治疗剂存在于泡囊内部或囊泡壁的层之间,(ii)包含富勒烯核心和功能部分的取代的富勒烯,其中 治疗剂与取代的富勒烯相关,或(iii)碳纳米管,其中治疗剂与碳纳米管相关联。