ORALLY BIOAVAILABLE STILBENOIDS- COMPOSITIONS AND THERAPEUTIC APPLICATIONS THEREOF
    8.
    发明申请
    ORALLY BIOAVAILABLE STILBENOIDS- COMPOSITIONS AND THERAPEUTIC APPLICATIONS THEREOF 审中-公开
    ORALLY BIOAVAILABLE STILBENOIDS-COMPOSITIONS AND THERAPEUTIC APPLICATIONS WITHEROF

    公开(公告)号:US20100204340A1

    公开(公告)日:2010-08-12

    申请号:US12499239

    申请日:2009-07-08

    IPC分类号: A61K31/09 C07C43/243 A61P3/04

    摘要: A novel, bioavailable and safe stilbenoid 3,5-dimethoxy-3,4′-dihydroxystilbene represented by STR#1 with an unexpected enhanced ability to prevent the accumulation of lipids accompanying the terminal differentiation of adipocytes, thereby inhibiting adipogenesis, and nutraceutical and cosmeceutical compositions comprising 3,5-dimethoxy-3,4′-dihydroxystilbene useful for anti-obesity and anti-cellulite therapy, are disclosed. Further the enhanced SIRT-1 activation ability of 3,5-dimethoxy-3,4′-dihydroxystilbene represented by STR#1 and 2,3′,5′,6-tetrahydroxy-trans-stilbene represented by STR#II are disclosed. The enhancement of SIRT-1 polypeptide activity of the said compounds is unexpectedly much higher than resveratrol or its natural analog pterostilbene. Sirtuin modulating compositions comprising an orally bioavailable SIRT-1 enhancing compounds (i) 3,5-dimethoxy-3,4′-dihydroxystilbene represented by STR#I and (ii) 2,3′,5′,6-tetrahydroxy-trans-stilbene represented by STR#II are also disclosed. An additional embodiment, also discloses the enhanced anti-Propionibacterium acnes activity of 3,5-dimethoxy-3,4′-dihydroxystilbenes represented by STR#I and compositions thereof.

    摘要翻译: 由STR#1代表的一种新颖,生物可利用和安全的扁桃体3,5-二甲氧基-3,4'-二羟基茋,具有意想不到的增强的防止伴随脂肪细胞末端分化的脂质积聚的能力,从而抑制脂肪形成,以及营养和药妆 公开了包含可用于抗肥胖和抗脂肪团治疗的3,5-二甲氧基-3,4'-二羟基茋的组合物。 另外,公开了由STR#1代表的3,5-二甲氧基-3,4'-二羟基茋的增强的SIRT-1活化能力和由STR#II表示的2,3',5',6-四羟基 - 反式 - 二苯乙烯。 所述化合物的SIRT-1多肽活性的增强出乎意料地高于白藜芦醇或其天然类似物p芪烯。 包含口服生物可利用的SIRT-1增强化合物(i)由STR#I表示的3,5-二甲氧基-3,4'-二羟基茋和(ⅱ)2,3',5',6-四羟基 - 也公开了由STR#II代表的二苯乙烯。 另外的实施方案还公开了由STR#I表示的3,5-二甲氧基-3,4'-二羟基茋的增强的抗丙酸杆菌痤疮活性及其组合物。

    Peptides modified with triterpenoids and small organic molecules: synthesis and use in cosmeceuticals
    9.
    发明授权
    Peptides modified with triterpenoids and small organic molecules: synthesis and use in cosmeceuticals 有权
    用三萜类化合物和小有机分子修饰的肽:合成和用于药妆品

    公开(公告)号:US08383594B2

    公开(公告)日:2013-02-26

    申请号:US11835165

    申请日:2007-08-07

    IPC分类号: A61K38/08 A61K8/64

    CPC分类号: A61Q19/08 A61K8/64 A61Q19/00

    摘要: The present invention relates to the Synthesis of Triterpenoid peptides and mechanism of action for Anti ageing and skin care. The present invention is directed towards anti-aging skin care compositions comprising peptides which are made by linking herbal actives to a pentapeptide for enhanced anti ageing activity by regenerating the dermal matrix. In detail, the present invention relates to the synthesis of Triterpenoid peptides, providing an enhanced and synergistic activity for reducing the consequences of ageing such as appearance of fine expression lines and wrinkles on the skin by cosmetic modes of application. The Triterpenoid peptides of the present invention with its novel dual action mode can be used for skin ageing & collagen insufficiency. Its Triterpenoid group acts by preventing oxidation and excess activity of serine proteases like elastase and collagenase that result in wrinkling of skin. With added peptides which boost the collagen and other matrix protein, Triterpenoid peptides provide a complete protection against pre mature ageing and functions as a best anti ageing ingredient.

    摘要翻译: 本发明涉及三萜类肽的合成及抗衰老和皮肤护理的作用机理。 本发明涉及抗衰老皮肤护理组合物,其包含通过将草药活性物质与五肽连接而制成的肽,以通过再生真皮基质来增强抗衰老活性。 详细地说,本发明涉及三萜类肽的合成,提供增强的和协同的活性,以减少老化的后果,例如通过美容方式在皮肤上表现出细小的表达线和皱纹。 具有其新颖双作用模式的本发明的三萜类肽可用于皮肤老化和胶原蛋白不足。 其三萜类化合物通过防止丝氨酸蛋白酶如弹性蛋白酶和胶原酶的氧化和过度活性而起作用,导致皮肤起皱。 通过添加增强胶原蛋白和其他基质蛋白质的肽,三萜类肽提供了完全保护,防止成熟老化,并作为最好的抗衰老成分。