首页> 外国专利> COMPOSITIONS OF STABLE BIOACTIVE METABOLITES OF DOCOSAHEXAENOIC (DHA) AND EICOSAPENTAENOIC (EPA) ACIDS

COMPOSITIONS OF STABLE BIOACTIVE METABOLITES OF DOCOSAHEXAENOIC (DHA) AND EICOSAPENTAENOIC (EPA) ACIDS

机译:二十二碳六烯酸(DHA)和二十碳五烯酸(EPA)酸的稳定生物活性代谢物的组成

摘要

An invention that adduces cogent evidence to establish that oxygenated dibenzo-alpha-pyrones (DBPs and their conjugates), the major bioactives of shilajit (Ayurvedic vitalizer), have their origin, at least partly, in EPA and DHA. Earlier research has shown that, in mammals, C-20 PUFAs are metabolized by oxygenases and other enzymes to produce short-lived prostaglandins, leukotrienes and thromboxanes that bind to specific G-protein-coupled receptors and signal cellular responses, e.g., inflammation, vasodilation, blood pressure, pain etc. But never before it was suggested/shown that CSUB20:5n-3 /SUB(and CSUB22:6 n-3/SUB) PUFAs, e.g., EPA (and DHA), are transformed into stable aromatic metabolites, DBPs, which elicit a large array of bioactivities in the producer organisms and also control the synthesis and metabolism of arachidonate-derived prostaglandins. The major beneficial effects attributed to EPA and DHA are now found to be largely contributed by DBPs and their aminoacyl conjugates and the dibenzo-alpha-pyrone-chromoproteins (DCPs). Because of the highly unstable nature of EPA and DHA, when administered, they are metabolized into a large array of uncontrolled products, several of which are systemically undesirable. By contrast, DBPs, because of their stability, perform the biological response modifier (BRM) functions in a directed and sustained way. Many of the biological effects of DBPs described in this invention, were earlier attributed to EPA and DHA,-the precursors of DBPs.
机译:这项发明提供了有力的证据来证明,氧化的二苯并-α-吡喃酮(DBPs和它们的结合物)是shilajit(阿育吠陀活力剂)的主要生物活性物质,至少部分起源于EPA和DHA。较早的研究表明,在哺乳动物中,C-20 PUFA被加氧酶和其他酶代谢,产生短寿命的前列腺素,白三烯和血栓烷,它们与特定的G蛋白偶联受体结合并发出细胞反应,例如炎症,血管舒张,血压,疼痛等。但是从未有人建议/证明过C 20:5n-3 (和C 22:6 n-3 )PUFA,例如, EPA(和DHA)被转化为稳定的芳香族代谢物DBP,在生产者生物体内引发了多种生物活性,还控制了花生四烯酸衍生的前列腺素的合成和代谢。现在发现归因于EPA和DHA的主要有益作用主要是由DBP及其氨酰基缀合物和二苯并α-吡喃酮色蛋白(DCP)引起的。由于EPA和DHA的高度不稳定特性,在给药时会被代谢成许多不受控制的产物,其中有些是系统上不希望的。相比之下,DBP由于其稳定性,可以有针对性地,持续地执行生物反应调节剂(BRM)功能。本发明中描述的DBP的许多生物学作用,较早地归因于EPA和DHA,即DBP的前体。

著录项

  • 公开/公告号EP1765324A4

    专利类型

  • 公开/公告日2009-07-01

    原文格式PDF

  • 申请/专利权人 NATREON INC.;

    申请/专利号EP20050758080

  • 发明设计人 GHOSAL SHIBNATH;

    申请日2005-06-08

  • 分类号A61K31/35;A61K31/366;A61K31/665;A61P1/04;A61P3/02;A61P7/06;A61P25/28;A61P39/06;

  • 国家 EP

  • 入库时间 2022-08-21 19:17:53

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