Compositions of stable bioactive metabolites of docosahexaenoic (DHA) and eicosapentaenoic (EPA) acids
申请人:Ghosal Shibnath
公开号:US20050282781A1
公开(公告)日:2005-12-22
An invention that adduces cogent evidence to establish that oxygenated dibenzo-α-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 C
20:5n-3
(and C
22:6 n-3
) 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-α-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.
一项发明提供了有力证据,证明含氧二苯并-α-吡喃酮(DBPs及其共轭物)是希拉吉(阿育吠陀活力剂)的主要生物活性成分,其起源至少部分源自EPA和DHA。早期研究表明,在哺乳动物中,C-20多不饱和脂肪酸通过氧化酶和其他酶代谢,产生短寿命的前列腺素、白三烯和血栓素,这些物质结合特定的G蛋白偶联受体并传递细胞反应,如炎症、血管舒张、血压、疼痛等。但以前从未提出/展示过C20:5n-3(和C22:6 n-3)多不饱和脂肪酸,如EPA(和DHA),会转化为稳定的芳香代谢物DBPs,这些物质在生产者生物体中引发大量生物活性,并且还控制花生四烯酸衍生的前列腺素的合成和代谢。现在,归因于EPA和DHA的主要益处效应在很大程度上是由DBPs及其氨酰共轭物和二苯并-α-吡喃酮-色蛋白(DCPs)贡献的。由于EPA和DHA的高度不稳定性,当其被施用时,它们会代谢成大量无法控制的产物,其中一些在全身上是不可取的。相比之下,由于其稳定性,DBPs以有针对性和持续的方式执行生物反应调节剂(BRM)功能。本发明描述的DBPs的许多生物效应,以前被归因于EPA和DHA,即DBPs的前体。