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Publication Number
US-9453082-B2
Publication Date
2016-09-27
Expiration Date
Abstract
There is provided a composition comprising a polysaccharide obtainable from the microalgae, Prasinococcus capsulatus and strains related to P. capsulatus for use prophylactically and/or therapeutically in the treatment of disorders of the immune system, for example in psoriasis and dermatological conditions, internal immune system disorders, in particular gut inflammatory conditions and respiratory conditions. Further, there is provided derivatives of a polysaccharide obtainable from the microalgae, Prasinococcus capsulatus or an algal strain related to P. capsulatus and the use of such derivatives prophylactically and/or therapeutically in the treatment of disorders of the immune system.
Core Innovation
The invention relates to an oligosaccharide derivative of a gel forming polysaccharide obtainable from microalgal cells from the order Prasinococcus capsulatus. The gel forming polysaccharide is a sulfated heteropolymer having a molecular weight of at least 670 kDa and comprising glucose, galactose, arabinose and uronic acid units. The derivative has a molecular weight in the range of about 2 kDa to 60 kDa.
The described polysaccharide is specified as a sulfated heteropolymer with targeted characteristics, including molecular weight, sulphate content, and monosaccharide composition ranges. Further disclosed derivatives include oligosaccharide and low- and high-molecular-weight fractions, including ranges of about 2–10 kDa and about 20–60 kDa. The document also characterizes gel-forming and viscosity-related properties as part of the polysaccharide framework.
The document also associates the described derivatives with immunomodulatory effects relevant to inflammatory immune disorders. Stated biological activities include inhibition of neutrophil elastase activity, reduction of neutrophil reactive oxygen species (ROS), and inhibition of cytokine/IL-8 gene expression and release in keratinocytes. Additional stated effects include inhibition of interferon gamma (IFN-γ) in PBMCs, and reduced neutrophil/monocyte chemotaxis and reduced IMQ-induced mouse skin inflammation.
Claims Coverage
The partial content identifies one independent claim (clm-00001) directed to oligosaccharide derivatives of a gel forming sulfated heteropolymer from microalgal cells of Prasinococcus capsulatus with a defined derivative molecular-weight range. The dependent claims in the partial content further refine composition constraints and state specific quantitative immunomodulatory inhibition outcomes, and narrow the immune system disorder types to skin and gut inflammatory conditions.
Oligosaccharide derivative from Prasinococcus capsulatus gel forming sulfated heteropolymer
An oligosaccharide derivative of a gel forming polysaccharide obtainable from microalgal cells of the order Prasinococcus capsulatus, wherein the gel forming polysaccharide is a sulfated heteropolymer of molecular weight of at least 670 kDa comprising glucose, galactose, arabinose and uronic acid units, and wherein said derivative has a molecular weight in the range of about 2 kDa to 60 kDa.
Defined derivative monosaccharide and uronic acid composition ranges
The derivative contains, by weight, about 30 to 40% glucose, 30 to 40% galactose, 8 to 14% arabinose, 7 to 11% uronic acid, and 1 to 10% of other sugar units.
Quantified inhibition of neutrophil elastase release
The derivative inhibits neutrophil elastase release by about 70 to 90%.
Quantified inhibition of keratinocyte IL-8 gene expression and release
The derivative inhibits human keratinocyte IL-8 gene expression and IL-8 release by about 70 to 100% relative to keratinocyte to which derivative has not been provided.
Inflammatory skin condition selection for immune system disorder
The immune system disorder is an inflammatory skin condition selected from the group consisting of eczema, psoriasis and atopic dermatitis.
Inflammatory gut condition selection for immune system disorder
The immune system disorder is an inflammatory condition of the gut selected from the group consisting of irritable bowel syndrome, Crohn’s disease and ulcerative colitis.
Across the partial claim set, coverage is centered on an oligosaccharide derivative (about 2–60 kDa) derived from a gel forming sulfated heteropolymer (at least 670 kDa; glucose, galactose, arabinose, uronic acid; from Prasinococcus capsulatus). Dependent refinements disclosed in the partial content include specific monosaccharide/uronic-acid composition ranges, and quantified inhibition of neutrophil elastase release and of keratinocyte IL-8 gene expression/release, with disorder scope narrowed to eczema/psoriasis/atopic dermatitis and to IBS/Crohn’s/ulcerative colitis.
Stated Advantages
Inhibits neutrophil elastase release.
Reduces neutrophil reactive oxygen species (ROS).
Inhibits keratinocyte IL-8 gene expression and IL-8 release.
Inhibits interferon gamma (IFN-γ) in PBMCs.
Reduces neutrophil and monocyte chemotaxis.
Reduces IMQ-induced mouse skin inflammation.
Documented Applications
Prophylactic/therapeutic use in inflammatory immune disorders, including inflammatory skin conditions such as psoriasis/eczema/atopic dermatitis.
Prophylactic/therapeutic use in gut inflammatory diseases, including irritable bowel syndrome, Crohn’s disease, and ulcerative colitis.
Prophylactic/therapeutic use in respiratory inflammatory conditions, including asthma and cystic fibrosis.
Cosmetic preparation.
Nutritional supplement.
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