Abstract
A lipid-rich extract, preparared by supercritical fluid extraction of fresh stabilized mussel powder (Lyprinol), showed significant anti-inflammatory (AI) activity given therapeutically and prophylactically po to Wistar and Dark Agouti rats developing either (a) adjuvant-induced polyarthritis or (b) collagen(II)-induced autoallergic arthritis, with ED50≤15 mg/kg; c.f. naproxen≥25 mg/kg or various therapeutic oils (flaxseed, evening primrose, fish)≥1800 mg/kg given orally. Lyprinol showed little or no activity in acute irritation assays (carrageenan, kaolin, histamine) indicating it is not mimicking rapid-acting NSAIDs.
Incorporating Lyprinol into arthritigenic adjuvants composed of heat-killed Mycobacterium. tuberculosis suspended in olive oil or squalane, effectively prevented arthritis development at a dose of 5 mg/rat. By contrast, ‘dummy adjuvants’ prepared with Mycobacterium tuberculosis and flaxseed, evening primrose or fish oils were still arthritigenic in Dark Agouti rats (doses of oil=90 mg/rat).
Lyprinol subfractions inhibited leukotriene-B4 biosynthesis by stimulated human polymorphonuclear leukocytes in vitro, and prostaglandin-E2 production by activated human macrophages in vitro. Much of this AI activity was associated with polyunsaturated fatty acids and natural antoxidants (carotenoids, etc.).
In contrast to NSAIDs, Lyprinol is non-gastrotoxic in disease-stressed rats at 300 mg/kg po and does not seem to affect platelet aggregation (human, rat). These data show Lyprinol to be a reproducible, relatively stable, source of bioactive lipids with much greater potency than plant/marine oils currently used as nutritional supplements to ameliorate signs of inflammation.
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Whitehouse, M.W., Macrides, T.A., Kalafatis, N. et al. Anti-inflammatory activity of a lipid fraction (lyprinol) from the NZ green-lipped mussel. Inflammopharmacol 5, 237–246 (1997). https://doi.org/10.1007/s10787-997-0002-0
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DOI: https://doi.org/10.1007/s10787-997-0002-0