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 ED(50)</=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-B(4) biosynthesis by stimulated human polymorphonuclear leukocytes in vitro, and prostaglandin-E(2) 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.