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Anti-Inflammatory, Anti-Allergic, Respiratory & GI Agents

Patent Evaluation: Nonapeptide Phospholipase A2 Inhibitors

Pages 1608-1609 | Published online: 02 Mar 2011
 

Summary

Novelty: A nonapeptide sequence of human lipocortin V (residues 204-212) is claimed to have anti-inflammatory properties and be useful for dermatological and collagen inflammatory conditions.

Biology: Data are presented which indicate that the peptide can inhibit PGE2 release from rat leukocytes and human fibroblasts (94% inhibition at 100 μg/ml), inhibit PLA2-induced contractions in rat stomach strip (60% at 20 μg/ml), inhibit PLA2-induced oedema in rat paw in vivo and of carrageenin-induced oedema in rat paw (37% inhibition at 4 hours with 2 mg/kg).

Chemistry: The peptide is synthesized by solid phase methodology and has the structure given below.

Structure:

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