Basische Peptide des Bienengifts, VI. Struktur-Aktivitäts-Untersuchungen zur entzündungshemmenden Wirkung von Derivaten und Fragmenten des MCD-Peptids

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Abstract
Mastcell-degranulating [MCD] peptide from bee venom exhibits anti-inflammatory activity in the carrageenan-inflammation model on mice and rats. Its dose/response relationship corresponds to that of dexamethasone. In the 125I-rat serum albumin-test the substance shows an inhibitory effect of 87% on the developing Carrageenan edema at a dose of 1 mg/kg; in contrast the bee venom peptides apamin and melittin exhibit small edema suppressing effects. The anti-inflammatory characteristics of MCD-peptide are related to its high basicity and specific molecular structure, determined by 2 disulfide-bridges. Derivatives with acetylated amino groups or with alkylated cysteine residues show no significant activity. A pentapeptide in the C-terminal region of MCD-peptide (Lys-Ile-Cys-Gly-Lys)2 inhibits the carrageenan edema to 55% at a dose of 10 mg/kg.