[Basic peptides in bee venom, VI. Structure-activity studies on the anti-inflammatory effects of derivatives and fragments of the MCD-peptide (author's transl)].
Mastcell-degranulating peptide from bee venom exhibits anti-inflammatory activity in the Carrageenine-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 Carrageenine edema at a dose of 1 mg/kg; in contrast the bee venom peptides apamin and melittin exhibit small edema supressing effects. The anti-inflammatory characteristics of MCD-peptide have to be considered with regard to its high basicity and specific molecular structure, determined by two disulfide-bridges for the derivaties with acetylated amino groups respectively 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 carrageenin edema to 55% at a dose of 10 mg/kg.
D000595:Amino Acid Sequence; D000818:Animals; D000893:Anti-Inflammatory Agents; D001030:Apamin; D001514:Bee Venoms / Q000494:pharmacology*; D002351:Carrageenan / Q000494:pharmacology; D003907:Dexamethasone / Q000494:pharmacology; D004220:Disulfides / Q000032:analysis; D008407:Mast Cells / Q000187:drug effects*; D008555:Melitten; D051379:Mice; D010455:Peptides / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
D000893:Anti-Inflammatory Agents; D001514:Bee Venoms; D004220:Disulfides; D010455:Peptides; D008555:Melitten; D001030:Apamin; D003907:Dexamethasone; D002351:Carrageenan
Basische Peptide des Bienengifts, VI. Struktur-Aktivitäts-Untersuchungen zur entzündungshemmenden Wirkung von Derivaten und Fragmenten des MCD-Peptids.