[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)].

Abstract

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.

• Authors: W Martin, P Hartter
• Journal: Hoppe-Seyler's Zeitschrift fur physiologische Chemie (Hoppe Seylers Z Physiol Chem) Vol. 361 Issue 4 Pg. 525-35 (Apr 1980) ISSN: 0018-4888 [Print] Germany
• Vernacular Title: Basische Peptide des Bienengifts, VI. Struktur-Aktivitäts-Untersuchungen zur entzündungshemmenden Wirkung von Derivaten und Fragmenten des MCD-Peptids.
• PMID: 7380393 (Publication Type: Comparative Study, English Abstract, Journal Article)

Chemical References

• Anti-Inflammatory Agents
• Bee Venoms
• Disulfides
• Peptides
• Melitten
• Apamin
• Dexamethasone
• Carrageenan

Topics

• Amino Acid Sequence
• Animals
• Anti-Inflammatory Agents
• Apamin
• Bee Venoms (pharmacology)
• Carrageenan (pharmacology)
• Dexamethasone (pharmacology)
• Disulfides (analysis)
• Mast Cells (drug effects)
• Melitten
• Mice
• Peptides (pharmacology)
• Rats
• Structure-Activity Relationship