ANTI‐INFLAMMATORY PROPERTY OF 401 (MCD‐PEPTIDE), A PEPTIDE FROM THE VENOM OF THE BEE Apis mellifera (L.)

Abstract

1 Peptide 401, a potent mast cell degranulating factor from bee venom, substantially inhibited the oedema provoked by subplantar injection of carrageenin or intra-articular injection of turpentine in the rat. The ED₅₀ of 401 was c. 0.1 mg/kg. The anti-inflammatory effect was assessed by measurement of the increased ¹²⁵I-albumin content of an injected site in comparison with an uninjected contralateral site. 2 Peptide 401 also suppressed the increased vascular permeability due to intradermal injection of various smooth muscle spasmogens (histamine, bradykinin, 5-hydroxytryptamine (5-HT), and prostaglandins). 3 Other comparable mast cell degranulating agents (48/80 and melittin) showed little evidence of anti-inflammatory activity when tested at comparable dosage on turpentine arthritis and carrageenin oedema. 4 The anti-inflammatory effects were not abolished by pretreatment with mepyramine and methysergide, which abolished the increased vascular permeability produced by local injection of 401. 5 The anti-inflammatory action of 401 was not affected by regional denervation or pretreatment with phenoxybenzamine, and was reduced but not abolished by adrenalectomy. 6 Measurement of skin temperature, fractional extraction of ⁸⁶Rb and blood flow in perfused mesentery gave no evidence that the anti-inflammatory action of 401 was due to reduced tissue perfusion. 7 It is concluded that 401 may exert its anti-inflammatory action directly by making the vascular endothelium anergic to phlogistic stimuli.