Mastoparan N-terminal and C-terminal tetrapeptides inhibit mastoparan-stimulated histamine release from rat peritoneal mast cells.

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  • マストパランのN末端およびC末端4残基フラグメントはマストパランによる肥満細胞からのヒスタミン放出を阻害する

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Mastoparan(MP), a tetradecapeptide from wasp venom, acts as a secretagogue and stimulates histamine(Him)release from rat peritoneal mast cells and catecholamine(CA)release from adrenal chromaffin cells. The N-terminal tetrapeptide(INLK-NH_2 ; N-4)and C-terminal tetrapeptide(KKIL-NH_2 ; C-4)of MP inhibited acetylcholine-stimulated CA release from adrenal chromaffin cells. We synthesized five MP fragments including N-4 and C-4, and measured the activity of MP fragments themselves to induce Him release from mast cells. In addition, we investigated whether MP fragments inhibited MP-stimulated Him release from mast cells. It was shown that MP fragments except C-terminal heptapeptide(ALAKKIL-NH_2 ; C-7)of MP had no Him releasing activity. The activity of 30μM MP was inhibited to about 70% by the addition of 3 mM N-4 or C-4. The peptides may possibly block the MP interaction site(s)on mast cells. We are now synthesizing more active peptides by amino acid replacements, which are expected to be potent medicines for Him-related diseases.

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