Ma X J, Kunimatsu M, Ozaki Y, Fujimoto S, Sasaki M
Department of Biochemistry, Nagoya City University Medical School, Japan.
Life Sci. 1995;57(5):463-71. doi: 10.1016/0024-3205(95)00280-j.
N-formyl and N-acetyl peptides with the N-terminal sequence of the calpain small subunit were prepared and their spasmogenic activity was examined using guinea pig ileum preparations. Sections of ileum were found to contract in the presence of all N-formyl peptides used (tri- to nonapeptides and tridecapeptide) but failed to contract with N-acetyl peptides, although both N-formyl and N-acetyl peptides have chemotactic activity, indicating that spasmogenic activity and chemotactic activity involve different mechanisms. A formyl peptide antagonist, Boc-Phe-Leu-Phe-Leu-Phe, suppressed contraction by formyl peptides whereas a histamine antagonist, diphenhydramine, suppressed contraction by formyl peptides as well as by histamine. In addition, formyl peptide-induced contractions were noted after an approximately 20-sec time lag, and their profiles were bell-shaped and roughly symmetrical. On the other hand, histamine- and acetylcholine-induced contractions exhibited a much shorter time lag. These data led us to conclude that contraction induced by formyl peptides may not occur as a direct response but may be due to the histamine released from mast cells present in the tissues of the small intestine.
制备了具有钙蛋白酶小亚基N端序列的N-甲酰基和N-乙酰基肽,并使用豚鼠回肠制剂检测了它们的致痉活性。发现所有使用的N-甲酰基肽(三肽至九肽和十三肽)均能使回肠段收缩,但N-乙酰基肽则不能使其收缩,尽管N-甲酰基和N-乙酰基肽均具有趋化活性,这表明致痉活性和趋化活性涉及不同的机制。一种甲酰基肽拮抗剂Boc-Phe-Leu-Phe-Leu-Phe可抑制甲酰基肽引起的收缩,而一种组胺拮抗剂苯海拉明则可抑制甲酰基肽以及组胺引起的收缩。此外,甲酰基肽诱导的收缩在约20秒的时间滞后出现,其曲线呈钟形且大致对称。另一方面,组胺和乙酰胆碱诱导的收缩的时间滞后要短得多。这些数据使我们得出结论,甲酰基肽诱导的收缩可能不是直接反应,而是可能由于小肠组织中肥大细胞释放的组胺所致。