Shefcyk J, Molski T F, Volpi M, Naccache P H, Sha'afi R I
Biochim Biophys Acta. 1983 Feb 9;728(1):97-102. doi: 10.1016/0005-2736(83)90441-8.
We have studied the effect of phloretin, a compound known to interfere with carrier mediated transport processes, on the functional responsiveness of rabbit neutrophils. Phloretin was found to inhibit neutrophil degranulation, aggregation and calcium uptake stimulated by the chemotactic peptide fMet-Leu-Phe. Part of these effects of phloretin may be accounted for by its interference with the binding of the synthetic peptide to its plasma membrane receptors. However, phloretin also inhibits the arachidonic acid and leukotriene B4 induced calcium uptake. These results imply that phloretin affects a component of membrane structure which is central to the activation sequences available to the neutrophils. The results of the present experiments demonstrate that phloretin can interfere with stimulus-response coupling in soluble mediator ('hormone') responsive cells.
我们研究了根皮素（一种已知会干扰载体介导转运过程的化合物）对兔中性粒细胞功能反应性的影响。发现根皮素可抑制趋化肽fMet-Leu-Phe刺激的中性粒细胞脱颗粒、聚集和钙摄取。根皮素的这些作用部分可能是由于其干扰了合成肽与质膜受体的结合。然而，根皮素也抑制花生四烯酸和白三烯B4诱导的钙摄取。这些结果表明，根皮素影响了膜结构的一个成分，该成分对于中性粒细胞可用的激活序列至关重要。本实验结果表明，根皮素可干扰可溶性介质（“激素”）反应性细胞中的刺激-反应偶联。
