Shibata H, Mio M, Tasaka K
Biochim Biophys Acta. 1985 Jul 30;846(1):1-7. doi: 10.1016/0167-4889(85)90102-8.
Substance P causes release of histamine from rat peritoneal mast cells; the structure-activity relationship shows that N-terminal residue is essential and the hydrophobic region of C-terminal plays an important role. Electrical conductivity of black lipid membrane containing phosphatidic acid was augmented by substance P. In this case, N-terminal residues and C-terminal hydrophobicity were also unavoidable. The partitioning of substance P into the organic phase increased in the presence of phosphatidic acid. The CD spectrum of substance P was changed from the unordered form to beta-form by coexistence of phosphatidic acid/PC liposomes in the medium. The addition of calcium or magnesium in the test solution is effective to prevent either of these phenomena. These findings indicate that substance P probably binds to negatively charged sites of membrane lipids, and subsequent penetration of C-terminal into the hydrophobic core of lipid bilayer may induce an increase of membrane permeability and the following histamine release.
P物质可引起大鼠腹膜肥大细胞释放组胺；构效关系表明N端残基至关重要，C端的疏水区域起重要作用。含磷脂酸的黑色脂质膜的电导率因P物质而增强。在这种情况下，N端残基和C端疏水性也是必不可少的。在磷脂酸存在下，P物质在有机相中的分配增加。通过介质中共存磷脂酸/磷脂酰胆碱脂质体，P物质的圆二色光谱从无序形式转变为β-形式。在测试溶液中添加钙或镁可有效防止这些现象中的任何一种。这些发现表明，P物质可能与膜脂的负电荷位点结合，随后C端渗透到脂质双层的疏水核心中可能会导致膜通透性增加以及随后的组胺释放。
