Feigin A M, Aronov E V, Bryant B P, Teeter J H, Brand J G
Monell Chemical Senses Center, Philadelphia, PA 19104-3308, USA.
Neuroreport. 1995 Nov 13;6(16):2134-6. doi: 10.1097/00001756-199511000-00009.
The irritating, pungent compound, capsaicin (10-20 microM), induces the formation of non-selective ion channels with a wide variety of conductances in protein-free lipid bilayers form from a mixture of zwitterionic phospholipids. The channel-forming activity of capsaicin and four of its analogs followed the sequence: resiniferatoxin > capsaicin = pelargonic acid vanillylamide > methylcapsaicin >> veratrylamine. The ability to form channels correlated with the biological activity of these compounds observed in other studies that measured 45Ca uptake into rat dorsal root ganglion cells. The correlation obtained suggests that an interaction with the lipid bilayer may be an important component of the biological activity of capsaicin.
刺激性辛辣化合物辣椒素(10 - 20微摩尔)可在由两性离子磷脂混合物形成的无蛋白脂质双分子层中诱导形成具有多种电导的非选择性离子通道。辣椒素及其四种类似物的通道形成活性顺序如下:树脂毒素>辣椒素 = 壬酸香草酰胺>甲基辣椒素>>藜芦胺。形成通道的能力与在其他测量45Ca摄取到大鼠背根神经节细胞中的研究中观察到的这些化合物的生物活性相关。所获得的相关性表明,与脂质双分子层的相互作用可能是辣椒素生物活性的重要组成部分。