Tirzite D, Koronova J, Plotniece A
Latvian Institute of Organic Synthesis, Riga, Latvia.
Biochem Mol Biol Int. 1998 Jul;45(4):849-56. doi: 10.1080/15216549800203282.
1,4-Dihydropyridine derivatives possess various physiological activities but their mechanism of membranotropic action is not completely investigated yet. We have examined the membranotropic effects of 4-beta-pyridyl-1,4-Dihydropyridine derivatives containing different length alkyl chain substituent at N-quaternised 4-beta-pyridyl moiety. The results show the relation between incorporation of 1,4-dihydropyridine derivatives in the liposomal membranes and influence on bilayer fluidity. The compound with hexadecyl (C16H33) substituent in the 4-beta-pyridyl moiety possess the most pronounced incorporation ability and fluidizing effect. This compound causes the remarkable release of fluorescent probe calcein from liposomes and induces the hemolysis of human erythrocytes as well. The obtained results suggest that the length of alkyl chain at quaternized 4-beta-pyridyl moiety is significant for the expression of membranotropic effects of tested compounds.
1,4 - 二氢吡啶衍生物具有多种生理活性，但其膜作用机制尚未得到充分研究。我们研究了在N - 季铵化的4 - β - 吡啶基部分含有不同长度烷基链取代基的4 - β - 吡啶基 - 1,4 - 二氢吡啶衍生物的膜作用效果。结果表明了1,4 - 二氢吡啶衍生物掺入脂质体膜与对双层流动性影响之间的关系。在4 - β - 吡啶基部分带有十六烷基（C16H33）取代基的化合物具有最显著的掺入能力和流化作用。该化合物可使荧光探针钙黄绿素从脂质体中显著释放出来，并且还能诱导人红细胞溶血。所得结果表明，季铵化的4 - β - 吡啶基部分的烷基链长度对于测试化合物膜作用效果的表达具有重要意义。
