Bandyopadhyay Punam, Bandyopadhyay Prasun, Regen Steven L
Department of Chemistry, Lehigh University, Bethlehem, Pennsylvania 18015, USA.
Bioconjug Chem. 2002 Nov-Dec;13(6):1314-8. doi: 10.1021/bc0255539.
A family of conjugates has been synthesized from spermine, putrescine, lysine, gamma-aminobutyric acid, sarcosine, cholic acid, glycocholic acid, 3alpha,7alpha-dihydroxycholic acid, and 3alpha,12alpha-dihydroxycholic acid, based on a design principle previously reported (Bandyopadhyay, P., Janout, V., Zhang, L., Regen, S. L. (2001) J. Am. Chem. Soc. 123, 7691). Each of these conjugates was found to exhibit significant activity in promoting the transport of Na(+) across liposomal membranes derived from 1,2-dimyristoleoyl-sn-glycero-3-phosphocholine, and also from 1,2-dipalmitoleoyl-sn-glycero-3-phosphocholine. In all cases, plots of pseudo first-order rate constants, k(obsd) vs (mol % of ion conductor)(2) were found to be linear, indicating that transport-active dimers are involved and that only a small fraction of the conjugates are in an aggregated form. An operational comparison that has been made within this series of conjugates indicates that Na(+) transport activity and membrane selectivity have a moderate dependency on the composition and the structure of the ion conductor.
基于先前报道的设计原则（Bandyopadhyay, P., Janout, V., Zhang, L., Regen, S. L. (2001) J. Am. Chem. Soc. 123, 7691），已从精胺、腐胺、赖氨酸、γ-氨基丁酸、肌氨酸、胆酸、甘氨胆酸、3α,7α-二羟基胆酸和3α,12α-二羟基胆酸合成了一系列共轭物。发现这些共轭物中的每一种在促进Na⁺跨源自1,2-二肉豆蔻酰-sn-甘油-3-磷酸胆碱以及1,2-二棕榈酰-sn-甘油-3-磷酸胆碱的脂质体膜运输方面均表现出显著活性。在所有情况下，伪一级速率常数k(obsd)对（离子导体的摩尔百分比）²的图均为线性，表明涉及运输活性二聚体，且只有一小部分共轭物呈聚集形式。在这一系列共轭物中进行的操作比较表明，Na⁺运输活性和膜选择性对离子导体的组成和结构有适度的依赖性。
