Delort A M, Jeminet G, Sareth S, Riddle F G
Laboratoire de Synthèse, Université Blaise Pascal-CNRS, Aubiere, France.
Chem Pharm Bull (Tokyo). 1998 Oct;46(10):1618-20. doi: 10.1248/cpb.46.1618.
Cationomycin, isolated from Actinomadura azurea belongs to a large family of carboxylic polyether antibiotics, transporting monovalent cations through membranes by a mobile carrier mechanism, leading globally to an H+, M+ exchange. In this report the cation transporting properties of cationomycin were characterized in large unilamellar vesicles (LUVs) by 23Na- and 39K-NMR. Kinetic studies showed that cationomycin transported potassium more rapidly than sodium, and the more stable complex was formed with potassium at the water/membrane interface. The transport rate constants measured for cationomycin were compared with those obtained for monensin. Cationomycin transports Na+ more slowly than monensin and has a lower stability complex with Na+ because of the lower formation rate for the complex on the membrane surface. Our results show that transport selectivity of cationomycin is in favour of K+ versus Na+ while the reverse situation is observed for monensin. The relationships between the ionophore properties of cationomycin and monensin with their biological activities are discussed.
从天蓝马杜拉放线菌中分离出的阳离子霉素属于一大类羧酸聚醚抗生素,它通过移动载体机制使单价阳离子透过膜,总体上导致H⁺、M⁺交换。在本报告中,通过²³Na-和³⁹K-NMR对大单层囊泡(LUVs)中阳离子霉素的阳离子转运特性进行了表征。动力学研究表明,阳离子霉素转运钾的速度比钠快,并且在水/膜界面与钾形成的复合物更稳定。将阳离子霉素测得的转运速率常数与莫能菌素的进行了比较。阳离子霉素转运Na⁺的速度比莫能菌素慢,并且由于在膜表面复合物的形成速率较低,其与Na⁺的复合物稳定性也较低。我们的结果表明,阳离子霉素的转运选择性有利于K⁺而非Na⁺,而莫能菌素则相反。文中讨论了阳离子霉素和莫能菌素的离子载体特性与其生物活性之间的关系。