Koo K I, Bae J H, Lee C H, Yoon C D, Pyun J H, Shin S H, Jeon Y C, Bae M K, Jang H O, Wood W G, Yun I
Department of Dental Pharmacology and Biophysics, Pusan National University, Busan, 602-739, South Korea.
Protoplasma. 2008 Dec;234(1-4):3-12. doi: 10.1007/s00709-008-0017-4. Epub 2008 Sep 17.
Fluorescent probe techniques were used to evaluate the effect of bupivacaine.HCl on the physical properties (transbilayer asymmetric lateral and rotational mobilities, annular lipid fluidity and protein distribution) of synaptosomal plasma membrane vesicles (SPMVs) isolated from bovine cerebral cortex. An experimental procedure was used based on selective quenching of both 1,3-di(1-pyrenyl)propane (Py-3-Py) and 1,6-diphenyl-1,3,5-hexatriene (DPH) by trinitrophenyl groups, and radiationless energy transfer (RET) from the tryptophans of membrane proteins to Py-3-Py. Bupivacaine.HCl increased the bulk lateral and rotational mobilities, and annular lipid fluidity in SPMVs lipid bilayers, and had a greater fluidizing effect on the inner monolayer than that of the outer monolayer. The magnitude of increasing effect on annular lipid fluidity in SPMVs lipid bilayer induced by bupivacaine.HCl was significantly far greater than magnitude of increasing effect of the drug on the lateral and rotational mobilities of bulk SPMVs lipid bilayer. It also caused membrane proteins to cluster. These effects of bupivacaine.HCl on neuronal membranes may be responsible for some, though not all, of the local anesthetic actions of bupivacaine.HCl.
采用荧光探针技术评估盐酸布比卡因对从牛大脑皮层分离的突触体细胞膜囊泡（SPMVs）物理性质（跨膜不对称横向和旋转流动性、环形脂质流动性和蛋白质分布）的影响。实验程序基于三硝基苯基对1,3 - 二（1 - 芘基）丙烷（Py - 3 - Py）和1,6 - 二苯基 - 1,3,5 - 己三烯（DPH）的选择性猝灭，以及膜蛋白色氨酸向Py - 3 - Py的无辐射能量转移（RET）。盐酸布比卡因增加了SPMVs脂质双层的整体横向和旋转流动性以及环形脂质流动性，并且对内膜层的流化作用大于外膜层。盐酸布比卡因诱导的SPMVs脂质双层环形脂质流动性增加的幅度明显远大于该药物对整体SPMVs脂质双层横向和旋转流动性增加的幅度。它还导致膜蛋白聚集。盐酸布比卡因对神经元膜的这些作用可能是盐酸布比卡因局部麻醉作用的部分（而非全部）原因。
