Studies on the interaction of anesthetic steroids with phosphatidylcholine using 2H and 13C solid state NMR.
Studies on the interaction of anesthetic steroids with phosphatidylcholine using 2H and 13C solid state NMR.
复制标题
使用 2H 和 13C 固态 NMR 研究麻醉类固醇与磷脂酰胆碱的相互作用。
DOI：
10.1016/0005-2736(86)90316-0
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发表时间：
1986
期刊：
影响因子：
--
通讯作者：
Griffin,RG
中科院分区：
文献类型：
--
作者：
Makriyannis,A;Siminovitch,DJ;DasGupta,SK;Griffin,RG
使用 13 C和 2 H固态核磁共振波谱研究了麻醉类固醇αxalone及其无活性类似物Δ16-αxalone对模型磷脂膜的影响。使用具有特异性 13 C 和 2 H 标记的二棕榈酰磷脂酰胆碱 (DPPC) 的水性多层分散体分别作为 sn-2 链的羰基和 C-7 亚甲基的内源探针来研究双层的构象和动力学特性随温度的变化。含有无活性类固醇的DPPC制剂和不含药物的DPPC的13C和2H光谱之间没有显着变化。然而，生理活性类固醇产生显着的光谱 2 H 和 13 C 变化。这些变化包括主相变温度的降低和相变范围的扩大。 Alphaxalone 还增加了 DPPC 液晶相中稀疏构象异构体的相对数量，并增加了凝胶相和液晶相中的轴向扩散速率。通过差示扫描量热法监测，上述制剂的热致性质与光谱数据一致。
The effects of the anesthetic steroid alphaxalone and its inactive analog Δ16-alphaxalone on model phospholipid membranes were studied using13C and2H solid-state nuclear magnetic resonance spectroscopy. Aqueous multilamellar dispersions of dipalmitoylphosphatidylcholine (DPPC) with specific13C and2H labels as endogenous probes at the carbonyl and the C-7 methylene groups, respectively, of thesn-2 chain were used to study the conformational and dynamical properties of the bilayer as a function of temperature. There were no significant changes between the13C and2H spectra of the DPPC preparation containing the inactive steroid and that of DPPC with no drug. However, the physiologically active steroid produces significant spectral2H and13C changes. These changes include a reduction of the main phase transition temperature and a broadening of that transition. Alphaxalone also increases the relative number ofgaucheconformers in the liquid-crystalline phase of DPPC and increases the rate of axial diffusion in both the gel and liquid-crystalline phase. The thermotropic properties of the above preparations, as monitored by differential scanning calorimetry, were congruent with the spectroscopic data.