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Structure–Property Relationships in Sodium Muricholate Derivative (Bile Salts) Micellization: The Effect of Conformation of Steroid Skeleton on Hydrophobicity and Micelle Formation–Pattern Recognition and Potential Membranoprotective Properties
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2017-09-13 00:00:00 , DOI: 10.1021/acs.molpharmaceut.7b00375 Mihalj Poša 1 , Kosta Popović 1
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2017-09-13 00:00:00 , DOI: 10.1021/acs.molpharmaceut.7b00375 Mihalj Poša 1 , Kosta Popović 1
Affiliation
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It is known that β-muricholic acid anions prevent membrane toxicity of hydrophobic bile acids, which are being used in therapy for solubilization of the cholesterol type bile stone. Better knowledge of these derivative micelles is very important for understanding their physiological and pharmacological effects. β-Axial (a) oriented hydroxyl group from the steroid skeleton decreases the hydrophobic surface of the convex side of the steroid skeleton. Therefore, the critical micellization concentration (CMC) for steroid surfactants with β-a–OH group should increase, but in the case of OH groups of different orientations forming H-bonds in the hydrophobic phase of the micelle, it has the opposite effect; the CMC decreses, and aggregation is more favored. The set of muricholic acids (MCs) is composed by α-MC, β-MC, γ-MC, and ω-MC, where α-MC and β-MC have β-axial–OH groups. The aggregation numbers (n) are determined using the Moroi–Matsuoka–Sugioka thermodynamic method. CMC, enthalpy of demicellization, and ΔCp are determined by isothermal titration calorimetry (ITC). This report pioneers in the study of MC derivatives micellization. Micelles of β-MC and γ-MC belong to the linear congeneric group (LCG) and their micelles above 85 mM have constant aggregation numbers n = 4–5. Micelles of α-MC and ω-MC are outliers in relation to the LCG, their aggregation number constantly increases; at 85 mM n = 6.8 (α-MC) and 6.5 (ω-MC). In micelles of derivatives β-MC and γ-MC, there is a low probability for the existence of hydrogen bonds. A micelle of α-MC probably has hydrogen bonds in its hydrophobic domain.
中文翻译：
巯基酸钠衍生物（胆汁盐）胶束的结构-性能关系：类固醇骨架的构型对疏水性和胶束形成的影响-模式识别和潜在的膜保护特性
众所周知，β-巯基乙酸根阴离子可防止疏水性胆汁酸的膜毒性，疏水性胆汁酸已被用于治疗胆固醇型胆汁结石的增溶。更好地了解这些衍生胶束对于了解其生理和药理作用非常重要。来自类固醇骨架的β-轴（a）定向羟基减少了类固醇骨架凸面的疏水表面。因此，具有β-α-OH基的甾族表面活性剂的临界胶束化浓度（CMC）应增加，但是在不同方向的OH基团在胶束的疏水相中形成H键的情况下，其相反作用；在CMC递减，聚集更受青睐。一组多元酚酸（MCs）由α-MC，β-MC，γ-MC和ω-MC组成，其中α-MC和β-MC具有β-轴-OH基团。聚集数（n）是使用Moroi–Matsuoka–Sugioka热力学方法确定的。CMC，demicellization的焓，Δ Ç p通过等温滴定量热法（ITC）测定。该报告是MC衍生物胶束化研究的先驱。β-MC和γ-MC的胶束属于线性同类基团（LCG），它们的胶束在85 mM以上具有恒定的聚集数n = 4-5。α-MC和ω-MC的胶束相对于LCG是离群值，它们的聚集数不断增加；在85毫米n= 6.8（α-MC）和6.5（ω-MC）。在衍生物β-MC和γ-MC的胶束中，存在氢键的可能性很小。α-MC的胶束可能在其疏水域中具有氢键。
更新日期：2017-09-14
中文翻译：
巯基酸钠衍生物（胆汁盐）胶束的结构-性能关系：类固醇骨架的构型对疏水性和胶束形成的影响-模式识别和潜在的膜保护特性
众所周知，β-巯基乙酸根阴离子可防止疏水性胆汁酸的膜毒性，疏水性胆汁酸已被用于治疗胆固醇型胆汁结石的增溶。更好地了解这些衍生胶束对于了解其生理和药理作用非常重要。来自类固醇骨架的β-轴（a）定向羟基减少了类固醇骨架凸面的疏水表面。因此，具有β-α-OH基的甾族表面活性剂的临界胶束化浓度（CMC）应增加，但是在不同方向的OH基团在胶束的疏水相中形成H键的情况下，其相反作用；在CMC递减，聚集更受青睐。一组多元酚酸（MCs）由α-MC，β-MC，γ-MC和ω-MC组成，其中α-MC和β-MC具有β-轴-OH基团。聚集数（n）是使用Moroi–Matsuoka–Sugioka热力学方法确定的。CMC，demicellization的焓，Δ Ç p通过等温滴定量热法（ITC）测定。该报告是MC衍生物胶束化研究的先驱。β-MC和γ-MC的胶束属于线性同类基团（LCG），它们的胶束在85 mM以上具有恒定的聚集数n = 4-5。α-MC和ω-MC的胶束相对于LCG是离群值，它们的聚集数不断增加；在85毫米n= 6.8（α-MC）和6.5（ω-MC）。在衍生物β-MC和γ-MC的胶束中，存在氢键的可能性很小。α-MC的胶束可能在其疏水域中具有氢键。
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