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首页> 外文期刊>Physical chemistry chemical physics: PCCP >Thermodynamics and structure of inclusion compounds of tauro- and glyco-conjugated bile salts and p-cyclodextrin
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Thermodynamics and structure of inclusion compounds of tauro- and glyco-conjugated bile salts and p-cyclodextrin

机译：牛磺酸和糖共轭胆汁盐与对环糊精的包合物的热力学和结构

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摘要

The interaction between natural p-cyclodextrin and bile salts common in rat, dog and man, taurocholate, tauro- P-muricholate, taurodeoxycholate, taurochenodeoxycholate, glycocholate, glycodeoxycholate and glycochenodeoxycholate, was studied using isothermal titration calorimetry, and the structural differences in the interaction were investigated by ~1H-ROESY NMR and molecular modeling. The p-cyclodextrin was selected based upon its frequent use in preformulation and drug formulation as oral excipients for the solubilization of drug substances with low aqueous solubility. All the investigated bile salts possessed affinity for the cyclodextrin, though with large variations in the stability constants. The variations in the enthalpic and entropic contributions to the overall Gibbs free energy and consequently the stability constants revealed differences in the binding mode between the investigated bile salts, i.e. the bile salts with a hydroxyl group on C12 interacted differently from the bile salts without this hydroxyl group. These observations were supported by both ~1H-ROESY NMR and molecular modeling, which suggested binding on the D-ring in the steroid structure for the former and on the C-ring for the latter bile salts.
机译：使用等温滴定量热法研究了大鼠，狗和人中常见的天然对-环糊精与胆汁盐，牛磺胆酸盐，牛磺-P-去甲胆酸盐，牛磺去氧胆酸盐，牛磺去氧胆酸盐，糖胆酸盐，糖脱氧胆酸盐和糖醛去氧胆酸盐之间的相互作用，以及相互作用的结构差异用〜1H-ROESY NMR和分子模型进行了研究。选择p-环糊精是基于其在预制剂和药物制剂中作为口服赋形剂的频繁使用，以溶解低水溶性的药物。所有研究的胆汁盐都对环糊精具有亲和力，尽管稳定性常数变化很大。焓和熵对总吉布斯自由能的变化以及因此的稳定性常数揭示了所研究的胆盐之间的结合方式的差异，即在C12上带有羟基的胆盐与没有这种羟基的胆盐的相互作用不同组。这些观察结果均得到〜1H-ROESY NMR和分子模型的支持，这表明前者在类固醇结构中的D环上结合，后者在胆汁盐上在C环上结合。

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