β-环糊精的超分子自组装：抗菌剂洗必泰的有效载体
Supramolecular self-assembly of beta-cyclodextrin: an effective carrier of the antimicrobial agent chlorhexidine.
作者信息
Denadai Angelo M L, Teixeira Karina I, Santoro Marcelo M, Pimenta Adriano M C, Cortés Maria E, Sinisterra Rubén D
机构信息
Departamento de Química, Instituto de Ciências Exactas, Universidade Federal de Minas Gerais, UFMG, Avenida Antônio Carlos 6627, 31270-901, Belo Horizonte, MG, Brazil.
出版信息
Carbohydr Res. 2007 Nov 5;342(15):2286-96. doi: 10.1016/j.carres.2007.05.002. Epub 2007 May 16.
The supramolecular assembly between chlorhexidine and cyclomaltoheptaose (beta-cyclodextrin, betaCD) was characterized using NMR spectroscopy ((1)H, T(1), and ROESY), ESIMS and ITC. NMR data suggest the formation of high ordered complexes. ESIMS and ITC allowed the confirmation of the average stoichiometry as 1:4 and the thermodynamic data, also obtained by ITC, showed that the assembly is strongly stabilized by short distance interactions, but suffers a strong, opposite effect of entropy reduction. The antimicrobial activity of 1:1, 1:2, 1:3, and 1:4 Clx/betaCD molar ratio mixtures was investigated in aqueous solution and after incorporation into mucoadhesive gels. These were used to determine the initial and the long-term antimicrobial activity, respectively, toward Actinobacillus actinomycetemcomitans (A.a.) (Y4-FDC) and Enterococcus faecalis (E.f.) (ATCC 14508) strains. The results showed that A.a. and E.f. were more susceptible to the 1:4 molar ratio mixture in either solution or gel (p<0.05).
使用核磁共振光谱（¹H、T₁和ROESY）、电喷雾离子化质谱（ESIMS）和等温滴定量热法（ITC）对洗必泰和环麦芽七糖（β-环糊精，βCD）之间的超分子组装进行了表征。核磁共振数据表明形成了高度有序的复合物。ESIMS和ITC证实了平均化学计量比为1:4，并且通过ITC获得的热力学数据表明，该组装通过短程相互作用得到了强烈稳定，但受到熵降低的强烈相反影响。研究了1:1、1:2、1:3和1:4的洗必泰/βCD摩尔比混合物在水溶液中以及掺入粘膜粘附凝胶后的抗菌活性。这些分别用于测定对伴放线放线杆菌（A.a.）（Y4-FDC）和粪肠球菌（E.f.）（ATCC 14508）菌株的初始和长期抗菌活性。结果表明，在溶液或凝胶中，A.a.和E.f.对1:4摩尔比混合物更敏感（p<0.05）。
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