Calabrò M L, Tommasini S, Donato P, Raneri D, Stancanelli R, Ficarra P, Ficarra R, Costa C, Catania S, Rustichelli C, Gamberini G
Dipartimento Farmaco-Chimico, Facoltà di Farmacia, Università di Messina, Viale Annunziata, 98168 Messina (ME), Italy.
J Pharm Biomed Anal. 2004 Apr 16;35(2):365-77. doi: 10.1016/j.jpba.2003.12.005.
Inclusion complexes of some flavonols (3-hydroxyflavone, morin and quercetin) have been obtained with alpha- and beta-cyclodextrins, by the co-evaporation method. Different analytical techniques (DSC, XRPD, FT-IR, 1H-NMR, UV-Vis) have been employed for a throughout investigation of the structural characteristics of such supramolecular aggregates, which exhibited distinct spectroscopic features and properties from both "guest" and "host" molecules. The stoichiometric ratios and stability constants describing the extent of formation of the complexes have been determined by phase-solubility studies; in all cases type-AL diagrams have been obtained (soluble 1:1 complexes). The effect of molecular encapsulation on the flavonols antioxidant activity has been afterwards evaluated, by means of different biological assays (Bathophenanthroline test; Comet assay; Lipid peroxidation). Complexation with cyclodextrins further improved the antioxidant activity, increasing drugs solubility in the biological moiety.
通过共蒸发法，已获得了一些黄酮醇（3-羟基黄酮、桑色素和槲皮素）与α-和β-环糊精的包合物。采用了不同的分析技术（差示扫描量热法、X射线粉末衍射法、傅里叶变换红外光谱法、核磁共振氢谱法、紫外-可见光谱法）对这类超分子聚集体的结构特征进行全面研究，这些超分子聚集体展现出与“客体”和“主体”分子均不同的光谱特征和性质。通过相溶解度研究确定了描述配合物形成程度的化学计量比和稳定常数；在所有情况下均获得了AL型图（可溶性1:1配合物）。随后通过不同的生物学测定法（bathophenanthroline试验；彗星试验；脂质过氧化）评估了分子包封对黄酮醇抗氧化活性的影响。与环糊精络合进一步提高了抗氧化活性，增加了药物在生物部分的溶解度。
