Calabrò M L, Tommasini S, Donato P, Stancanelli R, Raneri D, Catania S, Costa C, Villari V, Ficarra P, Ficarra R
Dipartimento Farmaco-Chimico, Facoltà di Farmacia, Università di Messina, Viale Annunziata, 98168 Messina, ME, Italy.
J Pharm Biomed Anal. 2005 Jan 4;36(5):1019-27. doi: 10.1016/j.jpba.2004.09.018.
In the present work the feasibility of beta-cyclodextrin complexation was explored, as a tool for improving the aqueous solubility and antioxidant efficacy of rutin. By means of 1H NMR, UV-vis and circular dichroism spectroscopy the single aromatic ring of rutin was found to be inserted into the beta-cyclodextrin cavity to form a 1:1 inclusion complex. The effect of beta-cyclodextrin on the spectral features of rutin was quantitatively investigated, in fully aqueous medium, by holding the concentration of the guest constant and varying the host concentration. The associated binding constants were estimated to be 142+/-20 and 153+/-20 M(-1), respectively, on the basis of the observed UV-vis absorption and circular dichroism intensities. The antioxidant activity of rutin was also investigated, as affected by molecular encapsulation within beta-cyclodextrin (batophenanthroline test; comet assay; lipid peroxidation); the inclusion complex revealed improved antioxidant efficacy that may be in part explained by an increased solubility in the biological moiety.
在本研究中，探索了β-环糊精包合作用的可行性，将其作为提高芦丁水溶性和抗氧化功效的一种手段。通过1H NMR、紫外可见光谱和圆二色光谱发现，芦丁的单个芳香环插入到β-环糊精腔内，形成1:1的包合物。在完全水介质中，通过保持客体浓度不变并改变主体浓度，定量研究了β-环糊精对芦丁光谱特征的影响。根据观察到的紫外可见吸收和圆二色强度，估算出相关的结合常数分别为142±20和153±20 M(-1)。还研究了芦丁的抗氧化活性，考察了其被β-环糊精分子包封后的影响（联苯菲罗啉试验；彗星试验；脂质过氧化）；包合物显示出提高的抗氧化功效，这可能部分归因于其在生物部分中溶解度的增加。
