Daruházi Agnes Emma, Szente Lajos, Balogh Balázs, Mátyus Péter, Béni Szabolcs, Takács Mária, Gergely András, Horváth Péter, Szoke Eva, Lemberkovics Eva
Department of Pharmacognosy, Semmelweis University, Ulloi út 26, H-1085 Budapest, Hungary.
J Pharm Biomed Anal. 2008 Nov 4;48(3):636-40. doi: 10.1016/j.jpba.2008.06.007. Epub 2008 Jun 24.
Isoflavones are suitable guest molecules for inclusion complex formation with cyclodextrins (CDs). The molecular encapsulation with CDs results in a solid, molecularly dispersed form and in a significantly improved aqueous solubility of isoflavones. Genistein, a key isoflavone constituent of Ononidis spinosae radix was found to form a supramolecular, non-covalent inclusion complex with both beta-cyclodextrin (beta-CD) and gamma-cyclodextrin (gamma-CD), while it did not form a stable complex with alpha-CD. The guest genistein was found to spatially located in the less polar cavity of cyclodextrin. The isolated binary genistein/CD complexes appeared novel crystalline lattices. The in vitro dissolution of genistein entrapped into both beta- and gamma-CD, significantly surpassed that of the plain isoflavone.
异黄酮是与环糊精（CDs）形成包合物的合适客体分子。用CDs进行分子包封会形成固体、分子分散形式，并显著提高异黄酮的水溶性。染料木黄酮是棘豆根中的一种关键异黄酮成分，发现它能与β-环糊精（β-CD）和γ-环糊精（γ-CD）形成超分子、非共价包合物，而它与α-CD不能形成稳定的复合物。发现客体染料木黄酮在环糊精极性较小的腔内定位。分离得到的二元染料木黄酮/CD复合物呈现出新颖的晶格结构。包封在β-和γ-CD中的染料木黄酮的体外溶出度显著超过普通异黄酮。
