二氢槲皮素- β-环糊精包合物的制备、表征及生物活性研究

Yaping Xu, Yue Wang, Chujie Li, Tao Han, Haiming Chen, Wenxue Chen, Qiuping Zhong, Jianfei Pei, Guido R. M. M. Haenen, Zhengwen Li, Mohamed Moalin, Ming Zhang, Weijun Chen
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摘要

摘要双氢槲皮素(DHQ)是一种天然存在的双氢黄酮醇,具有较强的抗氧化和抗菌活性。但其溶解度差,限制了其应用。本研究旨在通过与β-环糊精(β-CD)络合提高DHQ的水溶性,从而提高DHQ的生物活性。用β-CD包封DHQ,以1:1-M的比例冷冻干燥。采用傅里叶变换红外光谱、差示扫描量热法、x射线衍射、扫描电镜和核磁共振等手段对制备的DHQ/β-CD配合物的结构进行了表征。此外,分子对接进一步揭示了DHQ/β-CD配合物的两种能量有利构象,DHQ通过氢键与β-CD相互作用。实验结果表明,经β-CD包封后,DHQ的溶解度提高了22.63倍。包封可显著提高DHQ的溶出率、抗氧化活性和抗菌活性。β-CD包封解决了DHQ水溶性差的问题,为DHQ在医药和食品中促进健康作用的更优利用拓宽了途径。
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Preparation, characterization, and biological activity of the inclusion complex of dihydroquercetin and β-Cyclodextrin
Abstract Dihydroquercetin (DHQ) is a natural occurring dihydroflavonol that has strong antioxidant and antibacterial activities. However, its application is limited due to its poor solubility. This study aims to improve the aqueous solubility of DHQ by complexing DHQ with β-cyclodextrin (β-CD) to boost its biological activity. DHQ was encapsulated with β-CD by freeze drying at a 1:1-M ratio. The structure of DHQ/β-CD complex prepared was elucidated by using Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction, scanning electron microscopy, and 1 H nuclear magnetic resonance ( 1 H NMR). In addition, molecular docking further revealed two energetically favorable conformations of the DHQ/β-CD complex, in which DHQ interacted with β-CD via hydrogen bonds. Experimental results showed that the solubility of the DHQ increased 22.63-fold by encapsulating with β-CD. Also the dissolution rate, antioxidant activity and antibacterial activity of the DHQ were significantly improved by encapsulating. The encapsulating with β-CD solves the problem of the poor aqueous solubility of DHQ, and broadens the path for a more optimal use of the health promoting effect of DHQ in pharmaceutical and food products.
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