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
{"title":"二氢槲皮素- β-环糊精包合物的制备、表征及生物活性研究","authors":"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","doi":"10.1186/s41120-023-00083-8","DOIUrl":null,"url":null,"abstract":"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.","PeriodicalId":453,"journal":{"name":"AAPS Open","volume":"21 1","pages":"0"},"PeriodicalIF":0.0000,"publicationDate":"2023-10-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Preparation, characterization, and biological activity of the inclusion complex of dihydroquercetin and β-Cyclodextrin\",\"authors\":\"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\",\"doi\":\"10.1186/s41120-023-00083-8\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"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.\",\"PeriodicalId\":453,\"journal\":{\"name\":\"AAPS Open\",\"volume\":\"21 1\",\"pages\":\"0\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2023-10-03\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"AAPS Open\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.1186/s41120-023-00083-8\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"AAPS Open","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1186/s41120-023-00083-8","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0

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。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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.
求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
自引率
0.00%
发文量
0
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术官方微信