Encapsulating quercetin in cyclodextrin metal–organic frameworks improved its solubility and bioavailability

BACKGROUND Quercetin (Que) has many pharmacological activities, such as anticancer, antioxidant, cardiovascular protection, antihypertensive and lipid‐lowering activities. However, its poor water solubility greatly limits its application in medicine and food. γ‐Cyclodextrin metal–organic frameworks...

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Published in:Journal of the science of food and agriculture 2022-07, Vol.102 (9), p.3887-3896
Main Authors: Wang, Zhenjiong, Ma, Yiding, Jiang, Ying, Zhou, Feng, Wu, Yulong, Jiang, Haitao, Wang, Renlei, Xu, Qing, Hua, Chun
Format: Article
Language:English
Subjects:
Anticancer properties
Antihypertensives
Antioxidants
Bioavailability
Biocompatibility
Cadmium
Cholecystokinin
Cyclodextrin
Cyclodextrins
Cytotoxicity
Encapsulation
Flow cytometry
Food
Free radicals
G2 phase
Infrared analysis
Infrared spectroscopy
Lipids
Metal-organic frameworks
metal–organic framework
Molecular modelling
Quercetin
Scanning electron microscopy
Scavenging
Solubility
Thermogravimetric analysis
Toxicity
Tumors
water solubility
γ‐cyclodextrin
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Summary:BACKGROUND Quercetin (Que) has many pharmacological activities, such as anticancer, antioxidant, cardiovascular protection, antihypertensive and lipid‐lowering activities. However, its poor water solubility greatly limits its application in medicine and food. γ‐Cyclodextrin metal–organic frameworks (γ‐CD‐MOFs) are novel porous carriers for loading functional products. In this study, Que was successfully loaded into γ‐CD‐MOFs, and the new compound (Que‐CD‐MOFs) was characterised by X‐ray diffraction, infrared spectroscopy, thermogravimetric analysis and scanning electron microscopy. RESULTS The apparent solubility of Que‐CD‐MOFs was enhanced by 100‐fold compared with that of pure Que. The free radical scavenging ability of the encapsulated Que was significantly improved. The cytotoxicity of Que‐CD‐MOFs to HK‐2 cells was decreased, and their inhibition on HT‐29 tumour cells was maintained, as confirmed by CCK‐8 assays. Flow cytometry of HT‐29 cells showed that Que‐CD‐MOFs can inhibit G2 phase cells. Based on molecular modelling, Que molecules were preferentially located inside the cavities of γ‐CD pairs in γ‐CD‐MOFs. CONCLUSION γ‐CD‐MOFs are promising carriers for bioactive agents in food and pharmaceutical applications. © 2021 Society of Chemical Industry.
ISSN:0022-5142
1097-0010
DOI:10.1002/jsfa.11738