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Purification and characterization of a chicory polysaccharide and its application in stabilizing genistein for cancer
Lijuan Shi1, Zhen Lin1, Jiantong Hou1
1State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy, and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300350, People's Republic of China.
Abstract:
Genistein is an isoflavone with chemopreventive and therapeutic effects on various types of cancers. Apparently, in contrast to the advantages of multi-target therapy, the poor water solubility of this molecule is a major obstacle to its clinical application. In this work, zein/chicory polysaccharide nanoparticles (G-zein-P NPs) were prepared by pH-induced antisolvent precipitation method for the encapsulation of genistein. Firstly, an acidic polysaccharide (CIP70-2) with a molecular weight of 66.7 kDa was identified from the roots of chicory (Cichorium intybus). This natural macromolecule was identified as a plant pectin, for which the structure included RG-I (rhamnogalacturonan I) and HG (homogalacturonan) regions. Using this polysaccharide, G-zein-P NPs were prepared, in which the water solubility of genistein was improved by encapsulation. The encapsulation efficiency and loading efficiency of genistein by composite nanoparticles reached 99.0 % and 6.96 %, respectively. In vitro tumor inhibition experiments showed that the inhibitory effect of G-zein-P NPs on HepG2 cells was twice that of unencapsulated genistein. Moreover, the significant inhibition of tumor development and metastasis by G-zein-P NPs was observed in zebrafish xenograft models. The results suggested that zein/chicory polysaccharide nanoparticles may be a promising delivery carrier for genistein application in cancer prevention and therapy.
Insights
Zein/chicory polysaccharide nanoparticles effectively encapsulate genistein, improving its water solubility and enhancing its anti-cancer properties. These nanoparticles show significant potential for genistein delivery in cancer prevention and therapy.
Area of Science:
- Biomaterials Science
- Nanotechnology
- Pharmacology
Background:
- Genistein, an isoflavone, exhibits cancer chemopreventive and therapeutic potential.
- Poor water solubility of genistein hinders its clinical application.
- Novel delivery systems are needed to overcome genistein's solubility limitations.
Purpose of the Study:
- To develop zein/chicory polysaccharide nanoparticles (G-zein-P NPs) for genistein encapsulation.
- To enhance the water solubility and anti-cancer efficacy of genistein.
- To evaluate the anti-tumor effects of G-zein-P NPs in vitro and in vivo.
Main Methods:
- Preparation of G-zein-P NPs using a pH-induced antisolvent precipitation method.
- Identification and characterization of an acidic polysaccharide from chicory roots.
- In vitro cytotoxicity assays on HepG2 cells.
- In vivo tumor inhibition studies using zebrafish xenograft models.
Main Results:
- G-zein-P NPs successfully encapsulated genistein with high efficiency (99.0%) and loading (6.96%).
- Encapsulation significantly improved genistein's water solubility.
- G-zein-P NPs demonstrated twice the tumor inhibitory effect on HepG2 cells compared to free genistein.
- Significant inhibition of tumor development and metastasis was observed in zebrafish models.
Conclusions:
- Zein/chicory polysaccharide nanoparticles are a promising delivery system for genistein.
- This formulation enhances genistein's anti-cancer activity and overcomes solubility issues.
- G-zein-P NPs hold potential for cancer prevention and therapeutic applications.
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