期刊
CHEMISTRY & BIODIVERSITY
卷 18, 期 2, 页码 -出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cbdv.202000944
关键词
pharmaceutical complexes; genistein-adenine; pharmaceutical transportation; fluorescence; molecular docking
资金
- Zhejiang Public Welfare Technology Application Research Project [LGN20B070001]
- National and Local Joint Engineering Laboratory of High Efficiency and Superior-Quality Cultivation and Fruit Deep Processing Technology of Characteristic Fruit Trees in South Xinjiang [FE201802]
A GS-adenine pharmaceutical complex was prepared through solvent evaporation to improve the bioavailability of GS; the solubility of GS-adenine was five times higher than that of GS, and the cumulative release rate was 86%; the study provides a useful reference for synthesizing pharmaceutical complexes to improve solubility and exploring the mechanism of multiple pharmaceutical components in vivo.
Genistein (GS) exhibits various biological activities, but its clinical application is limited because of the low bioavailability. In this study, a GS-adenine pharmaceutical complex was prepared through solvent evaporation to improve the bioavailability of GS, and a molecular model of a two-component supramolecular pharmacological transport mechanism was established. The structure of GS-adenine was characterized, in addition, interaction patterns between GS and adenine were investigated using density functional theory. The results showed that the solubility of GS-adenine was five times higher than that of GS, and the cumulative release rate of GS-adenine was 86 %. The results of fluorescence spectroscopy and molecular dynamic simulations showed that GS-adenine bound to the Sudlow's site I of HSA mainly through hydrophobic interactions. This study provides a useful reference for synthesizing pharmaceutical complexes to improve solubility and for exploring the mechanism of multiple pharmaceutical components in vivo.
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