聚乙二醇化
白杨素
化学
溶解度
体外
水溶液
PEG比率
组合化学
生物活性
共轭体系
聚乙二醇
类黄酮
生物化学
有机化学
抗氧化剂
聚合物
财务
经济
作者
Julia Oggero,Fátima Belén Gasser,Silvia Mercedes Zacarías,Patricia Burns,María Eugenia Baravalle,María Sol Renna,Hugo H. Ortega,Santiago E. Vaillard,Victoria A. Vaillard
标识
DOI:10.1021/acs.jafc.3c06357
摘要
Chrysin is a natural flavonoid that despite having numerous biological properties, its therapeutic value is limited due to its very low solubility in aqueous media. In this work, chrysin was conjugated with methoxypolyethylene glycols (mPEGs) of different molecular weights (350, 500, 750, and 2000 g/mol), affording PEGylated chrysins with high yields and excellent purities. In all cases, an increase in the water solubility of the conjugates was observed, which was highest when 500 g/mol of mPEG was used in the PEGylation reaction. Furthermore, in aqueous solution, PEGylated chrysins formed aggregates of ellipsoid shape. Electrochemical studies showed that the redox properties were conserved after PEGylation. While in vitro antibacterial and antifungal studies probed that the intrinsic activity was conserved, in vitro antitumor activities against HepG2 (liver carcinoma cells) and PC3 (prostate cancer cell) showed that PEGylated chrysins retained the cytotoxic activity and the ability of induction of apoptosis for the evaluated human cancer cells.
科研通智能强力驱动
Strongly Powered by AbleSci AI