Dendrimeric anticancer prodrugs for targeted delivery of ursolic acid to folate receptor-expressing cancer cells: Synthesis and biological evaluation
作者： Yu Gao , Zhihong Li , Xiaodong Xie , Chaoqun Wang , Jiali You
DOI: 10.1016/J.EJPS.2015.01.007
关键词: Folate receptor 、 Biochemistry 、 Chemistry 、 MTT assay 、 Endocytosis 、 Ursolic acid 、 Cancer cell 、 Prodrug 、 HeLa 、 Targeted drug delivery
摘要: The anticancer efficacy of ursolic acid (UA) was limited by poor water solubility, non-specific tumor distribution, and low bioavailability. To overcome this problem, polyamidoamine (PAMAM) conjugated with UA folic (FA) as novel dendrimeric prodrugs were designed successfully synthesized a concise one-pot synthetic approach. Both FA covalently to the surface PAMAM through acid-labile ester bonds linked could be hydrolysed either in acidic (pH 5.4) or neutral 7.4) PBS solution. cellular uptake study indicated that presence enhanced folate receptor (FR) over-expressing Hela cells. due electrostatic absorptive endocytosis FR-mediated endocytosis. In contrast, for HepG2 cells, FR-negative cell line, conjugation on dendrimer showed no effect uptake. MTT assay cycle analysis, FA-modified significantly toxicity than non-FA-modified ones These results suggested have potential targeted delivery into cancer cells improve its anti-tumor efficacy.
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