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Reducible Bile Acid-Modified PEI Enhances Systemic siRNA Delivery and Inhibits Tumor Growth
김다훤,정지훈,( Yin Yue ),정재백 한국공업화학회 2019 한국공업화학회 연구논문 초록집 Vol.2019 No.0
RNA interference (RNAi), mediated by small interfering RNA (siRNA), has been considered as a potential therapeutic agent for cancer owing to its ability to suppress target genes in a sequence-specific manner. However, the inherent susceptibility of siRNA to degradation by nucleases in the blood and its poor cellular uptake have been considered major challenges for the clinical use of the systemic siRNA therapy. Therefore, an effective and stable systemic siRNA delivery system should be established. 4-fluorothiophenol-deoxycholic acid-polyethylenimine conjugates could generate stable nanoparticles with thiol-siRNA. The conjugates showed significant tumor growth inhibition effect in tumor-bearing mice after systemic administration. Therefore, the synthesized conugates could be considered as a candidate carrier for systemic cancer therapy using siRNA therapeutics.
김다훤,황위보,여사연,정지훈 한국고분자학회 2021 한국고분자학회 학술대회 연구논문 초록집 Vol.46 No.1
Small interfering RNA (siRNA) gene silencing, also known as RNA interference, has been considered as a potential therapeutic strategy for targeting cancer therapy. In this study, a conjugate of the low molecular weight polyethylenimine (PEI), and deoxycholic acid (DA) was further modified with 4-fluorothiophenol (FTP) (TP-DA-PEI) to achieve systemic siRNA delivery. The thiophenol group would be involved with disulfide bonds between the polymer chains and siRNA modified with free thiols (thiol-siRNA) to form and π-π interactions between the pendent aromatic groups and coprostane ring of the bile acid. The TP-DA-PEI conjugates could form stable nanoparticles with thiol-siRNA. The TP-DA-PEI conjugate not only enhanced intracellular uptake, serum stability, and transfection efficiency, but also showed high accumulation of the polyplex nanoparticles and significant tumor growth inhibition effect in tumor-bearing mice after systemic administration.
Systemic siRNA Delivery with Reducible Bile Acid-Modified PEI for Cancer Therapy
김다훤,임수연,김이슬,정재백,김동민,조희주,정지훈 한국공업화학회 2019 한국공업화학회 연구논문 초록집 Vol.2019 No.1
Small interfering RNA (siRNA) delivery has been considered as a potential cancer therapy because it contributes to RNA interference (RNAi) by inhibiting target gene expression in a sequence-specific manner. In this study, low molecular weight polyethylnimine (PEI, 1.8 kDa) was conjugated with deoxycholic acid (DA). A DA-PEI conjugate was further modified with 4-fluorothiophenol (FTP) (TP-DA-PEI) to enhance systemic siRNA delivery. The thiophenol group would be involved with disulfide bonds between the polymer chains and siRNA modified with free thiols (thiol-siRNA) to form and π-π interactions between the pendent aromatic groups and coprostane ring of the bile acid. The stabilized TP-DA-PEI conjugate with thiol-siRNA achieved enhanced intracellular uptake, serum stability, and transfection efficiency. In addition, it showed high accumulation of TP-DA-PEI/ thiol-siRNA polyplexes and significant tumor growth inhibition effect in tumor-bearing mice after systemic administration.