Medizinische Universität Graz Austria/Österreich - Forschungsportal - Medical University of Graz
Gewählte Publikation:
SHR Neuro Krebs Kardio Lipid Stoffw Microb
Ding, X; Wang, W; Wang, Y; Bao, X; Wang, Y; Wang, C; Chen, J; Zhang, F; Zhou, J.
Versatile reticular polyethylenimine derivative-mediated targeted drug and gene codelivery for tumor therapy.
Mol Pharm. 2014; 11(10):3307-3321
Doi: 10.1021/mp5001263
Web of Science
PubMed
FullText
FullText_MUG
- Co-Autor*innen der Med Uni Graz
- Zhang Fangrong
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- Abstract:
- The study is aimed to develop a versatile reticular polyethylenimine (PEI) derivative eprosartan-g-PEI (ESP) conjugate-mediated targeted drug and gene codelivery system for tumor therapy. Eprosartan (ES), an angiotensin II type 1 receptor blocker (ARB), which has been proven to exert beneficial effects on tumor progression, vascularization, and metastasis as the conventional antihypertensive drug, was conjugated with PEI-1.8K chains into ESP via a bis-amide bond of pH-sensitivity to overcome high cytotoxicity and nontargeted gene delivery of PEI-25K. P53 gene was encapsulated in the ESP to form the codelivery system of ESP/p53 complexes, and this system was comprehensively characterized. In vitro ESP/p53 complexes had a significant effect on inhibiting angiogenesis by reducing the expression and secretion of VEGF. In vivo the effective antitumor activity of ESP/p53 complexes was observed on nude mice bearing PANC-1 xenografts, and the microvessel density (MVD) examination demonstrated that ESP/p53 complex-produced antitumor efficacy was closely correlated with the efficient angiogenesis repression. These findings disclosed that the multifunctional ESP/p53 complexes might be a promising dual anticancer drug and gene codelivery system.
- Find related publications in this database (using NLM MeSH Indexing)
- Acrylates - chemistry
- Acrylates - therapeutic use
- Animals -
- Antineoplastic Agents - chemistry
- Antineoplastic Agents - therapeutic use
- Cell Line, Tumor -
- Drug Delivery Systems - methods
- Enzyme-Linked Immunosorbent Assay -
- Humans -
- Imidazoles - chemistry
- Imidazoles - therapeutic use
- Male -
- Mice -
- Mice, Inbred BALB C -
- Mice, Nude -
- Microscopy, Atomic Force -
- Microvessels - drug effects
- Neovascularization, Pathologic - drug therapy
- Neovascularization, Pathologic - metabolism
- Polyethyleneimine - chemistry
- Thiophenes - chemistry
- Thiophenes - therapeutic use
- Find related publications in this database (Keywords)
- polyethylenimine
- eprosartan
- p53
- codelivery
- angiotensin II type-1 receptor
- tumor therapy