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典型文献
Targeting the Rac1 pathway for improved prostate cancer therapy using polymeric nanoparticles to deliver of NSC23766
文献摘要:
Prostate cancer(PCa)is the second most commonly diagnosed cancer in men.The Rac1-GTP inhibitor NSC23766 has been shown to suppress PCa growth.However,these therapies have low tumor-targeting efficacy in vivo.Therefore,it is essential to produce a drug delivery system that specifically targets the tumor site.Herein,novel L-phenylalanine-based poly(ester amide)(Phe-PEA)polymers were synthesized and loaded with NSC23766(NSC23766@8P6 NPs),which had a small particle size(162.3±6.7 nm)and high NSC23766 loading(8.0%±1.1%)with a more rapid release of NSC23766 at pH 5.0.In vitro cellu-lar uptake and cytotoxicity assays demonstrated that NSC23766@8P6 NPs were rapidly taken up by PC3 cells and showed significant effects of PCa cell proliferation inhibition and G2/M phase arrest.Further-more,in vivo studies using PC3-bearing mice demonstrated that NSC23766@8P6 NPs delivered by in-travenous injection not only increased the drug concentration with prolonged retention(96 h)at the tumor site,but also inhibited tumor growth and induced apoptosis.In conclusion,we have discovered that NSC23766@8P6 NPs can serve as a delivery system that targets the tumor site and is therefore a promising therapeutic approach for PCa treatment.
文献关键词:
作者姓名:
Zean Li;Jun Huang;Tao Du;Yiming Lai;Kaiwen Li;Man-Li Luo;Dingjun Zhu;Jun Wu;Hai Huang
作者机构:
Department of Urology,Sun Yat-sen Memorial Hospital,Sun Yat-sen University,Guangzhou 510220,China;Guangdong Provincial Key Laboratory of Malignant Tumor Epigenetics and Gene Regulation,Sun Yat-sen Memorial Hospital,Sun Yat-sen University,Guangzhou 510120,China;Medical Research Center,Sun Yat-sen Memorial Hospital,Sun Yat-sen University,Guangzhou 510120,China;School of Biomedical Engineering,Sun Yat-sen University,Shenzhen 518107,China;Department of Obstetrics and Gynecology,Sun Yat-sen Memorial Hospital,Sun Yat-sen University,Guangzhou 510120,China;Department of Urology,The Sixth Affiliated Hospital of Guangzhou Medical University,Qingyuan People's Hospital,Qingyuan 511518,China
引用格式:
[1]Zean Li;Jun Huang;Tao Du;Yiming Lai;Kaiwen Li;Man-Li Luo;Dingjun Zhu;Jun Wu;Hai Huang-.Targeting the Rac1 pathway for improved prostate cancer therapy using polymeric nanoparticles to deliver of NSC23766)[J].中国化学快报(英文版),2022(05):2496-2500
A类:
NSC23766,8P6,travenous
B类:
Targeting,Rac1,pathway,improved,prostate,cancer,therapy,using,polymeric,nanoparticles,Prostate,PCa,second,most,commonly,diagnosed,GTP,inhibitor,been,shown,suppress,growth,However,these,therapies,have,low,tumor,targeting,efficacy,vivo,Therefore,essential,produce,drug,delivery,system,that,specifically,targets,site,Herein,novel,phenylalanine,ester,amide,Phe,PEA,polymers,were,synthesized,loaded,NPs,which,had,small,high,loading,more,release,In,vitro,cellu,lar,uptake,cytotoxicity,assays,demonstrated,rapidly,taken,by,PC3,cells,showed,significant,effects,proliferation,inhibition,G2,phase,arrest,Further,studies,bearing,mice,delivered,injection,not,increased,concentration,prolonged,retention,but,also,inhibited,induced,apoptosis,conclusion,discovered,serve,therefore,promising,therapeutic,approach,treatment
AB值:
0.536098
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