新疆家蚕抗菌肽(CecropinXJ,CEC)可抑制宫颈癌细胞生长,但缺乏靶向性,难以将药物精确地输送到肿瘤部位。纳米药物递送系统是解决这一问题的有效策略。本研究基于金属有机框架ZIF⁃8制备了一种新型叶酸官能化FA⁃ZIF⁃8@CEC纳米颗粒作为宫...新疆家蚕抗菌肽(CecropinXJ,CEC)可抑制宫颈癌细胞生长,但缺乏靶向性,难以将药物精确地输送到肿瘤部位。纳米药物递送系统是解决这一问题的有效策略。本研究基于金属有机框架ZIF⁃8制备了一种新型叶酸官能化FA⁃ZIF⁃8@CEC纳米颗粒作为宫颈癌靶向药物递送系统。红外光谱、紫外⁃可见吸收光谱、核磁氢谱、X射线衍射(X⁃ray diffraction,XRD)、扫描电镜(scanning electron microscopy,SEM)、透射电镜(transmission electron microscopy,TEM)等表征结果证明成功制备了FA⁃ZIF⁃8@CEC纳米颗粒。MTT结果显示,与游离CEC和ZIF⁃8@CEC相比,FA⁃ZIF⁃8@CEC在HeLa细胞中表现出更好的抗宫颈癌效果。本研究结果说明叶酸官能化的FA⁃ZIF⁃8@CEC纳米药物在宫颈癌靶向治疗中具有一定的应用前景。展开更多
目的通过文献计量学研究展示肾癌靶向治疗领域的现状、热点和前沿,为探索新的靶向策略提供参考。方法在Web of Science数据库核心合集(Web of Science Core Collection,WoSCC)中检索2009-2022年发表的相关文献1718篇及其记录的信息,采用...目的通过文献计量学研究展示肾癌靶向治疗领域的现状、热点和前沿,为探索新的靶向策略提供参考。方法在Web of Science数据库核心合集(Web of Science Core Collection,WoSCC)中检索2009-2022年发表的相关文献1718篇及其记录的信息,采用Citespace、R及Scimago Graphica软件进行文献计量学分析与可视化。结果美国出版物数量(414篇,24.10%)、出版物引用次数(20302次)及中介中心性(betweenness centrality,BC)(0.45)排名第1,对研究的贡献最大。美国印第安纳大学的CHENG L是最多产的研究人员(22篇),斯隆凯特琳癌症中心为研究产量最多的机构(38篇),Cancers为刊发研究最多的期刊(56篇)。目前的研究热点主要包括血管生成、肿瘤微环境(tumor microenvironment,TME)、靶向药物释放系统等。上皮间充质转换(epithelial-mesenchymal transition,EMT)、免疫检查点抑制剂(immune checkpoint inhibitors,ICIs)、肿瘤侵袭与扩散是该领域的研究前沿,正在不断发展。结论本项文献计量分析为肾癌靶向治疗的研究趋势,为相关热点及新兴前沿提供重要见解。本研究为寻求合作者的研究人员提供了有用的资源,并为未来研究提供参考。展开更多
The cationic folic acid(CFA) was prepared by introducing triethylenetetramine into folic acid with EDCI/NHS and characterized by IR, NMR and mass spectra. It was found that approximately one of two carboxyls in the ...The cationic folic acid(CFA) was prepared by introducing triethylenetetramine into folic acid with EDCI/NHS and characterized by IR, NMR and mass spectra. It was found that approximately one of two carboxyls in the folic acid molecule was substituted to form CFA. The conversion of γ-carboxyl is found to be 59% higher than 30% of γ-carboxyl. The CFA and doxorubicin hydrochloride can be loaded on the ionic shell of PTX-encapsulated micelle to form CFA loaded binary drug carrier via static interaction in aqueous solutions. The successful loading was demonstrated by zeta potential measurement and the drug load amount(DLA) of CFA was measured by HPLC. In vitro cytotoxicity results revealed the CFA drug carrier showed higher cytotoxicity to cancer cell MDA-MB-321 than the binary drug carrier without CFA and the positive control, while it showed lower cytotoxicity to normal cell HUVEC than the positive control, and similar cytotoxicity with the binary drug carrier without CFA. These results as well as confocal laser scanning microscopy observation indicate the synthesized CFA drug carrier possesses active tumor-targeting property.展开更多
文摘新疆家蚕抗菌肽(CecropinXJ,CEC)可抑制宫颈癌细胞生长,但缺乏靶向性,难以将药物精确地输送到肿瘤部位。纳米药物递送系统是解决这一问题的有效策略。本研究基于金属有机框架ZIF⁃8制备了一种新型叶酸官能化FA⁃ZIF⁃8@CEC纳米颗粒作为宫颈癌靶向药物递送系统。红外光谱、紫外⁃可见吸收光谱、核磁氢谱、X射线衍射(X⁃ray diffraction,XRD)、扫描电镜(scanning electron microscopy,SEM)、透射电镜(transmission electron microscopy,TEM)等表征结果证明成功制备了FA⁃ZIF⁃8@CEC纳米颗粒。MTT结果显示,与游离CEC和ZIF⁃8@CEC相比,FA⁃ZIF⁃8@CEC在HeLa细胞中表现出更好的抗宫颈癌效果。本研究结果说明叶酸官能化的FA⁃ZIF⁃8@CEC纳米药物在宫颈癌靶向治疗中具有一定的应用前景。
基金financially supported by National Undergraduate Training Programs for Innovation and Entrepreneurship(201310007048)the Basic Research Foundation of Beijing Institute of Technology(No.20120942005)the National Natural Science Foundation of China(No.21104005)
文摘The cationic folic acid(CFA) was prepared by introducing triethylenetetramine into folic acid with EDCI/NHS and characterized by IR, NMR and mass spectra. It was found that approximately one of two carboxyls in the folic acid molecule was substituted to form CFA. The conversion of γ-carboxyl is found to be 59% higher than 30% of γ-carboxyl. The CFA and doxorubicin hydrochloride can be loaded on the ionic shell of PTX-encapsulated micelle to form CFA loaded binary drug carrier via static interaction in aqueous solutions. The successful loading was demonstrated by zeta potential measurement and the drug load amount(DLA) of CFA was measured by HPLC. In vitro cytotoxicity results revealed the CFA drug carrier showed higher cytotoxicity to cancer cell MDA-MB-321 than the binary drug carrier without CFA and the positive control, while it showed lower cytotoxicity to normal cell HUVEC than the positive control, and similar cytotoxicity with the binary drug carrier without CFA. These results as well as confocal laser scanning microscopy observation indicate the synthesized CFA drug carrier possesses active tumor-targeting property.