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利用超小的金纳米颗粒靶向和抑制。

Targeting and Inhibiting Using Ultra-small Gold Nanoparticles.

机构信息

Department of Biomolecular Systems, Max Planck Institute of Colloids and Interfaces, Am Mühlenberg 1, 14476 Potsdam, Germany.

Department of Biology, Chemistry, Pharmacy, Freie Universität Berlin, Arnimallee 22, 14195 Berlin, Germany.

出版信息

ACS Appl Mater Interfaces. 2020 Sep 30;12(39):43380-43387. doi: 10.1021/acsami.0c09075. Epub 2020 Sep 16.

Abstract

Malaria, a mosquito-borne disease caused by species, claims more than 400,000 lives globally each year. The increasing drug resistance of the parasite renders the development of new anti-malaria drugs necessary. Alternatively, better delivery systems for already marketed drugs could help to solve the resistance problem. Herein, we report glucose-based ultra-small gold nanoparticles (Glc-NCs) that bind to cysteine-rich domains of surface proteins Microscopy shows that Glc-NCs bind specifically to extracellular and all intra-erythrocytic stages of Glc-NCs may be used as drug delivery agents as illustrated for ciprofloxacin, a poorly soluble antibiotic with low antimalarial activity. Ciprofloxacin conjugated to Glc-NCs is more water-soluble than the free drug and is more potent. Glyco-gold nanoparticles that target cysteine-rich domains on parasites may be helpful for the prevention and treatment of malaria.

摘要

疟疾是一种由疟原虫引起的蚊媒疾病,每年在全球导致超过 40 万人死亡。寄生虫的抗药性不断增加,使得开发新的抗疟药物变得必要。或者,已经上市的药物更好的输送系统也可以帮助解决抗药性问题。在此,我们报告了基于葡萄糖的超小金纳米颗粒(Glc-NCs),它可以与疟原虫表面蛋白的富含半胱氨酸的结构域结合。显微镜观察表明,Glc-NCs 特异性地结合到疟原虫的细胞外和所有内红细胞期。Glc-NCs 可作为药物输送剂,如以环丙沙星为例,环丙沙星是一种水溶性差、抗疟活性低的抗生素。与 Glc-NCs 结合的环丙沙星比游离药物更易溶于水,且更有效。针对寄生虫富含半胱氨酸结构域的糖基金纳米颗粒可能有助于疟疾的预防和治疗。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f345/7586288/8549973b73aa/am0c09075_0002.jpg

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