自组装肽偶联紫杉醇-多西他赛纳米颗粒的肿瘤特异性生化纳米转化

IF 13.4 2区 材料科学 Q1 MATERIALS SCIENCE, MULTIDISCIPLINARY
Hansol Lim, Jae-Hyeon Lee, So-Hyeon Park, Jun-Hyuck Lee, Hyesu Jang, Seong-Bin Yang, Minho Seo, Seokwoo Lee, Jooho Park
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引用次数: 0

摘要

多西紫杉醇(Docetaxel, DTX, 1)和紫杉醇(paclitaxel, PTX, 2)是广泛应用于癌症治疗的著名细胞毒性药物,但由于其对肿瘤细胞的特异性较低,往往导致严重的全身毒性。在传统的前药策略之外,本研究引入了一种新的纳米转化技术,通过化学修饰DTX形成自组装纳米颗粒(NPs), NPs随后转化为模拟紫杉醇的分子(PTXm, 3)。亲水性乙酰化的fe - arg - arg - phe肽((Ac)FRRF, 4)和疏水性多西紫杉醇结合制备自组装(Ac)FRRF-DTX NPs。癌细胞中丰富的组织蛋白酶B选择性切割Arg-Phe键,促进了PTXm(3)从(Ac)FRRF-DTX NPs的纳米转化,显示出有效的细胞毒性作用。利用肽和特定序列(如精氨酸-精氨酸-苯丙氨酸)的裂解位点,这种方法不仅可以作为前药,还可以使纳米材料转化为肿瘤内的另一种细胞毒性生物分子。(Ac)FRRF-DTX NPs具有显著的物理化学性质,优越的抗癌功效和低毒性,是肽偶联纳米药物的创新转化。与传统的前药化学不同,这种肿瘤特异性纳米转化过程涉及通过酶作用将DTX(1)生化转化为PTXm(3)。总的来说,这项研究提供了一个通过纳米转换概念进行化学药物分子修饰的杰出例子。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Tumor-specific biochemical nanoconversion of self-assembled peptide-conjugated paclitaxel-docetaxel-based nanoparticles

Docetaxel (DTX, 1) and paclitaxel (PTX, 2) are famous cytotoxic agents widely used in cancer therapy, however, their low specificity for tumor cells often results in severe systemic toxicity. Beyond conventional prodrug strategies, this study introduces a novel nanoconversion technology that chemically modifies DTX to form self-assembled nanoparticles (NPs), which subsequently convert into a paclitaxel-mimicking molecule (PTXm, 3). Hydrophilic acetylated Phe-Arg-Arg-Phe peptide ((Ac)FRRF, 4) and hydrophobic docetaxel were conjugated to prepare self-assembled (Ac)FRRF-DTX NPs. The selective cleavage of the Arg-Phe bond by cathepsin B, which is abundant in cancer cells, facilitated the nanoconversion of PTXm (3) from (Ac)FRRF-DTX NPs, demonstrating effective cytotoxic effects. Utilizing the cleavage site of peptide and specific sequences (ex. Arg-Arg-Phe), this approach does not simply act as a prodrug but allows the nanomaterial to transform into another cytotoxic biomolecule within tumors. (Ac)FRRF-DTX NPs exhibited remarkable physicochemical properties, superior anti-cancer efficacy, and low toxicity, showcasing an innovative conversion in peptide-conjugated nanomedicine. Unlike traditional prodrug chemistry, this tumor-specific nanoconversion process involves the biochemical transformation of DTX (1) into PTXm (3) via enzymatic action. Overall, this study provides an outstanding example of chemical drug molecular modification through the concept of nanoconversion.

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来源期刊
Nano Convergence
Nano Convergence Engineering-General Engineering
CiteScore
15.90
自引率
2.60%
发文量
50
审稿时长
13 weeks
期刊介绍: Nano Convergence is an internationally recognized, peer-reviewed, and interdisciplinary journal designed to foster effective communication among scientists spanning diverse research areas closely aligned with nanoscience and nanotechnology. Dedicated to encouraging the convergence of technologies across the nano- to microscopic scale, the journal aims to unveil novel scientific domains and cultivate fresh research prospects. Operating on a single-blind peer-review system, Nano Convergence ensures transparency in the review process, with reviewers cognizant of authors' names and affiliations while maintaining anonymity in the feedback provided to authors.
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