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Amphiphilic Peptide Nanorods Based on Oligo-Phenylalanine as a Biocompatible Drug Carrier
Bioconjugate Chemistry ( IF 4.0 ) Pub Date : 2017-08-11 00:00:00 , DOI: 10.1021/acs.bioconjchem.7b00247
Su Jeong Song 1 , Seulgi Lee 1 , Kyoung-Seok Ryu 2 , Joon Sig Choi 1
Affiliation  

Peptide nanostructure has been widely explored for drug-delivery systems in recent studies. Peptides possess comparatively lower cytotoxicity and are more efficient than polymeric carriers. Here, we propose a peptide nanorod system, composed of an amphiphilic oligo-peptide RH3F8 (Arg–His3–Phe8), as a drug-delivery carrier. Arginine is an essential amino acid in typical cell-penetration peptides, and histidine induces endo- and lysosomal escape because of its proton sponge effect. Phenylalanine is introduced to provide rich hydrophobicity for stable self-assembly and drug encapsulation. The self-assembled structure of RH3F8 showed nanorod-shaped morphology, positive surface charge, and retained formation in water for 35 days. RH3F8, labeled with Nile Red, showed high cellar uptake and accumulation in both cytoplasm and nucleus. The RH3F8 nanorods demonstrated negligible cytotoxicity, as shown by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT), lactate dehydrogenase (LDH), and hemolysis assays. To confirm the efficiency of drug delivery, curcumin was encapsulated in the RH3F8 nanorod system (RH3F8–Cur). RH3F8–Cur showed high encapsulation efficiency (24.63%) under the conditions of 200 μM curcumin. The RH3F8–Cur retained nanoscale size and positive surface charge, similar to those of the empty RH3F8 nanorods. RH3F8–Cur displayed a robust anticancer effect in HeLa and A549 cells, and inhibited the proliferation of cancer cells in a zebrafish model. These results indicate that the RH3F8 nanorods may be a promising candidate for a safe and effective drug-delivery system.

中文翻译:

基于寡苯丙氨酸的两亲性肽纳米棒作为生物相容性药物载体

在最近的研究中,肽纳米结构已广泛用于药物递送系统。肽具有相对较低的细胞毒性,并且比聚合载体更有效。在这里,我们提出了一种肽纳米棒系统,该系统由两亲寡肽RH 3 F 8(Arg–His 3 –Phe 8)组成,作为药物递送载体。精氨酸是典型的细胞穿透肽中的必需氨基酸,由于其质子海绵效应,组氨酸可诱导内体和溶酶体逸出。引入苯丙氨酸可提供丰富的疏水性,以实现稳定的自组装和药物封装。RH 3 F 8的自组装结构呈纳米棒状的形态,表面带正电荷,并在水中保持形成35天。带有尼罗红标记的RH 3 F 8在细胞质和细胞核中均表现出较高的地窖吸收和积累。RH 3 F 8纳米棒显示出可忽略的细胞毒性,如3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四唑溴化物(MTT),乳酸脱氢酶(LDH)和溶血试验所显示。为了确认药物输送的效率,姜黄素被封装在RH 3 F 8纳米棒系统(RH 3 F 8 –Cur)中。相对湿度3 F 8–Cur在200μM姜黄素的条件下显示出很高的包封效率(24.63%)。RH 3 F 8 -Cur保留纳米级尺寸和正表面电荷,类似于空的RH 3 F 8纳米棒。RH 3 F 8 –Cur在HeLa和A549细胞中显示出强大的抗癌作用,并在斑马鱼模型中抑制了癌细胞的增殖。这些结果表明,RH 3 F 8纳米棒可能是安全有效的药物递送系统的有希望的候选者。
更新日期:2017-08-12
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