Department of Chemistry and Environmental Science, College of Science and Liberal Arts , New Jersey Institute of Technology , 323 Martin Luther King, Jr. Boulevard , Newark , New Jersey 07102 , United States.
Department of Orthopaedic Surgery , Johns Hopkins School of Medicine , 601 Fifth Street South , St. Petersburg , Florida 33701 , United States.
Bioconjug Chem. 2019 Sep 18;30(9):2312-2316. doi: 10.1021/acs.bioconjchem.9b00465. Epub 2019 Aug 23.
Mitochondria are essential targets for treatment of diseases with mitochondrial disorders such as diabetes, cancer, and cardiovascular and neurodegenerative diseases. Mitochondria penetrating peptides (MPPs) are composed of cationic and hydrophobic amino acids that can target and permeate the mitochondrial membrane. Herein, a novel d-argine-phenylalanine-d-argine-phenylalanine-d-argine-phenylalanine-NH (rFrFrF) was tagged with a rhodamine-based fluorescent chromophore (TAMRA). This probe (TAMRA-rFrFrF) exhibited advantageous properties for long-term mitochondria tracking as demonstrated by fluorescence microscopy. Cell viability assays and oxygen consumption rates indicate low cytotoxicity and high biocompatibility of the new contrast agent. Colocalization studies suggest that TAMRA-rFrFrF is a promising candidate for continuous mitochondrial tracking for up to 3 days.
线粒体是治疗线粒体疾病（如糖尿病、癌症以及心血管和神经退行性疾病）的重要靶点。线粒体穿透肽（MPPs）由阳离子和疏水性氨基酸组成，可靶向和穿透线粒体膜。本文将一种新型的 d-精氨酸-苯丙氨酸-d-精氨酸-苯丙氨酸-d-精氨酸-苯丙氨酸-NH（rFrFrF）与基于罗丹明的荧光发色团（TAMRA）缀合。该探针（TAMRA-rFrFrF）通过荧光显微镜显示出长期线粒体跟踪的有利特性。细胞活力测定和耗氧量表明，新型造影剂具有低细胞毒性和高生物相容性。共定位研究表明，TAMRA-rFrFrF 是一种有前途的候选物，可连续跟踪线粒体长达 3 天。
