Mitochondria targeting and near-infrared fluorescence imaging of a nove... https://pubmed.ncbi.nlm.nih.

gov/28440435/

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Mol Med Rep. 2017 Jun;15(6):3761-3766. doi: 10.3892/mmr.2017.6451. Epub 2017 Apr 10.

Mitochondria targeting and near-infrared

fluorescence imaging of a novel heptamethine
cyanine anticancer agent
Juewei Ning  1 , Baozhan Huang  1 , Zeliang Wei  1 , Wen'en Li  2 , Huajie Zheng  3 , Limei Ma  2 , 
Zhihua Xing  1 , Hai Niu  1 , Wen Huang  1

Affiliations
PMID: 28440435 DOI: 10.3892/mmr.2017.6451

Abstract
The future of personalized cancer treatments relies on the development of functional agents that have
tumor-targeted anticancer activities and can be detected in tumors using imaging. However,
application of these functional agents in the clinic has been limited due to inefficient drug delivery,
low specificity for tumor imaging, development of drug resistance, low signal-to-noise ratio and
safety concerns regarding potential toxicity. Currently, the most common strategy to develop these
functional agents is to conjugate therapeutic agents with the appropriate fluorescent probe. The
present study synthesized a novel mitochondria-targeted heptamethine cyanine (Cy) derivative
Cy‑triphenylphosphonium. The newly developed compound exhibited stronger near infrared (NIR)
fluorescence and reacted with bovine serum albumin. In addition, it preferentially accumulated in the
mitochondria of cancer cells, as observed using confocal microscopy, and efficiently reduced cancer
cell viability (IC50=3.04 µM). This novel multifunctional heptamethine Cy derivative, with cancer
mitochondria targeting and NIR fluorescence imaging, may be promising as an alternative anticancer
agent.

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