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A pH-Responsive Glycyrrhetinic-Acid-Modified Small-Molecule Conjugate for NIR Imaging of Hepatocellular Carcinoma (HCC)
- Authors
- Singh, Hardev; Lim, Ja-Yun; Sharma, Amit; Yoon, Dae Wui; Kim, Ji Hyeon; Yang, Zhigang; Qu, Junle; Kim, Jinkwan; Lee, Seung Gwan; Kim, Jong Seung
- Issue Date
- 15-2월-2019
- Publisher
- WILEY-V C H VERLAG GMBH
- Keywords
- fluorescent probes; glycyrrhetinic acid; hepatocellular carcinoma; imaging agents; natural products
- Citation
- CHEMBIOCHEM, v.20, no.4, pp.614 - 620
- Indexed
- SCIE
SCOPUS
- Journal Title
- CHEMBIOCHEM
- Volume
- 20
- Number
- 4
- Start Page
- 614
- End Page
- 620
- ISSN
- 1439-4227
- Abstract
- We report a glycyrrhetinic-acid (GA)-decorated small-molecule conjugate for pH-triggered near-infrared (NIR) fluorescence imaging of hepatocellular carcinoma (HCC). Our in vitro studies demonstrated that the conjugate, referred to as NIR-GA, was efficiently taken up by liver cancer cell lines such as HepG2 and Huh7 through an endocytic pathway mediated by GA receptors. As suggested by co-localization studies, NIR-GA mainly localized in the lysosome, where the acidic pH results in the activation of the fluorescent dye through H+-triggered spirolactam ring opening to give strong fluorescence in the NIR region.
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