Azo-based small molecular hypoxia responsive theranostic for tumor-specific imaging and therapy
- Authors
- Zhou, Ying; Maiti, Mrinmoy; Sharma, Amit; Won, Miae; Yu, Le; Miao, Lan Xi; Shin, Jinwoo; Podder, Arup; Bobba, Kondapa Naidu; Han, Jiyou; Bhuniya, Sankarprasad; Kim, Jong Seung
- Issue Date
- 28-10월-2018
- Publisher
- ELSEVIER SCIENCE BV
- Citation
- JOURNAL OF CONTROLLED RELEASE, v.288, pp.14 - 22
- Indexed
- SCIE
SCOPUS
- Journal Title
- JOURNAL OF CONTROLLED RELEASE
- Volume
- 288
- Start Page
- 14
- End Page
- 22
- URI
- https://scholar.korea.ac.kr/handle/2021.sw.korea/72434
- DOI
- 10.1016/j.jconrel.2018.08.036
- ISSN
- 0168-3659
- Abstract
- We report herein, an azo-derivative (AzP1) of FDA approved antineoplastic drug SN-38 (irinotecan analogue) as a theranostic agent with a potential for both tumor hypoxia-specific activation and therapy. The theranostic AzP1 was found to be stable within a biologically relevant pH scale and was chemically inert towards other competitive biological analytes. However, upon treatment with rat-liver microsomes, AzP1 showed a self-calibrated fluorescence enhancement at lambda(em) = 560 nm. The cytotoxicity profile of AzP1 was tested in various cancer lines. Under hypoxic conditions, prodrug AzP1 exhibited activation to release the parent drug (SN-38) and enhanced cytotoxicity in cancer cells with concomitant fluorescence enhancement at 560 nm, which served to monitor both the drug activation and tracing purposes. The therapeutic potential of AzP1 for both tumor-specific activation and suppression of tumor weights was validated in xenograft mouse model. Collectively, the synthetic ease and hypoxia-sensitive activation along with promising therapeutic properties highlight the potential of theranostic AzPI in future cancer treatment programs.
- Files in This Item
- There are no files associated with this item.
- Appears in
Collections - College of Science > Department of Chemistry > 1. Journal Articles
Items in ScholarWorks are protected by copyright, with all rights reserved, unless otherwise indicated.