Azo-based small molecular hypoxia responsive theranostic for tumor-specific imaging and therapy

Ying Zhou, Mrinmoy Maiti, Amit Sharma, Miae Won, Le Yu, Lan Xi Miao, Jinwoo Shin, Arup Podder, Kondapa Naidu Bobba, Jiyou Han, Sankarprasad Bhuniya, Jong Seung Kim

Research output: Contribution to journalArticlepeer-review

47 Citations (Scopus)


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 λem = 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.

Original languageEnglish
Pages (from-to)14-22
Number of pages9
JournalJournal of Controlled Release
Publication statusPublished - 2018 Oct 28

ASJC Scopus subject areas

  • Pharmaceutical Science


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