Publication Type:

Journal Article


Journal of Controlled Release, Elsevier B.V., Volume 288, p.14-22 (2018)



A-549 cell line, animal experiment, animal model, animal tissue, Antineoplastic drugs, article, azo compound, azp 1, Biological analytes, Chemical activation, controlled study, Diseases, drug activation, drug cytotoxicity, drug release, female, firtecan, Fluorescence, Fluorescence enhancement, HeLa cell line, Hep-G2 cell line, human, human cell, Hypoxic condition, liver microsome, male, MCF-7 cell line, MDA-MB-231 cell line, mouse, mouse model, nonhuman, pH, priority journal, Prodrug, rat, Rat liver microsomes, Theranostic agents, Therapeutic potentials, Therapeutic properties, tumor hypoxia, tumor weight, tumor xenograft, Tumors, unclassified drug, WI-38 cell line


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 λ = 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.

Cite this Research Publication

Y. Zhou, Maiti, M., Sharma, A., Won, M., Yu, L., Miao, L. Xi, Shin, J., Podder, A., Bobba, K. Naidu, Han, J., Bhuniya, S., and Kim, J. Seung, “Azo-based small molecular hypoxia responsive theranostic for tumor-specific imaging and therapy.”, Journal of Controlled Release, vol. 288, pp. 14-22, 2018.