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

Journal of Controlled Release : Official Journal of the Controlled Release Society
Ying ZhouJong Seung Kim

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 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.

Citations

Nov 30, 2018·Chembiochem : a European Journal of Chemical Biology·Hardev SinghJong Seung Kim
Dec 24, 2018·Chemical Society Reviews·Amit SharmaJong Seung Kim
Nov 27, 2020·Advanced Healthcare Materials·Miffy Hok Yan ChengGang Zheng
Apr 8, 2020·European Journal of Medicinal Chemistry·Mengjiao ZhouFeifei An
Aug 11, 2020·Acta Biomaterialia·Mengmeng LongZhongping Chen
Jun 25, 2021·Biosensors & Bioelectronics·Jagpreet Singh SidhuNarinder Singh
Mar 11, 2019·ACS Biomaterials Science & Engineering·Yumin ZhangJianfeng Liu
Jul 16, 2019·Chemical Reviews·Rajesh KumarJong Seung Kim
Aug 28, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Thitima PewklangAnyanee Kamkaew

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