Hypoxia is one of the key characteristics of solid tumors. The over-expression of azoreductase resulting from hypoxia can be used as a target to visualize hypoxic levels and a trigger of the drug release system in tum...Hypoxia is one of the key characteristics of solid tumors. The over-expression of azoreductase resulting from hypoxia can be used as a target to visualize hypoxic levels and a trigger of the drug release system in tumor treatment. In this work, we developed a near-infrared fluorescent probe YLOD, composed of a near-infrared fluorophore, an azo bond, and an analogue of the anti-tumor drug melphalan. In the presence of azoreductase, YLOD displayed a red emission at 620 nm and released the anti-tumor drug concomitantly, thus achieving the integrated effects of hypoxic imaging and tumor treatment. Furthermore, YLOD successfully inhibited the growth of solid tumors during the tumor suppression experiments in nude mice. Considering all the results, YLOD emerges as a new fluorescence tool that can quickly determine the location and the edges of a tumor, showing concrete potential in clinical cancer treatment.展开更多
Hydrogen sulfide(H_(2) S) is a signaling molecule that plays important roles in biological systems.The exploration of H_(2) S as a new drug release trigger and its related fluorescent theranostic system is crucial for...Hydrogen sulfide(H_(2) S) is a signaling molecule that plays important roles in biological systems.The exploration of H_(2) S as a new drug release trigger and its related fluorescent theranostic system is crucial for cancer bio-imaging and therapy.Herein,we designed a new two-photon ratiometric fluorescent theranostic prodrug(compound 1) and studied its spectroscopic properties and application in in vivo imaging.Compound 1 specifically reacted with H_(2) S and released the free active therapeutic component of 7-ethyl-10-hydroxycamptothecin,which was accompanied with a red-shift fluorescence emission signal from 460 nm to 545 nm.The exogenous and endogenous H_(2) S in living cells were imaged by compound 1 under one-photon and two-photon excitation.Furthermore,compound 1 monitored the H_(2) S concentration changes in Caenorhabditis elegans by fluorescence imaging.Additionally,it showed effective drug release activation in situ tumor with exogenous and endogenous H_(2) S as the trigger.The H_(2) S-sensitive activation and drug-release properties highlight the potential of theranostic compound 1 in future cancer treatment and therapy.展开更多
基金supported by the National Natural Science Foundation of China (No. 22067019)China-Sweden Joint Mobility Project(No. 51811530018)the Scientific Researchof Yunnan Provincial Department of Education (No. 2021Y031)。
文摘Hypoxia is one of the key characteristics of solid tumors. The over-expression of azoreductase resulting from hypoxia can be used as a target to visualize hypoxic levels and a trigger of the drug release system in tumor treatment. In this work, we developed a near-infrared fluorescent probe YLOD, composed of a near-infrared fluorophore, an azo bond, and an analogue of the anti-tumor drug melphalan. In the presence of azoreductase, YLOD displayed a red emission at 620 nm and released the anti-tumor drug concomitantly, thus achieving the integrated effects of hypoxic imaging and tumor treatment. Furthermore, YLOD successfully inhibited the growth of solid tumors during the tumor suppression experiments in nude mice. Considering all the results, YLOD emerges as a new fluorescence tool that can quickly determine the location and the edges of a tumor, showing concrete potential in clinical cancer treatment.
基金the support of the National Natural Science Foundation of China (Nos.21867019,22067021,22067019)the “Youth Talent of Wan Ren Project” Foundation of Yunnan Province of Chinathe “Lian Da Scholar Project” of Yunnan Normal University。
文摘Hydrogen sulfide(H_(2) S) is a signaling molecule that plays important roles in biological systems.The exploration of H_(2) S as a new drug release trigger and its related fluorescent theranostic system is crucial for cancer bio-imaging and therapy.Herein,we designed a new two-photon ratiometric fluorescent theranostic prodrug(compound 1) and studied its spectroscopic properties and application in in vivo imaging.Compound 1 specifically reacted with H_(2) S and released the free active therapeutic component of 7-ethyl-10-hydroxycamptothecin,which was accompanied with a red-shift fluorescence emission signal from 460 nm to 545 nm.The exogenous and endogenous H_(2) S in living cells were imaged by compound 1 under one-photon and two-photon excitation.Furthermore,compound 1 monitored the H_(2) S concentration changes in Caenorhabditis elegans by fluorescence imaging.Additionally,it showed effective drug release activation in situ tumor with exogenous and endogenous H_(2) S as the trigger.The H_(2) S-sensitive activation and drug-release properties highlight the potential of theranostic compound 1 in future cancer treatment and therapy.
