Near-Infrared Fluorescent pH Responsive Probe for Targeted Photodynamic Cancer Therapy

• Published in: Scientific reports Vol. 10; no. 1; p. 1283
• Main Authors: Siriwibool, Siriwalee, Kaekratoke, Nantawat, Chansaenpak, Kantapat, Siwawannapong, Kittipan, Panajapo, Pannipa, Sagarik, Kritsana, Noisa, Parinya, Lai, Rung-Yi, Kamkaew, Anyanee
• Format: Journal Article
• Language: English
• Published: London Nature Publishing Group UK 28.01.2020; Nature Publishing Group
• Subjects: 631/67/1059/602; 639/638/403; 639/638/439/945; Cancer therapies; Carcinoma, Hepatocellular - drug therapy; Carcinoma, Hepatocellular - metabolism; Carcinoma, Hepatocellular - pathology; Efficiency; Fluorescent Dyes - chemistry; Fluorescent Dyes - pharmacology; HEK293 Cells; Hep G2 Cells; Hepatocellular carcinoma; Hepatocytes; Humanities and Social Sciences; Humans; Hydrogen-Ion Concentration; Infrared Rays; Liver cancer; Liver Neoplasms - drug therapy; Liver Neoplasms - metabolism; Liver Neoplasms - pathology; Models, Chemical; multidisciplinary; pH effects; Photochemotherapy; Photodynamic therapy; Phototoxicity; Reactive oxygen species; Science; Science (multidisciplinary); Tumors
• ISSN: 2045-2322; 2045-2322
• DOI: 10.1038/s41598-020-58239-5

We developed a pH dependent amino heptamethine cyanine based theranostic probe ( I 2 -IR783-Mpip ) that can be activated by near infrared light. I 2 -IR783-Mpip , in acidic condition, exhibited an intense, broad NIR absorption band (820–950 nm) with high singlet oxygen generation upon exposure to NIR light (~850 nm). Theoretical calculations showed that the protonation of the probe in an acidic environment decreased the molecular orbital energy gaps and increased the intramolecular charge transfer efficiency. I 2 -IR783-Mpip exhibited good photodynamic efficiency towards liver hepatocellular carcinoma cells under physiological and slightly acidic conditions while normal human embryonic kidney cells remained alive under the same conditions. Detection of intracellular reactive oxygen species (ROS) in cells treated with I 2 -IR783-Mpip after NIR light exposure confirmed PDT efficiency of the probe in acidic environment. Moreover, I 2 -IR783-Mpip also demonstrated efficient phototoxicity under deep-seated tumour cell system. We believed this is the first PDT agent that possesses intrinsic tumour binding and selectively eradicate tumour in acidic environment under 850 nm NIR lamp.