Low toxic ytterbium complexes of 2,4-dimethoxyhematoporphyrin IX for luminescence diagnostics of tumors

K S Shchamkhalov, Anatolii Yu Barishnikov,Adrian Ruhm, Georgii S Terentyuk,Andrey F Mironov, Alexandr S Ryabov, A Panas, Valerii M Markushev,I P Shilov,V D Rumyantseva,Andrey V Ivanov

Photonics & Lasers in Medicine(2013)

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摘要
Abstract:This article deals with the creation of new low-toxic photosensitizers on the basis of Ytterbium-2,4-dimethoxyhematoporphyrin IX (Yb-DMHP) and their application for the luminescence diagnostics of cancer. These substances were found to weakly generate singlet oxygen, exhibit pronounced luminescence, and retain the tumor-tropic properties of therapeutic photosensitizers. Basic photophysical properties of Yb-DMHP were studied, and the primary toxicological and pharmacokinetic investigations were performed in the organisms of experimental animals. The 4f-luminescence of Yb-DMHP in the near infrared (NIR) spectral region was observed. Comparative investigations were performed for one of the photodynamic medications which have been approved for clinical application: “Photoditazin”, a diglucosamine salt of chlorin e6. It was shown that the efficiency of singlet oxygen generation is lower by approximately one order of magnitude in the case of Yb-DMHP. The experimental data prove that Yb-DMHP-based substances are promising as non-toxic markers for the luminescence diagnostics of malignant tumors in the NIR spectral range (900–1100 nm), because they are free of the phototoxicity that is typical of conventional porphyrins, while at the same time providing a relatively high luminescence contrast and a selective accumulation in tumor tissue.
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