title: [Development of a new photosensitizer on the basis of ytterbium porphyrazine complex].
abstract: The tetraphenyltetracyanoporphyrazine complex of ytterbium has been studied as a potential photosensitizer for fluorescence diagnostics and photodynamic therapy (PDT) of cancer. It has been shown that the new compound has an intensive absorption and fluorescence in the "tissue optical window". In particular, the absorption maximum of the complex is at the wavelength of 590 nm, and the fluorescence emission maximum is at 640 nm. A strong fluorescence enhancement with a 50-fold increase in the quantum yield has been revealed in blood serum. The experiments on human cancer cells line have demonstrated that the complex penetrates the cells in vitro and is located around the nuclei. The biodistribution and pharmacokinetics of the complex in animals have been investigated in vivo by a new method of transillumination fluorescence imaging using a peculiar setup. It has been found that the period of maximum uptake of the complex in mouse cervical carcinoma is from 3 to 6 h after i.v. injection, with the half-life in the tumor being 24 h. However, the selectivity of the complex in the tumor is not high enough. The time of clearance from the body is about 48 h. The area of the strongest fluorescence in the abdominal cavity in in vivo images is anatomically recognized as the intestine. This indicates that the new compounds undergo mainly the hepatic clearance mainly. The conventional methods ex vivo (confocal microscopy and point spectroscopic measurements) have detected the largest content of the complex in the intestine, liver, skin and tumor tissue. In general, the optical characteristics of the ytterbium porphyrazine complex as well as the features of its interaction with biological objects make it promising drug candidate for the photodynamic therapy and/or fluorescence diagnostics of cancer. However, a search for other novel formulations possessing a higher tumor selectivity remains an urgent problem.
authors.forename: M V
authors.initials: MV
authors.lastname: Shirmanova
authors.forename: I V
authors.initials: IV
authors.lastname: Balalaeva
authors.forename: N Iu
authors.initials: NIu
authors.lastname: Lekanova
authors.forename: S A
authors.initials: SA
authors.lastname: Mysiagin
authors.forename: A A
authors.initials: AA
authors.lastname: Brilkina
authors.forename: L G
authors.initials: LG
authors.lastname: Klapshina
authors.forename: E V
authors.initials: EV
authors.lastname: Zagaĭnova
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D006801:Humans; D008665:Metalloporphyrins / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D051379:Mice; D008808:Mice, Inbred CBA; D009369:Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D009928:Organ Specificity; D010778:Photochemotherapy; D017319:Photosensitizing Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D013050:Spectrometry, Fluorescence; D023041:Xenograft Model Antitumor Assays; D015018:Ytterbium / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D008665:Metalloporphyrins; D017319:Photosensitizing Agents; D015018:Ytterbium