title: Riboflavin photoactivation by upconversion nanoparticles for cancer treatment.
abstract: Riboflavin (Rf) is a vitamin and endogenous photosensitizer capable to generate reactive oxygen species (ROS) under UV-blue irradiation and kill cancer cells, which are characterized by the enhanced uptake of Rf. We confirmed its phototoxicity on human breast adenocarcinoma cells SK-BR-3 preincubated with 30-μM Rf and irradiated with ultraviolet light, and proved that such Rf concentrations (60 μM) are attainable in vivo in tumour site by systemic intravascular injection. In order to extend the Rf photosensitization depth in cancer tissue to 6 mm in depth, we purpose-designed core/shell upconversion nanoparticles (UCNPs, NaYF4:Yb3+:Tm3+/NaYF4) capable to convert 2% of the deeply-penetrating excitation at 975 nm to ultraviolet-blue power. This power was expended to photosensitise Rf and kill SK-BR-3 cells preincubated with UCNPs and Rf, where the UCNP-Rf energy transfer was photon-mediated with ~14% Förster process contribution. SK-BR-3 xenograft regression in mice was observed for 50 days, following the Rf-UCNPs peritumoural injection and near-infrared light photodynamic treatment of the lesions.
authors.affiliation: Federal Scientific Research Centre "Crystallography and Photonics" of Russian Academy of Sciences, Leninsky pr. 59, Moscow, 119333, Russia.
authors.forename: E V
authors.initials: EV
authors.lastname: Khaydukov
authors.affiliation: Federal Scientific Research Centre "Crystallography and Photonics" of Russian Academy of Sciences, Leninsky pr. 59, Moscow, 119333, Russia.|Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry of the Russian Academy of Sciences, 16/10 Miklukho-Maklaya, Moscow 117997, Russia.
authors.forename: K E
authors.initials: KE
authors.lastname: Mironova
authors.affiliation: Federal Scientific Research Centre "Crystallography and Photonics" of Russian Academy of Sciences, Leninsky pr. 59, Moscow, 119333, Russia.
authors.forename: V A
authors.initials: VA
authors.lastname: Semchishen
authors.affiliation: Federal Scientific Research Centre "Crystallography and Photonics" of Russian Academy of Sciences, Leninsky pr. 59, Moscow, 119333, Russia.|Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry of the Russian Academy of Sciences, 16/10 Miklukho-Maklaya, Moscow 117997, Russia.
authors.forename: A N
authors.initials: AN
authors.lastname: Generalova
authors.affiliation: Federal Scientific Research Centre "Crystallography and Photonics" of Russian Academy of Sciences, Leninsky pr. 59, Moscow, 119333, Russia.|Institute of Fine Chemical Technologies, Moscow Technological University, 86 Prospect Vernadskogo, 119571 Moscow, Russia.
authors.forename: A V
authors.initials: AV
authors.lastname: Nechaev
authors.affiliation: Federal Scientific Research Centre "Crystallography and Photonics" of Russian Academy of Sciences, Leninsky pr. 59, Moscow, 119333, Russia.|FSBSI "N.N. Blokhin Russian Cancer Research Center" of Ministry of Health of the Russian Federation, 24 Kashirskoye shosse, Moscow, 115478, Russia.
authors.forename: D A
authors.initials: DA
authors.lastname: Khochenkov
authors.affiliation: FSBSI "N.N. Blokhin Russian Cancer Research Center" of Ministry of Health of the Russian Federation, 24 Kashirskoye shosse, Moscow, 115478, Russia.
authors.forename: E V
authors.initials: EV
authors.lastname: Stepanova
authors.affiliation: Laboratoire CRISMAT, UMR6508, CNRS-ENSIACEN, Universite Caen, 14050 Caen, France.
authors.forename: O I
authors.initials: OI
authors.lastname: Lebedev
authors.affiliation: Federal Scientific Research Centre "Crystallography and Photonics" of Russian Academy of Sciences, Leninsky pr. 59, Moscow, 119333, Russia.|ARC Centre of Excellence for Nanoscale BioPhotonics, Macquarie University, North Ryde, NSW 2109, Australia.
authors.forename: A V
authors.initials: AV
authors.lastname: Zvyagin
authors.affiliation: Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry of the Russian Academy of Sciences, 16/10 Miklukho-Maklaya, Moscow 117997, Russia.
authors.forename: S M
authors.initials: SM
authors.lastname: Deyev
authors.affiliation: Federal Scientific Research Centre "Crystallography and Photonics" of Russian Academy of Sciences, Leninsky pr. 59, Moscow, 119333, Russia.
authors.forename: V Ya
authors.initials: VY
authors.lastname: Panchenko
mesh_terms: D000818:Animals; D001943:Breast Neoplasms / Q000188:drug therapy; D016466:CHO Cells; D018827:Carcinoma, Lewis Lung / Q000188:drug therapy; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003412:Cricetulus; D005260:Female; D005459:Fluorides / Q000737:chemistry; D006801:Humans; D053768:Metal Nanoparticles / Q000737:chemistry / Q000627:therapeutic use; D051379:Mice; D008810:Mice, Inbred C57BL; D008811:Mice, Inbred DBA; D009374:Neoplasms, Experimental / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D010778:Photochemotherapy / Q000379:methods*; D017319:Photosensitizing Agents / Q000627:therapeutic use*; D017382:Reactive Oxygen Species / Q000378:metabolism; D012256:Riboflavin / Q000627:therapeutic use*; D013932:Thulium / Q000737:chemistry; D023041:Xenograft Model Antitumor Assays; D015018:Ytterbium / Q000737:chemistry; D015019:Yttrium / Q000737:chemistry
chemical_list: D017319:Photosensitizing Agents; D017382:Reactive Oxygen Species; C525362:sodium yttriumtetrafluoride; D015019:Yttrium; D013932:Thulium; D015018:Ytterbium; D005459:Fluorides; D012256:Riboflavin