title: Photophysical properties and in vitro and in vivo photoinduced antitumor activity of cationic salts of meso-tetrakis(N-alkyl-3-pyridyl)bacteriochlorins.
abstract: Physico-chemical properties, biodistribution in animal tissues, and PDT efficacy of bacteriochlorin photosensitizers, namely cationic salts of synthetic meso-tetrakis(N-alkyl-3-pyridyl)bacteriochlorins were studied in НЕр2 cell line and in the LLC mouse model. The tested compounds showed high stability in the dark and high in vitro phototoxicity against НЕр2 cells (the half maximal inhibitory concentration LD50 in the range from 0.34±0.03 to 1.5±0.03μm). Synthetic bacteriochlorins rapidly accumulate in mouse tumor tissue with tumor-to-normal tissue fluorescence contrast ratios of 2.3-3.3, possess high PDT activity against LLC cells: inhibition of tumor growth, TGI 85.8-100%, increase in life span, ILS 105.7-129.2%, response rate, RR 50-100%. The highest PDT efficacy was found for meso-tetrakis[1-(4'-bromobutyl)-3-pyridyl]bacteriochlorin tetrabromide (IC50 0.34±0.03μm in vitro, TGI and RR 100% in vivo).
authors: P.A. Hertzen Moscow Institute of Oncology, 3 Vtoroi Botkinsky Proezd, 125284 Moscow, Russia.
authors: Raisa I
authors: RI
authors: Yakubovskaya
authors: P.A. Hertzen Moscow Institute of Oncology, 3 Vtoroi Botkinsky Proezd, 125284 Moscow, Russia. Electronic address: plotnikovaekaterina62@gmail.com.
authors: Ekaterina А
authors: EА
authors: Plotnikova
authors: P.A. Hertzen Moscow Institute of Oncology, 3 Vtoroi Botkinsky Proezd, 125284 Moscow, Russia.
authors: Anna D
authors: AD
authors: Plyutinskaya
authors: P.A. Hertzen Moscow Institute of Oncology, 3 Vtoroi Botkinsky Proezd, 125284 Moscow, Russia.
authors: Natalya B
authors: NB
authors: Morozova
authors: P.A. Hertzen Moscow Institute of Oncology, 3 Vtoroi Botkinsky Proezd, 125284 Moscow, Russia.
authors: Valery I
authors: VI
authors: Chissov
authors: Organic Intermediates and Dyes Institute, ¼ B. Sadovaya, 123995 Moscow, Russia.
authors: Elena A
authors: EA
authors: Makarova
authors: Organic Intermediates and Dyes Institute, ¼ B. Sadovaya, 123995 Moscow, Russia.
authors: Semen V
authors: SV
authors: Dudkin
authors: Organic Intermediates and Dyes Institute, ¼ B. Sadovaya, 123995 Moscow, Russia.
authors: Evgeny A
authors: EA
authors: Lukyanets
authors: Organic Intermediates and Dyes Institute, ¼ B. Sadovaya, 123995 Moscow, Russia.
authors: Georgy N
authors: GN
authors: Vorozhtsov
mesh_terms: D000818:Animals; D018827:Carcinoma, Lewis Lung / Q000188:drug therapy* / Q000473:pathology; D005260:Female; D051379:Mice; D010778:Photochemotherapy; D017319:Photosensitizing Agents / Q000737:chemistry / Q000627:therapeutic use*; D011166:Porphyrins / Q000737:chemistry / Q000627:therapeutic use*; D012492:Salts; D047368:Tumor Burden / Q000187:drug effects
chemical_list: D017319:Photosensitizing Agents; D011166:Porphyrins; D012492:Salts; C452433:bacteriochlorin
keywords: Cell; Photocytotoxicity; Photodynamic therapy; Photosensitizer; Synthetic bacteriochlorins; Tissue