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Photophysical properties and in vitro and in vivo photoinduced antitumor activity of cationic salts of meso-tetrakis(N-alkyl-3-pyridyl)bacteriochlorins

Paper ID Volume ID Publish Year Pages File Format Full-Text
30427 44478 2014 6 PDF Available
Title
Photophysical properties and in vitro and in vivo photoinduced antitumor activity of cationic salts of meso-tetrakis(N-alkyl-3-pyridyl)bacteriochlorins
Abstract

•Cationic salts of meso-tetrakis (N-alkyl-3-pyridyl)bacteriochlorins were synthesized.•Synthetic photosensitizers having strong absorption in the long wavelength region.•High PDT efficacy of synthetic bacteriochlorin photosensitizers in vitro.•Synthetic bacteriochlorins rapidly accumulate in mouse tumor tissue.•PS possess high PDT activity against in mice bearing Lewis lung carcinoma.

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 ± 0.03 μm).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 ± 0.03 μm in vitro, TGI and RR 100% in vivo).

Keywords
Photodynamic therapy; Photosensitizer; Synthetic bacteriochlorins; Photocytotoxicity; Cell; Tissue
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Photophysical properties and in vitro and in vivo photoinduced antitumor activity of cationic salts of meso-tetrakis(N-alkyl-3-pyridyl)bacteriochlorins
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Publisher
Database: Elsevier - ScienceDirect
Journal: Journal of Photochemistry and Photobiology B: Biology - Volume 130, 5 January 2014, Pages 109–114
Authors
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Subjects
Physical Sciences and Engineering Chemical Engineering Bioengineering
Get Full-Text Now
Don't Miss Today's Special Offer
Price was $35.95
You save - $31
Price after discount Only $4.95
100% Money Back Guarantee
Full-text PDF Download
Online Support
Any Questions? feel free to contact us