Novel bacteriochlorophyll-based photosensitizers and their photodynamic activity

Author:

Grin Mikhail A.1,Reshetnikov Roman I.1,Yakubovskaya Raisa I.2,Plotnikova Ekaterina A.2,Morozova Nataliya B.2,Tsigankov Anatoliy A.3,Efremenko Anastasiya V.45,Ermakova Dariya E.14,Feofanov Alexey V.45,Mironov Andrey F.1

Affiliation:

1. Lomonosov Moscow State Academy of Fine Chemical Technologies, prospekt Vernadskogo 86, 119571 Moscow, Russia

2. P.A. Herzen Moscow Institute of Oncology, Vtoroi Botkinsky proezd 3, 125284 Moscow, Russia

3. Institute of Fundamental Problems of Biology of Russian Academy of Sciences, Puschino, Russia

4. Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, ul. Miklukho-Maklaya 16/10, 117997 Moscow, Russia

5. Biological Faculty of Lomonosov Moscow State University, Vorobyevi Gori 1, 119992 Moscow, Russia

Abstract

Bacteriochlorin derivatives were synthesized by reacting bacteriopheophorbide methyl ether with diaminoalkanes bearing alkyl groups of different chain length. Biotests demonstrated their high in vitro phototoxicity at nanomolar concentrations against different types of epithelial cells, as well as high dose-dependent in vivo antitumor efficacy in tumor laden mice. At the doses of 2.5 and 5.0 mg/kg, the tested photosensitizers (PS) provided 100% tumor growth inhibition and 100% response rate over 120 day follow-up period after PDT due to selective accumulation in the tumor tissue and rapid clearance from the body.

Publisher

World Scientific Pub Co Pte Lt

Subject

General Chemistry

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