Synthesis and Biological Properties of EGFR-Targeted Photosensitizer Based on Cationic Porphyrin

Author:

Bortnevskaya Yulia S.1,Shiryaev Nikita A.1,Zakharov Nikita S.1,Kitoroage Oleg O.1,Gradova Margarita A.2ORCID,Karpechenko Natalia Yu.34,Novikov Alexander S.56ORCID,Nikolskaya Elena D.7ORCID,Mollaeva Mariia R.7ORCID,Yabbarov Nikita G.7,Bragina Natal’ya A.1,Zhdanova Kseniya A.1

Affiliation:

1. Institute of Fine Chemical Technology, MIREA—Russian Technological University, Vernadsky pr., 86, 119571 Moscow, Russia

2. N. N. Semenov Federal Research Center for Chemical Physics, Russian Academy of Sciences, Kosygin St., 4, 119991 Moscow, Russia

3. N. N. Blokhin National Medical Research Center of Oncology, Ministry of Health of Russia, Kashirskoe Highway, 24, 115522 Moscow, Russia

4. Department of Medical Chemistry and Toxicology, Pirogov National Research Medical University, Ministry of Health of Russia, Ostrovityanova St., 1, 117997 Moscow, Russia

5. Institute of Chemistry, Saint Petersburg State University, Universitetskaya nab. 7–9, 199034 Saint Petersburg, Russia

6. Research Institute of Chemistry, Peoples’ Friendship University of Russia (RUDN University), Miklukho-Maklaya St., 6, 117198 Moscow, Russia

7. Emanuel Institute of Biochemical Physics, Russian Academy of Sciences, Kosygina St., 4, 119334 Moscow, Russia

Abstract

Photodynamic therapy (PDT) in oncology is characterized by low invasiveness, minimal side effects, and little tissue scarring. Increasing the selectivity of PDT agents toward a cellular target is a new approach intended to improve this method. This study is devoted to the design and synthesis of a new conjugate based on meso-arylporphyrin with a low-molecular-weight tyrosine kinase inhibitor, Erlotinib. A nano-formulation based on Pluronic F127 micelles was obtained and characterized. The photophysical and photochemical properties and biological activity of the studied compounds and their nano-formulation were studied. A significant, 20–40-fold difference between the dark and photoinduced activity was achieved for the conjugate nanomicelles. After irradiation, the studied conjugate nanomicelles were 1.8 times more toxic toward the EGFR-overexpressing cell line MDA-MB-231 compared to the conditionally normal NKE cells. The IC50 was 0.073 ± 0.014 μM for the MDA-MB-231 cell line and 0.13 ± 0.018 μM for NKE cells after irradiation for the target conjugate nanomicelles.

Funder

Russian Science Foundation

Publisher

MDPI AG

Subject

Pharmaceutical Science

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