5,15-Diphenyl-7-oxobenzochlorins. Novel long-wavelength absorbing photosensitizers for photodynamic therapy

Photodynamic therapy (PDT) represents a promising method for treatment of cancerous tumors. The chemical and physical properties of used photosensitizer (PS) play key roles in the treatment efficacy. In this study, a novel PS, 5,10,15,20-tetrakis((5-dipropylamino)pentyl)-chlorin (TDPC) which displayed a characteristic long wavelength absorption peak at 650 nm were synthesized. It also shows a singlet oxygen generation rate of 4.257 min-1. Generally, TDPC is localized in mitochondria and nucleus of cell. After light irradiation with 650 nm laser, it can kill many types of cell, in addition, TDPC–PDT can destroy ECA-109 tumor in nude mice and a necrotic scab was formed eventually. The expression levels of many genes which regulated cell growth and apoptosis were determined by RT-PCR following TDPC–PDT. The results showed that it either increased or decreased, among which, the expression level of TNFSF13, a member of tumor necrosis factor superfamily, increased significantly. In general, TDPC is an effective antitumor PS in vitro and in vivo and is worthy of further study as a new drug candidate. TNFSF13 will be an important molecular target for the discovery of new PSs.

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Rationally Designed Long-Wavelength Absorbing Ru(II) Polypyridyl Complexes as Photosensitizers for Photodynamic Therapy

Journal of the American Chemical Society ◽

10.1021/jacs.9b13620 ◽

2020 ◽

Vol 142 (14) ◽

pp. 6578-6587 ◽

Cited By ~ 18

Author(s):

Johannes Karges ◽

Franz Heinemann ◽

Marta Jakubaszek ◽

Federica Maschietto ◽

Chloé Subecz ◽

...

Keyword(s):

Photodynamic Therapy ◽

Polypyridyl Complexes ◽

Long Wavelength

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Enhanced Photodynamic Anticancer Activities of Multifunctional Magnetic Nanoparticles (Fe3O4) Conjugated with Chlorin e6 and Folic Acid in Prostate and Breast Cancer Cells

Nanomaterials ◽

10.3390/nano8090722 ◽

2018 ◽

Vol 8 (9) ◽

pp. 722 ◽

Cited By ~ 12

Author(s):

Kyong-Hoon Choi ◽

Ki Nam ◽

Guangsup Cho ◽

Jin-Seung Jung ◽

Bong Park

Keyword(s):

Photodynamic Therapy ◽

Folic Acid ◽

Magnetic Nanoparticles ◽

Cancer Cells ◽

Biological Effects ◽

Chlorin E6 ◽

Deep Penetration ◽

Promising Alternative ◽

Long Wavelength

Photodynamic therapy (PDT) is a promising alternative to conventional cancer treatment methods. Nonetheless, improvement of in vivo light penetration and cancer cell-targeting efficiency remain major challenges in clinical photodynamic therapy. This study aimed to develop multifunctional magnetic nanoparticles conjugated with a photosensitizer (PS) and cancer-targeting molecules via a simple surface modification process for PDT. To selectively target cancer cells and PDT functionality, core magnetic (Fe3O4) nanoparticles were covalently bound with chlorin e6 (Ce6) as a PS and folic acid (FA). When irradiated with a 660-nm long-wavelength light source, the Fe3O4-Ce6-FA nanoparticles with good biocompatibility exerted marked anticancer effects via apoptosis, as confirmed by analyzing the translocation of the plasma membrane, nuclear fragmentation, activities of caspase-3/7 in prostate (PC-3) and breast (MCF-7) cancer cells. Ce6, used herein as a PS, is thus more useful for PDT because of its ability to produce a high singlet oxygen quantum yield, which is owed to deep penetration by virtue of its long-wavelength absorption band; however, further in vivo studies are required to verify its biological effects for clinical applications.

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