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Open AccessArticle

Tumor Size-Dependent Anticancer Efficacy of Chlorin Derivatives for Photodynamic Therapy

by Ji-Eun Chang 1,†, Yang Liu 2,†, Tae Heon Lee 2, Woo Kyoung Lee 2, Il Yoon 2,* and Kwhanmien Kim 1,3,*
1
Department of Thoracic and Cardiovascular Surgery, Seoul National University Bundang Hospital, Seongnam-si, Gyeonggi-do 13620, Korea
2
Nano Manufacturing Institute, School of Nanoscience and Engineering, Inje University, Gimhae 50834, Korea
3
Department of Thoracic and Cardiovascular Surgery, Seoul National University College of Medicine, Seoul 03080, Korea
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Int. J. Mol. Sci. 2018, 19(6), 1596; https://doi.org/10.3390/ijms19061596
Received: 2 May 2018 / Revised: 18 May 2018 / Accepted: 26 May 2018 / Published: 29 May 2018
(This article belongs to the Section Molecular Pathology, Diagnostics, and Therapeutics)
Photodynamic therapy (PDT) with a suitable photosensitizer molecule is a promising anticancer treatment. We evaluated two chlorin molecules as potential photosensitizers, methyl pyropheophorbide a (MPPa) and N-methoxyl purpurinimide (NMPi), against A549 human lung adenocarcinoma cells in vitro as well as in A549 tumor-bearing mice in vivo. Cell viability, microscopy, and fluorescence-activated cell sorting (FACS) analyses were performed for the in vitro studies. MPPa and NMPi showed high phototoxicity in vitro, which was dependent on the concentration of the photosensitizers as well as the light irradiation time. In the animal study, tumor volume change, tumor surface alterations, and hematoxylin & eosin (H&E) and terminal deoxyribonucleotidyl transferse-mediated dUTP nick-end labelling (TUNEL) staining analyses were performed and compared between small (tumor volume of <50 mm3) and large (tumor volume of >50 mm3) size of initial tumors. MPPa and NMPi showed high anticancer efficacy against small-size tumors, indicating that early treatment with PDT is effective. Especially, repeated two times PDT with NMPi allowed almost complete eradication against small-size tumors. However, MPPa and NMPi were not effective against large-size tumors. In conclusion, the two chlorin derivatives, MPPa and NMPi, show good anticancer efficacy as promising photosensitizers for PDT in vitro and in vivo. Moreover, their activity in vivo was significantly dependent on the initial tumor size in mice, which confirms the importance of early cancer treatment. View Full-Text
Keywords: cancer treatment; chlorin; photodynamic therapy (PDT); photosensitizer; tumor size cancer treatment; chlorin; photodynamic therapy (PDT); photosensitizer; tumor size
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MDPI and ACS Style

Chang, J.-E.; Liu, Y.; Lee, T.H.; Lee, W.K.; Yoon, I.; Kim, K. Tumor Size-Dependent Anticancer Efficacy of Chlorin Derivatives for Photodynamic Therapy. Int. J. Mol. Sci. 2018, 19, 1596.

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