Phenylthiourea-Conjugated BODIPY as an Efficient Photosensitizer for Tyrosinase-Positive Melanoma-Targeted Photodynamic Therapy

Eugeine Jung, Inseob Shim, Jusung An, Myung Sun Ji, Paramesh Jangili, Sung Gil Chi, Jong Seung Kim

Research output: Contribution to journalReview articlepeer-review

11 Citations (Scopus)

Abstract

Melanoma is the most threatening form of metastatic skin cancer that develops from melanocytes and causes a large majority of deaths due to poor therapeutic prognosis. It has significant limitations in treatment because it shows great resistance to chemotherapy, radiotherapy, and other therapeutic methods. A noninvasive and clinically accepted therapeutic modality, photodynamic therapy (PDT), is a promising treatment option, but it is limitedly applied for melanoma skin cancer treatment. This is because most of the photosensitizers are unlikely to be expected to have a remarkable effect on melanoma due to drug efflux by melanin pigmentation and intrinsic antioxidant defense mechanisms. Moreover, melanin is a dominant absorber in the spectral region of 500-600 nm that can cause the decreased photoreaction efficiency of photosensitizers. Herein, to overcome these drawbacks, we have developed a phenylthiourea-conjugated BODIPY photosensitizer (PTUBDP) for tyrosinase-positive melanoma-targeted PDT. In light of our results, it exhibited an enhanced cytotoxic efficacy compared to BDP, a parallel PDT agent that absence of phenylthiourea unit. PTUBDP shows outstanding effects of increased oxidative stress by an enhanced cellular uptake of the tyrosinase positive melanoma cell line (B16F10). This work presents increased therapeutic efficacy through the combined therapeutic approach, enabling enhanced reactive oxygen species (ROS) generation as well as overcoming the critical limitations of melanoma.

Original languageEnglish
Pages (from-to)2120-2127
Number of pages8
JournalACS Applied Bio Materials
Volume4
Issue number3
DOIs
Publication statusPublished - 2021 Mar 15

Bibliographical note

Funding Information:
This work was supported by the National Research Foundation of Korea (NRF) funded by the Ministry of Science and ICT (CRI Project Nos. 2018R1A3B1052702 and 2019M3E5D1A01068998, J.S.K.) and (No. 2018R1A2A1A05020236 to S.-G.C.).

Publisher Copyright:
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Keywords

  • BODIPY
  • melanoma
  • phenylthiourea
  • photodynamic therapy
  • tyrosinase

ASJC Scopus subject areas

  • General Chemistry
  • Biomaterials
  • Biomedical Engineering
  • Biochemistry, medical

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