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New hybrid radio-fluorescent probes [(131)I]-BPF-01 and [(131)I]-BPF-02 for visualisation of cancer cells: Synthesis and preliminary in vitro and ex vivo evaluations
We synthesised and biologically evaluated two new hybrid probes [(131)I]BPF-01 and [(131)I]BPF-02 which were built from three structural entities: benzothiazole-phenyl, fluorescein isothiocyanate (FITC), and iodine-131. These probes were designed for potential applications in assisting surgical proc...
Autores principales: | , , , , , , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Elsevier
2023
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10582398/ https://www.ncbi.nlm.nih.gov/pubmed/37860547 http://dx.doi.org/10.1016/j.heliyon.2023.e20710 |
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author | Wongso, Hendris Kurniawan, Ahmad Forentin, Alfian M. Susilo, Veronika Y. Setiadi, Yanuar Mahendra, Isa Febrian, Muhamad B. Rosdianto, Aziiz M. Setiawan, Iwan Goenawan, Hanna Susianti, Susianti Supratman, Unang Widyasari, Eva M. Wibawa, Teguh H.A. Sriyani, Maula E. Halimah, Iim Lesmana, Ronny |
author_facet | Wongso, Hendris Kurniawan, Ahmad Forentin, Alfian M. Susilo, Veronika Y. Setiadi, Yanuar Mahendra, Isa Febrian, Muhamad B. Rosdianto, Aziiz M. Setiawan, Iwan Goenawan, Hanna Susianti, Susianti Supratman, Unang Widyasari, Eva M. Wibawa, Teguh H.A. Sriyani, Maula E. Halimah, Iim Lesmana, Ronny |
author_sort | Wongso, Hendris |
collection | PubMed |
description | We synthesised and biologically evaluated two new hybrid probes [(131)I]BPF-01 and [(131)I]BPF-02 which were built from three structural entities: benzothiazole-phenyl, fluorescein isothiocyanate (FITC), and iodine-131. These probes were designed for potential applications in assisting surgical procedures of solid cancers. The cytotoxicity study demonstrated that fluorescent probes BPF-01 (31.23 μg/mL) and BPF-02 (250 μg/mL) were relatively not toxic to normal immortalized human keratinocytes (HaCaT) cells, as indicated by the percentage of cell survival above 50 %. Furthermore, both probes displayed low to moderate anticancer activity against the breast cancer cells (MDA-MB-231) and prostate cancer cells (LNCaP and DU-145). The probe BPF-01 apparently showed an accumulation in the tumour tissues, as suggested by ex vivo fluorescence examinations. In addition, the cellular uptake study suggests that hybrid probe [(131)I]-BPF-01 was potentially accumulated in the MCF-7 cell line with the highest uptake of 16.11 ± 1.52 % after 2 h of incubation, approximately 50-fold higher than the accumulation of iodine-131 (control). The magnetic bead assay suggests that [(131)I]-BPF-02 and [(131)I]-BPF-02 showed a promising capability to interact with translocator protein 18 kDa (TSPO). Moreover, the computational data showed that the binding scores for ligands 7–8, BPF-01 and BPF-02, and [(131)I]-BPF-01 and [(131)I]-BPF-02 in the TSPO were considerably high. Accordingly, fluorescent probes BPF-01 and BPF-02, and hybrid probes [(131)I]BPF-01 and [(131)I]BPF-02 can be further developed for targeting cancer cells during intraoperative tumour surgery. |
format | Online Article Text |
id | pubmed-10582398 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | Elsevier |
record_format | MEDLINE/PubMed |
spelling | pubmed-105823982023-10-19 New hybrid radio-fluorescent probes [(131)I]-BPF-01 and [(131)I]-BPF-02 for visualisation of cancer cells: Synthesis and preliminary in vitro and ex vivo evaluations Wongso, Hendris Kurniawan, Ahmad Forentin, Alfian M. Susilo, Veronika Y. Setiadi, Yanuar Mahendra, Isa Febrian, Muhamad B. Rosdianto, Aziiz M. Setiawan, Iwan Goenawan, Hanna Susianti, Susianti Supratman, Unang Widyasari, Eva M. Wibawa, Teguh H.A. Sriyani, Maula E. Halimah, Iim Lesmana, Ronny Heliyon Research Article We synthesised and biologically evaluated two new hybrid probes [(131)I]BPF-01 and [(131)I]BPF-02 which were built from three structural entities: benzothiazole-phenyl, fluorescein isothiocyanate (FITC), and iodine-131. These probes were designed for potential applications in assisting surgical procedures of solid cancers. The cytotoxicity study demonstrated that fluorescent probes BPF-01 (31.23 μg/mL) and BPF-02 (250 μg/mL) were relatively not toxic to normal immortalized human keratinocytes (HaCaT) cells, as indicated by the percentage of cell survival above 50 %. Furthermore, both probes displayed low to moderate anticancer activity against the breast cancer cells (MDA-MB-231) and prostate cancer cells (LNCaP and DU-145). The probe BPF-01 apparently showed an accumulation in the tumour tissues, as suggested by ex vivo fluorescence examinations. In addition, the cellular uptake study suggests that hybrid probe [(131)I]-BPF-01 was potentially accumulated in the MCF-7 cell line with the highest uptake of 16.11 ± 1.52 % after 2 h of incubation, approximately 50-fold higher than the accumulation of iodine-131 (control). The magnetic bead assay suggests that [(131)I]-BPF-02 and [(131)I]-BPF-02 showed a promising capability to interact with translocator protein 18 kDa (TSPO). Moreover, the computational data showed that the binding scores for ligands 7–8, BPF-01 and BPF-02, and [(131)I]-BPF-01 and [(131)I]-BPF-02 in the TSPO were considerably high. Accordingly, fluorescent probes BPF-01 and BPF-02, and hybrid probes [(131)I]BPF-01 and [(131)I]BPF-02 can be further developed for targeting cancer cells during intraoperative tumour surgery. Elsevier 2023-10-05 /pmc/articles/PMC10582398/ /pubmed/37860547 http://dx.doi.org/10.1016/j.heliyon.2023.e20710 Text en © 2023 The Authors. Published by Elsevier Ltd. https://creativecommons.org/licenses/by-nc-nd/4.0/This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/). |
spellingShingle | Research Article Wongso, Hendris Kurniawan, Ahmad Forentin, Alfian M. Susilo, Veronika Y. Setiadi, Yanuar Mahendra, Isa Febrian, Muhamad B. Rosdianto, Aziiz M. Setiawan, Iwan Goenawan, Hanna Susianti, Susianti Supratman, Unang Widyasari, Eva M. Wibawa, Teguh H.A. Sriyani, Maula E. Halimah, Iim Lesmana, Ronny New hybrid radio-fluorescent probes [(131)I]-BPF-01 and [(131)I]-BPF-02 for visualisation of cancer cells: Synthesis and preliminary in vitro and ex vivo evaluations |
title | New hybrid radio-fluorescent probes [(131)I]-BPF-01 and [(131)I]-BPF-02 for visualisation of cancer cells: Synthesis and preliminary in vitro and ex vivo evaluations |
title_full | New hybrid radio-fluorescent probes [(131)I]-BPF-01 and [(131)I]-BPF-02 for visualisation of cancer cells: Synthesis and preliminary in vitro and ex vivo evaluations |
title_fullStr | New hybrid radio-fluorescent probes [(131)I]-BPF-01 and [(131)I]-BPF-02 for visualisation of cancer cells: Synthesis and preliminary in vitro and ex vivo evaluations |
title_full_unstemmed | New hybrid radio-fluorescent probes [(131)I]-BPF-01 and [(131)I]-BPF-02 for visualisation of cancer cells: Synthesis and preliminary in vitro and ex vivo evaluations |
title_short | New hybrid radio-fluorescent probes [(131)I]-BPF-01 and [(131)I]-BPF-02 for visualisation of cancer cells: Synthesis and preliminary in vitro and ex vivo evaluations |
title_sort | new hybrid radio-fluorescent probes [(131)i]-bpf-01 and [(131)i]-bpf-02 for visualisation of cancer cells: synthesis and preliminary in vitro and ex vivo evaluations |
topic | Research Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10582398/ https://www.ncbi.nlm.nih.gov/pubmed/37860547 http://dx.doi.org/10.1016/j.heliyon.2023.e20710 |
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