Cargando…

Re-Evaluation of Chemotherapeutic Potential of Pyoktanin Blue

Background: Pyoktanin blue (PB) is used for staining tissues and cells, and it is applied in photodynamic therapy due to its potent bactericidal activity. However, clinical application of PB as an antiviral and antitumor agent has been limited due to its potent toxicity. For clinical application, th...

Descripción completa

Detalles Bibliográficos
Autores principales: Sakagami, Hiroshi, Furukawa, Toshiko, Satoh, Keitaro, Amano, Shigeru, Iijima, Yosuke, Koshikawa, Takuro, Asai, Daisuke, Fukuchi, Kunihiko, Takemura, Hiromu, Kanamoto, Taisei, Yokose, Satoshi
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8305689/
https://www.ncbi.nlm.nih.gov/pubmed/34206186
http://dx.doi.org/10.3390/medicines8070033
_version_ 1783727633040670720
author Sakagami, Hiroshi
Furukawa, Toshiko
Satoh, Keitaro
Amano, Shigeru
Iijima, Yosuke
Koshikawa, Takuro
Asai, Daisuke
Fukuchi, Kunihiko
Takemura, Hiromu
Kanamoto, Taisei
Yokose, Satoshi
author_facet Sakagami, Hiroshi
Furukawa, Toshiko
Satoh, Keitaro
Amano, Shigeru
Iijima, Yosuke
Koshikawa, Takuro
Asai, Daisuke
Fukuchi, Kunihiko
Takemura, Hiromu
Kanamoto, Taisei
Yokose, Satoshi
author_sort Sakagami, Hiroshi
collection PubMed
description Background: Pyoktanin blue (PB) is used for staining tissues and cells, and it is applied in photodynamic therapy due to its potent bactericidal activity. However, clinical application of PB as an antiviral and antitumor agent has been limited due to its potent toxicity. For clinical application, the antitumor and antiviral activity as well as the neurotoxicity of PB were re-evaluated with a chemotherapeutic index. Methods: Tumor-specificity (TS) was determined by the ratio of CC(50) against normal oral cells/oral squamous cell carcinoma (OSCC); neurotoxicity by that of normal oral/neuronal cells; antiviral activity by that of mock-infected/virus-infected cells; and potency-selectivity expression (PSE) by dividing TS by CC(50) (OSCC). Results: Antitumor activity of PB (assessed by TS and PSE) was comparable with that of DXR and much higher than that of 5-FU and melphalan. PB induced caspase-3 activation and subG1 cell accumulation in an OSCC cell line (Ca9-22). PB and anticancer drugs showed comparable cytotoxicity against both neuronal cells and OSCC cell lines. PB showed no detectable anti-HIV/HSV activity, in contrast to reverse transferase inhibitors, sulfated glucans, and alkaline extract of leaves of S.P. Conclusions: PB showed first-class anticancer activity and neurotoxicity, suggesting the importance of establishing the safe treatment schedule.
format Online
Article
Text
id pubmed-8305689
institution National Center for Biotechnology Information
language English
publishDate 2021
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-83056892021-07-25 Re-Evaluation of Chemotherapeutic Potential of Pyoktanin Blue Sakagami, Hiroshi Furukawa, Toshiko Satoh, Keitaro Amano, Shigeru Iijima, Yosuke Koshikawa, Takuro Asai, Daisuke Fukuchi, Kunihiko Takemura, Hiromu Kanamoto, Taisei Yokose, Satoshi Medicines (Basel) Article Background: Pyoktanin blue (PB) is used for staining tissues and cells, and it is applied in photodynamic therapy due to its potent bactericidal activity. However, clinical application of PB as an antiviral and antitumor agent has been limited due to its potent toxicity. For clinical application, the antitumor and antiviral activity as well as the neurotoxicity of PB were re-evaluated with a chemotherapeutic index. Methods: Tumor-specificity (TS) was determined by the ratio of CC(50) against normal oral cells/oral squamous cell carcinoma (OSCC); neurotoxicity by that of normal oral/neuronal cells; antiviral activity by that of mock-infected/virus-infected cells; and potency-selectivity expression (PSE) by dividing TS by CC(50) (OSCC). Results: Antitumor activity of PB (assessed by TS and PSE) was comparable with that of DXR and much higher than that of 5-FU and melphalan. PB induced caspase-3 activation and subG1 cell accumulation in an OSCC cell line (Ca9-22). PB and anticancer drugs showed comparable cytotoxicity against both neuronal cells and OSCC cell lines. PB showed no detectable anti-HIV/HSV activity, in contrast to reverse transferase inhibitors, sulfated glucans, and alkaline extract of leaves of S.P. Conclusions: PB showed first-class anticancer activity and neurotoxicity, suggesting the importance of establishing the safe treatment schedule. MDPI 2021-06-22 /pmc/articles/PMC8305689/ /pubmed/34206186 http://dx.doi.org/10.3390/medicines8070033 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Sakagami, Hiroshi
Furukawa, Toshiko
Satoh, Keitaro
Amano, Shigeru
Iijima, Yosuke
Koshikawa, Takuro
Asai, Daisuke
Fukuchi, Kunihiko
Takemura, Hiromu
Kanamoto, Taisei
Yokose, Satoshi
Re-Evaluation of Chemotherapeutic Potential of Pyoktanin Blue
title Re-Evaluation of Chemotherapeutic Potential of Pyoktanin Blue
title_full Re-Evaluation of Chemotherapeutic Potential of Pyoktanin Blue
title_fullStr Re-Evaluation of Chemotherapeutic Potential of Pyoktanin Blue
title_full_unstemmed Re-Evaluation of Chemotherapeutic Potential of Pyoktanin Blue
title_short Re-Evaluation of Chemotherapeutic Potential of Pyoktanin Blue
title_sort re-evaluation of chemotherapeutic potential of pyoktanin blue
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8305689/
https://www.ncbi.nlm.nih.gov/pubmed/34206186
http://dx.doi.org/10.3390/medicines8070033
work_keys_str_mv AT sakagamihiroshi reevaluationofchemotherapeuticpotentialofpyoktaninblue
AT furukawatoshiko reevaluationofchemotherapeuticpotentialofpyoktaninblue
AT satohkeitaro reevaluationofchemotherapeuticpotentialofpyoktaninblue
AT amanoshigeru reevaluationofchemotherapeuticpotentialofpyoktaninblue
AT iijimayosuke reevaluationofchemotherapeuticpotentialofpyoktaninblue
AT koshikawatakuro reevaluationofchemotherapeuticpotentialofpyoktaninblue
AT asaidaisuke reevaluationofchemotherapeuticpotentialofpyoktaninblue
AT fukuchikunihiko reevaluationofchemotherapeuticpotentialofpyoktaninblue
AT takemurahiromu reevaluationofchemotherapeuticpotentialofpyoktaninblue
AT kanamototaisei reevaluationofchemotherapeuticpotentialofpyoktaninblue
AT yokosesatoshi reevaluationofchemotherapeuticpotentialofpyoktaninblue