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Article

Re-Evaluation of Chemotherapeutic Potential of Pyoktanin Blue

1
Research Institute of Odontology (M-RIO), Meikai University, 1-1 Keyakidai, Sakado, Saitama 350-0283, Japan
2
Division of Endodontics and Operative Dentistry, School of Dentistry, Meikai University, 1-1 Keyakidai, Sakado, Saitama 350-0283, Japan
3
Division of Pharmacology, Meikai University School of Dentistry, 1-1 Keyakidai, Sakado, Saitama 350-0283, Japan
4
Department of Oral and Maxillofacial Surgery, Saitama Medical Center, Saitama 350-8550, Japan
5
Department of Microbiology, St. Marianna University School of Medicine, 2-16-1 Sugao, Miyamae-ku, Kawasaki 216-8511, Japan
6
Laboratory of Microbiology, Showa Pharmaceutical University, 3-3165 Higashi-Tamagawagakuen, Machida, Tokyo 194-8543, Japan
7
Graduate School of Health Sciences, Showa University, 1-5-8 Hatanodai, Shinagawa-ku, Tokyo 142-8555, Japan
*
Author to whom correspondence should be addressed.
Academic Editor: Makoto Endo
Received: 17 May 2021 / Revised: 4 June 2021 / Accepted: 15 June 2021 / Published: 22 June 2021
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 CC50 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 CC50 (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. View Full-Text
Keywords: pyoktanin; anticancer activity; oral cancer; apoptosis; chemotherapeutic index; caspase-3; subG1 accumulation; anti-HIV; anti-HSV pyoktanin; anticancer activity; oral cancer; apoptosis; chemotherapeutic index; caspase-3; subG1 accumulation; anti-HIV; anti-HSV
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MDPI and ACS Style

Sakagami, H.; Furukawa, T.; Satoh, K.; Amano, S.; Iijima, Y.; Koshikawa, T.; Asai, D.; Fukuchi, K.; Takemura, H.; Kanamoto, T.; Yokose, S. Re-Evaluation of Chemotherapeutic Potential of Pyoktanin Blue. Medicines 2021, 8, 33. https://0-doi-org.brum.beds.ac.uk/10.3390/medicines8070033

AMA Style

Sakagami H, Furukawa T, Satoh K, Amano S, Iijima Y, Koshikawa T, Asai D, Fukuchi K, Takemura H, Kanamoto T, Yokose S. Re-Evaluation of Chemotherapeutic Potential of Pyoktanin Blue. Medicines. 2021; 8(7):33. https://0-doi-org.brum.beds.ac.uk/10.3390/medicines8070033

Chicago/Turabian Style

Sakagami, Hiroshi, Toshiko Furukawa, Keitaro Satoh, Shigeru Amano, Yosuke Iijima, Takuro Koshikawa, Daisuke Asai, Kunihiko Fukuchi, Hiromu Takemura, Taisei Kanamoto, and Satoshi Yokose. 2021. "Re-Evaluation of Chemotherapeutic Potential of Pyoktanin Blue" Medicines 8, no. 7: 33. https://0-doi-org.brum.beds.ac.uk/10.3390/medicines8070033

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