Topical Collection "Antitumor Potential and Side Effects of Natural and Synthetic Compounds"

Editor

Prof. Dr. Hiroshi Sakagami
E-Mail Website
Guest Editor
Meikai University Research Institute of Odontology (M-RIO), 1-1 Keyakidai, Sakado, Saitama 350-0283, Japan
Interests: informatics; information network; pharmacy; biological pharmacy; basic medicine; general pharmacology; boundary medicine; laboratory medicine; dentistry
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Topical Collection Information

Dear Colleagues,

Although many antitumor substances have been isolated from the natural kingdom, most authors have shown their cytotoxicity against malignant cells, but not against non-malignant cells. Recently, synthetic compounds of chromones and α,β-unsaturated ketones have shown very high antitumor potential, sometimes exceeding that of anticancer drugs.

This Topical Collection calls for papers exploring the antitumor potential of natural and synthetic compounds against both malignant and non-malignant cells and their adverse effects. The papers that focus on the exploration of preparative or synthetic methods and the elucidation of action mechanisms are also within the scope of this issue.

Prof. Dr. Hiroshi Sakagami
Guest Editor

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Published Papers (2 papers)

2021

Article
Re-Evaluation of Chemotherapeutic Potential of Pyoktanin Blue
Medicines 2021, 8(7), 33; https://0-doi-org.brum.beds.ac.uk/10.3390/medicines8070033 - 22 Jun 2021
Viewed by 1246
Abstract
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. [...] Read more.
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. Full article
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Article
Design, Syntheses, and Bioevaluations of Some Novel N2-Acryloylbenzohydrazides as Chemostimulants and Cytotoxic Agents
Medicines 2021, 8(6), 27; https://0-doi-org.brum.beds.ac.uk/10.3390/medicines8060027 - 03 Jun 2021
Viewed by 1545
Abstract
A series of novel N2-acryloylhydrazides 1a–m and a related series of compounds 6a–c were prepared as potential chemostimulants. In general, these compounds are cytotoxic to human HCT 116 colon cancer cells, as well as human MCF-7 and MDA-MB-231 breast cancer cell [...] Read more.
A series of novel N2-acryloylhydrazides 1a–m and a related series of compounds 6a–c were prepared as potential chemostimulants. In general, these compounds are cytotoxic to human HCT 116 colon cancer cells, as well as human MCF-7 and MDA-MB-231 breast cancer cell lines. A representative compound N1-(3,4-dimethoxyphenylcarbonyl)-N2-acryloylhydrazine 1m sensitized HCT 116 cells to the potent antineoplastic agent 3,5-bis(benzylidene)-4-piperidone 2a, and also to 5-fluorouracil. A series of compounds was prepared that incorporated some of the molecular features of 2a and related compounds with various N2-acryloylhydrazides in series 1. These compounds are potent cytotoxins. Two modes of action of representative compounds are the lowering of mitochondrial membrane potential and increasing the concentration of reactive oxygen species. Full article
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Figure 1

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