(3,3’-Methylene)bis-2-hydroxy-1,4-naphthoquinones induce cytotoxicity against DU145 and PC3 cancer cells by inhibiting cell viability and promoting cell cycle arrest

Freitas, Paula Priscilla de; Ribeiro, Ruan Stevan de Almeida; Guimarães, Isabella dos Santos; Moreira, Caroline S.; Rocha, David R. da; Silva, Fernando de Carvalho da; Ferreira, Vı́tor F.; Gimba, Etel Rodrigues Pereira

doi:10.1007/s11033-021-06406-w

Cited by 4 publications

(2 citation statements)

References 44 publications

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“…In this research, the apoptosis induced by CNN1 was confirmed by phosphatidylserine externalization in K-562 (p < 0.001) and FEPS (p < 0.001) cell lines, similar findings were reported on in vitro models of breast cancer [56], lung adenocarcinoma [57], and colon carcinoma [33]. Apoptosis deregulation is a remarkable hallmark of cancer, enabling cancer cells to develop MDR phenotype, additionally, this feature had been highlighted as the major cause of chemotherapy failure in CML [58].…”

Section: Discussionsupporting

confidence: 88%

“…The naphthoquinones present different pharmacological properties, among them anticancer action, antifungal, antibacterial and antiviral activities, as well as allelopathic activities [ 30 , 31 , 32 , 33 ]. There are many studies that describe the effect of naphthoquinones, or its analogs, in several type of tumors and demonstrate an in vitro and in vivo chemotherapeutic potential of these compounds [ 34 , 35 , 36 ].…”

Section: Discussionmentioning

confidence: 99%

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1,4-Naphthoquinone (CNN1) Induces Apoptosis through DNA Damage and Promotes Upregulation of H2AFX in Leukemia Multidrug Resistant Cell Line

Portilho

Silva

Bezerra

et al. 2022

IJMS

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The multidrug resistance (MDR) phenotype is one of the major obstacles in the treatment of chronic myeloid leukemia (CML) in advantage stages such as blast crisis. In this scenario, more patients develop resistance mechanisms during the course of the disease, making tyrosine kinase inhibitors (TKIs) target therapies ineffective. Therefore, the aim of the study was to examine the pharmacological role of CNN1, a para-naphthoquinone, in a leukemia multidrug resistant cell line. First, the in vitro cytotoxic activity of Imatinib Mesylate (IM) in K-562 and FEPS cell lines was evaluated. Subsequently, membrane integrity and mitochondrial membrane potential assays were performed to assess the cytotoxic effects of CNN1 in K-562 and FEPS cell lines, followed by cell cycle, alkaline comet assay and annexin V-Alexa Fluor® 488/propidium iodide assays (Annexin/PI) using flow cytometry. RT-qPCR was used to evaluate the H2AFX gene expression. The results demonstrate that CNN1 was able to induce apoptosis, cell membrane rupture and mitochondrial membrane depolarization in leukemia cell lines. In addition, CNN1 also induced genotoxic effects and caused DNA fragmentation, cell cycle arrest at the G2/M phase in leukemia cells. No genotoxicity was observed on peripheral blood mononuclear cells (PBMC). Additionally, CNN1 increased mRNA levels of H2AFX. Therefore, CNN1 presented anticancer properties against leukemia multidrug resistant cell line being a potential anticancer agent for the treatment of resistant CML.

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Section: Discussionsupporting

confidence: 88%

Section: Discussionmentioning

confidence: 99%

1,4-Naphthoquinone (CNN1) Induces Apoptosis through DNA Damage and Promotes Upregulation of H2AFX in Leukemia Multidrug Resistant Cell Line

Portilho

Silva

Bezerra

et al. 2022

IJMS

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Molecular biological mechanism of action in cancer therapies: Juglone and its derivatives, the future of development

Tang

Chu

et al. 2022

Biomedicine & Pharmacotherapy

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8-Methoxy-α-lapachone and lawsone: antiproliferative effects on bladder tumour cells

Ferreira,

Lima,

Sousa

et al. 2023

Natural Product Research

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Quinones are chemical compounds produced from the oxidation of phenols. Among the quinones, naphthoquinones stand out as potential antitumor agents. Bladder tumor is the tenth most diagnosed in the world. Based on this, using a urothelial carcinoma cell line (T24), two naphthoquinones had their cytotoxicity tested by the MTT colorimetric method and were submitted to assays of clonogenic survival, morphology, cell cycle, cell migration and species reactive oxygen. The results showed 8-methoxy-α-lapachone and lausone presented selectivity indexes (19.5 and 28.0, respectively) for T24 cells. Moreover, the two naphthoquinones reduced the cell viability, interfered with the process of cell migration, changed the cell cycle kinectics and induced the production of species reactive oxygen (ROS). Additionaly, 8-methoxy-αlapachone altered the morphology of the cells. In conclusion, the studied naphthoquinones showed potential antiproliferative effects in bladder cancer cells, interfering in cellular processes, possibly through oxidative stress.

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(3,3’-Methylene)bis-2-hydroxy-1,4-naphthoquinones induce cytotoxicity against DU145 and PC3 cancer cells by inhibiting cell viability and promoting cell cycle arrest

Cited by 4 publications

References 44 publications

1,4-Naphthoquinone (CNN1) Induces Apoptosis through DNA Damage and Promotes Upregulation of H2AFX in Leukemia Multidrug Resistant Cell Line

1,4-Naphthoquinone (CNN1) Induces Apoptosis through DNA Damage and Promotes Upregulation of H2AFX in Leukemia Multidrug Resistant Cell Line

Molecular biological mechanism of action in cancer therapies: Juglone and its derivatives, the future of development

8-Methoxy-α-lapachone and lawsone: antiproliferative effects on bladder tumour cells

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