Chemosensitizer effect of cisplatin-treated bladder cancer cells by phenazine-5,10-dioxides

Hernández, Paola; Alem, Diego; Nieves, Marcos; Cerecetto, Hugo; González, Mercedes; Martínez‐López, Wilner; Lavaggi, María Laura

doi:10.1016/j.etap.2019.03.015

Cited by 8 publications

(11 citation statements)

References 25 publications

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“…Moreover, HDAC3 inhibitor has been found to hold strong proapoptosis ability and might suppress cancer stemness [5][6][7]10]. Some evidence has also indicated that HDACi might increase the therapeutic effect of chemotherapy [13]. HDAC inhibitors, e.g., SAHA for cutaneous T-lymphocyte tumors, Mocetinostat for bladder cancer, and Panobinostat for multiple myeloma, were approved by the U.S. FDA [14, Fig.…”

Section: Discussionmentioning

confidence: 99%

Valeric acid acts as a novel HDAC3 inhibitor against prostate cancer

Han

Yang

et al. 2022

Med Oncol

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Prostate cancer is the second cause of cancer-related deaths in men worldwide, and new agents for curing the disease are still needed. In this study, we theoretically and experimentally demonstrated that valeric acid (VA) was a HDAC inhibitor, and anti-cancer efficacy of VA in prostate cancer cells was also observed using either 2D or 3D culture systems. VA was cytotoxic for prostate cancer cells but low toxic to normal cells. VA significantly inhibited E2F1/E2F3 expression but increased CASP3 activity. In vivo mouse models further showed its anti-cancer activity and potential property of chemosensitizer with promoting apoptosis. The findings suggest that VA acts as a HDAC3 inhibitor with anti-cancer effect on prostate cancer by regulating E2F1/E2F3/CASP3 axis.

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Section: Discussionmentioning

confidence: 99%

Valeric acid acts as a novel HDAC3 inhibitor against prostate cancer

Han

Yang

et al. 2022

Med Oncol

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“…[56] The combination of PDO derivatives with an incorporated benzyl group, e. g., 7(8)-bromo-2-(4-nitrobenzyloxy)-PDO, 7(8)-bromo-2-(4-chlorobenzyloxy)-PDO and 7(8)bromo-2-(4-methylthiobenzyloxy)-PDO (7) are new selective hypoxic cytotoxins with additional ability to inhibit DNA topoisomerase II activity. [57] Hernández et al [58] showed the chemosensitizer effect of the PDO analogs such as 8 to cisplatin and the mechanism of action on bladder cancer cells. The cinnamoyl-PDO derivative [76] did not exhibit antiproliferative activity but after combining with a subtoxic dose of cisplatin the mixture showed a significant increase in the antiproliferative activity.…”

Section: Phenazine N 5 N 10 -Dioxide Derivativesmentioning

confidence: 99%

The Phenazine Scaffold Used as Cytotoxic Pharmacophore Applied in Bactericidal, Antiparasitic and Antitumor Agents

Miksa

2022

Helvetica Chimica Acta

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Phenazine derivatives are important bactericidal antibiotics and antiparasitic compounds which can be used in synergistic combinations with anticancer drugs in chemotherapy treatments. The development of synthetic phenazines with anticancer activity improves the effectiveness of chemotherapy. Chemical variations introduced at the phenazine core which is known as a chromophore with fluorescent properties provide advanced theranostic agents useful in optical bioimaging techniques and photodynamic anticancer therapy. This review summarizes the field of structural modifications of phenazine derivatives which have been tested against different parasitic and bacterial infections. The report highlights advances in design and biological evaluations of phenazines as anticancer drugs for the development of new chemotherapeutic as well as bio‐imaging reagents.

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“…Scientists have been exploring combination approaches for cancer treatment, in which other therapeutic agents are usually co‐administered with chemotherapeutic drugs . Such efforts are motivated by their chemosensitizing or synergetic/additive effects against malignant tumors .…”

Section: Introductionmentioning

confidence: 99%

“…[6] Scientists have been exploring combination approaches for cancer treatment, in which other therapeutic agents are usually co-administered with che-motherapeutic drugs. [7] Such efforts are motivated by their chemosensitizing or synergetic/additive effects against malignant tumors. [8] In this context, bioactive compounds from natural products have been explored to act as potent chemosensitizer in combination with conventional chemotherapeutic drugs.…”

Section: Introductionmentioning

confidence: 99%

Chemosensitizing Effect of Cernumidine Extracted from Solanum cernuum on Bladder Cancer Cells in Vitro

Miranda

Mondal

Singh

et al. 2019

Chemistry & Biodiversity

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Cernumidine (CER) is a guanidinic alkaloid isolated from Solanum cernuum leaves. In this work, we investigated the cytotoxicity, chemosensitizing effect of cernumidine to cisplatin (cDDP) and the possible mechanism of action of the combination on bladder cancer cells. Cernumidine showed cytotoxicity and could sensitize bladder cancer cells to cisplatin. The combination of CER+cDDP inhibited cell migration on T24 cells. CER+cDDP down‐regulated MMP‐2/9 and p‐ERK1/2, while it increased EGFR activity corroborating the observed cell migration inhibition. Down‐regulation of Bcl‐2 and up‐regulation pro‐apoptotic Bax and further depletion of the mitochondrial membrane potential (ΔΨm) indicates that mitochondria play a central role in the combination treatment inducing the mitochondrial signaling pathway of apoptosis in T24 cells. Our data showed that the alkaloid cernumidine is worthy of further studies as a chemosensitizing agent to be used in complementary chemotherapy.

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Chemosensitizer effect of cisplatin-treated bladder cancer cells by phenazine-5,10-dioxides

Cited by 8 publications

References 25 publications

Valeric acid acts as a novel HDAC3 inhibitor against prostate cancer

Valeric acid acts as a novel HDAC3 inhibitor against prostate cancer

The Phenazine Scaffold Used as Cytotoxic Pharmacophore Applied in Bactericidal, Antiparasitic and Antitumor Agents

Chemosensitizing Effect of Cernumidine Extracted from Solanum cernuum on Bladder Cancer Cells in Vitro

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