Novel activity of acriflavine against colorectal cancer tumor cells

Hassan, Saadia Bashir; Laryea, Daniel; Mahteme, Haile; Felth, Jenny; Fryknäs, Mårten; Fayad, Walid; Linder, Stig; Rickardson, Linda; Gullbo, Joachim; Graf, Wilhelm; Påhlman, Lars; Glimelius, Bengt; Larsson, Rolf; Nygren, Peter

doi:10.1111/j.1349-7006.2011.02097.x

Cited by 58 publications

(53 citation statements)

References 34 publications

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“…Administration of other chemotherapy drugs in combination with 5-FU is reported to improve the response rate of patients (9,11). In the present study, the effect of ACF on the anticancer activity (19) demonstrated that ACF has a cytotoxic effect in monolayer and multicellular spheroid culture of CRC cells, and their results demonstrated that ACF has a good cellular penetration and cytotoxic activity against hypoxic CRC cells.…”

Section: Discussionsupporting

confidence: 57%

“…It appears that pretreatment with ACF predisposes CRC cells to the cytotoxic effect of the main drug, i.e. 5-FU, through the inhibition of HIF-1α and topoisomerase 2 activity as suggested previously (17,19). However, the exact molecular mechanism of ACF cytotoxicity against CRC cells remains to be elucidated (19).…”

Section: Ic 50 Value µM --------------------------------------------mentioning

confidence: 79%

“…Studies by Shay et al (17) and Hassan et al (19) proposed that cytotoxic property of ACF in CRC cells may be associated with inhibition of topoisomerase 2 and HIF-1α activity. However, the exact molecular mechanism of action of ACF against CRC remains to be determined (19). To the best of our knowledge, it has not been investigated previously whether ACF is able to act through the alteration of mRNA expression of these two important proteins in CRC cells.…”

Section: Introductionmentioning

confidence: 99%

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Acriflavine enhances the antitumor activity of the chemotherapeutic drug 5‑fluorouracil in colorectal cancer cells

et al. 2018

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Abstract. 5-Fluorouracil (5-FU)-based chemotherapy improves the overall survival rates of patients with colorectal cancer (CRC). However, only a small proportion of patients respond to 5-FU when used as a single agent. The aim of the present study was to investigate whether the anticancer property of 5-FU is potentiated by combination treatment with acriflavine (ACF) in CRC cells. Additionally, the potential underlying molecular mechanisms of the cytotoxic effect of ACF were determined. The cytotoxic effects of ACF, 5-FU and irinotecan on different CRC cell lines with different p53 status were investigated using an MTT assay. SW480 cells that express a mutated form of p53 and two other CRC cell lines were used, HCT116 and LS174T, with wild-type p53. To determine the effect of ACF on the sensitivity of cells to 5-FU, cells were co-treated with the 30% maximal inhibitory concentration (IC 30 ) of ACF and various concentrations of 5-FU, or pretreated with the IC 30 of ACF and various concentrations of 5-FU. To assess the mechanism of action of ACF, cells were treated with IC 30 values of the compound and then the reverse transcription-quantitative polymerase chain reaction was used to evaluate mRNA levels of hypoxia-inducible factor-1α (HIF-1α) and topoisomerase 2. Results indicate that pretreatment with ACF markedly sensitized CRC cells to the cytotoxic effects of 5-FU, whereas simultaneous treatment with ACF and 5-FU were not able to alter the resistance of CRC cells to 5-FU. In comparison with irinotecan, ACF was a more potent agent for enhancing the antitumor activity of 5-FU. ACF did not alter the mRNA levels of either HIF-1α or topoisomerase 2. The results of the present study reveal for the first time that pretreatment of CRC cells with ACF markedly increases the cytotoxic effects of 5-FU, regardless of the p53 status of cells.

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Section: Discussionsupporting

confidence: 57%

Section: Ic 50 Value µM --------------------------------------------mentioning

confidence: 79%

Section: Introductionmentioning

confidence: 99%

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Acriflavine enhances the antitumor activity of the chemotherapeutic drug 5‑fluorouracil in colorectal cancer cells

et al. 2018

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“…Several studies have indicated that acridines possess properties that inhibit tumor growth and cancer cell proliferation (21)(22)(23)(24). Acriflavine, an acridine derivative has previously been used as an imaging contrast agent due to the ability to pass through the cell membrane and strongly label acidic constituents (25,26).…”

Section: Discussionmentioning

confidence: 99%

Proflavin suppresses the growth of human osteosarcoma MG63 cells through apoptosis and autophagy

Zhang

Fuwen

2015

Oncology Letters

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Abstract. Proflavin is one of the novel acridine derivatives that possess various pharmacological effects. Although numerous studies have been performed to investigate proflavin, its effects have not been investigated on the human osteosarcoma MG63 cell line. The core aim of the present study was to test the effects of proflavin on the viability of MG63 cells and the induction of apoptosis and autophagy in MG63 cells. The induction of apoptosis was examined by measuring the changes in the expression of the B-cell lymphoma 2 (Bcl-2) and Bcl-2-associated X protein mRNA and proteins. Apoptotic cell death was identified by the proteolytic cleavage of poly (adenosine diphosphate-ribose) polymerase and caspase-3 and caspase-9. In addition, the autophagic effects of proflavin were examined by the quantitation of the mRNA expression of autophagy protein 5 and Beclin 1, in addition to the identification of the accumulation of microtubule-associated protein 1 light chain 3-II. The present results revealed that proflavin inhibited the proliferation of MG63 cells in a dose-dependent manner. Proflavin-induced cell death was attributed to apoptosis and autophagy. Overall, the present results indicated that the antiseptic agent proflavin exerts anticancer potential through the synergistic activity of apoptosis and autophagy.

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“…However, this observation period does not exclude potential carcinogenic effects at later time points. Finally, acriflavine showed anticancer activity in vitro in recently published studies [18,19]. Thus, acriflavine might be an interesting substance for various diagnostic and therapeutic purposes in humans.…”

Section: Staining Agentmentioning

confidence: 99%

Confocal laser endomicroscopy for diagnosing lung cancerin vivo

et al. 2012

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Confocal laser endomicroscopy is a novel endoscopic technique that may allow imaging of living cells in lung tissue in vivo. We assessed the potential of this technique for the detection of histology during screening bronchoscopy for lung cancer.32 patients with suspected malignancies underwent bronchoscopy with endomicroscopy using acriflavine hydrochloride. Standardised areas and localised lesions were analysed by in vivo confocal imaging during bronchoscopy and biopsies were taken. Confocal images were graded and correlated prospectively with conventional histology from biopsies.Acriflavine hydrochloride yielded high-quality confocal images and strongly labelled airway epithelial cells. No side-effects were noted. 75 522 confocal images from 56 different locations were compared prospectively with histological data from biopsy specimens. Endomicroscopy allowed subsurface imaging with detailed analysis of cellular and subcellular structures. Neoplastic changes could be predicted with high accuracy (sensitivity 96.0%, specificity 87.1%, accuracy 91.0%).Confocal laser endomicroscopy with acriflavine is a novel diagnostic tool for the analysis of living cells during bronchoscopy and permits virtual histology of neoplastic changes in the airways with high accuracy. This technique may enable the rapid diagnosis of neoplasia during ongoing endoscopy in patients with suspected lung cancer.

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Novel activity of acriflavine against colorectal cancer tumor cells

Cited by 58 publications

References 34 publications

Acriflavine enhances the antitumor activity of the chemotherapeutic drug 5‑fluorouracil in colorectal cancer cells

Acriflavine enhances the antitumor activity of the chemotherapeutic drug 5‑fluorouracil in colorectal cancer cells

Proflavin suppresses the growth of human osteosarcoma MG63 cells through apoptosis and autophagy

Confocal laser endomicroscopy for diagnosing lung cancerin vivo

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