The in-vitro and in-vivo inhibitory activity of biflorin in melanoma

Vasconcellos, Marne Carvalho de; Bezerra, Daniel P.; Fonseca, Aluísio Marques da; Araújo, Ana Jérsia; Pessoa, Cláudia; Lemos, Telma L. G.; Costa-Lotufo, Letı́cia V.; Moraes, Manoel Odoríco de; Montenegro, Raquel Carvalho

doi:10.1097/cmr.0b013e328343ecc4

Cited by 18 publications

(15 citation statements)

References 27 publications

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“…The effect of biflorin on different tumor cell lines have been previously screened at a range of biflorin concentrations (0.39-25 µg/mL) similar to the one reported in this study (5-50 µg/mL) (Vasconcellos et al, 2005(Vasconcellos et al, , 2007(Vasconcellos et al, , 2011. Recently, Montenegro et al (2013a) revealed that biflorin (1-20 µM) exerted cytotoxic effects on breast cancer SK-Be3 cells; additionally, biflorin treatment was seen to exert selective cytotoxicity against cancer cells in relation to normal cells, as observed in this study.…”

Section: Discussionmentioning

confidence: 92%

“…The relation between cancer and apoptosis has being emphasized for a long time, suggesting that tumor progression involves the inhibition of apoptotic stages in tumor cells (Yang et al, 2006;Vasconcellos et al, 2011). Apoptosis, autophagy, and necrosis are the three main forms of cell death, each one presenting a unique set of biochemical and morphological changes that occur within the dying cell (Elmore, 2007;Ouyang et al, 2012).…”

Section: Discussionmentioning

confidence: 99%

“…Mouse in vivo studies have also revealed that biflorin coupling increased the effectiveness of 5-fluoracil chemotherapy (5-FU), and reduced the systemic toxicity (Vasconcellos et al, 2007). Moreover, the administration of 25 mg/day biflorin to animals transplanted with melanoma B16 for ten days induced significant tumor growth inhibition with no systemic toxicity (Vasconcellos et al, 2011).…”

Section: Introductionmentioning

confidence: 97%

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O-naphthoquinone isolated from Capraria biflora L. induces selective cytotoxicity in tumor cell lines

et al. 2015

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ABSTRACT.Biflorin is an o-naphthoquinone isolated from the roots of the plant Capraria biflora L. (Scrophulariaceae). In this study, the cytotoxic effects of biflorin were verified, and late apoptosis was detected in various cancer cell lines by in situ analysis. The cytotoxicity was further evaluated exclusively for 48 h of treatment in different tumor and non-tumor cell lines (Hep-2, HeLa, HT-29, A-375, and A-549, and HEK-293, respectively). The results indicated that biflorin induced selective cytotoxicity in tumor cells. HeLa cells were more susceptible to biflorin, followed by HT-29, A-549, A-375, and Hep-2 at all concentrations (range 5-50 µg/mL), and the highest half-maximal inhibitory concentration IC 50 (56.01 ± 1.17 µg/mL) was observed in HEK-293 cells. Late apoptotic/necrotic events, observed by in situ immunostaining with Annexin V, varied with each cell line; an increase in late apoptotic events was observed corresponding to the increase in biflorin dosage. Hep-2 cells showed a greater percentage of late apoptotic events among the tumor cell lines when treated with higher concentrations of biflorin (69.63 ± 2.28%). The non-tumor HEK-293 line showed greater resistance to late apoptotic events, as well as a lower level of cytotoxicity (77.69 ± 6.68%) than the tested tumor lines. The data presented indicate that biflorin showed an important, possibly selective, cytotoxicity against tumor cell lines, thereby revealing a promising novel substance with potential anticancer activity for tumor therapy.

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Section: Discussionmentioning

confidence: 92%

Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 97%

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O-naphthoquinone isolated from Capraria biflora L. induces selective cytotoxicity in tumor cell lines

et al. 2015

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“…1), an ortho-naphthoquinone, can be isolated from the roots of Capraria biflora L. (Schrophulariaceae),a perennial shrub that was originally found in the Antilles and South America (Acosta et al, 2003). This quinone has been shown to have anticancer properties in vitro and in vivo, increasing the survival of mice with melanoma tumors, without diminishing the tumor size (Vasconcellos et al, 2005(Vasconcellos et al, , 2007(Vasconcellos et al, , 2011. As such, the aim of this work is to investigate the role of biflorin in MDA-MB-435, an invasive melanoma cancer cell, in vitro.…”

Section: Introductionmentioning

confidence: 99%

A novel o-naphtoquinone inhibits N-cadherin expression and blocks melanoma cell invasion via AKT signaling

Montenegro

Vasconcellos

Barbosa

et al. 2013

Toxicology in Vitro

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The down-regulation or loss of epithelial markers is often accompanied by the up-regulation of mesenchymal markers. E-cadherin generally suppresses invasiveness, whereas N-cadherin promotes invasion and metastasis in vitro. The aim of this work is to investigate the role of biflorin, a naphthoquinone with proven anticancer properties, on the expression of N-cadherin and AKT proteins in MDA-MB-435 invasive melanoma cancer cells after 12h of exposure to 1, 2.5 and 5 μM biflorin. Biflorin inhibited MDA-MB-435 invasion in a dose-dependent manner (p<0.01). Likewise, biflorin down-regulated N-cadherin and AKT-1 expression in a dose-dependent manner. Biflorin did not inhibit the adhesion of MDA-MB-435 cells to any tested substrates. Additionally, biflorin blocked the invasiveness of cells by down-regulating N-cadherin, most likely via AKT-1 signaling. As such, biflorin may be a novel anticancer agent and a new prototype for drug design.

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“…Moreover, when coupled with 5-fluoracil chemotherapy (5-FU), biflorin increased the effectiveness in addition to reducing systemic toxicity (Vasconcellos et al 2007). In experiments with animals transplanted with B16 melanoma cells, biflorin was administered at 25 mg/day for 10 days, and there was a significant inhibition of tumor growth with no systemic toxicity (Vasconcellos et al 2011). A metastasis assay GABRIELLE G.N.S.…”

Section: Biological Activity Of Biflorinmentioning

confidence: 99%

Biflorin: an o-naphthoquinone of clinical significance

Wisintainer

Simões

Lemos

et al. 2014

An. Acad. Bras. Ciênc.

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Biflorin is an o-naphthoquinone with proven cytotoxic effects on tumor cells showing antimicrobial, antitumor and antimutagenic activities. Biflorin is an isolated compound taken from the roots of the plant Capraria biflora L. (Schrophulariaceae), indigenous of the West Indies and South America, which is located in temperate or tropical areas. This compound has shown to be strongly active against grampositive and alcohol-acid-resistant bacteria. It has been efficient in inhibiting the proliferation tumor cell lines CEM, HL-60, B16, HCT-8 and MCF-7. Recently, SK-Br3 cell line was treated with biflorin showing important cytotoxic effects. In this article, information related to the first structural characterization studies are presented, as well as the latest reports concerning the biological activity of this molecule.

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The in-vitro and in-vivo inhibitory activity of biflorin in melanoma

Cited by 18 publications

References 27 publications

O-naphthoquinone isolated from Capraria biflora L. induces selective cytotoxicity in tumor cell lines

O-naphthoquinone isolated from Capraria biflora L. induces selective cytotoxicity in tumor cell lines

A novel o-naphtoquinone inhibits N-cadherin expression and blocks melanoma cell invasion via AKT signaling

Biflorin: an o-naphthoquinone of clinical significance

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