ABCG2/BCRP interaction with the sea grass <i>Thalassia testudinum</i>

Miguel, Verónica; Otero, Jon A.; Barrera, Borja; Rodeiro, Idania; Prieto, J. E.; Merino, Gracia; Álvarez, Ana Bernardo

doi:10.1515/dmpt-2015-0013

Cited by 2 publications

(2 citation statements)

References 19 publications

(27 reference statements)

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“…In addition, Th shows acute anti-inflammatory effects in mice [ 36 ] and it displays selective anti-proliferative activity against cancer cells compared to normal cells [ 37 ]. Besides, the extract also inhibits drug efflux by ABCG2/breast cancer resistance protein (BCRP) and ABCB1/P-glycoprotein (MDR1 gene), increasing intracellular accumulation of anticancer agents [ 38 , 39 ]. Thus, the marine angiosperm T. testudinum has been considered a natural source of potential antitumor agents.…”

Section: Introductionmentioning

confidence: 99%

Interaction of Thalassia testudinum Metabolites with Cytochrome P450 Enzymes and Its Effects on Benzo(a)pyrene-Induced Mutagenicity

Delgado-Roche¹,

Santes-Palacios

Herrera

et al. 2020

Marine Drugs

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The aim of the present work was to evaluate the effects of Thalassia testudinum hydroethanolic extract, its polyphenolic fraction and thalassiolin B on the activity of phase I metabolizing enzymes as well as their antimutagenic effects. Spectrofluorometric techniques were used to evaluate the effect of tested products on rat and human CYP1A and CYP2B activity. The antimutagenic effect of tested products was evaluated in benzo[a]pyrene (BP)-induced mutagenicity assay by an Ames test. Finally, the antimutagenic effect of Thalassia testudinum (100 mg/kg) was assessed in BP-induced mutagenesis in mice. The tested products significantly (p < 0.05) inhibit rat CYP1A1 activity, acting as mixed-type inhibitors of rat CYP1A1 (Ki = 54.16 ± 9.09 μg/mL, 5.96 ± 1.55 μg/mL and 3.05 ± 0.89 μg/mL, respectively). Inhibition of human CYP1A1 was also observed (Ki = 197.1 ± 63.40 μg/mL and 203.10 ± 17.29 μg/mL for the polyphenolic fraction and for thalassiolin B, respectively). In addition, the evaluated products significantly inhibit (p < 0.05) BP-induced mutagenicity in vitro. Furthermore, oral doses of Thalassia testudinum (100 mg/kg) significantly reduced (p < 0.05) the BP-induced micronuclei and oxidative damage, together with an increase of reduced glutathione, in mice. In summary, Thalassia testudinum metabolites exhibit antigenotoxic activity mediated, at least, by the inhibition of CYP1A1-mediated BP biotransformation, arresting the oxidative and mutagenic damage. Thus, the metabolites of T. testudinum may represent a potential source of chemopreventive compounds for the adjuvant therapy of cancer.

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Section: Introductionmentioning

confidence: 99%

Interaction of Thalassia testudinum Metabolites with Cytochrome P450 Enzymes and Its Effects on Benzo(a)pyrene-Induced Mutagenicity

Delgado-Roche¹,

Santes-Palacios

Herrera

et al. 2020

Marine Drugs

Self Cite

View full text Add to dashboard Cite

show abstract

“…In addition, Th shows acute antiinflammatory effects in mice [36] and it displays selective anti-proliferative activity against cancer cells compared to normal cells [37]. Besides, the extract also inhibits drug efflux by ABCG2/breast cancer resistance protein (BCRP) and ABCB1/P-glycoprotein (MDR1 gene), increasing intracellular accumulation of anticancer agents [38,39]. Thus, the marine angiosperm T. testudinum has been considered a natural source of potential antitumor agents.…”

Section: Introductionmentioning

confidence: 99%

Interaction of Thalassia testudinum Metabolites with Cytochrome P450 Enzymes and Its Effects on Benzo(a)pyrene-Induced Mutagenicity

Delgado-Roche¹,

Santes-Palacios²,

Herrera³

et al. 2020

Preprint

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View full text Add to dashboard Cite

The aim of the present work was to evaluate the effects of Thalassia testudinum hydroethanolic extract, its polyphenolic fraction, and thalassiolin B on the activity of phase I metabolizing enzymes as well as their antimutagenic effects. Spectrofluorometric techniques were used to evaluate the effect of tested products on rat and human CYP1A and CYP2B activity. The antimutagenic effect of tested products was evaluated in benzo[a]pyrene (BP)-induced mutagenicity assay by Ames test. Finally, the antimutagenic effect of Thalassia testudinum (100 mg/kg) was assessed in a BP-induced mutagenesis in mice. The tested products significantly (p<0.05) inhibit rat CYP1A1 activity, acting as mixed-type inhibitors of rat CYP1A1 (Ki = 54.16±9.09 μg/mL, 5.96±1.55 μg/mL and 3.05±0.89 μg/mL, respectively). Inhibition of human CYP1A1 was also observed (Ki = 197.1±63.40 μg/mL and 203.10±17.29 μg/mL for the polyphenolic fraction and for thalassiolin B, respectively). In addition, the evaluated products significantly inhibit (p<0.05) benzo[a]pyrene (BP)-induced mutagenicity in vitro. Furthermore, oral doses of Thalassia testudinum (100 mg/kg) significantly reduced (p<0.05) the BP-induced micronuclei and oxidative damage, together with an increase of glutathione, in mice. In summary, Thalassia testudinum metabolites exhibit antigenotoxic activity mediated, at least, by the inhibition of CYP1A1-mediated BP biotransformation. Thus, the metabolites of T. testudinum may represent a potential source of chemopreventive compounds for adjuvant therapy of cancer.

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ABCG2/BCRP interaction with the sea grass Thalassia testudinum

Cited by 2 publications

References 19 publications

Interaction of Thalassia testudinum Metabolites with Cytochrome P450 Enzymes and Its Effects on Benzo(a)pyrene-Induced Mutagenicity

Interaction of Thalassia testudinum Metabolites with Cytochrome P450 Enzymes and Its Effects on Benzo(a)pyrene-Induced Mutagenicity

Interaction of Thalassia testudinum Metabolites with Cytochrome P450 Enzymes and Its Effects on Benzo(a)pyrene-Induced Mutagenicity

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