Drug metabolism and personalized therapy · 2015
ABCG2/BCRP interaction with the sea grass Thalassia testudinum.
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Miguel Verónica, Otero Jon A, Barrera Borja, Rodeiro Idania, Prieto Julio G, Merino Gracia, Álvarez Ana I
Аннотация
BACKGROUND: The aqueous ethanolic extract from leaves of the marine plant Thalassia testudinum has shown antioxidant, cytoprotective, and neuroprotective properties. The chemical composition of this extract, rich in polyphenols, could interfere with active transport of drugs out of the cell and circumvent the phenomenon of multidrug resistance (MDR). The extract can act as an MDR modulator through its interaction with efflux transporters. The ABCG2/BCRP has been shown to confer MDR acting in tumor cells.
METHODS: To evaluate the interaction of ABCG2/BCRP with the extract, studies in cells overexpressing human BCRP transporter and its murine ortholog Bcrp1 were performed.
RESULTS AND CONCLUSIONS: T. testudinum extract could be included as MDR modulator, as interaction with ABCG2/BCRP has been shown through flow cytometry and MTT assays. The cells overexpressing ABCG2/BCRP in the presence of the extract (25-150 μg/mL) decreased the survival rates of the anti-tumoral mitoxantrone. Our results support its inclusion as a possible MDR modulator against tumor cells that overexpress ABCG2/BCRP.
METHODS: To evaluate the interaction of ABCG2/BCRP with the extract, studies in cells overexpressing human BCRP transporter and its murine ortholog Bcrp1 were performed.
RESULTS AND CONCLUSIONS: T. testudinum extract could be included as MDR modulator, as interaction with ABCG2/BCRP has been shown through flow cytometry and MTT assays. The cells overexpressing ABCG2/BCRP in the presence of the extract (25-150 μg/mL) decreased the survival rates of the anti-tumoral mitoxantrone. Our results support its inclusion as a possible MDR modulator against tumor cells that overexpress ABCG2/BCRP.
Предметные рубрики MeSH
ATP Binding Cassette Transporter, Subfamily G, Member 2ATP-Binding Cassette TransportersAnimalsAntineoplastic AgentsCells, CulturedDiketopiperazinesDrug Resistance, MultipleDrug Resistance, NeoplasmHerb-Drug InteractionsHeterocyclic Compounds, 4 or More RingsHumansHydrocharitaceaeLethal Dose 50MiceMitoxantroneNeoplasm ProteinsPlant ExtractsPlant Leaves