The n-hexane root extracts from Echinacea pallida, Echinacea angustifolia and Echinacea purpurea were evaluated for inhibitionof the multidrug transporter P-glycoprotein (Pgp) activity,the product of the ABCB1 gene, involved in cancer multidrug resistance (MDR) and in herb-drug or drug-drug interactions. Thebiological assay was performed using the human proximal tubule HK-2 cell line that constitutively expresses ABCB1. The n-hexaneextracts of all three species reduced the efflux of the Pgp probe calcein-AM from HK-2 cells two-fold in a concentration-dependent manner, and E. pallida was found to be the most active species. For the first time, two polyacetylenes and three polyenes, isolated from the n-hexane extract of E. pallida roots by a bioassay- guided fractionation, were found to be able to reduce Pgp activity. Pentadeca-(8Z,13Z)-dien-11-yn-2-one was the most efficient compound, being able to decrease the calcein-AM efflux about three-fold with respect to the control at 30 μg/mL.

P-Glycoprotein inhibitory activity of lipophilic constituents of Echinacea pallida roots in a human proximal tubular cell line / N., Romiti; Pellati, Federica; P., Nieri; Benvenuti, Stefania; B., Adinolfi; E., Chieli. - In: PLANTA MEDICA. - ISSN 0032-0943. - STAMPA. - 74:(2008), pp. 264-266. [10.1055/s-2008-1034308]

P-Glycoprotein inhibitory activity of lipophilic constituents of Echinacea pallida roots in a human proximal tubular cell line

PELLATI, Federica;BENVENUTI, Stefania;
2008-01-01

Abstract

The n-hexane root extracts from Echinacea pallida, Echinacea angustifolia and Echinacea purpurea were evaluated for inhibitionof the multidrug transporter P-glycoprotein (Pgp) activity,the product of the ABCB1 gene, involved in cancer multidrug resistance (MDR) and in herb-drug or drug-drug interactions. Thebiological assay was performed using the human proximal tubule HK-2 cell line that constitutively expresses ABCB1. The n-hexaneextracts of all three species reduced the efflux of the Pgp probe calcein-AM from HK-2 cells two-fold in a concentration-dependent manner, and E. pallida was found to be the most active species. For the first time, two polyacetylenes and three polyenes, isolated from the n-hexane extract of E. pallida roots by a bioassay- guided fractionation, were found to be able to reduce Pgp activity. Pentadeca-(8Z,13Z)-dien-11-yn-2-one was the most efficient compound, being able to decrease the calcein-AM efflux about three-fold with respect to the control at 30 μg/mL.
74
264
266
P-Glycoprotein inhibitory activity of lipophilic constituents of Echinacea pallida roots in a human proximal tubular cell line / N., Romiti; Pellati, Federica; P., Nieri; Benvenuti, Stefania; B., Adinolfi; E., Chieli. - In: PLANTA MEDICA. - ISSN 0032-0943. - STAMPA. - 74:(2008), pp. 264-266. [10.1055/s-2008-1034308]
N., Romiti; Pellati, Federica; P., Nieri; Benvenuti, Stefania; B., Adinolfi; E., Chieli
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11380/611760
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