Abstract
The n-hexane root extracts from Echinacea pallida, Echinacea angustifolia and Echinacea purpurea were evaluated for inhibition of 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. The biological assay was performed using the human proximal tubule HK-2 cell line that constitutively expresses ABCB1. The n-hexane extracts 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.
Abbreviations
Calcein-AM:calcein acetoxymethyl ester
Pgp:P-glycoprotein
Key words
Echinacea pallida
- Asteraceae - polyacetylenes - polyenes - HK-2 cells - P-glycoprotein
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Prof. Dr. Elisabetta Chieli
Dipartimento di Patologia Sperimentale
Sezione di Patologia Generale e Clinica
Università degli Studi di Pisa
Scuola Medica
via Roma 55
56126 Pisa
Italy
Phone: +39-050-2218550
Fax: +39-050-2218557
Email: chieli@biomed.unipi.it
