Effects of Two Natural Bisbenzylisoquinolines,Curine and Guattegaumerine,Extracted from Isolona hexaloba on Rhodamine Efflux by Abcb1b from Rat Glycocholic-Acid-Resistant Hepatocarcinoma Cells |
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| Authors: | Jacques-Auré lien Sergent,Hilarion Mathouet,Christian Hulen,Pedro Lameiras,Marc Feuilloley,Abdelhakim Elomri,Nour-Eddine Lomri |
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| Affiliation: | 1.Department of Biology, UFR Sciences and Techniques, University of Cergy-Pontoise, 2 Ave A. Chauvin, 95302 Cergy-Pontoise, France;2.UNIROUEN, INSA Rouen, CNRS, COBRA (UMR 6014), Normandie University, 76000 Rouen, France; (H.M.); (P.L.);3.Bacterial Communication and Antimicrobial Strategies Research Unit, University of Rouen Normandy, 55 rue Saint Germain, 2700 Evreux, France; (C.H.); (M.F.) |
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| Abstract: | To develop new therapeutic molecules, it is essential to understand the biological effects and targets of clinically relevant compounds. In this article, we describe the extraction and characterization of two alkaloids from the roots of Isolona hexaloba—curine and guattegaumerine. The effect of these alkaloids on the multidrug efflux pump ABCB1 (MDR1/P-Glycoprotein) and their antiproliferative properties were studied. Compared to verapamil, a widely used inhibitor of P-gp, curine and guattegaumerine were found to be weak inhibitors of MDR1/P-Glycoprotein. The highest inhibition of efflux produced by verapamil disappeared in the presence of curine or guattegaumerine as competitors, and the most pronounced effect was achieved with curine. Altogether, this work has provided new insights into the biological effects of these alkaloids on the rat Mdr1b P-gp efflux mechanism and would be beneficial in the design of potent P-gp inhibitors. |
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| Keywords: | alkaloids curine guattegaumerine verapamil efflux pump inhibition MDR1 |
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