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Inhibition of P-glycoprotein by two artemisinin derivatives

Natural Products and Bioprospecting 2012年第2期2卷 59-64页

作者： Babette STEGLICH Anne MAHRINGER Ying LI Gary H.POSNER gert fricker Thomas EFFERTH Department of Pharmaceutical Biology Institute of Pharmacy and BiochemistryJohannes Gutenberg UniversityStaudinger Weg 5551 MainzGermany Institute of Pharmacy and Molecular Biotechnology Karl Ruprecht UniversityHeidelbergGermany Department of Synthetic Chemistry Shanghai Institute of Materia MedicaChinese Academy of SciencesShanghaiChina Department of Chemistry Johns Hopkins UniversityBaltimore MDUSA

P-Glycoprotein/MDR1 represents an important component of the blood brain barrier and contributes to multidrug *** investigated two derivatives of the anti-malarial artemisinin,SM616 and GHP-AJM-3/23,concerning their ability to interact with *** ability of the two compounds to inhibit P-glycoprotein(P-gp)activity was examined in sensitive CCRF-CEM and P-gp over-expressing and multidrug-resistant CEM/ADR5000 cells as well as in porcine brain capillary endothelial cells(PBCEC)by means of calcein-AM *** as well-known P-gp inhibitor was used as control ***/ADR5000 cells exhibited cross-resistance to GHP-AJM-3/23,but slight collateral sensitivity to ***,SM616 inhibited calcein efflux both in CEM/ADR5000 and PBCEC,whereas GHP-AJM-3/23 did only increase calcein fluorescence in PBCEC,but not CEM/*** may be explained by the fact that CEM/ADR5000 only express P-gp but not other ATP-binding cassette transporters,whereas PBCEC are known to express several ABC transporters and calcein is transported by more than one ABC ***,SM616 may be the more specific P-gp *** conclusion,the collateral sensitivity of SM616 as well as the inhibition of calcein efflux in both CEM/ADR5000 cells and PBCEC indicate that this compound may be a promising P-gp inhibitor to treat cancer therapy and to overcome the blood brain barrier.

关键词： blood brain barrier calcein multidrug resistance P-glycoprotein

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