Ligustrazine_derivate_DLJ14_reduces_multidrug_resistance_of_K562A02_cells_by_modulating_GSTπ_activi1.pdfVIP

Toxicology in Vitro 25 (2011) 937–943 Contents lists available at ScienceDirect Toxicology in Vitro journal homepage: www.elsevi /locate/toxinvit Ligustrazine derivate DLJ14 reduces multidrug resistance of K562/A02 cells by modulating GSTp activity Yu-Ning Song a, Xiu-Li Guo a,⇑, Bei-Bei Zheng a, Xin-Yong Liu b, Xue Dong a, Lu-Gang Yu c, Yan-Na Cheng a a Department of Pharmacology, School of Pharmaceutical Sciences, Shandong University, Jinan 250012, PR China b Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Jinan 250012, PR China c The Henry Wellcome Laboratory of Molecular and Cellular Gastroenterology, Liverpool Centre for Glycobiology, School of Clinical Sciences, University of Liverpool, Liverpool L69 3BX, United Kingdom a r t i c l e i n f o a b s t r a c t Article history: Multidrug resistance (MDR) of tumor cells is a major obstacle in chemotherapeutic cancer treatment. Received 20 May 2010 Over-expression of glutathione S-transferase p (GSTp) is one of the mechanisms contributing to MDR. Accepted 2 March 2011 In this study, we investigated the reversal of MDR by DLJ14, a ligustrazine derivate, in adriamycin Available online 12 March 2011 (Adr) resistant human myelogenous leukemia (K562/A02) cells by modulating the expression of GSTp and the activity of GST-related enzymes. In the MTT test, DLJ14 showed a weak inhibition on proliferation Keywords: of both K562/A02 and K562 cells, while verap