Piperlongumine (PLGM) was considered as an anti-cancer agent since it was involved in suppressing of many types of cancer. To investigate the functions and mechanisms of PLGM on drug resistance reversal in human retinoblastoma cell lines, drug resistance cell lines HXO-RB44/VCR and SO-Rb50/CBP were established. We found that after treatment with PLGM, drug sensitivity and apoptosis rate of these drug resistance cancer cells were improved, cell cycle was arrested, the expressions of P-gp, MDR1, MRP1, Top-II, GST-π, Survivin, Bcl-2, CDK1, ABCB1 and ABCG1 was decreased, while the activities of caspase-3/8 and intracellular content of Rh-123 was increased. Furthermore, the activities of PI3K/AKT and PKCζ pathways were suppressed following PLGM treatment. Therefore, this study suggests that PLGM could reverse the drug resistance of human retinoblastoma cell lines HXO-RB44/VCR and SO-Rb50/CBP. This drug resistance reversing effect might exert via PI3K/AKT and PKCζ pathways.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4440067PMC

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